AU2008201550B2 - Method of inhibiting remnant lipoprotein production - Google Patents

Description

AUSTRALIA Patents Act COMPLETE SPECIFICATION (ORIGINAL) Class Int. Class Application Number: Lodged: Complete Specification Lodged: Accepted: Published: Priority Related Art: Name of Applicant: Japan Tobacco Inc. Actual Inventor(s): Noboru Furukawa, Hiroshi Okamoto, Tomohiko Sasase Address for Service and Correspondence: PHILLIPS ORMONDE & FITZPATRICK Patent and Trade Mark Attorneys 367 Collins Street Melbourne 3000 AUSTRALIA Invention Title: METHOD OF INHIBITING REMNANT LIPOPROTEIN PRODUCTION Our Ref: 820797 POF Code: 215996/215996 The following statement is a full description of this invention, including the best method of performing it known to applicant(s): -1 - DESCRIPTION METHOD OF INHIBITING REMNANT LIPOPROTEIN PRODUCTION This is a divisional application of AU 2004275637, the disclosure of which is incorporated by way of reference. 5 Technical Field The present invention relates to a method of inhibiting remnant lipoprotein production, which comprises administering a compound having a CETP (cholesteryl ester transfer protein) inhibitory activity to an administration subject, and a remnant 10 lipoprotein production inhibitor comprising a compound having a CETP inhibitory activity as an active ingredient. The present invention further relates to a prophylactic or therapeutic agent for hyper-remnant lipoproteinemia, which comprises such compound having a CETP inhibitory activity as an active 15 ingredient. Background Art The fat components in blood are present in lipoproteins that are bound with apolipoprotein. These serum lipoproteins are classified into chylomicron (CM), chylomicron remnant, very 20 low density lipoprotein (VLDL), intermediate-density lipoprotein (remnant lipoprotein; IDL), low density lipoprotein (LDL) and high density lipoprotein (HDL), based on the densities thereof. The remnant lipoprotein is a lipoprotein as an 25 intermediate form produced by metabolism of CM or VLDL (triglyceride (TG)-rich lipoproteins) in blood due to enzymes such as lipoprotein lipase (LPL) and the like. For example, an intermediate metabolite on conversion of VLDL to LDL is VLDL remnant, and similarly, a metabolite of CM is CM remnant. 30 For production of remnant lipoproteins, two main routes can be mentioned. First, CM that transports exogenous fat is produced in the small intestine, flows through mesenteric lymph node and flows into blood from the thoracic duct. The CM in blood flow is subject to the 1A action of LPL, and TG in CM particle is hydrolyzed to produce CM remnant. On the other hand, VLDL that transports endogenous fat is produced in the liver and directly released into 5 the blood from the liver. Thereafter, like CM, TG is dissociated from VLDL due to the action of LPL, and VLDL remnant is produced. These remnant lipoproteins are clinically important as arteriosclerosis-promoting lipoproteins. 10 Hyperlipidemia of the type associated with increased remnant lipoprotein in fasting serum in the early morning is called hyper-remnant lipoproteinemia. The hyper-remnant lipoproteinemia includes hereditary hyper-remnant lipoproteinemia such as familial 15 dysbetalipidemia, familial lipase deficiency, familial combined hyperlipidemia and the like, and secondary hyper remnant lipoproteinemia that expresses subsequent to diabetic hypertriglyceridemia, hypothyroidism, nephritic syndrome and the like. 20 Many lipoproteins are considered to be capable of causing arteriosclerosis, intraarterial thrombosis, coronary artery diseases and the like. Particularly, remnant lipoprotein is considered to be deeply involved in the formation of arteriosclerotic lesion, because, unlike 25 LDL etc., it is englobed by macrophage and promotes foaming, without undergoing further modification. In contrast, it is known that CETP is involved in the metabolism of lipoproteins in plasma physiologically, and of those, particularly involved strongly in the metabolism 30 of HDL. Inasmuch as HDL prevents accumulation of cholesterol in peripheral cells through the actions of cholesterol uptake and antioxidation, it is considered to be a lipoprotein that acts defensively against arteriosclerosis. In fact, a number of epidemiological 35 researches have shown that a decrease in CE (cholesteryl C:VDocumens and SettingsahedVLocal 2ttngsVTemporary Intemet FileaVOLK85VSpeelfication of AU2008201550 (changes tracked) (2).doc ester) of HDL in blood is one of the risk factors of coronary artery diseases. It has been also clarified that the CETP activity varies among animal species, wherein arteriosclerosis due to cholesterol-loading is hardly 5 induced in animals with lower CETP activity, and in reverse, easily induced in animals with higher CETP activity, and that hyper-HDL-cholesterolemia and hypo-LDL (low density lipoprotein)-cholesterolemia are induced in the case of CETP deficiency, thus rendering the development of 10 arteriosclerosis difficult, which in turn led to the recognition of the significance of blood HDL, as well as significance of CETP as a risk factor of arteriosclerosis. The remnant lipoprotein is known to have, besides macrophage foaming-promoting action, plural actions 15 leading to the onset and progression of arteriosclerosis, such as platelet aggregation-promoting action, inhibitory action on endothelium-dependent vascular relaxing response and the like. In fact, increase in the remnant lipoprotein is reported to increase coronary artery events 20 and sudden cardiac death. Meanwhile, blood concentration of remnant lipoprotein is known to show a strong positive correlation with blood concentration of small dense LDL, which is said to be a very bad lipoprotein, and it is widely recognized that lowering blood concentration of 25 remnant lipoprotein is highly useful for the prophylaxis or treatment of arteriosclerosis. However, while involvement of LPL in the remnant lipoprotein production has been pointed out, nothing else is known. Since, when the fat compositions of CM/VLDL and 30 remnant lipoprotein are compared, remnant lipoproteins show increased CE content and decreased TG content as compared to CM/VLDL, there is a possibility that transfer of CE in HDL to CM/VLDL due to CETP and transfer of TG in CM/VLDL to HDL may lead to the production of remnant 35 lipoproteins (see NIPPONRINSHO vol. 59, extra number 2 C.Docments and Sesng aheadLocal tngsWTemporary Intrmet FiesaOLKB5WSpeafictidon of AU2008201550 (changes tracked) (2).doc (2001), pp. 545-549). However, transfer of CE in HDL to CM/VLDL due to CETP, which leads to the production of remnant lipoprotein, has not been demonstrated, and there is no experimental proof of this 5 action. A reference herein to a patent document or other matter which is given as prior art is not to be taken as an admission that that document or matter was known or that the information it contains was part of the common general 10 knowledge as at the priority date of any of the claims. Disclosure of the Invention An aspect of the present invention is to provide a method of inhibiting remnant lipoprotein production, which comprises administering a compound having a CETP inhibitory 15 activity to an administration subject, and a remnant lipoprotein production inhibitor comprising a compound having a CETP inhibitory activity as an active ingredient. A further aspect is to provide a prophylactic or therapeutic agent for hyper-remnant lipoproteinemia and the 20 like, which comprises such compound having a CETP inhibitory activity as an active ingredient. The present inventors have conducted intensive studies to achieve the above-mentioned aspects and actually found that CETP transfers CE in HDL to CM and/or VLDL to promote of 25 remnant lipoprotein production. Moreover, they have found that a CETP inhibitor inhibits transfer of CE in HDL to CM and/or VLDL and inhibits of remnant lipoprotein production, which resulted in the completion of the present invention. That is, the present invention provides the following. 30 In a first aspect the invention relates to a method for treating or preventing hyper-remnant lipoproteinemia in a patient, which method comprises administering an effective amount of a compound having a CETP inhibitory activity, wherein said compound is trans-(4-{ [N-(2-{ [N'-[3,5 4 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, together with a pharmaceutically 5 acceptable carrier to the patient. In a second aspect the invention relates to use of an effective amount of trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyll-5-methyl-4-trifluoromethylphenyl)-N 10 ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier in the preparation of a medicament for the treatment or prevention of hyper-remnant lipoproteinemia in a patient. 15 In a third aspect the invention relates to a method for inhibit transfer of cholesteryl ester in HDL to chylomicron and/or VLDL which method comprises administering an effective amount of trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 20 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier to an administration subject. In a fourth aspect the invention relates to the use of a 25 compound of trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof in the preparation of a medicament to 30 inhibit transfer of cholesteryl ester in HDL to chylomicron and/or VLDL. Preferably in the method of the first aspect the trans 5 (4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl 2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, inhibits 5 the production of chylomicron remnant, more preferably a VLDL remnant. Preferably in the use of the second aspect the trans-(4 {[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl) 10 N-ethylamino]methyllcyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, inhibits the production of chylomicron remnant, more preferably VLDL remnant. In a fifth aspect the invention relates to an inhibitor 15 of transfer of cholesteryl ester in HDL to chylomicron and/or VLDL, which comprises a compound of trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically 20 acceptable salt thereof having a CETP inhibitory activity as an active ingredient. Preferably in the inhibitor of the fifth aspect the compound having CETP inhibitory activity has a remnant lipoprotein production inhibitory activity. Preferably the 25 remnant lipoprotein is a chylomicron remnant or a VLDL remnant. In a further aspect the invention relates to an agent when used for the treatment or prophylaxis of hyper-remnant lipoproteinemia in a patient, which comprises a compound of trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 30 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically 6 acceptable salt thereof having a CETP inhibitory activity as an active ingredient. Compounds having a CETP inhibitory activity may also include S-{2-([[l-(2-ethylbutyl)cyclohexyl]carbonyl]amino) 5 phenyl} 2-methylpropanethioate. The inhibitor may also be S-{2-([[1-(2 ethylbutyl)cyclohexyl]carbonyl]amino)phenyl} 2 methylpropanethioate. The compound having a CETP inhibitory activity may also 6a be ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)benzyl] (methoxycarbonyl)amino]-2-ethyl-6-(trifluoromethyl)-3,4 dihydroquinoline-1(2H)-carboxylic acid ester, an anhydride thereof, an ethanolate thereof, or a crystal thereof. 5 The inhibitor may also include the compound having a CETP inhibitory activity being ethyl (2R,4S)-4-[[3,5 bis(trifluoromethyl)benzyl](methoxycarbonyl)amino]-2-ethyl-6 (trifluoromethyl)-3,4-dihydroquinoline-l(2H)-carboxylic acid ester, an anhydride thereof, an ethanolate thereof, or a 10 crystal thereof. The inhibitor may also be ethyl (2R,4S)-4-[[3,5 bis(trifluoromethyl)benzyl]-(methoxycarbonyl)amino]-2-ethyl 6-(trifluoromethyl)-3,4-dihydroquinoline-l(2H)-carboxylic acid ester, an anhydride thereof, an ethanolate thereof, or a 15 crystal thereof. The method may also include the compound having a CETP inhibitory activity being methyl (3-cyano-5 trifluoromethylbenzyl)-[6-(N-cyclopentyl- methyl-N ethylamino)indan-5-ylmethyl)-carbamate. 20 The inhibitor may also include the compound having a CETP inhibitory activity being methyl (3-cyano-5 trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N ethylamino)indan-5-ylmethyl]-carbamate. The inhibitor may also be methyl (3-cyano-5 25 trifluoromethylbenzyl)-[6-(N-cyclopentyl- methyl-N ethylamino)indan-5-ylmethyl]-carbamate. The compound having a CETP inhibitory activity may also be trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 30 trifluoromethylphenyl)-N-ethylamino]methyllcyclohexyl)acetic acid methanesulfonate. C:Voocumr .ts end Seingsahe.dV.. oc., ettngskremporary Intemet Files*OLK85VSpecification of AU2008201550 (changes tracked) (2).doc The inhibitor may also include the compound having a CETP inhibitory activity being trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethyl- phenyl)-N 5 ethylaminolmethyl}cyclohexyl)acetic acid methanesulfonate. The method may also include the compound having a CETP inhibitory activity being a compound represented by the formula (VII) R-YN NH X1 z X2 X4

X

3 10 wherein R is a straight chain or branched C 1

-

10 alkyl group, a straight chain or branched C2- 10 alkenyl group, a halogenated C1- 4 lower alkyl group, an optionally substituted C3- 10 cycloalkyl group, an optionally substituted C 5

-

8 cycloalkenyl 15 group, an optionally substituted C3- 10 cycloalkyl C 1

-

10 alkyl group, an optionally substituted aryl group, an optionally substituted aralkyl group or an optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom; 20 X 1 , X 2 , X3 and X 4 are the same or different and each is a hydrogen atom, a halogen atom, a C1-4 lower alkyl group, a halogenated C1-4 lower alkyl group, a C1-4 lower alkoxy group, a cyano group, a nitro group, an acyl group or an aryl 25 group; Y is -CO- or -SO 2 -; and Z is a hydrogen atom or a mercapto protecting group, a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. 30 The inhibitor may also include the compound having a C Docment and Smrmgeaneam 1oa 1ttngsvTemporary Intrnet FiT.sVOLK85VSpecfiction ol AU2008201550 (change tracked) (2).doc CETP inhibitory activity being a compound of the formula (VII), a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. 5 The inhibitor may also be compound of the formula (VII), a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. The method may also include the compound having a CETP inhibitory activity being a compound represented by the 10 formula (VIII) R--YN NH I VI(V) X2 X4

X

3 wherein R is a straight chain or branched Ci_ 10 alkyl group, a straight chain or branched C2-o alkenyl group, a 15 halogenated C1-4 lower alkyl group, a C3-10 cycloalkyl group, a Cs-8 cycloalkenyl group, a C3-10 cycloalkyl Cl-10 alkyl group (wherein these cycloalkyl group, cycloalkenyl group and cycloalkylalkyl group are each optionally 20 substituted by a group selected from straight chain or branched C1-10 alkyl group, straight chain or branched C2-10 alkenyl group, C310 cycloalkyl group, C5-8 cycloalkenyl group, C3-10 cycloalkyl C 1

-

10 alkyl group, aryl group, amino group, C1-4 lower 25 alkylamino group, acylamino group, oxo group, aralkyl group and arylalkenyl group), an aryl group, an aralkyl group or a 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom (wherein these aryl group, aralkyl 30 group and heterocyclic group are each optionally substituted by a group selected from straight chain CVDom enta and SetngsIaheadILoc ngsVTemporary Intemet FilasIOLKB5VSpeafication of AU2008201550 (changes tracked) (2).doc or branched Cl-io alkyl group, straight chain or branched C2-10 alkenyl group, halogen atom, nitro group, amino group optionally substituted by C1-4 lower alkyl group or acyl group, hydroxyl group, 5 C14 lower alkoxy group, C14 lower alkylthio group, halogenated C1-4 lower alkyl group, acyl group and oxo group);

X

1 , X 2 , X 3 and X 4 may be the same or different and each is a hydrogen 20 atom, a halogen atom, a C1-4 lower alkyl group, a halogenated C1-4 lower alkyl group, a C1-4 lower alkoxy group, a cyano group, a nitro group, an acyl group or an aryl group; Y is -CO- or -SO 2 -; 15 Z is a hydrogen atom or a mercapto-protecting group selected from a group that forms a disulfide form, which is a dimer, C1-4 lower alkoxymethyl group, C1-4 lower alkylthiomethyl group, aralkyloxymethyl group, aralkylthiomethyl group, C3-10 cycloalkyloxymethyl 20 group, C5-8 cycloalkenyloxymethyl group, C3-10 cycloalkyl Cli-o alkoxymethyl group, aryloxymethyl group, arylthiomethyl group, acyl group, acyloxy group, aminocarbonyloxymethyl group, thiocarbonyl group 25 and thio group, a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula 30 (VIII), a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. The inhibitor may also be a compound of the formula (VIII), a prodrug compound thereof, a pharmaceutically 35 acceptable salt thereof, or a hydrate thereof or a solvate cywooc.merft and So..gs.a.me IocseingTemporary intemet Filos-OLKB5VSpeciflc.ton of AU2008201550 (change tracked) (2).doc thereof. The method may also include the compound of the formula (VIII) being a compound selected from a group consisting of 5 bis-[2-(pivaloylamino)phenyl]disulfide; bis-[2-(2 propylpentanoylamino)phenyl]disulfide; bis-[2-(l methylcyclohexanecarbonylamino)phenyl]disulfide; bis-[2 (1-isopentylcyclopentanecarbonylamino)phenyl]disulfide; bis-[2-(1 2o isopentylcyclohexanecarbonylamino)phenyl]disulfide; N-(2 mercaptophenyl)-2,2-dimethylpropionamide; N-(2 mercaptophenyl)-1-isopentylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-methylcyclohexanecarboxamide; N-(2 mercaptophenyl)-l-isopentylcyclopentanecarboxamide; N-(2 15 mercaptophenyl)-l-isopropylcyclohexanecarboxamide; N-(4,5 dichloro-2-mercaptophenyl)-1 isopentylcyclohexanecarboxamide; N-(4,5-dichloro-2 mercaptophenyl)-l-isopentylcyclopentanecarboxamide; N-(2 mercapto-5-methylphenyl)-1 20 isopentylcyclohexanecarboxamide; N-(2-mercapto-4 methylphenyl)-1 isopentylcyclohexanecarboxamide; thioacetic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl) ester; 2,2 dimethylthiopropionic acid S-[2-(l 25 methylcyclohexanecarbonylamino)phenyl] ester; phenylthioacetic acid S-[2-(pivaloylamino)phenyl] ester; 2,2-dimethylthiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 acetylamino-3-phenylthiopropionic acid S-[2-(1 30 isopentylcyclohexanecarbonylamino)phenyl] ester; 3 pyridinethiocarboxylic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; chlorothioacetic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl] ester; 35 methoxythioacetic acid S-[2-(l C:VDocuments a SetingsvaheadVLo S ngsVemporry Intemot FIle.sOLK85VSpecflcation of AU2008201550 (changes tracked) (2).doc isopentylcyclohexanecarbonylamino)phenyl) ester; thiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; phenoxythioacetic acid S-[2-(l 5 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 methylthiopropionic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl] ester; 4 chlorophenoxythioacetic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 10 cyclopropanethiocarboxylic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl) ester; 2 acetylamino-4-carbamoylthiobutyric acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 hydroxy-2-methylthiopropionic acid S-[2-(1 15 isopentylcyclohexanecarbonylamino)phenyl) ester; 2,2 dimethylthiopropionic acid S-[2-(1 isopentylcyclopentanecarbonylamino)phenyl] ester; thioacetic acid S-[2-(l isopentylcyclopentanecarbonylamino)phenyl] ester; 2,2 20 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(l isopentylcyclopentanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[2-(1 25 isopentylcyclohexanecarbonylamino)-4 trifluoromethylphenyl] ester; thiocarbonic acid 0-methyl ester S-[2-(l-isopentylcyclohexanecarbonylamino)phenyl] ester; dithiocarbonic acid S-[2-(l methylcyclohexanecarbonylamino)phenyl] ester S-phenyl 30 ester; N-phenylthiocarbamic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[2-(pivaloylamino)-4 trifluoromethylphenyl] ester; 2,2-dimethylthiopropionic acid S-[4,5-dichloro-2-(1 35 cyclopropylcyclohexanecarbonylamino)phenyl] ester; 2,2 C:cD m.t,.s .n S ..mng.saiLe caS Temgporw y IntemetFmesOLK85Specdicaton of AU2008201550 (change tracKed) (2).doc dimethylthiopropionic acid S-[4,5-dichloro-2-(2 cyclohexylpropionylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 pentylcyclohexanecarbonylamino)phenyl] ester; 2,2 5 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 cyclopropylmethylcyclohexanecarbonylamino)phenyl] ester; 2,2-dimethylthiopropionic acid S-[4,5-dichloro-2-(1 cyclohexylmethylcyclohexanecarbonylamino)phenyl] ester; 2,2-dimethylthiopropionic acid S-[4,5-dichloro-2-(1 10 isopropylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopentylcycloheptanecarbonylamino)phenyl) ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopentylcyclobutanecarbonylamino)phenyl] ester; 2,2 15 dimethylthiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)-4-nitrophenyl] ester; 2,2-dimethylthiopropionic acid S-[4-cyano-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4-chloro-2-(1 20 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[5-chloro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4-fluoro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 25 dimethylthiopropionic acid S-[4,5-difluoro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[5-fluoro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; bis-[4,5 dichloro-2-(1-isopentylcyclohexanecarbonylamino)phenyl] 30 disulfide; 2-tetrahydrofurylmethyl 2-(1 isopentylcyclohexanecarbonylamino)phenyl disulfide; N-(2 mercaptophenyl)-1-ethylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-propylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-butylcyclohexanecarboxamide; N-(2 35 mercaptophenyl)-1-isobutylcyclohexanecarboxamide; C:VDocuments and SettingsvahadVLOcuS JngsVTemporawy Inemet FilMswOLX851Spcfcation of AU2008201550 (change tracked) (2).doc cyclohexanethiocarboxylic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; thiobenzoic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl] ester; 5 5 carboxythiopentanoic acid S-[2-(l isopentylcyclohexanecarbonylamino)phenyl] ester; thioacetic acid S-[2-(l isopentylcyclohexanecarbonylamino)-4-methylphenyl] ester; bis-[2-[1-(2-ethylbutyl)cyclohexanecarbonylaminophenyl] 10 disulfide; N-(2-mercaptophenyl)-l-(2 ethylbutyl)cyclohexanecarboxamide; 2-methylthiopropionic acid S-[2-[1-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 2 methylthiopropionic acid S-[2-(1 15 isobutylcyclohexanecarbonylamino)phenyl] ester; 1 acetylpiperidine-4-thiocarboxylic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; thioacetic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 2,2 20 dimethylthiopropionic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; methoxythioacetic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 2 hydroxy-2-methylthiopropionic acid S-[2-[1-(2 25 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 4 chlorophenoxythioacetic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 4 chlorophenoxythioacetic acid S-[2-(1 isobutylcyclohexanecarbonylamino)phenyl] ester; and 1 30 acetylpiperidine-4-thiocarboxylic acid S-[2-(l isobutylcyclohexanecarbonylamino)phenyl] ester, a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. The inhibitor may also be the compound of the formula 35 (VIII) is a compound selected from a group consisting of C:Vocument and SettingaNaheadVncSSngsTemporary intomet FdoeOLK854Specification of AU2008201550 (changes tracked) (2).doc bis-[2-(pivaloylamino)phenyl] disulfide; bis-[2-(2 propylpentanoylamino)phenyl] disulfide; bis-[2-(1 methylcyclohexanecarbonylamino)phenyl] disulfide; bis-[2-(1 isopentylcyclopentanecarbonylamino)phenyl] disulfide; bis 5 [2-(1-isopentylcyclohexanecarbonylamino)phenyl] disulfide; N-(2-mercaptophenyl)-2,2-dimethylpropionamide; N-(2 mercaptophenyl)-1-isopentylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-methylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-isopentylcyclopentanecarboxamide; N-(2 10 mercaptophenyl)-1-isopropylcyclohexanecarboxamide; N-(4,5 dichloro-2-mercaptophenyl)-1 isopentylcyclohexanecarboxamide; N-(4,5-dichloro-2 mercaptophenyl)-1-isopentylcyclopentanecarboxamide; N-(2 mercapto-5-methylphenyl)-1-isopentylcyclohexanecarboxamide; 15 N-(2-mercapto-4-methylphenyl)-1 isopentylcyclohexanecarboxamide; thioacetic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[2-(1 methylcyclohexanecarbonylamino)phenyl] ester; 20 phenylthioacetic acid S-[2-(pivaloylamino)phenyl] ester; 2,2-dimethylthiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 acetylamino-3-phenylthiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 3 25 pyridinethiocarboxylic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; chlorothioacetic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; methoxythioacetic acid S-[2-(1 30 isopentylcyclohexanecarbonylamino)phenyl) ester; thiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; phenoxythioacetic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 35 methylthiopropionic acid S-[2-(1 C oco.nts s.d So n.Mn. hom W~ ngsyTemporary Intenet FilsOOLK5VSpecification of AU2008201550 (changes tracked) (2).doc isopentylcyclohexanecarbonylamino)phenyl] ester; 4 chlorophenoxythioacetic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; cyclopropanethiocarboxylic acid S-[2-(l 5 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 acetylamino-4-carbamoylthiobutyric acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2 hydroxy-2-methylthiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 10 dimethylthiopropionic acid S-[2-(1 isopentylcyclopentanecarbonylamino)phenyl] ester; thioacetic acid S-[2-(1 isopentylcyclopentanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 15 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopentylcyclopentanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[2-(1 isopentylcyclohexanecarbonylamino)-4 20 trifluoromethylphenyl] ester; thiocarbonic acid 0-methyl ester S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl] ester; dithiocarbonic acid S-[2-(l methylcyclohexanecarbonylamino)phenyl] ester S-phenyl ester; N-phenylthiocarbamic acid S-[2-(l 25 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[2-(pivaloylamino)-4 trifluoromethylphenyl] ester; 2,2-dimethylthiopropionic acid S-[4,5-dichloro-2-(l cyclopropylcyclohexanecarbonylamino)phenyl] ester; 2,2 30 dimethylthiopropionic acid S-[4,5-dichloro-2-(2 cyclohexylpropionylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 pentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(l 35 cyclopropylmethylcyclohexanecarbonylamino)phenyl] ester; C:VDocuments and SetngsVaheaSdVoc ~ngsTe nporary Intemet Files&OLK85VSpecication of AU2008201550 (changes tracked) (2) doc 2,2-dimethylthiopropionic acid S-[4,5-dichloro-2-(1 cyclohexylmethylcyclohexanecarbonylamino)phenyl] ester; 2,2-dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopropylcyclohexanecarbonylamino)phenyl] ester; 2,2 5 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopentylcycloheptanecarbonylamino)phenyl) ester; 2,2 dimethylthiopropionic acid S-[4,5-dichloro-2-(1 isopentylcyclobutanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[2-(1 10 isopentylcyclohexanecarbonylamino)-4-nitrophenyl] ester; 2,2-dimethylthiopropionic acid S-[4-cyano-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4-chloro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 15 dimethylthiopropionic acid S-[5-chloro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4-fluoro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[4,5-difluoro-2-(1 20 isopentylcyclohexanecarbonylamino)phenyl] ester; 2,2 dimethylthiopropionic acid S-[5-fluoro-2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; bis-[4,5 dichloro-2-(1-isopentylcyclohexanecarbonylamino)phenyl) disulfide; 2-tetrahydrofurylmethyl 2-(1 25 isopentylcyclohexanecarbonylamino)phenyl disulfide; N-(2 mercaptophenyl)-1-ethylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-propylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-butylcyclohexanecarboxamide; N-(2 mercaptophenyl)-1-isobutylcyclohexanecarboxamide; 30 cyclohexanethiocarboxylic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; thiobenzoic acid S-[2-(1 isopentylcyclohexanecarbonylamino)phenyl] ester; 5 carboxythiopentanoic acid S-[2-(1 35 isopentylcyclohexanecarbonylamino)phenyl] ester; C: Documents and Sottngs aadVoc SorngsvTporay Intemet FilesOLK85VSpedficaton of AU2008201550(changes tracked) (2).doc thioacetic acid S-[2-(l-isopentylcyclohexanecarbonylamino)-4 methylphenyl] ester; bis-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] disulfide; N-(2 mercaptophenyl)-1-(2-ethylbutyl)cyclohexanecarboxamide; 2 5 methylthiopropionic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 2 methylthiopropionic acid S-[2-(l isobutylcyclohexanecarbonylamino)phenyl] ester; 1 acetylpiperidine-4-thiocarboxylic acid S-[2-[l-(2 10 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; thioacetic acid S-[2-[1-(2-ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 2,2-dimethylthiopropionic acid S-[2-[l-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; methoxythioacetic acid S-[2-[l-(2 15 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 2-hydroxy-2 methylthiopropionic acid S-[2-[1-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 4 chlorophenoxythioacetic acid S-[2-[1-(2 ethylbutyl)cyclohexanecarbonylamino]phenyl] ester; 4 20 chlorophenoxythioacetic acid S-[2-(l isobutylcyclohexanecarbonylamino)phenyl] ester; and 1 acetylpiperidine-4-thiocarboxylic acid S-[2-(1 isobutylcyclohexanecarbonylamino)phenyl] ester, a prodrug compound thereof, a pharmaceutically acceptable salt thereof, 25 or a hydrate thereof or a solvate thereof. In a sixth aspect the invention relates to a method for treating or preventing hyper-remnant lipoproteinemia in a patient, which method comprises administering to the patient an effective amount of a compound having a CETP inhibitory 30 activity, wherein said compound is represented by the formula (IX) 18 (R)n B N (X) A R R 5

R

4 wherein RI and R 2 are the same or different and each is a halogen atom, a nitro group, a cyano group or a C1-6 alkyl 5 group optionally substituted by halogen atom;

R

3 , R 4 and R 5 are the same or different and each is a hydrogen atom, a halogen atom, a Ci-6 alkyl group optionally substituted by halogen atom, a C1-6 alkylthio group optionally substituted by halogen atom or a C1-6 alkoxy group optionally 10 substituted by halogen atom, or R 3 and R 4 or R 4 and R 5 may form, together with a carbon atom they are bonded to, a homocyclic ring optionally having substituent(s) or a heterocyclic ring optionally having substituent(s); A is 15 -N(R ) (R8) (wherein R7 and R8 are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein CI-6 alkyl group is optionally substituted by phenyl group or

-(CH

2 )m-COOR 9 (wherein R 9 is a hydrogen atom or a C1-6 alkyl group and m is 0 or an integer of 1 to 5)) or a C4-io 20 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C1-6 alkoxy group, C1-6 alkyl group (wherein Ci-6 alkyl group is optionally substituted by hydroxyl group, C1-6 25 alkoxy group or phosphono group), -(CH2)q-CON(R 2) (R21) C VDocuments and SettingwahedVLa S ngswromporary Intemot FeswOLK8S5Specificfion of AU2008201550 (changes traed) (2).doc (wherein R20 and R are the same or different and each is hydrogen atom or C1-6 alkyl group and q is 0 or an integer of 1 to 5) or -(CH2)r-COOR' 0 (wherein R1 0 is hydrogen atom or C1-6 alkyl group and r is 0 or an integer of 1 to 5)), 5 -C(R ) (R ) (R") (wherein R , R1 and R are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by phenyl group or -COOR9 (wherein R 9 is as defined above) ) or a C4-10 cycloalkylalkyl group (wherein C4-io cycloalkylalkyl group is 10 optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C1-6 alkoxy group, C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group, C1-6 alkoxy group or phosphono group), -(CH 2 )q-CON(R20) (R 2) (wherein 15 R 20 , R21 and q are as defined above) or -(CH 2 )r-COOR1 0 (wherein R and r are as defined above))) or -0-C(R ) (R ) (R 3) (wherein 11 12 13 R , R and R are as defined above); ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, an 20 amino group, a hydroxyl group, a cyano group, an acyl group, a C1-6 alkoxy group, a C2-6 alkenyl group or a Ci-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group or -COOR" (wherein R1 4 is a hydrogen atom or a C1-6 alkyl group)); and 25 n is an integer of 1 to 3 or a prodrug thereof or a pharmaceutically acceptable salt thereof. In a seventh aspect the present invention relates to use of an effective amount of a compound having CETP inhibitory 30 activity in the preparation of a medicament for the treatment or prevention of hyper-remnant lipoproteinemia in a patient, wherein said compound is represented by the formula (IX) 20 (R6)n B N (IX) A R R 5

R

4 wherein Ri and R 2 are the same or different and each is a halogen 5 atom, a nitro group, a cyano group or a C1-6 alkyl group optionally substituted by halogen atom;

R

3 , R 4 and Rs are the same or different and each is a hydrogen atom, a halogen atom, a C 1

-

6 alkyl group optionally 10 substituted by halogen atom, a C1-6 alkylthio group optionally substituted by halogen atom or a C1-6 alkoxy group optionally substituted by halogen atom, or R 3 and R 4 or R 4 and R 5 may form, together with a carbon atom they are bonded to, a 15 homocyclic ring optionally having substituent(s) or a heterocyclic ring optionally having substituent(s); A is -N(R7) (R8) (wherein R and R8 are the same or different and each is a hydrogen atom, a C1-6 alkyl 20 group (wherein C1-6 alkyl group is optionally substituted by phenyl group or

-(CH

2 )m-COOR 9 (wherein R 9 is a hydrogen atom or a C1 6 alkyl group and m is 0 or an integer of 1 to 5)) or a C4-10 cycloalkylalkyl group (wherein C4-10 25 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C1-6 alkoxy group, C1-6 alkyl group (wherein C WDomments and S. ngawaheadLocQingsMTemporary Intenet FilsOLK85USpcflicaion of AU2008201550 (changes tracked} (2).doc Ci-6 alkyl group is optionally substituted by hydroxyl group, Ci-6 alkoxy group or phosphono 20) 21) 20 21 group) , - (CH 2 ) q-CON (R ) (R ) (wherein R20 and R are the same or different and each is hydrogen atom or 5 C1-6 alkyl group and q is 0 or an integer of 1 to 5) or -(CH 2 ) r-COOR 10 (wherein R 10 is hydrogen atom or C1-6 alkyl group and r is 0 or an integer of 1 to 5)), -C(Ru) (R1) (R") (wherein R11, R and R are the same or different and each is a hydrogen atom, 10 a C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by phenyl group or -COOR 9 (wherein R 9 is as defined above) ) or a C4-10 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl group is optionally substituted by 1 to 3 15 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C1-6 alkoxy group, Ci-6 alkyl group (wherein Ci-6 alkyl group is optionally substituted by hydroxyl group, C1-6 alkoxy group or phosphono 2020) 21) 20 21 20 group) , - (CH2) q-CON( ) (R ) (wherein R , R and q are as defined above) or -(CH 2 )r-COOR' 0 (wherein R 10 and r are as defined above))) or -0 C (R") (R1) (R") (wherein R11, R and R3 are as defined above) ; 25 ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, an amino group, a hydroxyl group, a cyano group, an acyl group, a C1-6 alkoxy group, a C2-6 alkenyl group or a C1-6 alkyl group (wherein C1-6 alkyl group is 30 optionally substituted by hydroxyl group or -COOR 14 (wherein R is a hydrogen atom or a C1-6 alkyl group)); and n is an integer of 1 to 3 or a prodrug thereof or a pharmaceutically acceptable salt 35 thereof. C :Documents anid SttigsvaheadV ngsWTemporary Intenet FBeWOU.K85VSpecflcaticn of AU2008201550 (chwa tracked) (2).doc In a preferred aspect the compound of the formula (IX) is a compound selected from a group consisting of N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-[3,5 5 bis(trifluoromethyl)benzyl]-(2-methyl-2H-tetrazol-5 yl)amine, 3-{[N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-(2-methyl-2H-tetrazol 5-yl)amino)methyl}-5-trifluoromethylbenzonitrile, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2 methyl-2H-tetrazol-5-yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2 15 methyl-2H-tetrazol-5-yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(2H-tetrazol-5-yl)-[3,5 bis(trifluoromethyl)benzyl]amine, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 20 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl]-(pyrimidin-2 yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl]-(5-methyl-lH pyrazol-3-yl)amine, 25 5-{N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino}pentanoic acid hydrochloride, methyl trans-4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 30 yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl cyclohexanecarboxylate, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyll-N-(2-methyl-2H-tetrazol-5-yl)amino]methyll-5 trifluoromethylbenzonitrile, 35 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' C Documenits and Sotng.ah..dVaoc!gngsTomporary Intenet Filos&OLKB5OSpecfication of AU2008201550 {chang.8 tracked) (2).doc cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2 ethyl-2H-tetrazol-5-yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1 5 methyl-1H-[1,2,4]triazol-3-yl)amine, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-phenylamino}methyl)-5 trifluoromethylbenzonitrile, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 10 ylmethyl]-N-(4,5-dimethylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl) (thiazol-2-yl)amine hydrochloride, 15 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(thiazol-2-yl)amino}methyl)-5 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(oxazol 20 2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 25 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4,5 dimethylthiazol-2-yl)amine hydrochloride, 30 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan- 5 ylmethyl]-N-(5-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(4-methylthiazol-2-yl)amino]methyl}-5 35 trifluoromethylbenzonitrile hydrochloride, CVD m.en e a S. .V.m... c ungyTe mporary Intomet Fl OLKB5USpecifIcation of AU2008201550(change tracked) (2) doc N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyll-(4 methyloxazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 5 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-(3 methylisothiazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-(5 methylisoxazol-3-yl)amine hydrochloride, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 methylisoxazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1 15 methyl-1H-pyrazol-3-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1 methyl-1H-pyrazol-4-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 20 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methyl-[1,3,4]thiadiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methyl-[l,3,4]oxadiazol-2-yl)amine hydrochloride, 25 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-pyridin 3-ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-pyridin 30 2-ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl)-N-[2-(N' cyclopentylmethyl-N'-ethylamino)-5-trifluoromethylbenzyl] (2-methyl-2H-tetrazol-5-yl)amine hydrochloride, 3-{[N-[2-(N'-cyclopentylmethyl-N'-ethylamino)-5 35 trifluoromethylbenzyl]-N-(2-methyl-2H-tetrazol-5 C:VDocuments and Settingsvahe ngsTemporry Intermt FilesOLK85VSpecifiction of AU2008201550 (changes tracked) (2).doc yl)amino]methyl}-5-trifluoromethylbenzonitrile hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)aminolmethyl}indan-5-yl)-N 5 ethylamino]pentanoate hydrochloride, methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-ylmethyl) N-ethylamino]pentanoate hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (1-methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 15 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N 20 ethylaminolpentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, methyl trans-4-{[N-(3-{[N'-[3,5 25 bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino]methyl)cyclohexanecarboxylate hydrochloride, methyl trans-4-{[N-(3-{[N'-(3-cyano-5 trifluoromethylbenzyl)-N'-(1-methyl-lH-pyrazol-3 30 yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-pyrazol-3-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N 35 ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, CD"o"""a md """''"e** e ngsvTmporay IMemeit FlUVOLK85VSpecfication of AU2008201550 (changes tracked) (2).doc trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methyl-[1,2,4]oxadiazol-3-yl)amine hydrochloride, methyl trans-4-{[N-(6-{[N'-(3,5 bis(trifluoromethyl)benzyl]-N'-(1-methyl-1H-pyrazol-3 10 yl)amino]methyllindan-5-yl)-N ethylaminolmethyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 15 methyl trans-4-{[N-(6-{[N'-(3-cyano-5 trifluoromethylbenzyl)-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylate, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 20 (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 25 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 35 (1-methyl-lH-pyrazol-3-yl)amino]methyl)indan-5-yl)-N C:VDocuments and SettngsVahodLooe engs#Temporary Intemet FUesOLK85USpecificatlon of AU2008201550 (changes tracked) (2) doc ethylaminolpentanoate hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methyl-isoxazol-5-yl)amino]methyllindan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-1H-[1,2,4]triazol-3-yl)amino]methyllindan-5-yl)-N 10 ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methylIindan-5-yl) N-ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, 15 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-iH-[1,2,41triazol-3-yl)amino]methyl}indan-5-yl) N-ethylamino]methyl}cyclohexanecarboxylic acid, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 20 methyl-[1,2,4]thiadiazol-5-yl)amine, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 25 (1-methyl-1H-pyrazol-3-yl)amino]methyl)-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 30 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid 35 hydrochloride, C VDouments ad SettigsWahedW n;gyTemporary Intemewt FlIasVOLK95VSpecification of AU2008201550 (changes tracked) (2).doc 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylaminolpentanoic acid hydrochloride, 5 trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl)-5,6,7,8 15 tetrahydronaphthalen-2-yl)-N ethylamino]methyl }cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methyl)-5,6,7,8 tetrahydronaphthalen-2-yl)-N 20 ethylamino]methyl}cyclohexanecarboxylic acid, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (3-methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 25 trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (3-methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 2-(5-{N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 30 cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]amino}tetrazol-2-yl)ethanol hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate 35 hydrochloride, CADoam ent. .. d S aes.. oe, g ngsTemporary Intemet FiI.nOLK85*Specfction of AU2008201550 (changes tracked) (2).doc methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 5 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylaminolpentanoic acid hydrochloride, 5-[N-(3-{(N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l 10 methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6, 7 ,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyll-5,6,7,8 15 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid 20 hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 25 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 30 (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl) N-ethylamino]methyllcyclohexanecarboxylic acid, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl)-4 trifluoromethoxyphenyl)-N-ethylamino]pentanoic acid 35 hydrochloride, C*om""t" a" " Se'"" ''e' * oc"" ingsgTemporary Intemet FIIesvOLKS5VSpecification of AU2008201550 (changes tracked) (2).doc 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl)-4 trifluoromethylphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5 5-[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-ethyl 2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 15 ethylaminolpentanoic acid hydrochloride, 5-{N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5-yl]-N ethylaminolpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 20 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 25 ethylamino]-2,2-dimethylpentanoic acid hydrochloride, 6-[N-(6-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N ethylamino]-hexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 30 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 35 (1-{2-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 Cocumn ets and Se totngsahea o U ngsMTemporary Intemet Files&OLK85VSpecificaton of AU2008201550 (changes trackod) (2).doc methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]ethylicyclopentyl)acetic acid hydrochloride, trans-4-({N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5 5 yl]-N-ethylamino}methyl)cyclohexanecarboxylic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 10 (1-{2-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)aminolmethyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]ethyl}cyclopentyl)acetic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 15 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 20 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-({N-[3-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yllamino}methyl) 5,6,7,8-tetrahydronaphthalen-2-yl]-N 25 ethylamino}methyl)cyclohexanecarboxylic acid hydrochloride, l-{3-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N ethylamino]propyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 30 methyl-lH-pyrazol-3-yl)amino]methyllindan-5-yl)-N ethylamino]-3,3-dimethylpentanoic acid, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 35 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 eoocX ... .nd Sutbnqsg a d..VL nsv onpary Inemet FdilsOLKB5VSpcilcation of AU2008201550 changeo tracked) (2) doc methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3 dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 5 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-4 10 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-1H-pyrazol-3-yl)amino]methyll-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3 15 dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyll-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3 dimethylpentanoic acid hydrochloride, 20 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 25 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]hexanoic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 30 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 35 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N C:VDocuments .nd Sathngaahea LocajgnsVTempory Intemet FilosOLK85VSpecifcation of AU2008201550 (changes tracked) (2).doc ethylamino]-3,3-dimethylhexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-4,4-dimethylpentanoic acid hydrochloride, 5 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl)-4 15 trifluoromethylphenyl)-N-ethylaminol-4,4-dimethylhexanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N 20 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, 25 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-5,5-dimethylhexanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (2-methyl-2H-tetrazol-5-yl)aminolmethyl}-4 30 trifluoromethoxyphenyl)-N propylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 35 trifluoromethoxyphenyl)-N C:VDocuents and SetngsVahaodVLoca TngsVTemporary Intemat FiesWOLKSVSpecIficaton of AU2008201550 (c ageas tracked) (2).doc isobutylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 5 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexanecarboxylic acid amide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl)-4 trifluoromethoxyphenyl)-N 10 ethylamino]methyl}cyclohexanecarboxylic acid methylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid dimethylamide, 15 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-chlorophenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N 20 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (m-tolyl)amino]methyl)-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{(N-(2-{[N'-(3,5-dichlorobenzyl)-N'-(2-methyl-2H 25 tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) N'-(3-methyl-5-trifluoromethylbenzyl)amino]methyl}-4 trifluoromethoxyphenyl)amino]methyl}cyclohexanecarboxylic 30 acid hydrochloride, trans-4-{[N-(2-{[N'-(3-chloro-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 35 trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) C:IfDocuents and SettingsgahemoadV iigsUmporary I ntemnot FilosMOLK85VSpecification of AU2008201550 (changesn tracked) (2) doc N'-(3-nitro-5-trifluoromethylbenzyl)amino]methyl}-4 trifluoromethoxyphenyl)amino]methyllcyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 5 (2-methyl-2H-tetrazol-5-yl)amino]methyll-2,2 difluorobenzo[1,3]dioxol-5-yl)-N ethylaminolmethyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 10 difluorobenzo[1,3]dioxol-5-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-3-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 15 ethylamino]methyl}cyclohexyl)propionic acid hydrochloride, trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3 tetrafluoro-2,3-dihydrobenzo[l,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, 20 trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3 tetrafluoro-2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-2-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl] 25 N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3 tetrafluoro-2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)acetamide hydrochloride, trans-N-[3,5-bis(trifluoromethyl)benzyl]-N-{2-[N'-ethyl N'-(4-(methoxymethyl)cyclohexylmethyl)amino]-5 30 trifluoromethoxybenzyl}-(2-methyl-2H-tetrazol-5-yl)amine hydrochloride, trans-2-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 35 ethylaminolmethyl}cyclohexyl)ethanol hydrochloride, C:VDocments and SetnSVaheadV ca ngsVTeporay Intem, FilesVOLK85VSpedccton of AU2008201550 (changes tracked) (2) doc trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, 5 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N ethylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 15 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexylmethyl)phosphonic acid, trans-4-{[N-(2-{[N'-(3-bromo-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 20 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4-bromophenyl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 25 (2-methyl-2H-tetrazol-5-yl)amino)methyl}-4-bromophenyl)-N ethylaminolmethyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol 30 hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-methoxyphenyl)amino]methyl)-4-trifluoromethoxyphenyl) N-ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 35 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' C:VDocuments and SotigsaheadVLoca e ingsVTemporary Intemet FiesOLK85VSpecffictIon of AU2008201550 (changes tracked) (2) doc (2-methyl-2H-tetrazol-5-yl)aminolmethyl}-5-methoxy-4 methylphenyl)-N-ethylamino]methyllcyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 5 (2-methyl-2H-tetrazol-5-yl)aminolmethyl}-4,5 dimethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 10 trifluoromethylthiophenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid 15 hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N propylamino]methyl}cyclohexyl)acetic acid hydrochloride, 20 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-4-({N-[2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' 25 (2-methyl-2H-tetrazol-5-yl)aminolmethyl}-4-(2,2,2 trifluoroethyl)phenyl]-N ethylamino}methyl) cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 30 trifluoromethylphenyl)-N propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 35 propylaminolmethyllcyclohexyl)acetic acid hydrochloride, CDocumets and SM .n.ahe.dVLoca1ng*Temporary Inemet FiVOLK85VSpecificaton of AU2008201550(ch a ng tracked) (2) doc trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-ethylphenyl)amino]methyl)-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' -5 (2-methyl-2H-tetrazol-5-yl)aminolmethyl}-4 trifluoromethoxyphenyl)-N ethylamino]methylIcyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-isopropenylphenyl)amino]methyll-4 10 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyllcyclohexyl)acetic acid dihydrochloride, 15 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 25 trifluoromethylphenyl)-N propylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N 30 propylamino]methyl)cyclohexyl)acetic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid, 35 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' CXDocoents and SeIngsvahneaMoca ngsITompr omet FdoseOLK85USpecnlcation of AU2008201550 (dnges tracked) (2).doc (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid methanesulfonate, ethyl trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 5 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyllcyclohexyl)acetate, and trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 10 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl) acetic acid, a prodrug thereof or a pharmaceutically acceptable salt thereof. In an eighth aspect the present invention relates to an agent when used for the treatment or prevention of hyper 15 remnant lipoproteinemia in a patient, which comprises a compound having CETP inhibitory activity and is selected from a group consisting of N-[3-(N'-cyclopentylmethyl-N'-ethylamino) 5,6,7,8-tetrahydronaphthalen-2-ylmethyl]-N-[3,5 bis(trifluoromethyl)benzyl]-(2-methyl-2H-tetrazol-5-yl)amine, 20 3-{[N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(2-methyl-2H-tetrazol-5 25 yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(2-methyl-2H-tetrazol-5 yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-N 30 (2H-tetrazol-5-yl)-[3,5-bis(trifluoromethyl)benzyl]amine, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-N [3,5-bis(trifluoromethyl)benzyl]-(pyrimidin-2-yl)amine hydrochloride 40 N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl]-(5-methyl-lH pyrazol-3-yl)amine, 5-{N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyllindan-5-yl)-N ethylamino}pentanoic acid hydrochloride, methyl trans-4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-4-trifluoromethoxyphenyl)-N 10 ethylamino]methyl}cyclohexanecarboxylate, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(2-methyl-2H-tetrazol-5-yl)amino]methyll-5 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 15 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2 ethyl-2H-tetrazol-5-yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1 methyl-lH-[1,2,4]triazol-3-yl)amine, 20 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-phenylamino}methyl)-5 trifluoromethylbenzonitrile, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(4,5-dimethylthiazol-2-yl)amino]methyl)-5 25 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl] (thiazol-2-yl)amine hydrochloride, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 30 ylmethyl]-N-(thiazol-2-yl)amino}methyl)-5 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(oxazol 2-yl)amine hydrochloride, 35 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' CWDocoments and S.oongswaheaLocalf ngsWeTnporary Internet FIIeswOLX85VSpooflcation of AU2008201550 (changes tracked) (2).doc cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 5 methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4,5 dimethylthiazol-2-yl)amine hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 10 ylmethyl]-N-(5-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(4-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, 15 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 methyloxazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 20 methylisothiazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methylisoxazol-3-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 25 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-(3 methylisoxazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1 methyl-lH-pyrazol-3-yl)amine hydrochloride, 30 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1 methyl-lH-pyrazol-4-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 35 methyl-[1,3,4]thiadiazol-2-yl)amine hydrochloride, CD**"'nt"a"n S 'gs'*headV"l"" * f ngsWTmporary Inteml FilesOLK8SSpocfcabon of AU2008201550 (changes tracked) (2) doc N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methyl-[1,3,4]oxadiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 5 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-pyridin 3-ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-pyridin 2-ylamine hydrochloride, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[2-(N' cyclopentylmethyl-N'-ethylamino)-5-trifluoromethylbenzyl] (2-methyl-2H-tetrazol-5-yl)amine hydrochloride, 3-{[N-[2-(N'-cyclopentylmethyl-N'-ethylamino)-5 trifluoromethylbenzyl]-N-(2-methyl-2H-tetrazol-5 15 yl)amino]methyl}-5-trifluoromethylbenzonitrile hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, 20 methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-ylmethyl) N-ethylamino]pentanoate hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N 25 ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 30 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 35 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 C:WDocurmns and SetingsWaheadwL.-ca ingswTempoary intemet FOesMOLK85WSpocification of AU20018201550 (changes tracked) (2).doc methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, methyl trans-4-{[N-(3-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(l-methyl-1H-pyrazol-3 5 yl)aminolmethyll-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylate hydrochloride, methyl trans-4-{ [N-(3-{[N'-(3-cyano-5 trifluoromethylbenzyl)-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyll-5,6,7,8-tetrahydronaphthalen-2-yl)-N 10 ethylamino]methyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 15 trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 20 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyll-(5 methyl-[1,2,4]oxadiazol-3-yl)amine hydrochloride, methyl trans-4-{[N-(6-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}indan-5-yl)-N 25 ethylamino]methyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methylIcyclohexanecarboxylic acid hydrochloride, methyl trans-4-{[N-(6-{[N'-(3-cyano-5 30 trifluoromethylbenzyl)-N'-(l-methyl-1H-pyrazol-3 yl)amino]methyllindan-5-yl)-N ethylamino]methyl cyclohexanecarboxylate, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N 35 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, C:4Docuents and SettingsvaheadVLoca ngsVTemporay intemet Fhes&OLK85VSpedficadon of AU2008201550 (changes traced) (2).doc trans-4-{[N-(6-{ [N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methylIcyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 5 (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methylIcyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 10 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyllindan-5-yl)-N 15 ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methyl-isoxazol-5-yl)amino]methyllindan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 20 methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoic acid hydrochloride, 25 trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl) N-ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 30 (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl)indan-5-yl) N-ethylamino]methyl}cyclohexanecarboxylic acid, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 methyl-[1,2,4]thiadiazol-5-yl)amine, 35 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l C:Vcumm...ts and SomngsaV oa.. oc IngaTemporary Intenet FdOOLKB5VSpecfication of AU2008201550 (changes tracked) (2).doc methyl-lH-[1,2,4]triazol-3-yl)amino]methyllindan-5-yl)-N ethylamino]pentanoic acid hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 5 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate 10 hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylaminolpentanoic acid hydrochloride, 15 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid, 35 trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' C:Vocunents and SetngsaheadWLon ngdTemporary Inteonet FlesVOLK85VSpecfIcation of AU2008201550 (changes tracked) (2) doc (3-methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{ [N'-(3-cyano-5-trifluoromethylbenzyl)-N' 5 (3-methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, 2-(5-{N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5 10 ylmethyl]amino}tetrazol-2-yl)ethanol hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 15 methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-iH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 20 methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-1H-[1,2,4]triazol-3-yl)amino]methyll-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid 30 hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 35 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 C: Wocuments and SettingsgaheadVLoca e ngsVTemporary Intemnet FiloVOt.K85USpecication of AU2008201550 (changes tracked) (2).doc methyl-2H-tetrazol-5-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{ [N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 5 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl) 10 N-ethylamino]methyllcyclohexanecarboxylic acid, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]pentanoic acid hydrochloride, 15 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-1H-pyrazol-3-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l 20 methyl-lH-pyrazol-3-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 25 trifluoromethylphenyl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-ethyl 2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 30 5-{N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5-yl]-N ethylamino}pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 35 trifluoromethoxyphenyl)-N-ethylamino]pentanoic acid C:oo0 mwms and S.agsaNO V1..* f8ngsVTmporry Intomet FiemVOLK85VSpekation of AU2008201550 (d gos trcked) (2).doc hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-2,2-dimethylpentanoic acid hydrochloride, 5 6-[N-(6-{[N'-(3,5-bis(trifluoromethyl)benzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-hexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N 10 ethylamino]-3,3-dimethylpentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, (1-{2-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 15 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N ethylaminolethyl cyclopentyl)acetic acid hydrochloride, trans-4-({N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5 yl]-N-ethylamino}methyl)cyclohexanecarboxylic acid, 20 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, (1-{2-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 25 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]ethyl}cyclopentyl)acetic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 30 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 35 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, C:VDocments and SettngsaheadVLoca jqngsT mporary Intemet Files&OLK85Specificaion of AU2008201550 (changes tracked) (2) doc trans-4-({N-[3-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]aminoImethyl) 5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino}methyl) cyclohexanecarboxylic acid hydrochloride, 5 1-{3-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]propyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N 10 ethylamino]-3,3-dimethylpentanoic acid, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 15 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3 dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl)-4 20 trifluoromethylphenyl)-N-ethylamino)-3,3-dimethylpentanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(1 methyl-lH-pyrazol-3-yl)aminolmethyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3 dimethylpentanoic acid hydrochloride, 30 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3 dimethylpentanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 35 (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyll-4 C VDocume"s and Soeaaheadoca ing&Tomporary Irnemot FilsdOLK85VSpedfcation of AU2008201550 (change tracked) (2).doC trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 6-[N-(2-{(N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 5 trifluoromethoxyphenyl)-N-ethylamino]hexanoic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 10 6-[N-(6-{(N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 15 ethylamino]-3,3-dimethylhexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]-4,4-dimethylpentanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 25 trifluoromethoxyphenyl)-N-ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]-4,4-dimethylhexanoic 30 acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 35 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' C:VDouments and SettngswahedVLoc~ 1 ngsVTemporary Internet FilosOLKBSSSpecifiscaton of AU2008201550 (changes tracked) (2).doc (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 5 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N ethylamino]-5,5-dimethylhexanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 10 propylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N 15 isobutylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 20 ethylamino]methyl}cyclohexanecarboxylic acid amide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid methylamide, 25 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid dimethylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 30 (4-chlorophenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 35 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' C:W-~ a on.t nd S*VXae " fns Teparnt.en.1 FdssVOU(85VSpaoflwtoo of AU2008201550 (chnges tracked) (2) doo (m- tolyl)amino]methyll-4-trifluoromethoxyphenyl)-N ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, trans-4-{(N-(2-{[N'-(3,5-dichlorobenzyl)-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N 5 ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) N'-(3-methyl-5-trifluoromethylbenzyl)amino]methyl)-4 trifluoromethoxyphenyl)aminolmethylicyclohexanecarboxylic acid hydrochloride, 10 trans-4-{[N-(2-{[N'-(3-chloro-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) 15 N'-(3-nitro-5-trifluoromethylbenzyl)amino]methyl)-4 trifluoromethoxyphenyl)amino]methyllcyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)aminolmethyl}-2,2 20 difluorobenzo(1,3]dioxol-5-yl)-N ethylamino]methyllcyclohexyl)methanol hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 difluorobenzo[1,3]dioxol-5-yl)-N 25 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-3-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N ethylamino]methyl cyclohexyl)propionic acid hydrochloride, 30 trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-2,2,3,3 tetrafluoro-2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 35 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3 CXDc~wo t and S. o . ooaV L ._.g ingsTemporary Intermt FIWOI LK8S.SpeelfIcation of AU2008201550 (changes Iracked) (2) don tetrafluoro-2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-2-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyll-2,2,3,3 5 tetrafluoro-2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyllcyclohexyl)acetamide hydrochloride, trans-N-[3,5-bis(trifluoromethyl)benzyl]-N-{2-[N'-ethyl N'-(4-(methoxymethyl)cyclohexylmethyl)amino]-5 trifluoromethoxybenzyl}-(2-methyl-2H-tetrazol-5-yl)amine 10 hydrochloride, trans-2-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexyl)ethanol hydrochloride, 15 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N ethylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 25 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 30 ethylamino]methyl}cyclohexylmethyl)phosphonic acid, trans-4-{[N-(2-{[N'-(3-bromo-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl)-4 trifluoromethoxyphenyl)-N ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, 35 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' C"D*'me'"" and S"'-ah*"dVIocasTemporary Intemet FilOLK85WSpedficatIcn of AU2008201550 (changes trscked) (2).doc (2-methyl-2H-tetrazol-5-yl)amino]methyl)-4-bromophenyl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-bromophenyl)-N 5 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, 10 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-methoxyphenyl)amino]methyl}-4-trifluoromethoxyphenyl) N-ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 15 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methoxy-4 methyiphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4,5 20 dimethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylthiophenyl)-N 25 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 30 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 35 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methoxy-4 C .Do .me.ts and Sot.ngsf. e ngsTmporary inteet FilesOLK85VSpecifction of AU2008201550(canges tracked) (2).do methylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-4-({N-[2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-(2,2,2 5 trifluoroethyl)phenyl]-N ethylaminoImethyl) cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N 10 propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N propylamino]methyllcyclohexyl)acetic acid hydrochloride, 15 trans-4-{[N-(2-{ [N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-ethylphenyl)amino]methyll-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{ [N'-(3-cyano-5-trifluorcmethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl)-4 20 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-isopropenylphenyl)amino]methyl}-4 trifluoromethoxyphenyl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexyl)acetic acid dihydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 30 (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 35 trifluoromethylphenyl)-N C:VDomena an SangahsMcdVaU1ingsATomporary Intemet FIIsaOLK5VSpecfication of AU2008201550 (chang tracked) (2).doc ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl)-5-methyl-4 trifluoromethylphenyl)-N 5 propylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N propylamino]methyl}cyclohexyl)acetic acid, 10 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4-methyl-5 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 15 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid methanesulfonate, ethyl trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 20 yl)amino]methyll-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetate, and trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N 25 ethylamino]methyl}cyclohexyl)acetic acid, a prodrug thereof or a pharmaceutically acceptable salt thereof. The method may also include the compound having a CETP inhibitory activity being a compound represented by the formula (X) C:VDocuments and Setnpgwahea e nca5 rigsTemporary Intemet Filesv1K65%Specification of AU2008201550(changes tracked) (2) doc Y2 N

Y

4 (X Y5 X 1 A (X)

X

2 X4

X

3 wherein X 1

-X

4 and Y 1

-Y

5 are the same or different and each is a hydrogen atom or any substituent, Z is the formula (XI); -Zi-Z 2 wherein Zi is -CO-, -CS- or -SO 2 -, Z 2 is a 5 hydrogen atom, an optionally substituted hydrocarbon group having 1 to 20 carbon atoms, an optionally substituted amino group, an optionally substituted alkoxy group or an optionally substituted alkylthio group, A is a disubstituted amino group, an optionally substituted 10 alkoxy group, an optionally substituted alkylthio group or an optionally substituted hydrocarbon group having 1 to 20 carbon atoms, or X 2 and X 3 , X 3 and X 4 or X 4 and A may be taken together to form a homocyclic ring group optionally having substituents or a heterocyclic group optionally 15 having substituents, or a salt thereof. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (X), or a salt thereof. The inhibitor may also be a compound of the formula 20 (X), or a salt thereof. The method may also include the compound of the formula (X) being a compound selected from the group consisting of Methyl(3-cyano-5-trifluoromethylbenzyl)-[6-(N 25 cyclopentylmethyl-N-ethylamino)indan-5-ylmethyl]-carbamate, methyl [6-(N-butyl-N-ethylamino)indan-5-ylmethyl]-(3 cyano-5-trifluoromethylbenzyl)-carbamate, methyl (3-nitro 5-trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N C:VDocments and SettingVsa haMaca ngsVTemporary Intemet FUesVOLK85VSpcdfcation of AU2008201550 (dwgs tacked) (2).doc ethylamino)indan-5-ylmethyl]-carbamate, methyl [6-(N butyl-N-ethylamino)indan-5-ylmethyl]-(3,5-dichlorobenzyl) carbamate, methyl [6-(N-butyl-N-ethylamino)indan-5 ylmethyl]-(3-chloro-5-trifluoromethylbenzyl)-carbamate, 5 methyl (3-bromo-5-trifluoromethylbenzyl)-[6-(N-butyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl [6-(N butyl-N-ethylamino)indan-5-ylmethyl]-(3-methyl-5 trifluoromethylbenzyl)-carbamate, methyl [6-(N-butyl-N ethylamino)indan-5-ylmethyl]-(3-nitro-5 10 trifluoromethylbenzyl)-carbamate, methyl [6-(N cyclopentylmethyl-N-ethylamino)tetralin-5-ylmethyl]-(3 methylsulfonyl-5-trifluoromethylbenzyl)-carbamate, methyl (3-cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl N-ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 15 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclobutylmethyl-N ethylamino)tetralin-5-ylmethyll-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopropylmethyl-N ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopropylethyl-N 2o ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-2-methylpropyl-N ethylamino)tetralin-5-ylmethyl)-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N ethylamino)-6,7,8,9-tetrahydro-5H-benzocycloheptan-2 25 ylmethyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[2,2-dimethyl-6-(N-butyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-propyl-N-ethylamino)indan 5-ylmethyl]-carbamate, methyl (3,5 30 bistrifluoromethylbenzyl)-[6-(N-butyl-N-ethylamino)indan 5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N,N-dipropylamino)indan-5 ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-butyl-N-propylamino)indan 35 5-ylmethyl]-carbamate, methyl (3,5 C:M mens and SMngaVaheadVLocaq ingsTemporay Intemt FIlosOOLK85VSpeiflcawon of AU2008201550 (chane tracked) (2).doc bistrifluoromethylbenzyl)-[6-(N-3-methylbutyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-3,3-dimethylbutyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 5 bistrifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-3-butylenyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-benzyl-N 10 propylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-1-methylethyl-N propylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(6-piperidylindan-5-ylmethyl) carbamate, methyl benzyl-[6-(N,N-dipropylamino)indan-5 15 ylmethyl]-carbamate, methyl [6-(N,N-dipropylamino)indan-5 ylmethyl]-(3-trifluoromethylbenzyl)-carbamate, methyl [6 (N,N-dipropylamino)indan-5-ylmethyl]-(3-methylbenzyl) carbamate, methyl (3-chlorobenzyl)-[6-(N,N dipropylamino)indan-5-ylmethyl)-carbamate, methyl [6-(N,N 20 dipropylamino)indan-5-ylmethyl]-(3-nitrobenzyl)-carbamate, methyl (3-cyanobenzyl)-[6-(N,N-dipropylamino)indan-5 ylmethyl]-carbamate, methyl [6-(N,N-dipropylamino)indan-5 ylmethyl]-(3-methoxycarbonylbenzyl)-carbamate, methyl (3,5-dinitrobenzyl)-[6-(N,N-dipropylamino)indan-5 25 ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 methylbenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 chlorobenzyl)-carbamate, methyl (3,5 30 bistrifluoromethylbenzyl)-(2-dipropylamino-5 methoxybenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 trifluoromethyloxybenzyl)-carbamate, methyl [2-(N-butyl-N ethylamino)-5-trifluoromethyloxybenzyl]-(3-nitro-5 35 trifluoromethylbenzyl)-carbamate, methyl (3-cyano-5 C:Documents and SttingsVaheadwLoc ngsVTemporary Intemet FiOsVOLK85VSpecificadon of AU2008201550 changess tracked) (2).doc trifluoromethylbenzyl) - [2- (N-butyl-N-ethylamino) -5 trifluoromethyloxybenzyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-4,5 dimethylbenzyl)-carbamate, (3,5-bistrifluoromethylbenzyl) 5 [6-(N-dipropylamino)indan-5-ylmethyl]-acetamide, (3,5 bistrifluoromethylbenzyl)-[6-(N-dipropylamino)indan-5 ylmethyl]-urea, (3,5-bistrifluoromethylbenzyl)-[6-(N dipropylamino)indan-5-ylmethyl)-formamide, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 10 trifluoromethylbenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylaminobenzyl) carbamate, methyl (3,5-bistrifluoromethylbenzyl)-(2 dipropylamino-4,5-dichlorobenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-4-chloro-5 15 trifluoromethyloxybenzyl)-carbamate, methyl [3-(N-butyl-N ethylamino)naphthalen-2-ylmethyl]-(3-cyano-5 trifluoromethylbenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-4 methyloxybenzyl)-carbamate, methyl (3,5 20 bistrifluoromethylbenzyl)-[6-(N-propionyl-N propylamino)indan-5-ylmethyl]carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-ethoxycarbonyl-N propylamino)indan-5-ylmethyl]carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(1-propylbutoxy)indan-5 25 ylmethyl]carbamate, methyl (3,5-bistrifluoromethylbenzyl) [6-(l-ethylpropyloxy)indan-5-ylmethyl]carbamate, methyl (3,5-bistrifluoromethylbenzyl)-[4,5-dimethyl-2-(1 propylbutyl)benzyl]carbamate and methyl (3-cyano-5 trifluoromethylbenzyl)-[6-(1-propylbutyl)indan-5 30 ylmethyl]-carbamate, or a salt thereof. Preferably in the inhibitor of the invention the compound of the formula (X) is a compound selected from the group consisting of methyl (3-cyano-5-trifluoromethylbenzyl)-[6 (N-cyclopentylmethyl-N-ethylamino)indan-5-ylmethyl] 35 carbamate, methyl [6-(N-butyl-N-ethylamino)indan-5 C:Iac..rot an.d S.onaho.e..m..ngshTemporary Intemert FilesOLK8SVSpecificatIon of AU2008201550 (changes tracked) (2).doc ylmethyl]-(3-cyano-5-trifluoromethylbenzyl)-carbamate, methyl (3-nitro-5-trifluoromethylbenzyl)-[6-(N cyclopentylmethyl-N-ethylamino)indan-5-ylmethyl)-carbamate, methyl [6-(N-butyl-N-ethylamino)indan-5-ylmethyl]-(3,5 5 dichlorobenzyl)-carbamate, methyl [6-(N-butyl-N ethylamino)indan-5-ylmethyl]-(3-chloro-5 trifluoromethylbenzyl)-carbamate, methyl (3-bromo-5 trifluoromethylbenzyl)-[6-(N-butyl-N-ethylamino)indan-5 ylmethyl]-carbamate, methyl [6-(N-butyl-N 10 ethylamino)indan-5-ylmethyl)-(3-methyl-5 trifluoromethylbenzyl)-carbamate, methyl (6-(N-butyl-N ethylamino)indan-5-ylmethyl]-(3-nitro-5 trifluoromethylbenzyl)-carbamate, methyl [6-(N cyclopentylmethyl-N-ethylamino)tetralin-5-ylmethyl)-(3 15 methylsulfonyl-5-trifluoromethylbenzyl)-carbamate, methyl (3-cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl N-ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclobutylmethyl-N ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 20 cyano-5-trifluoromethylbenzyl)-(6-(N-cyclopropylmethyl-N ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopropylethyl-N ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-2-methylpropyl-N 25 ethylamino)tetralin-5-ylmethyl]-carbamate, methyl (3 cyano-5-trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N ethylamino)-6,7,8,9-tetrahydro-5H-benzocycloheptan-2 ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[2,2-dimethyl-6-(N-butyl-N 30 ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-propyl-N-ethylamino)indan 5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-butyl-N-ethylamino)indan 5-ylmethyl]-carbamate, methyl (3,5 35 bistrifluoromethylbenzyl)-[6-(N,N-dipropylamino)indan-5 C:VDomet and SstingsWahe Lc% fngsTemporay intemM FlesOLKSnpecification of AU200B201550 changes tracked) (2).doc ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-butyl-N-propylamino)indan 5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-3-methylbutyl-N 5 ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-3,3-dimethylbutyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 10 bistrifluoromethylbenzyl)-[6-(N-3-butylenyl-N ethylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-benzyl-N propylamino)indan-5-ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-1-methylethyl-N 15 propylamino)indan-5-ylmethyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(6-piperidylindan-5-ylmethyl) carbamate, methyl benzyl-[6-(N,N-dipropylamino)indan-5 ylmethyl]-carbamate, methyl [6-(N,N-dipropylamino)indan-5 ylmethyl)-(3-trifluoromethylbenzyl)-carbamate, methyl [6 20 (N,N-dipropylamino)indan-5-ylmethyl]-(3-methylbenzyl) carbamate, methyl (3-chlorobenzyl)-[6-(N,N dipropylamino)indan-5-ylmethyl]-carbamate, methyl [6-(N,N dipropylamino)indan-5-ylmethyl]-(3-nitrobenzyl)-carbamate, methyl (3-cyanobenzyl)-[6-(N,N-dipropylamino)indan-5 25 ylmethyl]-carbamate, methyl [6-(N,N-dipropylamino)indan-5 ylmethyl]-(3-methoxycarbonylbenzyl)-carbamate, methyl (3,5-dinitrobenzyl)-[6-(N,N-dipropylamino)indan-5 ylmethyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 30 methylbenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 chlorobenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 methoxybenzyl)-carbamate, methyl (3,5 35 bistrifluoromethylbenzyl)-(2-dipropylamino-5 C:UDoments and Setnga aheadVLoc n rgTemporary Intmet Fis&OLK85VSpecflcaton of AU2008201550 (changes tracked) (2) doc trifluoromethyloxybenzyl)-carbamate, methyl [2-(N-butyl-N ethylamino)-5-trifluoromethyloxybenzyl]-(3-nitro-5 trifluoromethylbenzyl)-carbamate, methyl (3-cyano-5 trifluoromethylbenzyl)-[2-(N-butyl-N-ethylamino)-5 5 trifluoromethyloxybenzyl]-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-4,5 dimethylbenzyl)-carbamate, (3,5-bistrifluoromethylbenzyl) [6-(N-dipropylamino)indan-5-ylmethyl]-acetamide, (3,5 bistrifluoromethylbenzyl)-[6-(N-dipropylamino)indan-5 10 ylmethyl)-urea, (3,5-bistrifluoromethylbenzyl)-[6-(N dipropylamino)indan-5-ylmethyl]-formamide, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-5 trifluoromethylbenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylaminobenzyl) 15 carbamate, methyl (3,5-bistrifluoromethylbenzyl)-(2 dipropylamino-4,5-dichlorobenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-4-chloro-5 trifluoromethyloxybenzyl)-carbamate, methyl [3-(N-butyl-N ethylamino)naphthalen-2-ylmethyl]-(3-cyano-5 20 trifluoromethylbenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-(2-dipropylamino-4 methyloxybenzyl)-carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(N-propionyl-N propylamino)indan-5-ylmethyl]carbamate, methyl (3,5 25 bistrifluoromethylbenzyl)-[6-(N-ethoxycarbonyl-N propylamino)indan-5-ylmethyl]carbamate, methyl (3,5 bistrifluoromethylbenzyl)-[6-(1-propylbutoxy)indan-5 ylmethyl]carbamate, methyl (3,5-bistrifluoromethylbenzyl) [6-(1-ethylpropyloxy)indan-5-ylmethyl]carbamate, methyl 30 (3,5-bistrifluoromethylbenzyl)-[4,5-dimethyl-2-(l propylbutyl)benzyl]carbamate and methyl (3-cyano-5 trifluoromethylbenzyl)-[6-(1-propylbutyl)indan-5 ylmethyl]-carbamate, or a salt thereof. The method may also include the compound having a 3 CETP inhibitory activity being a compound of the formula C:Docun.ts and Stngswahead T Inteme.t FilsOLK85VSpcfi.ation of AU2008201550 (changes tracked) (2) doc (I) 3

R

5 N OR 6 R 6>(* (I) R 1 6 4

R

7 2

R

8 R wherein Ri is a hydrogen, Y, W-X or W-Y; 5 W is carbonyl, thiocarbonyl, sulfinyl or sulfonyl; X is -O-Y, -S-Y, -N(H)-Y or -N-(Y)2; wherein Y in each case is independently Z or a fully saturated, partially unsaturated or fully unsaturated 1- to 10-membered straight chain or 10 branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen, and the carbon may be independently mono-, di- or tri-substituted by 15 halo, the carbon may be mono-substituted by hydroxy, the carbon may be mono-substituted by oxo, the sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the carbon chain may be mono 20 substituted by Z; Z is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen, or a bicyclic 25 ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6 membered rings, taken independently, which may have 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen; 30 the Z substituent may be independently mono-, di or tri-substituted by halo, (C 2

-C

6 )alkenyl, (Ci Cfocm. a.nd SiM ngshe.ad.oc.ggngsvTemporary lntemet FilsOLK85VSpedflcaton of AU2008201550(chng.stracked) (2) doc C6)alkyl, hydroxy, (Ci-C 6 )alkoxy, (C 1

-C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cl

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, wherein the (Ci-C 6 )alkyl substituent 5 may be independently mono-, di- or tri-substituted by halo, hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Cr

C

6 )alkylamino and the (Ci-C 6 )alkyl substituent may 10 be substituted by 1 to 9 fluorines; R2 is a partially saturated, fully saturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with 1 or 15 2 heteroatoms independently selected from oxygen, sulfur and nitrogen, the carbon atom may be independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by oxo, the carbon may be mono-substituted by hydroxy, the 20 sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo; or R2 is a partially saturated, fully saturated or fully unsaturated 3- to 7-membered ring optionally having 1 or 2 heteroatoms independently selected 25 from oxygen, sulfur and nitrogen, wherein the R 2 ring may be bonded via (Ci-C 4 )alkyl; wherein the R 2 ring may be independently mono-, di or tri-substituted by halo, (C 2

-C

6 )alkenyl, (Cr C6)alkyl, hydroxy, (Ci-C6)alkoxy, (Ci-C4)alkylthio, 30 amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci Cd)alkylamino, and the (Ci-C 6 )alkyl substituent may be independently mono-, di- or tri-substituted by halo, hydroxy, (Ci-C)alkoxy, (Ci-C4)alkylthio, oxo 35 or (Ci-C 6 )alkyloxycarbonyl; C;VDocuments and SettIngsvahaidVL o ngaTemporary Interm FIles]OLK85VSpeefcation of AU2008201550 (changes tracked) (2) doc provided that R 2 is not methyl;

R

3 is a hydrogen or Q; wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered 5 straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen, the carbon may be independently mono-, di- or tri-substituted by halo, 10 the carbon may be mono-substituted by hydroxy, the carbon may be mono-substituted by oxo, the sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the carbon chain may be mono-substituted by V; 15 V is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen or a bicyclic ring consisting of two fused partially saturated, fully 20 saturated or fully unsaturated 3- to 6-membered rings, taken independently, which may have 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the V substituent may be independently 25 mono-, di- or tri-substituted by halo, (Ci-Cs)alkyl,

(C

2

-C

6 )alkenyl, hydroxy, (Cl-CE)alkoxy, (Ci

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxamoyl, mono-N- or di-N,N-(C 1

-C

6 )alkylcarboxamoyl, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci 30 C)alkylamino, wherein the (Ci-C)alkyl or (C2

C

6 )alkenyl substituent may be independently mono-, di- or tri-substituted by hydroxy, (Ci-C)alkoxy,

(CI-C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci 35 C)alkylamino, and the (Ci-C)alkyl substituent or C:VDocuments and SettingseaheadVLoca ngdgToemporary Intemet FilesdOLK8S5Specification of AU2008201550 (changes tracked) (2.doc

(C

2

-C

6 )alkenyl substituent may be substituted by 1 to 9 fluorines;

R

4 is Q 1 or V1; wherein Q1 is a fully saturated, partially 5 unsaturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen, the carbon may be 10 independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by hydroxy, the carbon may be mono-substituted by oxo, the sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the 15 carbon chain may be mono-substituted by V1;

V

1 is a partially saturated, fully saturated or fully unsaturated 3- to 6-membered ring optionally having 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen; 20 V 1 substituent may be independently mono-, di-, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Ci-C 6 )alkoxy, amino, nitro, cyano, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino wherein the (Ci-C)alkyl substituent 25 is optionally mono-substituted independently by oxo or the (Ci-C 6 )alkyl substituent is optionally substituted by 1 to 9 fluorines; wherein any R 3 should contain V, or R 4 should contain VI; and 30 R', R 6 , R 7 and Re are each independently a hydrogen, a bond, a nitro or a halo, wherein the bond is substituted by T or a partially saturated, fully saturated or fully unsaturated (Ci-C 12 ) straight chain or branched 35 carbon chain wherein the carbons may be replaced C VDocuments and StingsvahedVLoca rings&Tomporary Intemet FfiesVOLKS5VSpedfication of AU2008201550 (changes tracked) (2) doc with 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen, wherein the carbon atom may be independently mono-, di- or tri substituted by halo, the carbon may be mono 5 substituted by hydroxy, the carbon may be mono substituted by oxo, the sulfur may be mono or di substituted by oxo, the nitrogen may be mono or di substituted by oxo, and the carbon may be mono substituted by T; 10 T is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, 15 fully saturated or fully unsaturated 3- to 6 membered rings, taken independently, which may have 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the T substituent is independently mono-, 20 di- or tri-substituted by halo, (Ci-C 6 )alkyl, (C 2 C 6 ) alkenyl, hydroxy, (Ci-C6) alkoxy, (C1-C4) alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, the (Ci-C 6 )alkyl substituent is 25 optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C)alkoxy, (Ci

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, and the (Ci-C 6 )alkyl substituent is 30 optionally substituted by 1 to 9 fluorines; and 5 66 8 R and R 6 , or R and R , and/or R and R8 may be linked to form a partially saturated or fully unsaturated 4- to 8-membered ring optionally having 1 to 3, at least 1, heteroatom independently 35 selected from nitrogen, sulfur and oxygen; C:VDommnt.. nd Se .hneadVoco lngsVTomporary Intoemet FilesVOLK85USpecffication of AU200820155 (dnges tracked) (2).doc wherein the ring (one or plural) formed by R 5 and R , or R 6 and R 7 , and/or R and R 8 may be independently mono-, di- or tri-substituted by halo,

(C

1

-C

6 ) alkyl, (C 1

-C

4 ) alkylsulfonyl, (C2-C6) alkenyl, 5 hydroxy, (Ci-C)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, the (Ci-C)alkyl substituent may be independently mono-, di- or tri-substituted by 10 hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, and the (Ci-C 6 )alkyl substituent may be substituted by 1 to 9 fluorines; 15 provided that when R 2 is carboxyl or (Cr

C

4 )alkylcarboxyl, R1 is not a hydrogen, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also include the compound having a 20 CETP inhibitory activity being a compound of the formula (I), a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also be a compound of the formula (I), a prodrug thereof or a pharmaceutically acceptable 25 salt of the compound or the prodrug. The method may also include the compound of the formula (I) being a compound selected from a group consisting of [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 30 methoxycarbonyl-amino]-2-isopropyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-1-carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-chloro-2-cyclopropyl-3,4-dihydro 2H-quinoline-l-carboxylic acid isopropyl ester; 35 [2S,4S]2-cyclopropyl-4-[(3,5-dichloro-benzyl) C:VDocurnent. .d S.tg ehe o. 7 ing.WTmporary Intemet FRil..OLK8a5Spdfio.t n of AU2008201550 (chag.. traked) (2) doc methoxycarbonyl-amino]-6-trifluoromethyl-3,4-dihydro-2H quinoline-1-carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-aminol-2-cyclopropyl-6-trifluoromethyl 5 3,4-dihydro-2H quinoline-1-carboxylic acid tert-butyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl 10 ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclobutyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 15 methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-1-carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methoxymethyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-1-carboxylic acid isopropyl 20 ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid 2-hydroxy-ethyl ester; 25 [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 30 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid propyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 35 methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 C:VDocuments and SottngsaheadVLocaM fngATemporry Intmet FlOOLK8V6SpOciflation of AU2008201550 changeo tracked) (2).doc dihydro-2H-quinoline-1-carboxylic acid propyl ester, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also be the compound of the 5 formula (I) being a compound selected from a group consisting of [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl amino]-2-isopropyl-6-trifluoromethyl-3,4-dihydro-2H 10 quinoline-1-carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-chloro-2-cyclopropyl-3,4-dihydro 2H-quinoline-l-carboxylic acid isopropyl ester; [2S,4S]2-cyclopropyl-4-[(3,5-dichloro-benzyl) 15 methoxycarbonyl-amino]-6-trifluoromethyl-3,4-dihydro-2H quinoline-1-carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid tert-butyl 20 ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; 25 [2S,4SJ4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-aminol-2-cyclobutyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-1-carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 30 dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino)-2-methoxymethyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; 35 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) CkVocumeds and SeMingsuahsadV ocw 1ngsVTemporay Intnemt FileVOLK85Specification of AU2008201550 (changes tracked) (2).doc methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid 2-hydroxy-ethyl ester; [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 5 methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; 10 [2S,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-cyclopropyl-6-trifluoromethyl 3,4-dihydro-2H-quinoline-l-carboxylic acid propyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4 15 dihydro-2H-quinoline-l-carboxylic acid propyl ester, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The method may also include the compound having a CETP inhibitory activity being a compound of the formula 20 (11) : 0 R OR 6 4 (II) 17 & R7 )CH 3 8 1 R R wherein R 1 is hydrogen, Y, W-X, W-Y; W is carbonyl, thiocarbonyl, sulfinyl or sulfonyl; X is -O-Y, -S-Y, -N(H)-Y or -N-(Y)2; 25 Y in each case is independently, Z or a fully saturated, partially unsaturated or fully unsaturated 1- to 10 membered straight or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently from oxygen, C oments and SetngsaahaVMLocaj ngsXTemporwy Intermt FIles*OLK85VSpoCincation of AU2008201550 (chnes trcked) (2)doc sulfur and nitrogen and aforementioned carbon is optionally mono-, di- or tri-substituted independently by halo, the aforementioned carbon is optionally mono substituted by hydroxy, the aforementioned carbon is 5 optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di-substituted by oxo, the aforementioned nitrogen is optionally mono- or di substituted by oxo, and the aforementioned carbon chain is optionally mono-substituted by Z; 10 Z is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 15 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the aforementioned Z substituent is optionally mono-, di- or tri-substituted independently by halo, (C2 20 C)alkenyl, (C 1 -C)alkyl, hydroxy, (C 1

-C

6 )alkoxy, (Cr

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr C6)alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino wherein the aforementioned (C 1

-C

6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by 25 halo, hydroxy, (C 1

-C

6 )alkoxy, (C 1

-C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (C 1

-C

6 )alkyloxycarbonyl, mono N- or di-N,N-(Ci-C 6 )alkylamino, the aforementioned (Cr

C

6 )alkyl is optionally substituted by 1 to 9 fluorines;

R

3 is hydrogen or Q; 30 wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen, the aforementioned carbon is 35 optionally mono-, di- or tri-substituted independently by C:VDocuments and Settngsvahe ing Tmpoa Inerrnet Fde OLK85VSpenfction of AIJ2008201550 (dranges tracked) (2).doc halo, the aforementioned carbon is optionally mono substituted by hydroxy, the aforementioned carbon is optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di-substituted by oxo, the 5 aforementioned nitrogen is optionally mono- or di substituted by oxo, and the aforementioned carbon chain is optionally mono-substituted by V; wherein V is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 10 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected 15 independently from nitrogen, sulfur and oxygen; the aforementioned V substituent is optionally mono-, di-, tri- or tetra-substituted independently by halo, (Ci

C

6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Ci-C 6 )alkoxy, (Cl

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxamoyl, mono 20 N- or di-N,N-(Ci-C 6 )alkylcarboxamoyl, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the aforementioned (Ci-C)alkyl or (C 2 -C)alkenyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, 25 amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino or the aforementioned (Ci-C 6 )alkyl or (C 2

-C

6 )alkenyl substituent is optionally substituted by 1 to 9 fluorines;

R

4 is Q 1 or V1; 30 wherein Q1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen and the aforementioned carbon 35 is optionally mono-, di- or tri-substituted independently C.IDocuments and Semngsahead Loc ngsUTmporary Intenet FilasVOLK85OSpoeifiction of AU2008201550 (changes tracked) (2) doc by halo, the aforementioned carbon is optionally mono substituted by hydroxy, the aforementioned carbon is optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di-substituted by oxo, the 5 aforementioned nitrogen is optionally mono- or di substituted by oxo, and the aforementioned carbon chain is optionally mono-substituted by V'; wherein V 1 is a partially saturated, fully saturated or fully unsaturated 3- to 6-membered ring optionally having 10 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the aforementioned V 1 substituent is optionally mono-, di-, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Ci-C 6 )alkoxy, amino, nitro, cyano, 15 (C 1

-C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, the aforementioned (Ci-C)alkyl substituent is optionally mono-substituted by oxo, the aforementioned (Ci-C 6 )alkyl substituent is optionally substituted by 1 to 9 fluorines; 20 wherein either R 3 should contain V or R 4 should contain V'; and R 5 , R 6 , R 7 and R 8 are each independently hydrogen, a bond, nitro or halo wherein the aforementioned bond is substituted by T or a partially saturated, fully saturated or fully unsaturated straight or branched carbon chain 25 having 1 to 12 carbon atoms wherein the carbons may be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen wherein the aforementioned carbon atom is optionally mono- di- or tri substituted independently by halo, the aforementioned 30 carbon is optionally mono-substituted by hydroxy, the aforementioned carbon is optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di substituted by oxo, the aforementioned nitrogen is optionally mono- or di-substituted by oxo, and the 35 aforementioned carbon is optionally mono-substituted by T; C:VDoc ents and Settngsvahad ngvTmporary Intomot FUOVOLK85 pecifction of AU2008201550 (dags tracked) (2).doc wherein T is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen or a bicyclic ring consisting of two 5 fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the aforementioned T substituent is optionally 10 mono-, di- or tri-substituted independently by halo, (Cl

C

6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Cl-C6)alkoxy, (Cr

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(CI-C 6 )alkylamino wherein the aforementioned (C 1

-C

6 )alkyl substituent is 15 optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C 6 )alkoxy, (Cr-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (Ci-C 6 )alkyl substituent is optionally substituted by 1 to 9 fluorines; 20 provided that at least one of substituents Rs, R 6 , R 7 and R8 is not hydrogen and is not linked to the quinoline moiety through oxy, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. 25 The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (I), a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also be a compound of the formula 30 (II), a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The method may also include the compound of the formula (II) being a compound selected from a group consisting of 35 [2R,4SJ4-[(3,5-bis-trifluoromethyl-benzyl) CA m.oc .no wid S.i.s.ah... ocerpngsToemporary Intemet FilenVOLK85VSidfication of AU2008201550(changestracked) (2) doc methoxycarbonyl-amino]-2-methyl-7-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-7-chloro-2-methyl-3,4-dihydro-2H 5 quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl amino]-6-chloro-2-methyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; 10 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2,6,7-trimethyl-3,4-dihydro-2H quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6,7-diethyl-2-methyl-3,4-dihydro 15 2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-ethyl-2-methyl-3,4-dihydro-2H quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 20 methoxycarbonyl-amino]-2-methyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid isopropyl ester, a 25 prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also include the compound of the formula (II) being a compound selected from a group consisting of 30 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-7-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-7-chloro-2-methyl-3,4-dihydro-2H 35 quinoline-l-carboxylic acid ethyl ester; C:VDocum ents wd SettngsvaheadVLochq IngsTemporary Intemt FilsUOLK85VSpeflcation of AU2008201550 (changes tracked) (2)doc [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-chloro-2-methyl-3,4-dihydro-2H quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 5 methoxycarbonyl-amino]-2,6,7-trimethyl-3,4-dihydro-2H quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6,7-diethyl-2-methyl-3,4-dihydro 2H-quinoline-1-carboxylic acid ethyl ester; 10 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-ethyl-2-methyl-3,4-dihydro-2H quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-6-trifluoromethyl-3,4 15 dihydro-2H-quinoline-1-carboxylic acid ethyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-6-trifluoromethyl-3,4 dihydro-2H-quinoline-l-carboxylic acid isopropyl ester, a prodrug thereof or a pharmaceutically acceptable salt of 20 the compound or the prodrug. The method may also include the compound having a CETP inhibitory activity being a compound of the formula (III)

R

3 R4

R

5 N 6 4 (III)

R

8

R

1 25 wherein R' is Y, W-X or W-Y; wherein W is a carbonyl, thiocarbonyl, sulfinyl or sulfonyl; X is -O-Y, -S-Y, -N(H)-Y or -N-(Y)2; Y in each case is independently Z or fully saturated, 30 partially unsaturated or fully unsaturated 1- to 10 C:VDocuments and SettngswaheadVLoca 5ngsVTempora fntomet FilasOLK85VSpecificaion of AU2008201550 (changes tracked) (2).doc membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen and the carbon may be 5 mono-, di- or tri-substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is optionally mono or di-substituted by oxo, the nitrogen is optionally mono or di-substituted by oxo, and the 10 carbon chain is optionally mono-substituted by Z; wherein Z is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two 15 fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms from nitrogen, sulfur and oxygen; wherein the Z substituent is optionally mono-, di- or tri 20 substituted independently by halo, (C 2

-C

6 )alkenyl, (Cr

C

6 )alkyl, hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono N- or di-N,N-(Ci-C 6 )alkylamino wherein the (C 1

-C

6 )alkyl substituent is optionally mono-, di- or tri-substituted 25 independently by halo, hydroxy, (C 1 -C)alkoxy, (Ci

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino, the (Ci-C 6 )alkyl substituent is optionally substituted by 1 to 9 fluorines; 30 R 2 is a partially saturated, fully saturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen wherein the 35 carbon atom is optionally mono-, di- or tri-substituted C-VDocmmerit and Set~ngS~aheadV ngsUTemporry Internt FilVOLK85VSpecficaton of AU2008201550 (changes tracked) (2).doc independently by halo, the carbon is optionally mono substituted by oxo, the carbon is optionally mono substituted by hydroxy, the sulfur is optionally mono or di-substituted by oxo, the nitrogen is optionally mono or 5 di-substituted by oxo; or the R 2 is a partially saturated, fully saturated or fully unsaturated 3- to 7-membered ring optionally having 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen, wherein the R2 ring is optionally bonded via (C1-C 4 )alkyl; 10 wherein the R2 ring is optionally mono-, di- or tri substituted by halo, (C 2 -C)alkenyl, (C 1 -C)alkyl, hydroxy, (CI-C6)alkoxy, (C1-C4)alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino wherein the (C1-C 6 )alkyl substituent is 15 optionally mono-, di- or tri-substituted independently by halo, hydroxy, (C1-C6) alkoxy, (Ci-C4) alkylthio, oxo or (Ci C6)alkyloxycarbonyl;

R

3 is hydrogen or Q; wherein Q is a fully saturated, partially unsaturated or 20 fully unsaturated 1- to 6-membered straight chain or branched carbon chain wherein the carbons, other than connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently 25 by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is mono or di-substituted by oxo, the nitrogen is optionally mono or di-substituted by oxo, and the carbon chain is optionally mono-substituted by V; 30 wherein V is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully 35 unsaturated 3- to 6-membered rings, taken independently, C.focuments and SettingswaheadwLoc rngsVTemporary Internet FIlIsVOLK85VSpe~fcinatn of AU2008201550 (changes tracked) (2).doc optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the V substituent is optionally mono, di, tri- or tetra-substituted independently by halo, (C 1

-C

6 )alkyl, (C2 5 C 6 )alkenyl, hydroxy, (Cl-C6)alkoxy, (C1-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxamoyl, mono-N- or di-N,N-(C1

C

6 )alkylcarboxamoyl, carboxy, (C 1 -C)alkyloxycarbonyl, mono-N- or di-N,N-(C1-C 6 )alkylamino wherein the (Ci

C

6 )alkyl substituent or (C 2 -C)alkenyl substituent is 10 optionally mono-, di- or tri-substituted independently by hydroxy, (C 1

-C

6 )alkoxy, (C1-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, the (C 1

-C

6 )alkyl substituent or

(C

2

-C

6 )alkenyl substituent is also optionally substituted 15 by 1 to 9 fluorines;

R

4 is cyano, formyl, W'Q 1 , W'V 1 , (Ci-C 4 )alkylene V 1 or V2 wherein W1 is carbonyl, thiocarbonyl, SO or SO 2 ; Q1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or branched 20 carbon chain wherein the carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono substituted by hydroxy, the carbon is optionally mono 25 substituted by oxo, the sulfur is optionally mono or di substituted by oxo, the nitrogen is optionally mono or di substituted by oxo, and the carbon chain is optionally mono-substituted by V'; wherein V 1 is a partially saturated, fully saturated or 30 fully unsaturated 3- to 6-membered ring optionally having 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, 35 optionally having 1 to 4 heteroatoms selected C c an -d S.ng.MaheadVo ggWTmporry IMe FIIesOLK85VSpedc Aion of AU2008201550 (changes tracked) (2) doc independently from nitrogen, sulfur and oxygen; wherein the V 1 substituent is optionally mono, di, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Ci

C

6 )alkoxy, hydroxy, oxo, amino, nitro, cyano, (Ci 5 C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(CI-C6)alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono substituted by oxo, the (Ci-C 6 )alkyl substituent is also optionally substituted by 1 to 9 fluorines; wherein V 2 is a partially saturated, fully saturated or 10 fully unsaturated 5- to 7-membered ring containing 1 to 4 heteroatoms independently from oxygen, sulfur and nitrogen; wherein the V 2 substituent is optionally mono-, di- or tri-substituted independently by halo, (Ci-C 2 )alkyl, (Ci 15 C 2 )alkoxy, hydroxy or oxo, wherein the (Ci-C 2 )alkyl optionally has 1 to 5 fluorines; and wherein R 4 does not include oxycarbonyl linked directly to the C4 nitrogen; wherein either R 3 should contain V or R 4 should contain V1; 20 R 5 , R 6 , R 7 and R 8 are independently hydrogen, a bond, nitro or halo wherein the bond is saturated with T or a partially saturated, fully saturated or fully unsaturated straight chain or branched carbon chain having 1 to 12 carbon atoms wherein the carbons may be replaced with 1 or 25 2 heteroatoms selected independently from oxygen, sulfur and nitrogen, wherein the carbon atom is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is 30 optionally mono or di-substituted by oxo, the nitrogen is optionally mono or di-substituted by oxo, and the carbon chain is optionally mono-substituted by T; wherein T is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 35 1 to 4 heteroatoms selected independently from oxygen, C:UDoc eds and Soengswahead*Loca ~ingseTemporary Intemet FilsOOLK65VSpecificatIon of AU2008201550 (changes tracked) (2).doc sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected 5 independently from nitrogen, sulfur and oxygen; wherein the T substituent is optionally mono-, di- or tri substituted by halo, (Ci-C 6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy,

(C

1 -C)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C6)alkyloxycarbonyl, mono-N- or di-N,N-(Cr 10 C 6 )alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (C 1

-C

6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C6)alkylamino, and the (Ci-C6)alkyl substituent 15 also optionally has 1 to 9 fluorines; wherein R 5 and R 6 , or R 6 and R 7 , and/or R 7 and R 8 may also be linked to form at least one ring that is a partially saturated or fully unsaturated 4- to 8-membered ring optionally having 1 to 3 heteroatoms independently 20 selected from nitrogen, sulfur and oxygen; wherein the ring formed by R 5 and R 6 , or R 6 and R 7 , and/or

R

7 and R 8 are optionally mono-, di- or tri-substituted independently by halo, (Ci-C 6 )alkyl, (Ci-C 4 )alkylsulfonyl, (C2-C6)alkenyl, hydroxy, (Ci-C6)alkoxy, (Ci-C4)alkylthio, 25 amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the (C

C

6 )alkyl substituent is optionally mono-, di- or tri substituted independently by hydroxy, (Ci-C 6 )alkoxy, (C1

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci 30 C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, and the (Ci-C 6 )alkyl substituent also optionally has 1 to 9 fluorines, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also include the compound having a 35 CETP inhibitory activity being a compound of the formula C:ADocumwnts and SetingswaheadV Ungs*Temporwy Intemet FdiesOLK85VSpecficadon of AU2008201550 (chans tracked) (2).doc (III), a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also be a compound of the formula (III), a prodrug thereof or a pharmaceutically acceptable 5 salt of the compound or the prodrug. The method may also include the compound of the formula (III) being a compound selected from a group consisting of [2S,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 10 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid propyl ester; 15 [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid tert-butyl ester; [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 20 carboxylic acid isopropyl ester; [2R,4S)4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2S,4S]4-[l-(3,5-bistrifluoromethylbenzyl)-ureido]-2 25 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 carboxylic acid isopropyl ester; [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 carboxylic acid ethyl ester; 30 [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 methoxymethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline 1-carboxylic acid isopropyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 35 carboxylic acid isopropyl ester; C:VDoomn-dt.. S .o.h..oca.dingsUTemporary Ilntemet FileswOLK85VSpedficaton of AU2008201550 (ch.nges tracked) (2) doc [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 5 methoxymethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline 1-carboxylic acid isopropyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid propyl ester; 10 [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino)-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 15 carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 carboxylic acid ethyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 20 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; 25 [2S,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 30 carboxylic acid isopropyl ester; [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-ethyl-6 35 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid C:Uocuments and SetingsvaheadVO ngsVTemporwy Intemt FifesV.KO85VSpecfication of AU2008201550 (changes tracked) (2).doc ethyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-ethyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid propyl ester; 5 [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-ethyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; [2S,4S]4-(3,5-bistrifluoromethylbenzylamino)-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 10 carboxylic acid ethyl ester; [2S,4S]4-(3,5-bistrifluoromethylbenzylamino)-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid propyl ester; and [2S,4S]4-(3,5 bistrifluoromethylbenzylamino)-2-cyclopropyl-6 15 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also include the compound of the formula (III) being a compound selected from a group 20 consisting of [2S,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2S,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino)-2 25 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid propyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid tert-butyl ester; 30 [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 35 carboxylic acid ethyl ester; C:ocuments and SottngsaheadVLoca e ngaWTomporary Intenet FiloseOLK85BSpecificaton of AU2008201550 (changes tracked) (2).doc [2S,4S]4-[1-(3,5-bistrifluoromethylbenzyl)-ureido]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 5 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 carboxylic acid ethyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 methoxymethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline 1-carboxylic acid isopropyl ester; 10 [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 carboxylic acid propyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 15 carboxylic acid ethyl ester; [2R,4S]4-((3,5-bistrifluoromethylbenzyl)-formylamino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 20 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2S,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinolinecarboxylic acid isopropyl ester; 25 [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2S,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 30 carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bistrifluoromethylbenzyl)-formylamino]-2 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid isopropyl ester; [2R,4S]4-[acetyl-(3,5-bistrifluoromethylbenzyl)-amino]-2 35 methyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l C:VDocuments and Stingsvahaa inge&Tomporary Intomet FilsOLKB5VSpedficauan of AU2008201550 (hango. tracked) (2).doc carboxylic acid isopropyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-methyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; 5 [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-methyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid propyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-methyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 10 isopropyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-ethyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-ethyl-6 15 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid propyl ester; [2R,4S]4-(3,5-bistrifluoromethylbenzylamino)-2-ethyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; 20 [2S,4S]4-(3,5-bistrifluoromethylbenzylamino)-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; (2S,4S]4-(3,5-bistrifluoromethylbenzylamino)-2 cyclopropyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l 25 carboxylic acid propyl ester; and [2S,4S]4-(3,5 bistrifluoromethylbenzylamino)-2-cyclopropyl-6 trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. 30 The method may also include the compound having a CETP inhibitory activity being a compound of the formula (IV): CVDocurr-.ts and S. w 1sM OLc.ggngsTemoporary Intemet FilesVOLK85VSpecficaton of AU2008201550 (changes tracked) (2).doc 0 R3

R

5 N OR 4 R6 4 (IV)

R

7 I ri CH 3 R8 R 1 wherein R' is hydrogen, Y, W-X, W-Y; wherein W is a carbonyl, thiocarbonyl, sulfinyl or sulfonyl; 5 X is -O-Y, -S-Y, -N(H)-Y or -N-(Y)2; Y for each occurrence is independently Z or a fully saturated, partially unsaturated or fully unsaturated 1 to 10-membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may 10 be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the 15 sulfur is optionally mono- or di-substituted by oxo, the nitrogen is optionally mono- or di-substituted by oxo, and the carbon chain is optionally mono-substituted by Z; wherein Z is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 20 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected 25 independently from nitrogen, sulfur and oxygen; wherein Z substituent is optionally mono-, di- or tri substituted independently by halo, (C 2

-C

6 )alkenyl, (C 1 C 6 )alkyl, hydroxy, (Ci-C 6 )alkoxy, (C 1

-C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (C 1

-C

6 ) alkyloxycarbonyl, mono C:VDocunenlts and SettngsVaheadvLoca ngsVTemporry Intenot FilesOLK85VSpeelfication of AU2008201550 (changes tracked) (2).doc N- or di-N,N-(C 1

-C

6 )alkylamino wherein (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by halo, hydroxy, (Ci-C)alkoxy, (Cl

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cl 5 C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, the (Ci-C 6 )alkyl is optionally substituted by 1 to 9 fluorines;

R

3 is hydrogen or Q; wherein Q is a fully saturated, partially unsaturated or 10 fully unsaturated 1- to 6-membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom independently selected from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted 15 independently by halo, the carbon is optionally mono substituted by hydroxy, the carbon is optionally mono substituted by oxo, the sulfur is optionally mono- or di substituted by oxo, the nitrogen is optionally mono- or di-substituted by oxo, the carbon chain is optionally 20 mono-substituted by V; wherein V is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two 25 fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the V substituent is optionally mono-, di-, tri 30 or tetra-substituted independently by halo, (C 1 -C)alkyl, (C2-C6)alkenyl, hydroxy, (Ci-C 6 )alkoxy, (C1-C4)alkylthio, amino, nitro, cyano, oxo, carboxamoyl, mono-N- or di-N,N (Cl-C 6 )alkylcarboxamoyl, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the (Cl 35 C 6 )alkyl or (C 2

-C

6 )alkenyl substituent is optionally mono-, C:UDocuments and SettingsghadLoca r ngs&Temporary Internet FilsOLK85VSpedfcation of AU2008201550 (changes tracked) (2) doc di- or tri-substituted independently by hydroxy, (Cl

C

6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino or the (Ci-C 6 )alkyl or (C 2

-C

6 )alkenyl is 5 optionally substituted by 1 to 9 fluorines;

R

4 is Q 1 or V'; wherein Q 1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one 10 heteroatom selected independently from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is mono- or 15 di-substituted by oxo, the nitrogen is optionally mono- or di-substituted by oxo, the carbon chain is optionally mono-substituted by V'; wherein V 1 is a partially saturated, fully saturated or fully unsaturated 3- to 6 membered ring optionally having 1 or 2 heteroatoms 20 selected independently from oxygen, sulfur and nitrogen; the V1 substituent is optionally mono-, di-, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Cr

C

6 )alkoxy, amino, nitro, cyano, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the (C 1 25 C 6 )alkyl substituent is optionally mono-substituted by oxo, the (Ci-C 6 )alkyl substituent optionally has 1 to 9 fluorines; either R 3 should contain V or R 4 should contain Vi; and 5 6 7 8 R and R , or R 6 and R , and/or R and R8 are linked to form 30 at least one partially saturated or fully unsaturated 4 to 8-membered ring optionally having 1 to 3 heteroatoms independently selected from nitrogen, sulfur and oxygen; the rings (one or more) formed by R 5 and R 6 , or R 6 and R 7 , and/or R 7 and R 8 are optionally mono-, di- or tri 35 substituted independently by halo, (Ci-C 6 )alkyl, (Ci C:VDocuments a settingVahedVLoc IngsT mporay Intemet FlesVOLK85VSpedficalon of AU2008201550 (change tcked) (2).doc

C

6 )alkylsulfonyl, (C 2

-C

6 )alkenyl, hydroxy, (Cl-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono-, 5 di- or tri-substituted independently by hydroxy, (Cr

C

6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1 C 6 )alkylamino, and the (C 1

-C

6 )alkyl substituent optionally has 1 to 9 fluorines; provided that when the R , R 6 , R 7 10 and/or R 8 do not form at least one ring, they are each independently hydrogen, halo, (C 1

-C

6 )alkoxy or (Ci-C 6 )alkyl, wherein the (Ci-C 6 )alkyl optionally has 1 to 9 fluorines, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. 15 The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (IV), a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also be a compound of the formula 20 (IV), a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The method may also include the compound of the formula (IV) being a compound selected from a group consisting of 25 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-2,3,4,6,7,8-hexahydro cyclopenta[g]quinoline-l-carboxylic acid ethyl ester; [6R,8S]8-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl 30 amino]-6-methyl-3,6,7,8-tetrahydro-lH-2-thia-5-aza cyclopenta[b]naphthalene-5-carboxylic acid ethyl ester; [6R,8S]8-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-methyl-3,6,7,8-tetrahydro-2H furo[2,3-g]quinoline-5-carboxylic acid ethyl ester; 35 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) CADomments and SM .gsvah. LOca ngsToemporary Intemet FileswOLKa5VSpecication of AU2008201550 (cheges tracked) (2).doc methoxycarbonyl-amino]-2-methyl-3,4,6,8-tetrahydro-2H furo[3,4-g]quinoline-1-carboxylic acid ethyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-3,4,6,7,8,9-hexahydro-2H 5 benzo(g]quinoline-l-carboxylic acid propyl ester, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The inhibitor may also include the compound of the formula (IV) being a compound selected from a group 10 consisting of [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-2,3,4,6,7,8-hexahydro cyclopenta[g]quinoline-l-carboxylic acid ethyl ester; [6R,8S]8-[(3,5-bis-trifluoromethyl-benzyl) 15 methoxycarbonyl-amino]-6-methyl-3,6,7,8-tetrahydro-1H-2 thia-5-aza-cyclopenta[b]naphthalene-5-carboxylic acid ethyl ester; [6R,8S]8-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6-methyl-3,6,7,8-tetrahydro-2H furo[2,3-g]quinoline-5-carboxylic acid ethyl ester; 20 [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-3,4,6,8-tetrahydro-2H furo[3,4-g]quinoline-l-carboxylic acid ethyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-2-methyl-3,4,6,7,8,9-hexahydro-2H 25 benzo[g]quinoline-l-carboxylic acid propyl ester, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The method may also include the the compound having a CETP inhibitory activity being a compound of the formula 30 (V) C:UDocuments and SottingavaheaVLoc4ngTmporary Intemet FilesVOLK85USpecifncation of AU2006201550 (changes tracked) (2) doc 0 R3

R

5 N OR 4 R N CH 3

R

8 R wherein RT is a hydrogen, Y, W-X or W-Y; wherein W is carbonyl, thiocarbonyl, sulfinyl or 5 sulfonyl; X is -O-Y, -S-Y, -N(H)-Y or -N-(Y) 2 ; Y for each bond is independently Z or a fully saturated, partially unsaturated or fully unsaturated 1- to 10-membered straight chain or 10 branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with 1 or 2 heteroatoms selected from oxygen, sulfur and nitrogen as desired, the aforementioned carbon is independently mono-substituted, di-substituted or 15 tri-substituted by halogen as desired, the aforementioned carbon is mono-substituted by halogen, the aforementioned carbon is mono substituted by oxo as desired, the aforementioned sulfur is mono-substituted or di-substituted by oxo 20 as desired, the aforementioned nitrogen is mono substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono substituted by Z as desired; wherein Z is a partially saturated, fully saturated or fully 25 unsaturated 3- to 8-membered ring having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered C:VDocuments and SettngshadV~caY! ngsVTemporwy Inton F11sWOLK85WSpocifafion of AU2008201550 (changes tracked) (2).doc rings, taken independently, to have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen as desired; the aforementioned Z substituent is independently mono-substituted, di 5 substituted or tri-substituted as desired by halogen, (C 2

-C

6 )alkenyl, (C 1

-C

6 )alkyl, hydroxy, (Cl

C

6 )alkoxy, (C 1 -C4)alkylthio, amino, nitro, cyano, oxo, carboxyl, (Ci-C)alkyloxycarbonyl, mono-N-(Cr

C

6 )alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the l0 aforementioned (C 1 -C)alkyl substituent is independently mono-substituted, di-substituted or tri-substituted as desired by halogen, hydroxy, (Ci-C 6 ) alkoxy, (Ci-C 4 ) alkylthio, amino, nitro, cyano, oxo, carboxyl, (Ci-C)alkyloxycarbonyl, mono-N-(Cr 15 C 6 )alkylamino or di-N,N-(Ci-C 6 )alkylamino, the aforementioned (C 1

-C

6 )alkyl substituent is further substituted by 1 to 9 fluorines as desired;

R

3 is a hydrogen or Q; wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6 20 membered straight chain or branched carbon chain wherein the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen as desired, the aforementioned carbon is independently mono 25 substituted, di-substituted or tri-substituted by halogen as desired, the aforementioned carbon is mono-substituted by hydroxy as desired, the aforementioned carbon is mono-substituted by oxo as desired, the aforementioned sulfur is mono 30 substituted or di-substituted by oxo as desired, the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono-substituted by V as desired; 35 wherein V is a partially saturated, fully saturated C:V~ocuments and Stn aheadVLa gsV'TemWorary Intent FliesVOLKB5VSpaflcaon of AU2008201550 (changes tracked) (2) dc or fully unsaturated 3- to 8-membered ring having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, or a bicyclic ring consisting of two fused partially saturated, fully 5 saturated or fully unsaturated 3- to 6-membered rings, taken independently, to have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen as desired; the aforementioned V substituent is independently mono-substituted, di 10 substituted, tri-substituted or tetra-substituted as desired by halogen, (C-C6)alkyl, (C2-C6)alkenyl, hydroxy, (Ci-C) alkoxy, (Ci-C 4 ) alkylthio, amino, nitro, cyano, oxo, carbamoyl, mono-N-(Ci

C

6 )alkylcarbamoyl, di-N,N-(Ci-C 6 )alkylcarbamoyl, 15 carboxyl, (Ci-C 6 )alkyloxycarbonyl, mono-N-(Ci

C

6 )alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (Ci-C 6 )alkyl substituent or (C 2 C 6 )alkenyl substituent is independently mono substituted, di-substituted or tri-substituted as 20 desired by hydroxy, (Ci-C6)alkoxy, (Ci-C4)alkylthio, amino, nitro, cyano, oxo, carboxyl, (Ci

C

6 )alkyloxycarbonyl, mono-N-(Ci-C 6 )alkylamino or di N,N-(Ci-C 6 )alkylamino, the aforementioned (Ci

C

6 )alkyl substituent or (C 2

-C

6 )alkenyl substituent 25 is further substituted by 1 to 9 fluorines as desired;

R

4 is Q 1 or V1; wherein Q1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6 membered straight chain or branched carbon chain, 30 wherein the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen as desired, the aforementioned carbon is independently mono substituted, di-substituted or tri-substituted by 35 halogen as desired, the aforementioned carbon is C :Documents and SettjngsaheadLoca ngsVTemporary Intemet FilesOLK851Spedfication of AU2008201550 changes tracked) (2).doc mono-substituted by hydroxy as desired, the aforementioned carbon is mono-substituted by oxo as desired, the aforementioned sulfur is mono substituted or di-substituted by oxo as desired, 5 the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono-substituted by VI as desired; wherein V 1 is a partially saturated, fully saturated or fully unsaturated 3- to 6 10 membered ring having, as desired, 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen; the aforementioned V 1 substituent is independently mono-substituted, di substituted, tri-substituted or tetra-substituted 15 as desired by halogen, (Cl-C6)alkyl, (C1-C6)alkoxy, amino, nitro, cyano, (C-C 6 )alkyloxycarbonyl, mono N-(Cl-CE)alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (C 1

-C

6 )alkyl substituent is mono substituted as desired by oxo, and the 20 aforementioned (Ci-C 6 )alkyl substituent is further substituted by 1 to 9 fluorines as desired; R 3 should contain V or R 4 should contain V'; and 5 6 7R 8 R R , R 7 , and R are each independently hydrogen, hydroxy or oxy, wherein 25 the aforementioned oxy is substituted by T or a partially saturated, fully saturated or fully unsaturated 1- to 12 membered straight chain or branched carbon chain, the carbons other than a connecting carbons may be replaced with 1 or 2 heteroatoms selected from oxygen, sulfur and 30 nitrogen as desired, the aforementioned carbon is independently mono-substituted, di-substituted or tri substituted by halogen as desired, the aforementioned carbon is mono-substituted by hydroxy as desired, the aforementioned carbon is mono-substituted by oxo as 35 desired, the aforementioned sulfur is mono-substituted or C:b~ocuments and StingswaheadV" JngVTmporary Intemeot FilesOLK85VSpoafIcation of AU2008201550 (change tracked) (2).doc di-substituted by oxo as desired, the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono substituted as desired by T; wherein T is a partially 5 saturated, fully saturated or fully unsaturated 3- to 8 membered ring having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered 10 rings, taken independently, to have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen as desired; the aforementioned T substituent is independently mono-substituted, di-substituted or tri-substituted as desired by halogen, (Ci-C 6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, 15 (C 1

-C

6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (C 1

-C

6 )alkyloxycarbonyl, mono-N-(Ci-C 6 )alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (Ci

C

6 )alkyl substituent is independently mono-substituted, di-substituted or tri-substituted as desired by hydroxy, 20 (C1-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (C 1

-C

6 )alkyloxycarbonyl, mono-N-(Ci-C)alkylamino or di-N,N-(C1-C 6 )alkylamino, and the aforementioned (Ci

C

6 )alkyl substituent is further substituted as desired by 1 to 9 fluorines, 25 a prodrug thereof, a pharmaceutically acceptable salt of the compound or a pharmaceutically acceptable salt of the prodrug. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula 30 (V), a prodrug of the compound, a pharmaceutically acceptable salt of the compound or a pharmaceutically acceptable salt of the prodrug. The inhibitor may also be a compound of the formula (V), a prodrug of the compound, a pharmaceutically 35 acceptable salt of the compound or a pharmaceutically C Wooon. .. ds . n . VmoeaggingswmoraryIntent FioOLK85VSpecifiction of AU2008201550 (changstrcked) (2).doc acceptable salt of the prodrug. The method may also include the compound of the formula (V) being a compound selected from a group consisting of 5 [2R,4S]4-[(3,5-dichloro-benzyl)-methoxycarbonyl-amino] 6,7-dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2R,4SJ4-[(3,5-dinitro benzyl)-methoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; 10 [2R,4S]4-[(2,6-dichloro-pyridin-4-ylmethyl) methoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4-dihydro 2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S)4 [(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino] 6,7-dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l 15 carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis trifluoromethyl-benzyl)-methoxycarbonyl-amino]-6-methoxy 2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-7-methoxy-2-methyl-3,4-dihydro-2H 20 quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5 bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-6,7 dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl benzyl)-ethoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4 25 dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino]-6,7 dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2,2,2-trifluoro-ethyl ester; [2R,4S]4-[(3,5-bis 30 trifluoromethyl-benzyl)-methoxycarbonyl-amino-6,7 dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid propyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl benzyl)-methoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4 dihydro-2H-quinoline-l-carboxylic acid tert-butyl ester; 35 and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) C:VDocument and SettingsVahedVItoc WsTemporary Intermet FIlVOLK85VSpecicaton of AU2005201550 (dages tracked) (2).doc methoxycarbonyl-amino]-2-methyl-6-trifluoromethoxy-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable salt of the 5 prodrug. The inhibitor may also include the compound of the formula (V) being a compound selected from a group consisting of [2R,4S]4-[(3,5-dichloro-benzyl)-methoxycarbonyl-amino] 10 6,7-dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-1 carboxylic acid ethyl ester; [2R,4S]4-[(3,5-dinitro benzyl)-methoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4 dihydro-2H-quinoline-1-carboxylic acid ethyl ester; [2R,4S]4-[(2,6-dichloro-pyridin-4-ylmethyl) 15 methoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4-dihydro 2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4 [(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino] 6,7-dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis 20 trifluoromethyl-benzyl)-methoxycarbonyl-amino]-6-methoxy 2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) methoxycarbonyl-amino)-7-methoxy-2-methyl-3,4-dihydro-2H quinoline-l-carboxylic acid ethyl ester; [2R,4S]4-[(3,5 25 bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-6,7 dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid isopropyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl benzyl)-ethoxycarbonyl-amino] 6,7-dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-1 30 carboxylic acid ethyl ester; [2R,4S]4-[(3,5-bis trifluoromethyl-benzyl)-methoxycarbonyl-amino)-6,7 dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2,2,2-trifluoro-ethyl ester; [2R,4S]4-[(3,5-bis trifluoromethyl-benzyl)-methoxycarbonyl-amino]-6,7 35 dimethoxy-2-methyl-3,4-dihydro-2H-quinoline-l-carboxylic C:Vocuients and SettingswaheadVo ngswTemporary Intemet Fl s&OLK85VSpefcaion of AU2008201550 (changes tracked) (2) doc acid propyl ester; [2R,4S]4-[(3,5-bis-trifluoromethyl benzyl)-methoxycarbonyl-amino]-6,7-dimethoxy-2-methyl-3,4 dihydro-2H-quinoline-l-carboxylic acid tert-butyl ester; and [2R,4S]4-[(3,5-bis-trifluoromethyl-benzyl) 5 methoxycarbonyl-amino]-2-methyl-6-trifluoromethoxy-3,4 dihydro-2H-quinoline-l-carboxylic acid ethyl ester, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable salt of the prodrug. 10 The method may also include the compound having a CETP inhibitory activity being a compound having the formula (XII): Di 15 D21 R R4 R R16 6 R 5 R9 /R10 -/ / R2 n //2-Ri 1

R

3

R

1 4 R13 R12 (XII) or a pharmaceutically acceptable salt thereof, 15 wherein n is an integer selected from 1 through 4: X is oxy; Ri is selected from the group consisting of haloalkyl, haloalkenyl, haloalkoxymethyl, and haloalkenyloxymethyl 20 with the proviso that Ri has a higher Cahn-Ingold-Prelog stereochemical system ranking than both R 2 and (CHR 3 )n N(A)Q wherein A is the formula (XIII) and Q is the formula (XIV); C:VDocmet and SettingsheadVo I s sf porary Intemet FI0sVOLX85WSpecifcatiofn of AU200820155 (changes tracked) (2) doc R6 R6 R9 R10 R K R7 D J Y K2-R11 R4 D D2 R4 -- J4 (XIV) Z (XIII) R13 R12 R15

R

16 is selected from the group consisting of hydrido; alkyl; acyl; aroyl; heteroaroyl; trialkylsilyl; and a spacer selected from the group consisting of a covalent 5 single bond and a linear spacer moiety having a chain length of 1 to 4 atoms linked to the point of bonding of any aromatic substituent selected from the group consisting of R 4 , R 8 , R 9 and R 13 to form a heterocyclyl ring having from 5 through 10 continuous members: lo Di, D 2 , J 1 , J 2 and Ki are independently selected from the group consisting of C, N, 0, S and a covalent bond with the proviso that no more than one of D 1 , D 2 , J 1 , J 2 and Ki is a covalent bond; no more than one of Di, D 2 , J 1 , J 2 and Ki is 0; no more than one of D 1 , D 2 , J 1 , J 2 and Ki is S; one 15 of

D

1 , D 2 , J 1 , J 2 and Ki must be a covalent bond when two of D 1 ,

D

2 , J 1 , J 2 and Ki are 0 and S; and no more than four of Di , D2, J 1 , J 2 and Ki are N;

D

3 , D 4 , J3, J 4 and K 2 are independently selected from the 20 group consisting of C, N, 0, S and a covalent bond with the proviso that no more than one of D 3 , D4, J 3 , J 4 and K 2 is a covalent bond; no more than one of D3, D4, J 3 , J 4 and

K

2 is 0; no more than one of D 3 , D 4 , J 3 , J 4 and K 2 is S; no more than two of D 3 , D 4 , J 3 , J 4 and K 2 are 0 and S; one of 25 D3, D 4 , J 3 , J 4 and K 2 must be a covalent bond when two of D3, D4, J 3 , J 4 and K 2 are 0 and S; and no more than four of D3,

D

4 , J 3 , J 4 and K 2 are N;

R

2 is selected from the group consisting of hydrido, aryl, aralkyl, alkyl, alkenyl, alkenyloxyalkyl, haloalkyl, C:VDocurents and SettingwaheadVoc 1 I mporary Intmet FdesVOLK85VSpecifcation of AU2008201550 (changes tracked) (2).doc haloalkenyl, halocycloalkyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, dicyanoalkyl, and carboalkoxycyanoalkyl with 5 the proviso that R 2 has a lower Cahn-Ingold-Prelog system ranking than both R 1 and (CHR 3 )n-N(A)Q;

R

3 is selected from the group consisting of hydrido, hydroxy, cyano, aryl, aralkyl, acyl, alkoxy, alkyl, alkenyl, alkoxyalkyl, heteroaryl, alkenyloxyalkyl, lo haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, monocyanoalkyl, dicyanoalkyl, carboxamide, and carboxamidoalkyl with the provisos that

(CHR

3 ),-N(A)Q has a lower Cahn Ingold-Prelog stereochemical system ranking than R 1 and a higher Cahn 15 Ingold-Prelog stereochemical system ranking than R 2 ; Y is selected from a group consisting of a covalent single bond, (C(R14)2)q wherein q is an integer selected from 1 and 2 and (CH(R1 4 ))g-W-(CH(R14))p wherein g and p are integers independently selected from 0 and 1; 20 R 14 is selected from the group consisting of hydrido, hydroxy, cyano, hydroxyalkyl, acyl, alkoxy, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, monocarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, 25 carboalkoxy, carboxamide, and carboxamidoalkyl; Z is selected from the group consisting of a covalent single bond, (C(Ris)2)q wherein q is an integer selected from 1 and 2, and (CH(Ri 5 ))j-W-(CH(Ri 5 ))k wherein j and k are integers independently selected from 0 and 1: 30 W is selected from the group consisting of 0, C(O), C(S), C(0)N(R 14 ), C(S)N(R 14 ), (R 14 )NC(0), (R 14 )NC(S), S, S(0), S (0)2, S(0) 2 N(Ri 4 ), (Ri 4 )NC(0) 2 , and N(R 1 4 ) with the proviso that R 1 4 is other than cyano;

R

15 is selected from the group consisting of hydrido, 35 cyano, hydroxyalkyl, acyl, alkoxy, alkyl, alkenyl, alkynyl, C:ADocuments and SettingsOah.dVol frVsVTemporary Intemet FUesaOLKB5VSpcnflcatIon of AU2008201550 (changes tracked) (2).doc alkoxyalkyl, haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, monocarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, carboalkoxy, carboxamide, and carboxamidoalkyl; 5 R 4 , R 5 , R 6 , R 7 , R 8 , R9, R 10 , R 11 , R 12 , and R 13 are independently selected from the group consisting of hydrido, carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aroylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, 10 aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, 15 heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, 20 halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl, hydroxy, amino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, 25 arylsulfonylalkyl, heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkyl-amidosulfonyl, dialkyl-amidosulfonyl, 30 monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl-monoaryl-amidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, 35 aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, C:UDocuments and SettingsWahad) tVTomporary Intemet FieOLK85VSpecification of AU2008201550 (changes tracked) (2) doc haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, 5 haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, heteroaralkynyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, lo heteroaralkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylaminodocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, 15 phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl with the proviso that R 4 , R 5 , R 6 ,

R

7 , R 8 , R 9 , Rio, R 11 , R 12 , and R 13 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of 20 sulfur, and the divalent nature of oxygen;

R

4 and R 5 , R 5 and R 6 , R 6 and R 7 , R7 and R 8 , R 9 and RIO, Rio and

R

11 , R 11 and R 12 , and R 12 and R 1 3 are independently selected to form spacer pairs wherein a spacer pair is taken 25 together to form a linear moiety having from 3 through 6 continuous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 continuous members, a partially saturated heterocyclyl 30 ring having 5 through 8 continuous members, a heteroaryl ring having 5 through 6 continuous members, and an aryl with the provisos that no more than one of the group consisting of spacer pairs R 4 and R 5 , R 5 and R 6 , R 6 and R 7 , and R 7 and 35 R 8 , is used at the same time and that no more than one of C:V u t Wnd Sutings..w " M sVTemporary Intemet FilVOLK5VSpocfcation of AU2008201550 (dwgs tracked) (2) doc the group consisting of spacer pairs R 9 and R 10 , R 10 and

R

11 , R 1 and R 12 , and R 1 2 and R 1 3 is used at the same time;

R

4 and R 9 , R 4 and R 13 , R 8 and R 9 , and R 8 and R 13 are independently selected to form a spacer pair wherein said 5 spacer pair is taken together to form a linear moiety wherein said linear moiety forms a ring selected from the group consisting of a partially saturated heterocyclyl ring having from 5 through 8 continuous members and a heteroaryl ring having from 5 through 6 continuous members 10 with the proviso that no more than one of the group consisting of spacer pairs R 4 and R 9 , R 4 and R 13 , R 8 and R 9 , and R 8 and R 13 is used at the same time. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula 15 (XII)or a pharmaceutically acceptable salt thereof. The inhibitor may also be a compound of the formula (XII) or a pharmaceutically acceptable salt thereof. The method may also include the compound of the formula (XII) being a compound selected from the group 20 consisting of (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl][[3-(1,1,2,2 25 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyllamino]-1,1,1-trifluoro-2 propanol; 30 (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(2,3-dichlorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 35 propanol; C :Documnte and SettingswahedVLocT I saW mporary Intemet Fis OLKB5VSpecIfication of AU2008201550 (changes tracked) (2).doc (2R)-3-[[3-(4-fluorophenoxy)phenyll[[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino)-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl][[3-(1,1,2,2 5 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; lo (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyll[[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl] [[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 15 trifluoro-2-propanol; (2R)-3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino)-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl][[3-(1,1,2,2 20 tetrafluoroethoxy)phenyl]methyl]amino)-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(3-ethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; 25 (2R)-3-[[3-(3-t-butylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenylimethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-methylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 30 propanol; (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[3 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(phenoxy)phenyl][[3-(1,1,2,2 35 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 C:VDocms and SettnaheadVl a I sTemporary Intemot FilesOLKOVSpeccation of AU2008201550 (changes trecked) (2).doc propanol; (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[3-(1,1,2, 2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro 2-propanol; 5 (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 [[3-(trifluoromethoxy)phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 [[3-(trifluoromethyl)phenyl]methoxy]phenyl]amino]-1,1,1 10 trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 [[3,5-dimethylphenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 15 [[3-(trifluoromethylthio)phenyl]methoxy]phenyl]amino] 1,1,1-trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 [[3,5-difluorophenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 20 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 [cyclohexylmethoxylphenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 25 propanol; (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 30 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxylphenyl][[3 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 35 (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[3 C:Dom nt.s ad S.ung.ahe. o " ggsvTemporary Intemn FlWaOLK857Spocifcation of AU2008201550 (chages tracked) (2).doc (1,1,2, 2-tetrafluoroethoxy) phenyl]methyll amino] -1,1, 1-tri fluoro-2-propanol; (2R)-3-[[3-(3-trifluoromethylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 5 propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl] [[3 (pentafluoroethyl) phenylimethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [[3 10 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl] ([3 (pentafluoroethyl) phenylimethyl] amino] -1,1, 1-trifluoro-2 propanol; 15 (2R)-3-[[3-(2,3-dichlorophenoxy)phenyl] [[3 (pentafluoroethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propa no 1; (2R)-3-[[3-(4-fluorophenoxy)phenyl] [[3 (pentafluoroethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 20 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluorO-2 propanol; (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl] [[3 25 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl] [[3 (pentafluoroethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; 30 (2R)-3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxylphenyl] [[3-(pentafluoroethyl)phenyllmethyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-[3-(pentafluoroethyl)phenoxylphenyl] [[3 (pentafluoroethyl)phenyllmethyllamino] -1,1, 1-trifluoro-2 35 propariol; C:Vvocumerfs and Sa paheadVL-cf e1ga*Tmporwy Internal Fibes*OU(8SVSpedflcation of AU2008201550 (charns trecaed) (2).doc (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-ethylphenoxy)phenyl][[3-(pentafluoroethyl) 5 phenyl]methyl]amino)-1,1,1-trifluoro-2-propanol; (2R)-3-[[3-(3-t-butylphenoxy)phenyl][[3-(pentafluoroethyl) phenylimethyl]amino]-1,1,1-trifluoro-2-propanol; (2R)-3-[[3-(3-(methylphenoxy)phenyl) [[3-(pentafluoroethyl) phenyl]methyl]amino]-1,1,1-trifluoro-2-propanol; 10 (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(phenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 15 propanol; (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 20 (trifluoromethoxy)phenyl]methoxylphenyl]aminol-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethyl)phenylimethoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 25 (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3,5 dimethylphenyl]methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethylthio)phenyl]methoxy]phenyl]amino]-1,1,1 30 trifluoro-2-propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3,5 difluorophenyl]methoxy]phenyl]amino)-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3 35 [cyclohexylmethoxy]phenyl]amino]-1,1,1-trifluoro-2 C:VDocuments and SetUngs~ahead l etnglsfTenporary Internet F9ilsOLKB5VSpoddficaton of AU2008201550 (changes tracked) (2).doc propanol; (2R)-3-[[3-(2-clifluoromethoxy-4-pyridyloxy)phenyl] [13 (pentafluoroethyl)phenyl]methylamino]-1,1,1-trifluoro-2 propanol; 5 (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(3-ciifluoromethoxyphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 10 propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxylphenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxylphelyl] [[3 15 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl] [[3 (pentafluoroethyl)phenylmethylamino]-1,1,1-trifluoro-2 propanol; 20 (2R)-3-[[3-(3-isopropylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyl]methyllamiflo]-1,1,1-trifluoro-2 25 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [13 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3--(3-(2-furyl)phenoxy)phenyl] ([3 30 (heptafluoroethyl)phenyllmethyl~amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(2,3-ciichlorophenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllaminol-1,1,1-trifluoro-2 propanol; 35 (2R)-3-[[3-(4-fluorophenoxy)phenyl] [[3 CM - t &Mo,,efl n Sattngs~ahabdlLoI ct e2 sTonipoary hflgr-I. Flles*OLK8SSpecdlcaon of AU2=0201550 (dwmg.4 tracked) (2) doc (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl][[3 (heptafluoroethyl)phenylimethyl]amino]-1,1,1-trifluoro-2 5 propanol; (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3 (heptafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[3 10 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-([3-[3-(1,1,2,2 tetrafluoroethoxy)phenoxy]phenyl][[3 (heptafluoroethyl)phenyllmethyl]amino)-1,1,1-trifluoro-2 15 propanol; (2R)-3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl][[3 20 (heptafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-ethylphenoxy)phenyl][[3 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 25 (2R)-3-[[3-(3-t-butylphenoxy)phenyl][[3 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-methylphenoxy)phenyl][[3 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 30 propanol; (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[3 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(phenoxy)phenyl][[3-(heptafluoroethyl)phenyl] 35 methyllamino]-1,1,1-trifluoro-2-propanol: C* De*"''"*" S "ag*"h""'"VLo"1"" Temporary Intemet FBesVOLK85VSpedlction of AU2008201550 (changes tracked) (2).doc (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyl]methyl] [3-[[3 5 (trifluoromethoxy)phenyllmethoxylphenyllamino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyl]rnethyl] [3-[[3 (trifluoromethyl)phenyllmethoxylphenyl]amino]-1, 1, 1 trifluoro-2-propanol; 10 (2R)-3-[[[3-(heptafluoropropyl)phenyllmethyl] [3-[[3,5 dimethylphenyllmethoxylphenyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyl]methyl] [3-[[3 (trifluoromethylthio)phenyl]methoxylphenyllamino]-1, 1, 1 15 trifluoro-2-propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyllmethyl] [3-[[3,5 cifluorophenyllmethoxy] phenyl] amino] -1,1. 1-trifluoro-2 propa no 1; (2R)-3-[[[3-(heptafluoropropyl)phenyl]methyl] [3 20 [cyclohexylmethoxylphenyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[ [3-(2-difluoromethoxy-4-pyrilyloxy)phenyl] [[3 (heptafluoropropyl)phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; 25 (2R)-3-[[3--(3-cifluoromethoxyphenoxy)phenyl] [[3 (heptafluoropropyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxylphelyl] [[3 (heptafluoropropyl)phenyllmethyl]amino]-1,1,1-trifluoro- 2 30 propanol; (2R)-3-[ [3-(4-chloro-3-trifluoromethylphenoxy)phenyl] [[3 (heptafluoropropyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl] [[2-fluoro-5 35 (trifluoromethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 C ADocunent aW S eaKadcj j~q sVemorary Intere FilasOLKS54Specifcaton of AU2005201550 changess tracked) (2).doc propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; 5 (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3--(3-(2-furyl)phenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 10 propanol; (2R)-3-[[3-(2,3-ciichlorophenoxy)phenyl] ([2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-fluorophenoxy)phenyl] [[2-fluoro-5 15 (trifluoromethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; 20 (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 25 propanol; (2R) -3- [[3- [3- (1,1,2,2 tetrafluoroethoxy)phenoxy]phenyl] [[2-fluoro-5 (trifluoromethyl) phenylimethyl] amino] -1,1, 1-trifluoro-2 propanol; 30 (2R)-3-[[3-[3-(pentafluoroethyl)phenoxylphenyl] [[2-fluoro 5- (trifluoromethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 35 propanol; C Documents and S. insaheadLocy eT .gQsVTe.porary Intenrel FRoeOLKMKUS.cficatlon of AUf2008O15,5O (ctrangos treaed) (2) doc (2R)-3-[[3-(3-ethylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3-t-butylphenoxy)phenyl] [[2-fluoro-5 5 (triflucromethyl)phenyllmethyllamino]-1,1, 1-trifluoro-2 propanol; (2R) -3- [(3- (3-methyiphenoxy) phenyl] [[2-fluoro-5 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; l0 (2R)-3-[[3-(5,6,7,8-tetrahyiro-2-naphthoxy)phelyl] [[2 fluoro-5-(trifluoromethyl)phenyl]methyljamilo]-1,1,1 trifluoro-2-propanol; (2R) -3- [[3- (phenoxy) phenyl] II[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 15 propanol; (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphelyl][[2 fluoro-5- (trifluoromethyl) phenyl]methyl] amino] -1, 1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro--(trifluoromfethyl)pheflyllmethyl] [3 20 ([3-(trifluoromethoxy)phenyllmethoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phelyl]methyl] [3 [[3- (trifluoromethyl)phenylmethoxypheylail-1,1,1 trifluoro-2-propanol; 25 (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phelyllmethyl] [3 [[3,5-dimethylphenyllmethoxylphenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phelyllmethyll [3 [[3- (trifluoromethylthio)phenyllmethoxylphenyllamilo] 30 1,1, 1-trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyllmethy1] [3 [[3,5-difluorophenyllmethoxylphenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyllmethyl] [3 35 [cyclohexylmethoxylphenyllamiflO-1,1,1-trifluoro- 2 CXDoa~wfts wW SeffngagaheadV~ o t egW"Wpoary InM~ro Fl sOLKB5VSpecnflcation of AU200820155W (chang.. trscked) (2).doc propanol; (2R)-3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[2 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 5 (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[2 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 10 propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[2 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][2 15 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenylimethyl]amino]-1,1,1-trifluoro-2 propanol; 20 (2R)-3-[[3-(3-isopropylphenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 25 propanol; (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(2,3-dichlorophenoxy)phenyl][2-fluoro-4 30 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-fluorophenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 35 (2R)-3-[[3-(4-methylphenoxy)phenyl][2-fluoro-4 C:V~ocuments and S.tngsaaheadVLocI Iepo rary Internet FilazVOLK85VSpecification of AU2008201550 (changes tracked) (2) doc (tritluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[ [3-(2-fluoro-5-bromophenoxy)phenyl] [2-fluoro-4 (trifluoromethyl)phenyl]methyl]amiflo]-1,1,trifluoro-2 5 propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl] [2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R) -3- [[3- [3- (1,1,2,2 lo tetrafluoroethoxy)phenoxylphenyl] [2-fluoro-4 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[ [3-[3-(pentafluoroethyl)phenoxylphenyl] [2-fluoro 4- (trifluoromethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 15 propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl] [2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(3-ethylphenoxy)phenyl] [2-fluoro-4 20 (trifluoromethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[ [3-(3-t-butylphenoxy)phenyl] [2-fluoro-4 (trifluoromethyl)phenyl]methyljamino]-1,1,1-trifluoro- 2 propanol; 25 (2R)-3-[[3-(3-methylphenoxy)phenyl] [2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl] [2 fluoro-4- (trifluoromethyl) phenyllmethyl] amino] -1,1,1 30 trifluoro-2-propanol; (2R)-3-[[3-(phenoxy)phenyl] [2-fluoro-4-(trifluoromethyl) phenyllmethyllamino]-1,1,1-trifluoro-2-propanol; (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl] [2-fluoro 4-(trifluoromethyl)phenyllmethyl)aminol-1,1,1-trifluoro-2 35 propanol; C:VDoc~ments and Seturngv~aheadVLoc 1 I jotgskTienporary Internt Fdan*OLK85VSpecficalon at AU20O2015WO (changes tracked) (2).0Cc (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3 [[3-(trifluoromethoxy)phenyl]methoxylphenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3 5 [[3,5-dimethylphenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3 [[3-(trifluoromethylthio)phenyl]methoxy]phenyl]amino] 1,1,1-trifluoro-2-propanol; 10 (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3 [[3,5-difluorophenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3 [cyclohexylmethoxy]phenyl]amino)-1,1,1-trifluoro-2 15 propanol; (2R)-3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][2 fluoro-4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][2 20 fluoro-4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 25 (2R)-3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][2 fluoro-4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; and (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][2 fluoro-4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 30 trifluoro-2-propanol, or a pharmaceutically acceptable salt thereof. The inhibitor may also include the compound of the formula (XII) being a compound selected from the group consisting of 35 (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 C:" ' 'd S *g s hoadkIocj lot VeTemporary Intemo FIlos*OLX85Specification of AU2008201550 (changes tacked) (2).doc tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 5 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl][[3-(1,1,2,2 10 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(2,3-dichlorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyllmethyl]amino]-1,1,1-trifluoro- 2 propanol; 15 (2R)-3-[[3-(4-fluorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl][[3-(1,1,2, 2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 20 propanol; (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[3-(1,1,2,2 25 tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl] [[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 30 (2R)-3-[[3-[3-(pentafluoroethyl)phenoxylphenyl][[3 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]methyl]amino)-1,1,1-trifluoro-2 35 propanol; cmomwf . S. n saMn.. Vs..soj ygsVTemporay Ineet FilesOLK85VSpecktion of AU2008201550 changeo trked) (2).doc (2R)-3-[[3-(3-ethylphenoxy)phenyl] [[3-(1,1,2,2 tetrafluoroethoxy)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-t-butylphenoxy)phenyl] [[3-(1,1,2,2 5 tetrafluoroethoxy)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-methylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; 10 (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl] [[3 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(phenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyllmethyllamino]-1,1, 1-trifluoro-2 15 propanol; (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl] [[3-(1,1,2, 2-tetrafluoroethoxy)phenyllmethyl]amino]-1,1,1-trifluoro 2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3 20 [[3-(trifluoromethoxy)phenyllmethoxyjphenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3 [3-(trifluoromethyl)phenyllmethoxylphenyllamino]-1,1,1 trifluoro-2-propanol; 25 (2R)-3-[[[3-(1,1,2,2--tetrafluoroethoxy)phenyl]methyl] [3 [[3,5-dimethylphenyllmethoxylphenyllamino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl] [3 [[3- (trifluoromethylthio)phenyllmethoxylphenyllamino] 30 1,1, 1-trifluoro-2-propanol; (2R)-3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3 [[3,5-difluorophenyllmethoxylphenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3 35 [cyclohexylmethoxylphenyllamino]-1, 1, 1-trifluoro-2 CIocumerts and S.Thngs~ah9&dVLOjI na~mpoeray Internet FileagOU(85VSpecidcadon of AU20082OS550(cIhangea tracked) (2),doc propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl] [[3-(1,1,2,2 tetrafluoroethoxy) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; 5 (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl] [[3 (1,1,2, 2-tetrafluoroethoxy) phenyl]methyl] amino] -1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl] [[3-(1,1,2,2 tetrafluoroethoxy) phenyl]methyl] amino] -1,1, 1-trifluoro-2 lo propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxylphenyl] [[3 (1,1,2, 2-tetrafluoroethoxy) phenyl]methyll amino] -1,1,1 trifluoro-2-propanol; (2R)-3-[ [3-(4-chloro-3-trifluoromethylphenoxy)phenyl] [[3 15 (1,1,2,2-tetrafluoroethoxy)phenyl]methyl]amino]-1,1,1-tri fluoro-2-propanol; (2R)-3-[[3-(3-trifluoromethylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro- 2 propanol; 20 (2R)-3-[[3-(3-isopropylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [[3 (pentafluoroethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 25 propanol; (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl] [[3 (pentafluoroethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(2,3--dichlorophenoxy)phenyl] [[3 30 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(4-fluorophenoxy)phenyl] [[3 (pentafjluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro- 2 propanol; 35 (2R)-3-[[3-(4-methylphenoxy)phenyl] [[3 C:40owmwit and Son~ngsnahodVLOI 21gsWTm~porary Internal Fia"VOLK&SWSpofcation of AU2009201550 (changes tracked) (2).doc (pentafluoroethyl)phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(2-ffluoro-5-bromophenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 5 propanol; (2R)-3-[ [3-(4-chloro-3-ethylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxylphenyl] 10 [[3-(pentafluoroethyl)phenyllmethyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-([3-[3-(pentafluoroethyl)phenoxylphenyl] ([3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; 15 (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3-ethylphenoxy)phenyl] [[3- (pentafluoroethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2-propanol; 20 (2R)-3-[[3-(3-t-butylphenoxy)phenyl] [[3- (pentafluoroethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2-propanol; (2R)-3-[[3-(3-(methylphenoxy)phenyl) [[3-(pentafluoroethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2-propanol; (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl] [[3 25 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R) -3- [[3- (phenoxy) phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; 30 (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl] [[3 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-triflucro-2 propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl] [3-[[3 (trifluoromethoxy)phenyl~methoxylphenyl]amino]-1,1, 1 35 trifluoro-2-propanol; C Voommw.t and SetfnglfhearfIocT A Wemo Internet FilsOOLX851fSpecilcation of AU2008201550 (cOngos tracked) (2) doc (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethyl)phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3,5 5 dimethylphenyllmethoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl](3-[[3 (trifluoromethylthio)phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 10 (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3,5 difluorophenyl]methoxy]phenyllamino)-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(pentafluoroethyl)phenyl]methyl][3 [cyclohexylmethoxy]phenyl]amino]-1,1,1-trifluoro-2 15 propanol; (2R)-3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3 20 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 25 (2R)-3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy]phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 30 propanol; (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl][[3 35 (heptafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 C:VDocummet and StingswaheadVLo 2v WTmporary Intemet Flis.OLK55VSpecinction of AU200820150 (chane tracked) (2).doc propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; 5 (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyl]aminol-1,1,1-trifluoro-2 10 propanol; (2R)-3-[[3-(2,3-dichlorophenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamiflo]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-fluorophenoxy)phenyl] [[3 15 (heptafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; 20 (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-triflucro-2 propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 25 propanol; (2R) -3- [[3- [3- (1, 1, 2,2 tetrafluoroethoxy)phenoxylphenyl] [[3 (heptafluoroethyl)phenyl~methyl]amino]-l,1,1-trifluoro-2 propanol; 30 (2R)-3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamiflo]-1,1,1-trifluoro-2 35 propanol; C:Woc-monM and SacrngsaoadVLof !r5VskTwporary Interet F~esVOLKS5WSpecdficmkon of AU2008201550 (changes tracked) (2) doc (2R) -3- [[3- (3-ethyiphenoxy) phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,l-trifluoro- 2 propanol; (2R)-3-[[3-(3-t-butylphenoxy)phenyll [[3 5 (heptafluoroethyl)phenyl]methyl]amino]-1,l,1-trifluoro- 2 propanol; (2R)-3-[[3-(3-methylphenoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyl~amino]-1,1,1-trifluoro-2 propanol; l0 (2R)-3-[[3-(5,6,7,8-tetrahyclro-2-naphthoxy)phenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,l,1-trifluoro-2 propanol; (2R)-3-[ [3- (phenoxy)phenyl] [[3-(heptafluoroethyl)phenyl] methyl] aminol -1,1, 1-trifluoro-2-propanol: 15 (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl] [[3 (heptafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyllmethyl] [3-[[3 (trifluoromethoxy)phenyllmethoxylphenyl]amilo] -1, 1, 1 20 trifluoro-2-propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyl]methyl] [3-[[3 (trifluoromethyl) phenyllmethoxy] phenyl] amino] -1,1,1 trifluoro-2-propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyl]methyl] [3-[[3,5 25 direthylphenyllmethoxylphenyllamino]-l,l,l-trifluoro-2 propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyllmethyl] [3-[[3 (trifluoromethylthio)phenyl]methoxylphenyllamino]-1, 1,1 trifluoro-2-propanol; 30 (2R)-3-([[3-(heptafluoropropyl)phenyllmethyl] [3-[[3,5 difluorophenyllmethoxy] phenyl] amino] -1,1. 1-trifluoro-2 propanol; (2R)-3-[[[3-(heptafluoropropyl)phenyl]methyl] [3 [cyclohexylmethoxylphenyllamino]-l,l,1-trifluoro- 2 35 propanol; C:VD-sraw.nt and Satnse vVofIt sT pry ln1..w Fd..VOLKB5VSpaoflction of AU2OLS201550 (changes tracked) (2) doc (2R)-3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl] [[3 (heptafluoropropyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl] [[3 5 (heptafJluoropropyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxylphenyl] [[3 (heptafluoropropyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; 10 (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl] [[3 (heptafluoropropyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl] [[2-fluoro-5 (trifluororethyl)phenyl]methyl]amino]-1,1,1--trifluoro-2 15 propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; (2R)-3-[ [3-(3-cyclopropylphenoxy)phenyl] [[2-fluoro-5 20 (trifluoromethyl)phenyllmethyl~amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 25 (2R)-3-[[3-(2,3-ciichlorophenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyllamino]-1,1,1-trifluoro--2 propanol; (2R)-3-[[3-(4-fluorophenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyl]aminol-1,1,1-trifluoro-2 30 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl] [[2-fluoro-5 35 (trifluoromethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 C VDoamerts "r Sso g.hesdVLof tlrpTmrprTy Inene FHsvOLK85VSpecflcton of AU200=21550 (dwas tracked) (2).doc, propanol; (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 5 (2R)-3-[ [3-[3-(1,1,2,2 tetrafluoroethoxy)phenoxy]phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-[3-(pentafluoroethyl)phenoxy]phenyll[[2-fluoro 1o 5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; 15 (2R)-3-[[3-(3-ethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino)-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-t-butylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro- 2 20 propanol; (2R)-3-[[3-(3-methylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[2 25 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(phenoxy)phenyl] [[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 30 (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[2 fluoro-5-(trifluoromethyl)phenyl]methyllaminol-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [[3-(trifluoromethoxy)phenyl]methoxy]phenyl]amino]-1,1,1 35 trifluoro-2-propanol; C:VDfocments and Settng~shedVLocf sVTmporary intmet Fd DLK85VSpd1c4cation of AU2008201550 (changes tracked) (2).doc (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [[3-(trifluoromethyl)phenyllmethoxy]phenyllamino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 5 [[3,5-dimethylphenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [[3-(trifluoromethylthio)phenyl]methoxy]phenyl]amino] 1,1,1-trifluoro-2-propanol; 1o (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [[3,5-difluorophenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [cyclohexylmethoxy]phenyl]amino]-1,1,1-trifluoro-2 15 propanol; (2R)-3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[2 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[2 20 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 25 (2R)-3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[2 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][2 fluoro-5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 30 trifluoro-2-propanol; (2R)-3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-isopropylphenoxy)phenyl][2-fluoro-4 35 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 C :Documents and Settingsahead Lo I 9gsVTemporary Intemet FilesOLK85USpecflcation of AU2008201550 (changes tracked) (2).doc propanol; (2R)-3-[[3-(3-cyclopropylphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 5 (2R)-3-[[3-(3-(2-furyl)phenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(2,3-dichlorophenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 10 propanol; (2R)-3-[[3-(4-fluorophenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(4-methylphenoxy)phenyl][2-fluoro-4 15 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(2-fluoro-5-bromophenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 20 (2R)-3-[[3-(4-chloro-3-ethylphenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R) -3- [[3- [3- (1,1,2,2 tetrafluoroethoxy)phenoxy]phenyl][2-fluoro-4 25 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][2-fluoro 4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 30 (2R)-3-[[3-(3,5-dimethylphenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(3-ethylphenoxy)phenyl][2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 35 propanol; C:VDocuments and SettingswaheadVLocI VsVTomporry Intenet FUOs*OLKB5VSpecfication of AU2008201550 (changes traced) (2).doc (2R)-3-[[3-(3-t-butylphenoxy)phenyl] [2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; (2R) -3- [[3- (3-methylphenoxy)phenyl] [2-fluoro-4 5 (trifluoromethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; (2R)-3-[[3-(5,6,7,8-tetrahyciro-2-naphthoxy)phenyll [2 fluoro-4- (trifluoromethyl) phenyl]methyl] amino] -1,1,1 trifluoro-2-propanol; 10 (2R)-3-[[3-(phenoxy)phenyll [2-fluoro-4-(trifluoromethyl) phenyllmethyl] amino] -1,1, 1-trifluoro-2-propanol; (2R)-3-[[3-[3-(N,N-dimethylamino)phenoxylphenyl] [2-fluoro 4-(trifluoromethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; 15 (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3 [[3- (trifluoromethoxy)phenyllmethoxylphenyllamino] -1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3 [[3,5-dimethylphenyllmethoxylphenyl]amino]-1,1,1 20 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3 [[3-(trifluoromethylthio)phenyllmethoxylphenyllamino] 1,1, 1-trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3 25 [[3,5-difluorophenyllmethoxylphenyl]amino]-1,1,1 trifluoro-2-propanol; (2R)-3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3 [cyclohexylmethoxylphenyllamino] -1,1, 1-trifluoro-2 propanol; 30 (2R)-3-[ [3-(2-difluoromethoxy-4-pyridyloxy)phenyl] [2 fluoro-4- (trifluoromethyl) phenyl]methyl] amino] -1,1,1 trifluoro-2-propanol; (2R)-3-[[3-(2-trifluoromethyl-4-pyrilyloxy)phenyl] [2 fluoro-4- (trifluoromethyl) phenyl]methyl] amino] -1,1,1 35 trifluoro-2-propanol; C:VD - r~nots nd Se. sahad'lo~f Ylto.076porary Intenme4 FilsOLK85WSpedfcalion of AU2008201550 (changes tracked) (2) doo (2R)-3-[[3-(3-difluoromethoxyphenoxy)phenyll[[2-fluoro-4 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; (2R)-3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][2 5 fluoro-4-(trifluoromethyl)phenyl]methyl)amino]-1,1,1 trifluoro-2-propanol; and (2R)-3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][2 fluoro-4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol, or a pharmaceutically acceptable 1o salt thereof. The method may also include the compound having a CETP inhibitory activity being a compound represented by the formula (XV): R6

R

5

K

1 K

R

7 ii2 RR X R4 z 1 (CR 3 H)n N R 15 (XV) R2 R9 RD3 D

R

1 3

-D

4

J

3

-R

1 0 J4=K2 /\ R12 R11 15 or a pharmaceutically acceptable salt thereof, wherein; n is an integer selected from 0 through 5; Ri is selected from the group consisting of haloalkyl, haloalkenyl, haloalkoxyalkyl and haloalkenyloxyalkyl; X is selected from the group consisting of 0, H, F, S, 20 S(0), NH, N(OH), N(alkyl), and N(alkoxy);

R

16 is selected from the group consisting of hydrido, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, C:Documents and Settingsahoa I S svTemporay Intemet FUes*OLKS5VSpeelfication of AU2008201550 changes traced) (2).doc aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, 5 haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, monocarboalkoxyalkyl, monocarboalkoxy, dicarboalkoxyalkyl, monocarboxamido, monocyanoalkyl, dicyanoalkyl, 10 carboalkoxycyanoalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, dialkoxyphosphonoalkyl, trialklylsilyl, and a spacer selected from the group consisting of a covalent single bond and a linear spacer moiety having from 1 through 4 continuous atoms linked to the point of bonding 15 of an aromatic substituent selected from the group consisting of R 4 , R 8 , R 9 , and R 13 to form a heterocyclyl ring having from 5 through 10 continuous members with the provisos that said spacer moiety is other than a covalent single bond when R 2 is alkyl and there is no R 16 wherein X 20 is H or F;

D

1 , D 2 , Ji, J 2 and Ki are independently selected from the group consisting of C, N, 0, S and a covalent bond with the provisos that no more than one of D 1 , D 2 , J 1 , J 2 and Ki is a covalent bond, no more than one of D 1 , D 2 , J 1 , J 2 and 25 Ki is 0, no more than one of D 1 , D 2 , J 1 , J 2 and Ki is S, one of D 1 , D2, Ji, J 2 and Ki must be a covalent bond when two of

D

1 , D2, J 1 , J 2 and Ki are 0 and S, and no more than four of Di, D2, J 1 , J 2 and Ki are N; D3, D4, J 3 , J 4 and K 2 are independently selected from 30 the group consisting of C, N, 0, S and a covalent bond with the provisos that no more than one of D3, D4, J 3 , J 4 and K 2 is a covalent bond, no more than one of D 3 , D 4 , J 3 , J 4 and

K

2 is 0, no more than one of D 3 , D4, J 3 , J 4 and K 2 is S, one of D3, D 4 , J 3 , J 4 and K 2 must be a covalent bond when two of 35 D3, D 4 , J 3 , J 4 and K 2 are 0 and S, and no more than four of C:VDocumwts and Se~ttngsaahoadVLocI siTmporary Inteln Fiw*OLX65VSpeciftion of AU2008201550 (changes tracked) (2).doc

D

3 , D 4 , J 3 , J 4 and K 2 are N;

R

2 is independently selected from the group consisting of hydrido, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, 5 aralkyl, aralkoxyalkyl, aryloxyalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, aralkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, lo halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, 15 monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, alkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, 20 aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, 25 aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl and diaralkoxyphosphonoalkyl;

R

2 and R 3 are taken together to form a linear spacer 30 moiety selected from the group consisting of a covalent single bond and a moiety having from 1 through 6 continuous atoms to form a ring selected from the group consisting of a cycloalkyl having from 3 through 8 continuous members, a cycloalkenyl having from 5 through 8 continuous members, 35 and a heterocyclyl having from 4 through 8 continuous C:Ulocuments and Setngswahe " tV sVTemporary Intemet FilesOLK65VSpecifIcaton of AU2008201550 (changes trcked) (2).doc members;

R

3 is selected from the group consisting of hydrido, hydroxy, halo, cyano, aryloxy, hydroxyalkyl, amino, alkylamino, dialkylamino, acyl, sulfhydryl, acylamido, 5 alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl, heteroarylthio, aralkylthio, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aroyl, heteroaroyl, aralkylthioalkyl, heteroaralkylthioalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, lo alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, 15 halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, 20 haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, 25 heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, 30 dialkoxyphosphonoalkyl and diaralkoxyphosphonoalkyl; Y is selected from a group consisting of a covalent single bond, (C(R14)2)q wherein q is an integer selected from 1 and 2, and (CH(R1 4 ))g-W-(CH(R1 4 ))p wherein g and p are integers independently selected from 0 and 1; 35 R 1 4 is independently selected from the group consisting C :VDooo..nt..n S.t.ng.s.heoc !gsTemporary Internt Fils&OLK85VSpecalion of AU2008201550 (changes trAked) (2) doc of hydrido, hydroxy, halo, cyano, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, 5 aralkyl, aryloxyalkyl, aralkoxyalkylalkoxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, l0 cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, 15 heteroarylthicalkyl, heteroaralkylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, 20 arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, 25 aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, a spacer selected from a moiety having a chain length of 3 to 6 30 atoms connected to the point of bonding selected from the group consisting of R 9 and R 13 to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 continuous members and a heterocyclyl ring having from 5 through 8 continuous members, and a spacer selected 35 from a moiety having a chain length of 2 to 5 atoms C:VDocments and Settingswahead" i sVTemporary Intemet FIIos&OLK85VSpedfication of AU2008201550 dangers traded) (2) doc connected to the point of bonding selected from the group consisting of R 4 and R 8 to form a heterocyclyl having from 5 through 8 continuous members with the proviso that, when Y is a covalent bond, R 14 substituent is not attached to Y; 5 R 14 and R 14 , when bonded to the different atoms, are taken together to form a group selected from the group consisting of a covalent bond, alkylene, haloalkylene, and a spacer selected from a group consisting of a moiety having a chain length of 2 to 5 atoms connected to form a 10 ring selected from the group of a saturated cycloalkyl having from 5 through 8 continuous members, a cycloalkenyl having from 5 through 8 continuous members, and a heterocyclyl having from 5 through 8 continuous members;

R

1 4 and R 14 , when bonded to the same atom, are taken 15 together to form a group selected from the group consisting of oxo, thiono, alkylene, haloalkylene, and a spacer selected from the group consisting of a moiety having a chain length of 3 to 7 atoms connected to form a ring selected from the group consisting of a cycloalkyl having 20 from 4 through 8 continuous members, a cycloalkenyl having from 4 through 8 continuous members, and a heterocyclyl having from 4 through 8 continuous members; W is selected from the group consisting of 0, C(0), C(S) , C(0) N (R 14 ) , C(S) N (R 14 ) , (R 14 ) NC (0) , (R 14 ) NC(S) , S, S (0), 25 S(0) 2 , S(0) 2

N(R

14 ), (R 14

)NS(O)

2 , and N(R 14 ) with the proviso that R 14 is selected from other than halo and cyano; Z is independently selected from a group consisting of a covalent single bond, (C(Ri5)2)q wherein q is an integer selected from 1 and 2, and (CH(R 15 ))j-W-(CH(R 15 ))k wherein j 30 and k are integers independently selected from 0 and 1 with the proviso that, when Z is a covalent single bond, R 15 substituent is not attached to Z;

R

15 is independently selected, when Z is (C(Ri5)2)q wherein q is an integer selected from 1 and 2, from the 35 group consisting of hydrido, hydroxy, halo, cyano, aryloxy, C:VDocWuents and SettingsVaheadVLocj I sWTemporry Internet Flos&OLK851Specication of AU2008201550 (changes tracked) (2) doc amino, alkylamino, dialkylamino, hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkyl, alkylsulfinylalkyl, 5 alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, lo halocycloalkenlyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, 15 monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, 20 cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, 25 carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, a spacer selected from a moiety having a chain length of 3 to 6 atoms connected to the point of bonding selected from the 30 group consisting of R 4 and R 8 to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 continuous members and a heterocyclyl ring having from 5 through 8 continuous members, and a spacer selected from a moiety having a chain length of 2 to 5 atoms 35 connected to the point of bonding selected from the group C:VDocuments and SettngsVaheadV oo I !r, temporary Intemet FilesOLK85OSpedfication of AU200201550 (change traced) (2).doc consisting of R 9 and R 13 , to form a heterocyclyl having from 5 through 8 continuous members;

R

15 and R 15 , when bonded to the different atoms, are taken together to form a group selected from the group 5 consisting of a covalent bond, alkylene, haloalkylene, and a spacer selected from a group consisting of a moiety having a chain length of 2 to 5 atoms connected to form a ring selected from the group consisting of a saturated cycloalkyl having from 5 through 8 continuous members, a io cycloalkenyl having from 5 through 8 continuous members, and a heterocyclyl having from 5 through 8 continuous members;

R

15 and R 15 , when bonded to the same atom, are taken together to form a group selected from the group consisting 15 of oxo, thiono, alkylene, haloalkylene, and a spacer selected from the group consisting of a moiety having a chain length of 3 to 7 atoms connected to form a ring selected from the group consisting of a cycloalkyl having from 4 through 8 continuous members, a cycloalkenyl having 20 from 4 through 8 continuous members, and a heterocyclyl having from 4 through 8 continuous members;

R

15 is independently selected, when Z is (CH(Ri 5 ))j-W

(CH(R

15 ))k wherein j and k are integers independently selected from 0 and 1, from the group consisting of hydrido, 25 halo, cyano, aryloxy, carboxyl, acyl, aroyl, heteroaroyl, hydroxyalkyl, heteroaryloxyalkyl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl, heteroaryloxyalkyl, aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfonylalkyl, 30 alkylsulfinylalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, 35 halocycloalkoxy, halocycloalkoxyalkyl, C:UDocumenmt and SettingswahedVLOI emporary Intemset FilesOLK85USpeedication of AU2008201550 (change tracked) (2).doc halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, 5 dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, 10 cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, 15 dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, a spacer selected from a linear moiety having a chain length of 3 to 6 atoms connected to the point of bonding selected from the group consisting of R 4 and R 8 to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 20 through 8 continuous members and a heterocyclyl ring having from 5 through 8 continuous members, and a spacer selected from a linear moiety having a chain length of 2 to 5 atoms connected to the point of bonding selected from the group consisting of R 9 and R 1 3 to form a heterocyclyl ring having 25 from 5 through 8 continuous members;

R

4 , R 5 , R 6 , R 7 , R 8 , R 9 , Rio, R 11 , R 12 , and R 13 are independently selected from the group consisting of perhaloaryloxy, alkanoylalkyl, alkanoylalkoxy, alkanoyloxy, N-aryl-N-alkylamino, heterocyclylalkoxy, heterocyclylthio, 30 hydroxyalkoxy, carboxamidoalkoxy, alkoxycarbonylalkoxy, alkoxycarbonylalkenyloxy, aralkanoylalkoxy, aralkenoyl, N alkylcarboxamido, N-haloalkylcarboxamido, N cycloalkylcarboxamido, N-arylcarboxamidoalkoxy, cycloalkylcarbonyl, cyanoalkoxy, heterocyclylcarbonyl, 35 hydrido, carboxy, heteroaralkylthio, heteroaralkoxy, C:VDocuments and S.ttJngsVaheaVLo I sVTomporary Intenet FiesVOLK85VSpecfIction of AU2008120550 (dhnges tracked) (2) doc cycloalkylamino, acylalkyl, acylalkoxy, aroylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, 5 halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, heteroarylamino, N heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, 10 haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl, hydroxy, amino, thio, nitro, 15 lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl, 20 haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkylamidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkylmonoarylamidosulfonyl, arylsulfinyl, arylsulfonyl, 25 heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloaralkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, 30 cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, heteroaralkynyl, aryloxy, aralkoxy, aryloxyalkyl, saturated 35 heterocyclyl, partially saturated heterocyclyl, heteroaryl, C:Mlocuments nd SottgahedVo tngsVTemporary Intemet FilesVOLK85*Specification of AU2008201550 (changes tracked) (2) doc heteroaryloxy, heteroaryloxyalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, 5 carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl with the proviso that there are one to five non-hydrido ring substituents R 4 , R 5 , R 6 , R 7 , 10 and R 8 present, that there are one to five non-hydrido ring substituents R 9 , Rio, Rii, R 12 , and R 13 present, and R 4 , R 5 ,

R

6 , R 7 , R 8 , R 9 , Rio, R 11 , R 1 2 , and R 13 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, 15 and the divalent nature of oxygen;

R

4 and R 5 , R 5 and R 6 , R 6 and R7, R 7 and R 8 , R 9 and Rio, Rio and R 11 , R 11 and R 12 , and R 12 and R 13 are independently selected to form spacer pairs wherein a spacer pair is taken together to form a linear moiety having from 3 20 through 6 continuous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 continuous members, a partially saturated heterocyclyl ring having 5 through 8 continuous members, a 25 heteroaryl ring having 5 through 6 continuous members, and an aryl with the provisos that no more than one of the group consisting of spacer pairs R 4 and R 5 , R 5 and R 6 , R 6 and R 7 , and R 7 and R8, is used at the same time and that no more than one of the group consisting of spacer pairs R 9 30 and RIO, Rio and R 11 , Rii and R 12 , and R 12 and R 13 is used at the same time;

R

4 and R 9 , R 4 and R 13 , R8 and R 9 , and R 8 and R 1 3 are independently selected to form a spacer pair wherein said spacer pair is taken together to form a linear moiety 35 wherein said linear moiety forms a ring selected from the C:Dc ents and SttngsVahea" 2 &Tm laTtomeot FileoOOLKSSVSp ficato1n of AU2008201550 (dag.. traked) (2).dogroup consisting of a partially saturated heterocyclyl ring having from 5 through 8 continuous members and a heteroaryl ring having from 5 through 6 continuous members with the proviso that no more than one of the group consisting of 5 spacer pairs R 4 and R 9 , R 4 and R 1 3, R 8 and R9, and R 8 and R 13 is used at the same time. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (XV) or a pharmaceutically acceptable salt thereof. 10 The inhibitor may also include a compound of the formula (XV) or a pharmaceutically acceptable salt thereof. The method may also include the compound of the formula (XV) being a compound selected from the group consisting of 15 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 20 propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl][[3-(1,1,2,2 25 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 30 3-[[3-(4-fluorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-methylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyllamino]-1,1,1-trifluoro-2 35 propanol; C:VDoceon ts and SetngsgaheadVoc 943_sVTemporary Internat Flo.VOLX85VSpecficaion of AU2008201550 dangers tracked) (2).doc 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(4-chloro-3-ethylphenoxy)phenyl) [[3-(1,1,2,2 5 tetrafluoroethoxy)phenyl]-methyl]amino]-l,1,1-trifluoro-2 propanol; 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[3-(1, 1,2,2-tetrafluoro-ethoxy)phenylimethyl]amino]-1,1,1 trifluoro-2-propanol; 10 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3,5-dimethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 15 propanol; 3-[[3-(3-ethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-t-butylphenoxy)phenyl][[3-(1,1,2,2 20 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-methylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 25 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyll[[3-(1,1, 2

,

2 tetrafluoro-ethoxy)phenyl]methyllamino]-1,1,1-trifluoro-2 propanol; 3-[[3-(phenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenylimethyl]amino]-1,1,1-trifluoro-2 30 propanol; 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[3-(1,1,2,2 tetrafluoro-ethoxy)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-[[3 35 (trifluoromethoxy)-phenyl]methoxylphenyl]amino]-1,1,1 C:VDocments and SttngsvaheadV t sVTemporay Intmt Fle.VOLK65VSpecfication of AU2006201550 (chages tracked) (2).doc trifluoro-2-propanol, 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-[[3 (trifluoromethyl)-phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 5 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-[[3,5 dimethylphenyl]methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-[[3 (trifluoromethylthio)-phenyl]methoxy]phenyl]amino]-1,1,1 10 trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-[[3,5 difluorophenyl]methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 '5 [cyclohexylmethoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 25 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[3 30 (1,1,2,2-tetrafluoroethoxy)-phenyllmethyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(3-isopropylphenoxy)phenyl][[3 C:VDocumnts and SettingsaheadVLoc4 gs Temporary Intenet FifesOLK85VSpecflction of AU2008201550 (changes tracked) (2) doc (pentafluoroethyl)phenyl]methyl)-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl[[3 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[3 10 (pentafluoroethyl)phenyllmethyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyllamino]-1,1,1-trifluoro-2 propanol; 15 3-[[3-(4-methylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3 (pentafluoroethyl)phenyllmethyl]-amino]-1,1,1-trifluoro-2 20 propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[3 25 (pentafluoroethyl)-phenyl]methyl]amino]-1,1,1-trifluoro- 2 propanol; 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3 (pentafluoroethyl)phenyll-methyl]amino]-1,1,1-trifluoro-2 propanol; 30 3-[[3-(3,5-dimethylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-ethylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 35 propanol; C:VDocuments and SettingaMaheadLoc 9sTeanporary Internet FilesVOLK85VSpelflcation of AU2008201550 (change tracked) (2) doc 3-([3-(3-t-butylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-methylphenoxy]phenyl][[3 5 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[3 (pentafluoroethyl)phenyl)-methyl]amino-i,1,1-trifluoro-2 propanol; 10 3-[[3-(phenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 15 propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethoxy)phenyl]-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 20 (trifluoromethyl)phenyl)-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl](3-[[3-5 dimethylphenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 25 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethylthio)phenyl]-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3,5 difluorophenyllmethoxy]-phenyllamino]-1,1,1-trifluoro-2 30 propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3 [cyclohexylmethoxy]phenyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[3 35 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 C:Document and Set tngsvaheadLoc mporry intmot FlsVOLK5Specification of AU2008201550 (changes tracked) (2).doc propanol; 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 5 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 10 propanol; 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[3 (pentafluoroethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3 15 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 20 3-[[3-(3-cyclopropylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 25 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][[3 30 (heptafluoropropyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-methylphenoxy)phenyl][[3 heptafluoropropyl]phenyl]methyl]amino)-1,1,1-trifluoro-2 propanol; 35 3-[[3-(2-fluoro-5-bromophenoxy)phenyl]([3 C:VDocunfts and Setswahs " vsVTemporay Intemet FilesVOLK85VSpedlcatJon of AU2008201550 (dages traced) (2).doc (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[3 (heptafluoropropyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3 10 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3,5-dimethylphenoxy)phenyl][[3 (heptafluoropropyl)phenyllmethyl]-amino]-1,1,1-trifluoro-2 propanol; 15 3-[[3-(3-ethylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,l-trifluoro-2 propanol; 3-[[3-(3-t-butylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-l,1,1-trifluoro-2 20 propanol; 3-[[3-(3-methylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[3 25 (heptafluoropropyl)phenyl]methyl]amino)-1,1,1-trifluoro-2 propanol; 3-[[3-(phenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 30 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyll [[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3 (trifluoromethoxy)phenyl]-methoxy]phenyl]amino]-1,1,1 35 trifluoro-2-propanol: C :Docurnents and SettingswaheadVLoc 2rpswTemporarVy Inteot FitoVOLK85VSpoficaton of AU2008201550 (changes tracked) (2).doc 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3 (trifluoromethyl)phenyl]-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3,5 5 dimethylphenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3 (trifluoromethylthio)phenyl]-methoxyiphenyl]amino]-1,1,1 trifluoro-2-propanol; 10 3-[[[3-(heptafluoropropyl)phenyl]methyl) [3-[[3,5 difluorophenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3 [cyclohexylmethoxy]phenyl]-amino]-1,1,1-trifluoro-2 15 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3 20 (heptafluoropropyl)phenyl)-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino)-1,1,1-trifluoro-2 propanol; 25 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol: 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[3 (heptafluoropropyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 30 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][[2-fluoro-5 35 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 C:VDocuments and SetingsVahadVLocI VTempoary Inteoet Fil.s&OLK85VSpdflcation of AU2008201550 (changes tracked) (2) doc propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 5 3-[[3-(3-(2-furyl)phenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[2-fluoro-5 (trifluorometyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 10 propanol; 3-[[3-(4-fluorophenoxy)phenyl][(2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-methylphenoxy)phenyl][[2-fluoro-5 15 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[2 fluoro-5-(trifluoro-methyl)-phenyl]methyl]amino]-1,1,1 25 trifluoro-2-propanol; 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol: 3-[[3-(3,5-dimethylphenoxy)phenyl][[2-fluoro-5 30 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-ethylphenoxy)phenyl)[[2-fluoro-5 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(3-t-butylphenoxy)phenyl][[2-fluoro-5 C :Documents and SettingsaheadwLoc nngsTemporary Intemet Filos&OLK85USpecfication of AU2008201550 (changes tracked) (2) doc (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-methylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][(2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(phenoxy)phenyl][[2-fluoro-5 1o (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyllamino]-1,1,1-trifluoro-2 propanol; 15 3-[[[2-fluoro-5-(trifluoromethyl)phenyllmethyl][3-[[3 (trifluoromethoxy)-phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3 (trifluoromethyl)-phenyl]methoxy]phenyl]amino]-1,1,1 20 trifluoro-2-propanol; 3-[[[2-fluoro-5-(trifluoromethyl)phenylmethyl][3-[[3,5 dimethylphenyl]-methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol: 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3 25 (trifluoromethylthio)-phenyl]methoxy]phenyl]aminol-1,1,1 trifluoro-2-propanol; 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3,5 difluorophenyl]-methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; 3o 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [cyclohexylmethoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl) [[2-fluoro-5 (trifluoromethyl)-phenylimethyl]amino]-1,1,1-trifluoro-2 35 propanol; C:VDocuments and SetUns ad oc 2sVTewmporary Intemet FUesXOLK5VSpecification of AU2008201550 (dwgs tracked) (2).doc 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-5 5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 10 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[2-fluoro 5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 15 propanol; 3-[[3-(3-isopropylphenoxy)phenyl] [[2-fluoro-4 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[2-fluoro-4 20 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]-methyllamino]-1,1,1-trifluoro-2 propanol; 25 3-[[3-(2,3-dichlorophenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][[2-fluoro-4 trifluoromethyl]phenyl]-methyl]amino]-1,1,1-trifluoro-2 30 propanol; 3-[[3-(4-methylphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[2-fluoro-4 35 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 C:Wfocumeons and SottngsdahedVLoc sTemporary Intemot Filos*OLK85VSpecification of AU2008201550 (changes tracked) (2).doc propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl] [[2-fluoro-4 (trifluoromethyl) -phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; 5 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxylphenyl] [[2 fluoro-4- (trifluoro-methyl) phenyl]methyl] amino] -1,1,1 trifluoro-2-propanol; 3-[ [3-[3-(pentafluoroethyl)phenoxy]phenyl] [[2-fluoro-4 (trifluoromethyl) -phenyllmethyl] amino] -1,1, 1-trifluoro-2 10 propanol; 3-[[3-(3,5-dimethylphenoxy)phenyll [[2-fluoro-4 (trifluoromethyl)phenyl]-methyllamino]-1,1,1-trifluoro-2 propanol; 3-[ [3-(3-ethylphenoxy)phenyl] [[2-fluoro-4 15 (trifluoromethyl)phenyllmethyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[ [3- (3-t-butylphenoxy)phenyl] [[2-fluoro-4 (trifluoromethyl)phenyl]methyl] -amino]-1,1, 1-trifluoro-2 propanol; 20 3-f [3-(3-methylphenoxy)phenyll [[2-fluoro-4 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl] [[2-fluoro-4 (trifluoromethyl)-phenyllmethyllamino]-1,1,1-trifluoro-2 25 propanol; 3- [[3- (phenoxy) phenyl] [[2-fluoro-4 (trifluoromethyl) phenyl]methyl] amino] -1,1, 1-trifluoro-2 propanol; 3-[[j3-3-(N,N-cimethylamino)phenoxy]phenyl] [[2-fluoro-4 30 (trifluoromethyl)-phenyllmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[ [[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3-f [3 (trifluoromethoxy) -phenyllmethoxylphenyllamino]-1,1, 1 trifluoro-2-propanol; 35 3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3-[[3 CX~conet and Sstinp~ahesdV1.o !tgsTmpory Intome FftVLKanCU6Sp Ancaton of AU2008201550 (change. tmawd) (2).doc (trifluoromethyl)-phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3-[[3,5 dimethylphenyl]methoxy]phenyl]amino]-1,1,1-trifluoro-2 5 propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenl]methyl][3-[[3 (trifluoromethylthio)-phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenyl)methyl][3-[[3,5 10 difluorophenyl]-methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl][3-[3 [cyclohexylmethoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 15 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyll[[2-fluoro-4 (trifluoromethyl)-phenylimethylamino]-1,1,1-trifluoro-2 20 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methylamino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[2-fluoro-4 25 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; and 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[2-fluoro 4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol, or a pharmaceutically acceptable salt thereof. 30 The inhibitor may also include the compound of the formula (XV) being a compound selected from the group consisting of 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 35 propanol; C:VDocurnents and SetngsVaheadVLoc I OTmporay Internet FiosOLKB5SVSpeaflcation of AU2008201550 (changes tracked) (2).doc 3-[[3-(3-isopropylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino)-1,1,1-trifluoro-2 propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[3-(1,1,2,2 5 tetrafluoroethoxy)phenyl)-methyllamino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 10 3-[[3-(2,3-dichlorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyll[[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 15 propanol; 3-[[3-(4-methylphenoxy)phenyll[[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3-(1,1,2,2 20 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(4-chloro-3-ethylphenoxy)phenyl) [[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 25 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[3-(1, 1,2,2-tetrafluoro-ethoxy)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 30 propanol; 3-[[3-(3,5-dimethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-ethylphenoxy)phenyl][[3-(1,1,2,2 35 tetrafluoroethoxy)phenyl]-methyl]amino]-1,1,1-trifluoro-2 C:Docuents and SettngsvaheadVLocI 4rs*Tmporary intend FIbasOLK85VSpecification of AU2008201550 (changes tracked) (2).doc propanol; 3-[[3-(3-t-butylphenoxy)phenyl] [[3-(l,1,2,2 tetrafluoroethoxy) phenyl] -methyl] amino] -1,1, l-trifluoro-2 propanol; 5 3-[[3-(3-methylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)phenyl]-methyljamino]-l,1,1-trifluoro-2 propanol; 3-[[3-(5,6,7,8-tetrahyclro-2-naphthoxy)phenyll[[3-(1,l,2,2 tetrafluoro-ethoxy)phenyllmethyl]amino] -1,1, l-trifluoro-2 10 propariol; 3-[f3-(phenoxy)phenyl] [[3-(l,l,2,2 tetrafluoroethoxy)phenyllmethyllamino]-1,l,1-trifluoro-2 propanol; 3-[[3-[3-(N,N-dimethylamino)phenoxylphenyll [[3-(1,l,2,2 15 tetrafluoro-ethoxy)phenyllmethyl]amino]-l,1,1-trifluoro-2 propanol; 3-[[(3-(l,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3-[[3 (trifluoromethoxy)-phenyllmethoxylphenyllamino]-l,l,l trifluoro-2-propanol, 20 3-[[[3-(l,1,2,2-tetrafluoroethoxy)phenyllmethyll [3-[[3 (trifluoromethyl) -phenylimethoxy] phenyl] amino] -1,1,1 trifluoro-2-propanol; 3-[[(3-(l,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3-[[3,5 dimethylphenyllmethoxyllphenyllamino] -1,1, l-trifluoro-2 25 propanol; 3-[[[3-(1,l,2,2-tetrafluoroethoxy)phenyllmethyl] [3-[[3 (trifluoromethylthio)-phenyl]methoxylphenyllamino]-1,l,1 trifluoro-2-propanol; 3-[[[3-(l,1,2,2-tetrafluoroethoxy)phenyllmethyl] [3-[[3,5 30 difluorophenyllmethoxylphenyllamino]-1,l,l-trifluoro-2 propanol; 3-[[[3-(l,l,2,2-tetrafluoroethoxy)phenyllmethyl] [3 [cyclohexylmethoxy]phenyllamino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(2-ciifluoromethoxy-4-pyriciyloxy)phenyl] [[3-(1,l,2,2 C IDoc,,1erts mM Sestinga~ahesdVtocy "ff0Tmporary Intonmel FilOLK85VSp.cificatfon of AU20DS201550 (chang" trclkod) (2) doc tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3-(1,1,2,2 10 tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[3 (1,1,2,2-tetrafluoroethoxy)-phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 15 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 20 propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl)-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl[[3 25 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 30 3-[[3-(4-fluorophenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,l-trifluoro-2 propanol; 3-[[3-(4-methylphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 35 propanol; C:VDoumenls and SettingsvaheadVLocI | rnporary Intemet FlesVOLK8VSpecifcaion of AU2008201550 (changes traked) (2).doc 3-[ [3-(2-fluoro-5-bromophenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyll -amino] -1,1, 1-trifluoro-2 propanol; 3-[ [3-(4-chloro-3-ethylphenoxy)phenyl] [[3 5 (pentafluoroethyl)phenyllmethyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(1,1,2,2-tetrafluoroethoxy)phenoxylphenyl] [[3 (pentafluoroethyl) -phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; io 3-[[3--[3-(pentafluoroethyl)phenoxy]phenyl] [[3 (pentafluoroethyl)phenyl]-methyllaminol-1,1,1-trifluoro-2 propanol; 3-[[3-(3,5-dimethylphenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyl]-amino]-1,1,1-trifluoro-2 15 propanol; 3- [[3- (3-ethyiphenoxy) phenyl] [[3 (pentatluoroethyl)phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; 3-[ [3-(3-t-butylphenoxy)phenyl] [[3 20 (pentafluoroethyl)phenyllmethyl]amino]-1,1,1-trifluoro-2 propa no 1; 3-[ [3-[3-methylphenoxylphenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 propanol; 25 3-[[3-[3-(5,6,7,8-tetrahyciro-2-naphthoxy)phenyl] [[3 Cpentafluoroethyi)phenyl] -methyllamino-1, 1, 1-trifluoro-2 propanol; 3-[[3-(phenoxy)phenyl] [[3 (pentafluoroethyl)phenyllmethyllamino]-1,1,1-trifluoro-2 30 propanol; 3-[ [3-[3-(N,N-dimethylamino)phenoxy]phenyl] [[3 (pentafluoroethyl)phenyl]-methyllamino]-1,1,1-trifluoro-2 propanol; 3-[[[3-Cpentafluoroethyl)phenyllmethyl] [3-[[3 35 (trifluoromethoxy)phenyl]-methoxylphenyllamino]-1,1,1 C Wooume.,ts and Satt~gs*hsmdYocI rsmnporwy IM-n~t F~ie.*OLK8SiSpmflmtioo or AU2008201 550 (e*w.eg.s tracoked) (2) doc trifluoro-2-propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethyl)phenyl)-methoxy]phenyl]amino)-1,1,1 trifluoro-2-propanol; 5 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3-5 dimethylphenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3 (trifluoromethylthio)phenyl]-methoxy]phenyl]amino]-1,1,1 10 trifluoro-2-propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3-[[3,5 difluorophenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(pentafluoroethyl)phenyl]methyl][3 15 [cyclohexylmethoxy]phenyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-difiuoromethoxy-4-pyridyloxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 25 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3 (pentafluoroethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl) [[3 30 (pentafluoroethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(3-isopropylphenoxy)phenyl][[3 C:VDocuments nd SetingsaheadVLo sTemporary Intemet FlisVOLKS5VSpecification of AU2008201550 (changes tracked) (2) doc (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-cyclopropylphenoxy)phenyll [[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[3 10 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 15 3-[[3-(4-methylphenoxy)phenyl][[3 heptafluoropropyl]phenyl]methyl]amino]-1,1,l-trifluoro-2 propanol; 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 20 propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[3 25 (heptafluoropropyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 30 3-[[3-(3,5-dimethylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-ethylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,l-trifluoro-2 35 propanol; C:VDocuments and SetngsaheadwLoc | gsTemporary Internet FilesOLK 5VSpecifIcation of AU2008201550 changess tracked) (2) doc 3-[[3-(3-t-butylphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-l,1,1-trifluoro- 2 propanol; 3-[[3-(3-methylphenoxy)phenyl][[3 5 (heptafluoropropyl)phenyl]methyl]amino)-1,1,1-trifluoro-2 propanol; 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 10 3-[[3-(phenoxy)phenyl][[3 (heptafluoropropyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 15 propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3 (trifluoromethoxy)phenyl]-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol: 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3 20 (trifluoromethyl)phenyl)-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3,5 dimethylphenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 propanol; 25 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3 (trifluoromethylthio)phenyl]-methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3-[[3,5 difluorophenyl]methoxy]-phenyl]amino]-1,1,1-trifluoro-2 30 propanol; 3-[[[3-(heptafluoropropyl)phenyl]methyl][3 [cyclohexylmethoxy]phenyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[3 35 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 C:%Docmnwts and Setings aheadVLocl sV Tmporary Intemet FilswOLK85kSpecificaUan of AU2008201550 (change tracked) (2) doc propanol; 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 5 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[3 (heptafluoropropyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 10 propanol: 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[3 (heptafluoropropyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[2-fluoro-5 15 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[3-(3-cyclopropylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-(2-furyl)phenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 25 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[2-fluoro-5 (trifluorometyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][[2-fluoro-5 30 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-methylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[2-fluoro-5 C:VDocuments and So egsahemdVLocf tt gsVTemporary Intemet FilesOOLK85WSpecification of AU2008201550 (changes tracked) (2) doc (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[2 fluoro-5-(trifluoro-methyl)-phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[3-[3-(pentafluoroethyl)phenoxy]phenyl][[2-fluoro-5 10 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol: 3-[[3-(3,5-dimethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 15 3-[[3-(3-ethylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-t-butylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl)-amino]-1,1,1-trifluoro-2 20 propanol; 3-[[3-(3-methylphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl][[2-fluoro-5 25 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(phenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3o 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3 (trifluoromethoxy)-phenyl]methoxy]phenyl]amino]-1,1,1 35 trifluoro-2-propanol; C:VDocuments and Settngsa~headLocf sTeOmporary Intrnet FilesOLK85VSpedficaion of AU200820155 [changes tracked) (2) doc 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3 (trifluoromethyl)-phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3,5 5 dimethylphenyl]-methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol: 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3 (trifluoromethylthio)-phenyl]methoxy]phenyl]amino]-1,1,1 trifluoro-2-propanol; 10 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3-[[3,5 difluorophenyl]-methoxy]phenyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[2-fluoro-5-(trifluoromethyl)phenyl]methyl][3 [cyclohexylmethoxy]-phenyl]amino)-1,1,1-trifluoro-2 15 propanol; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl]l[[2-fluoro-5 20 (trifluoromethyl)-phenyl]methyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 25 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[2-fluoro-5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[2-fluoro 5-(trifluoromethyl)phenyl]methyl]amino]-1,1,1-trifluoro-2 30 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyll[[2-fluoro-4 (trifluoromethyl)-phenylimethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][[2-fluoro-4 35 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 C:VDoc ents and SettingsWaheadwLoc ?t3gadTemporary Intemel FilesOLK85USpectfication of AU2008201550 (changes tracked) (2) doc propanol; 3-[[3-(3-cyclopropylphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyll-methyl]amino]-1,1,1-trifluoro-2 propanol; 5 3-[[3-(3-(2-furyl)phenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl)-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 10 propanol; 3-[[3-(4-fluorophenoxy)phenyl][[2-fluoro-4 trifluoromethyl]phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-methylphenoxy)phenyl) [[2-fluoro-4 15 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2-fluoro-5-bromophenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(1,1,2,2-tetrafluoroethoxy)phenoxy]phenyl][[2 fluoro-4-(trifluoro-methyl)phenyl]methyl]amino]-1,1,1 25 trifluoro-2-propanol; 3-[[3-[3-(pentafluoroethyl)phenoxylphenyl][[2-fluoro-4 (trifluoromethyl)-phenylimethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3,5-dimethylphenoxy)phenyl][[2-fluoro-4 30 (trifluoromethyl)phenyl]-methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-ethylphenoxy)phenyl][[2-fluoro-4 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(3-t-butylphenoxy)phenyl][[2-fluoro-4 C:VDocuments and SetingsvaheadVLo I gVTemporary Intemet FlowOLK65VSpcification of AU2008201550 (changes tracked) (2).doc (trifluoromethyl)phenyl]methyl]-amino]-1,11-trifluoro-2 propanol; 3-[[3-(3-methylphenoxy)phenyl] [[2-fluoro-4 (trifluoromethyl)phenyl]methyl]-amino]-1,1,1-trifluoro-2 5 propanol; 3-[[3-(5,6,7,8-tetrahydro-2-naphthoxy)phenyl] [[2-fluoro-4 (trifluoromethyl) -phenyllmethyl] amino] -1,1, 1-trifluoro-2 propanol; 3-[ [3- (phenoxy) phenyl] [[2-fluoro-4 .io (trifluoromethyl)phenylllmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-[3-(N,N-dimethylamino)phenoxy]phenyl] [[2-fluoro-4 (trifluoromethyl) -phenyllmethyl] aminol -1,1, 1-trifluoro-2 propanol; 15 3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3-[[3 (trifluoromethoxy)-phenyllmethoxylphenyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3-[[3 (trifluoromethyl) -phenyl]methoxy]phenyl] amino] -1,1,1 20 trifluoro-2-propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenyl]methyl] [3-[[3,5 dimethylphenyllmethoxylphenyllamino]-1, 1, 1-trifluoro-2 propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenljmethyl] [3-[[3 25 (trifluoromethylthio) -phenyllmethoxy]phenyl]aminol-1, 1,1 trifluoro-2-propanol; 3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethy.] [3-[[3,5 difluorophenyl] -methoxylphenyl] amino] -1,1, 1-trifluoro-2 propanol; 30 3-[[[2-fluoro-4-(trifluoromethyl)phenyllmethyl] [3-[3 [cyclohexylmethoxy] -phenyl] amino] -1,1, 1-trifluoro-2 propa no 1; 3-[[3-(2-difluoromethoxy-4-pyridyloxy)phenyl] [[2-fluoro-4 (trifluoromethyl) -phenyllmethyl] amino] -1,1, 1-trifluoro-2 35 propanol; C:V~ef w ettng .s~ahenddl g"dT7epomy IMntene Fir.8eOLKS54fSpendfction of AU2008201550 (chang.. trmod) (2) denc 3-[[3-(2-trifluoromethyl-4-pyridyloxy)phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-difluoromethoxyphenoxy)phenyl][[2-fluoro-4 5 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(3-trifluoromethylthio)phenoxy]phenyl][[2-fluoro-4 (trifluoromethyl)-phenyl]methyl]amino]-1,1,1-trifluoro-2 propanol; and 10 3-[[3-(4-chloro-3-trifluoromethylphenoxy)phenyl][[2 fluoro-4-(trifluoromethyl)phenyl]methyl]amino]-1,1,1 trifluoro-2-propanol, or a pharmaceutically acceptable salt thereof. The method may also include the compound having a 15 CETP inhibitory activity being a compound having the formula (XVI): R2I

R

3 (XVI) or a pharmaceutically acceptable salt thereof, wherein 20 n is an integer selected from 1 through 2; A and Q are independently selected from the group consisting of -CH 2

(CR

3

-R

38 ) ,- (CR 33

R

34 ) u-T- (CR 35

R

36 ) w-H, R6 R11 R31 AQ-1 AQ-2 \ 1 / RS1 R7 J3--K2 Rioi k R32 R4-D2 R8 and R 9 A__ -B R12 / R13 C:Dc ent and Se/tingsv I M sT 3 mporry Intmet FilesOLKSVSpecfc.ation of AU2008201550 (dnges tracked) (2) doc with the provisos that one of A and Q must be AQ-1 and that one of A and Q must be selected from the group consisting of AQ-2 and -CH2 (CR 37

R

38 ) - (CR 33

R

3 4 ) u-T- (CR 35

R

3 6 ) w H; 5 T is selected from the group consisting of a single covalent bond, 0, S, S(0), S(0) 2 , C(R 3 3

)=C(R

35 ), and C=C; v is an integer selected from 0 through 1 with the proviso that v is 1 when any one of R 33 , R 3 4 , R 35 , and R 36 is aryl or heteroaryl; 10 u and w are integers independently selected from 0 through 6;

A

1 is C(R 30 );

D

1 , D 2 , J 1 , J 2 and Ki are independently selected from the group consisting of C, N, 0, S and a covalent bond with 15 the provisos that no more than one of Di, D 2 , J 1 , J 2 and Ki is a covalent bond, no more than one of D 1 , D 2 , J 1 , J 2 and Ki is 0, no more than one of D 1 , D 2 , J 1 , J 2 and Ki is S, one of D 1 , D 2 , J 1 , J 2 and Ki must be a covalent bond when two of D 1 , D 2 , J 1 , J 2 and Ki are 0 and S, and no more than four 20 of D 1 , D 2 , J 1 , J 2 and Ki are N;

B

1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are independently selected from the group consisting of C, C (R 30 ) , N, 0, S and a covalent bond with the provisos that no more than 5 of B 1 ,

B

2 , D 3 , D 4 , J 3 , J 4 and K 2 are a covalent bond, no more than 25 two of B 1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are 0, no more than two of B 1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are S, no more than two of

B

1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are simultaneously 0 and S, and no more than two of B 1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are N; Bi and D 3 , D 3 and J 3 , J 3 and K 2 , K 2 and J 4 , J 4 and D 4 , and D 4 30 and B 2 are independently selected to form an in-ring spacer pair wherein said spacer pair is selected from the group consisting of C(R 33

)=C(R

35 ) and N=N with the provisos that AQ-2 must be a ring of at least five continuous members, that no more than two of the group of said spacer 35 pairs are simultaneously C (R 3 3 )=C (R 3 5 ) , and that no more C :Vou.nts a Settgsah..dVLoc sWTemporr Intemet FilsOLK85WSpecifcation of AU2008201550 (dnge. tracked) (2).doc than one of the group of said spacer pairs are N=N unless the other spacer pairs is other than C(R 33

)=C(R

35 ), 0, N, and S; Ri is selected from the group consisting of haloalkyl and 5 haloalkoxymethyl;

R

2 is selected from the group consisting of hydrido, aryl, alkyl, alkenyl, haloalkyl, haloalkoxy, haloalkoxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl and heteroaryl; 10 R 3 is selected from the group consisting of hydrido, aryl, alkyl, alkenyl, haloalkyl and haloalkoxyalkyl; Y is selected from a group consisting of a covalent single bond, (CH2)q wherein q is an integer selected from 1 through 2, and (CH 2 )j-O-(CH2)k wherein j and k are integers 15 independently selected from 0 through 1; Z is selected from the group consisting of a covalent single bond, (CH2)q wherein q is an integer selected from 1 through 2, and (CH 2 )j-O-(CH2)k wherein j and k are integers independently selected from 0 through 1; 20 R 4 , R 8 , Rg and R 13 are independently selected from the group consisting of hydrido, halo, haloalkyl and alkyl;

R

30 is selected from the group consisting of hydrido, alkoxy, alkoxyalkyl, halo, haloalkyl, alkylamino, alkylthio, alkylthioalkyl, alkyl, alkenyl, haloalkoxy, and 25 haloalkoxyalkyl with the proviso that R 3 0 is selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R

3 0 , when bonded to Ai, is taken together to form an intra 30 ring linear spacer connecting the Ai-carbon at the point of attachment of R 30 to the point of bonding of a group selected from the group consisting of Rio, Rii, R 1 2 , R 31 , and R 32 wherein said intra-ring linear spacer is selected from the group consisting of a covalent single bond and a 35 spacer moiety having from 1 through 6 continuous atoms to C:Documents nd Sottingsvahead sVTemporary Inflmet FilesVOLK85WSpecification of AU2008201550 (dages tracked) (2) doc form a ring selected from the group consisting of a cycloalkyl having from 3 through 10 continuous members, a cycloalkenyl having from 5 through 10 continuous members, and a heterocyclyl having from 5 through 10 continuous 5 members;

R

3 0 , when bonded to Ai, is taken together to form an intra ring branched spacer connecting the Ai-carbon at the point of attachment of R 30 to the points of bonding of each member of any one of substituent pairs selected from the 10 group consisting of subsitituent pairs R 10 and R 11 , R 10 and

R

31 , Rio and R 32 , Rio and R 12 , R 11 and R 31 , R 11 and R 32 , R 11 and

R

12 , R 3 1 and R 32 , R 3 1 and R 12 , and R 32 and R 1 2 and wherein said intra-ring branched spacer is selected to form two rings selected from the group consisting of cycloalkyl 15 having from 3 through 10 continuous members, cycloalkenyl having from 5 through 10 continuous members, and heterocyclyl having from 5 through 10 continuous members;

R

4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 1 2 , R 13 , R 3 1 , R 32 , R 33 , R 34 ,

R

35 , and R 36 are independently selected from the group 20 consisting of hydrido, carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aroylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, 25 aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, 30 alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl, hydroxy, amino, thio, nitro, 35 lower alkylamino, alkylthio, alkylthioalkyl, arylamino, C;4Documents and Stin hondVLc. 8pngsTemporary Intemet FilsvO.KB5VSSpecfication of AU2008201550 (changes tracked) (2) doc aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl, 5 haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl-monoaryl-amidosulfonyl, lo arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, 15 alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, 20 heteroaralkynyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, 25 arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl with the provisos that R 4 , R 5 , R 6 , 30 R7, R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R3 1 , R 32 , R 33 , R 34 , R 3 5 , and R 36 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen, that no more than three of the R 33 and 35 R 34 substituents are simultaneously selected from other C:VDom ets and SttngsvaheadV 8 WTeamporary Intemet Files&OLK85VSpecifIcation of AU2008201550 (changes traed) (2).doc than the group consisting of of hydrido and halo, and that no more than three of the R 35 and R 3 6 substituents are simultaneously selected from other than the group consisting of of hydrido and halo: 5 R 9 , Rio, Rii, R 12 , R 13 , R 31 , and R 32 are independently selected to be oxo with the provisos that B 1 , B 2 , D 3 , D 4 ,

J

3 , J 4 and K 2 are independently selected from the group consisting of C and S, no more than two of R9, Rio, R 11 , R 1 2 ,

R

13 , R 31 , and R 32 are simultaneously oxo, and that R 9 , Rio, 1o R 11 , R 12 , R 13 , R3 1 , and R 32 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R

4 and R 5 , R 5 and R 6 , R 6 and R7, R 7 and R 8 , R 9 and RIO, Rio 15 and R 11 , Rii and R31, R 31 and R 32 , R 32 and R 12 , and R 12 and R 13 are independently selected to form spacer pairs wherein a spacer pair is taken together to form a linear moiety having from 3 through 6 continuous atoms connecting the points of bonding of said spacer pair members to form a 20 ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 continuous members, a partially saturated heterocyclyl ring having 5 through 8 continuous members, a heteroaryl ring having 5 through 6 continuous members, and an aryl with the provisos that no more than 25 one of the group consisting of spacer pairs R 4 and R 5 , R 5 and R 6 , R 6 and R 7 , and R 7 and R 8 , are used at the same time and that no more than one of the group consisting of spacer pairs R 9 and Rio, Rio and R 11 , R 11 and R 31 , R 31 and R 32 ,

R

3 2 and R 12 , and R 12 and R 13 are used at the same time; 30 R 9 and R 11 , R 9 and R 12 , R9 and R 13 , R 9 and R 31 , R 9 and R 32 , Rio and R 12 , Rio and R 13 , Rio and R 3 1 , Rio and R 32 , R 11 and R1 2 , R 11 and R 13 , R 11 and R 32 , R 12 and R 31 , R 1 3 and R 31 , and R 13 and R 32 are independently selected to form a spacer pair wherein said spacer pair is taken together to form a linear spacer 35 moiety selected from the group consisting of a covalent C:VDocwnts and Settingsvah.edVLocT |8g sVTomporry Intomet FiesVOLKB5VSpecefcation of AU2008201550 (changes tracked) (2).doc single bond and a moiety having from 1 through 3 continuous atoms to form a ring selected from the group consisting of a cycloalkyl having from 3 through 8 continuous members, a cycloalkenyl having from 5 through 8 5 continuous members, a saturated heterocyclyl having from 5 through 8 continuous members and a partially saturated heterocyclyl having from 5 through 8 continuous members with the provisos that no more than one of said group of spacer pairs is used at the same time; 10 R 3 7 and R 38 are independently selected from the group consisting of hydrido, alkoxy, alkoxyalkyl, hydroxy, amino, thio, halo, haloalkyl, alkylamino, alkylthio, alkylthioalkyl, cyano, alkyl, alkenyl, haloalkoxy, and haloalkoxyalkyl. 15 The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (XVI) or a pharmaceutically acceptable salt thereof. The inhibitor may also be a compound of the formula (XVI) or a pharmaceutically acceptable salt thereof. 20 The method may also include the compound of the formula (XVI) being a compound selected from the group consisting of 3-[[3-(4-chloro-3-ethylphenoxy)phenyl] (cyclohexylmethyl)aminol-1,1,1-trifluoro-2-propanol; 25 3-[[3-(4-chloro-3-ethylphenoxy)phenyl] (cyclopentylmethyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl] (cyclopropylmethyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][(3 30 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][(3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 35 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][(3 C:*Douments and SetingssieadLocf I O Thempor ay Inteomet FUesVOLKB5VSpcifiction of AU2008201550 (chnq tracked) (2).doc trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 5 2-propanol; 3-[[3-(3 trifluoromethoxyphenoxy)phenyl][(cyclohexylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 10 trifluoromethoxyphenoxy)phenyl](cyclopentylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 trifluoromethoxyphenoxy)phenyl](cyclopropylmethyl)amino] 1,1,1]-trifluoro-2-propanol; 15 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl](3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 20 2-propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 25 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-isopropylphenoxy)phenyl](cyclohexylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 30 isopropylphenoxy)phenyl](cyclopentylmethyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(3 isopropylphenoxy)phenyl](cyclopropylmethyl)amino]-1,1,1 trifluoro-2-propanol; 35 3-[[3-(3-isopropylphenoxy)phenyl][(3 C:bDocmnt end SettnseheadVLoc I p VsWTemporary Iorgmet FilsVOLK85VSpedfication of AU20020I 550 (changes tracked) (2).doc trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][(3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 5 2-propanol; 3-[[3-(3-isopropylphenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-isopropylphenoxy)phenyl][3-(1,1,2,2 10 tetrafluoroethoxy)cyclohexyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(2,3 dichlorophenoxy)phenyl](cyclohexylmethyl)amino]-1,1,1 trifluoro-2-propanol; 15 3-[[3-(2,3 dichlorophenoxy)phenyl](cyclopentylmethyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(2,3 dichlorophenoxy)phenyl](cyclopropylmethyl)amino]-1,1,1 20 trifluoro-2-propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][(3 25 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 30 3-[[3-(2,3-dichlorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(4-fluorophenoxy)phenyl](cyclohexylmethyl)amino] 1,1,1-trifluoro-2-propanol; 35 3-[[3-(4-fluorophenoxy)phenyl](cyclopentylmethyl)amino C:VDouets and SsttingMahahd o saaTemporary intemet FesVOLK85VSpeelfcation of AU2008201550 (changes tracked) (2).doc 1,1,1-trifluoro-2-propanol; 3-[[3-(4-fluorophenoxy)phenyl](cyclopropylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(4-fluorophenoxy)phenyl][(3 5 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][(3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 10 3-[[3-(4-fluorophenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol, 3-[[3-(4-fluorophenoxy)phenyl][3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 15 2-propanol; 3-[[3-(3 trifluoromethoxybenzyloxy)phenyll(cyclohexylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 20 trifluoromethoxybenzyloxy)phenyl](cyclopentylmethyl)amino] -1,1,1-trifluoro-2-propanol; 3-[[3-(3 trifluoromethoxybenzyloxy)phenyl] (cyclopropylmethyl)amino] -1,1,1-trifluoro-2-propanol; 25 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][(3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 30 2-propanol; 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][[3-(1,1,2,2 35 tetrafluoroethoxy)cyclohexylmethyllamino]-1,1,1-trifluoro C:VDocuOts and SettigsvaheaVLoj 9?t 7 Vs&Temporary Intemet FI&OLK85VSpecincation of AU2008201550 (dages tracked) (2).doc 2-propanol; 3-[[3-(3 trifluoromethylbenzyloxy)phenyl](cyclohexylmethyl)amino] 1,1,1-trifluoro-2-propanol; 5 3-[[3-(3 trifluoromethylbenzyloxy)phenyll(cyclopentylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 trifluoromethylbenzyloxy)phenyl] (cyclopropylmethyl)aminol 10 1,1,1-trifluoro-2-propanol; 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][(3 15 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][[(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 20 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl](cyclohexyl)amino] 1,1,1-trifluoro-2-propanol; 25 3-[[[(3-pentafluoroethyl)phenyl]methyl) (cyclohexyl)aminol 1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](cyclohexyl)amino) 1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2 30 tetrafluoroethoxy)phenyl]methyl](cyclohexyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl](4 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][(4 35 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; C:Vocmnts and Setting.vahedVLocI e sVTrporay Intme FesVOLK95VSpeflication of AU2002O055O (change traced) (2).doc 3-[[[(3-trifluoromethoxy)phenyl]methyl][[4 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](4 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 5 3-[[[(3-trifluoromethyl)phenyl]methyl] (3-trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 10 propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](3 15 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][3-(4-chloro-3 20 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-(4 chloro-3-ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2 25 propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 30 3-([[(3-trifluoromethoxy)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl] (3 35 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; C:VDocuments and SettngsVaheadVLoc I S WTmporary Intrnet FilosOLKS5VSpeciflcaton of AU20082O550 (changes tracked) (2).doc 3-[[[(3-pentafluoroethyl)phenyllmethyl](3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 5 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 10 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 15 propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyllmethyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 20 isopropoxycyclohexyl)amino)-1,1,1-trifluoro-2-propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 25 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl][3-(4-chloro-3 3o ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl][3-(1,2,2 tetrafluoroethoxy)cyclohexyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 35 pentafluoroethylcyclohexyl)amino]-1,1,1-trifluoro-2 CVDocuments and SetigswaheadVLoc m Temporay Intermt FilsOOLK85VSpecification of AU2008201550 (changes tracked) (2) doc propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 trifluoromethoxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 5 3-[[[(3-trifluoromethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl][3-(4-chloro-3 10 ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-(4 chloro-3-ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl][3-(4-chloro-3 15 ethylphenoxy)-2,2-di-fluoropropyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)-2,2-difluoropropyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[[(3-trifluoromethoxy)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)-2,2-difluoropropyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-(4 chloro-3-ethylphenoxy)-2,2-difluoropropyl]amino]-1,1,1 25 trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl][3 (isopropoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][3 (isopropoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 30 3-[[[(3-trifluoromethoxy)phenyl]methyl][3 (isopropoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 (isopropoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; and C:VDocuments and SettngsVaheadLoc |ngsVTemporary Internet Filos*OLX85VSpecfication of AU2008201550 (changes tracked) (2).doc 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 (phenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol, or a pharmaceutically acceptable salt thereof. The inhibitor may also include the compound of the 5 formula (XVI) being a compound selected from the group consisting of 3-[[3-(4-chloro-3 ethylphenoxy)phenyl](cyclohexylmethyl)amino]-1,1,1 trifluoro-2-propanol; 10 3-[[3-(4-chloro-3 ethylphenoxy)phenyl](cyclopentylmethyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(4-chloro-3 ethylphenoxy)phenyl](cyclopropylmethyl)amino]-1,1,1 15 trifluoro-2-propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyll[(3 20 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyllamino]-1,1,1-trifluoro 2-propanol; 25 3-[[3-(4-chloro-3-ethylphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl] [(cyclohexylmethyl)amino]-1,1,1-trifluoro-2-propanol; 30 3-[[3-(3 trifluoromethoxyphenoxy)phenyl](cyclopentylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 trifluoromethoxyphenoxy)phenyl](cyclopropylmethyl)amino] 35 1,1,1]-trifluoro-2-propanol; C:UDocuments and Setings~agahm I s6VTemporary Intede FiesVOLK85VSpecfication of AU2008201550 changes tracked) (2).doc 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl](3 5 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 1o 3-[[3-(3-trifluoromethoxyphenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-isopropylphenoxy)phenyl](cyclohexylmethyl)amino) 1,1,1-trifluoro-2-propanol; 15 3-[[3-(3 isopropylphenoxy)phenyl) (cyclopentylmethyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(3 isopropylphenoxy)phenyl](cyclopropylmethyl)amino]-1,1,1 20 trifluoro-2-propanol; 3-[[3-(3-isopropylphenoxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-isopropylphenoxy)phenyl][(3 25 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-isopropylphenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 30 3-[[3-(3-isopropylphenoxy)phenyl][3-(1,1,2,2 tetrafluoroethoxy)cyclohexyl]methyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(2,3 dichlorophenoxy)phenyl](cyclohexylmethyl)amino]-1,1,1 35 trifluoro-2-propanol; C:VDocments and SMn gslaheadwILoT I .sfTemporary Internet FileskOLK85VSpsdecftion of AU2008201550 (changes tracked) (2).doc 3-[[3-(2,3 dichlorophenoxy)phenyl](cyclopentylmethyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(2,3 5 dichlorophenoxy)phenyl](cyclopropylmethyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl)amino]-1,1,1-trifluoro-2 propanol; 10 3-[[3-(2,3-dichlorophenoxy)phenyl][(3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 15 2-propanol; 3-[[3-(2,3-dichlorophenoxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(4-fluorophenoxy)phenyl](cyclohexylmethyl)amino] 20 1,1,1-trifluoro-2-propanol; 3-[[3-(4-fluorophenoxy)phenyl) (cyclopentylmethyl)amino 1,1,1-trifluoro-2-propanol; 3-[[3-(4-fluorophenoxy)phenyl](cyclopropylmethyl)amino] 1,1,1-trifluoro-2-propanol; 25 3-[[3-(4-fluorophenoxy)phenyll[(3 trifluoromethyl)cyciohexylmethyllamino]-1,1,1-trifluoro-2 propanol; 3-[[3-(4-fluorophenoxy)phenyl][(3 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 30 2-propanol; 3-[[3-(4-fluorophenoxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol, 3-[[3-(4-fluorophenoxy)phenyl][3-(1,1,2,2 35 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro C:UDocumenta and Soungsahes" 4 gs&Temporary Intefnt FliOsOLK85VSpecincation of AU2008201550 (d anges tracked) (2).doc 2-propanol; 3-[[3-(3 trifluoromethoxybenzyloxy)phenyl](cyclohexylmethyl)amino] 1,1,1-trifluoro-2-propanol; 5 3-[[3-(3 trifluoromethoxybenzyloxy)phenyl](cyclopentylmethyl)amino] -1,1,1-trifluoro-2-propanol; 3-[[3-(3 trifluoromethoxybenzyloxy)phenyl](cyclopropylmethyl)amino] 10 -1,1,1-trifluoro-2-propanol; 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl)[(3 15 pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 20 3-[[3-(3-trifluoromethoxybenzyloxy)phenyl][[3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3 trifluoromethylbenzyloxy)phenyl](cyclohexylmethyl)amino] 25 1,1,1-trifluoro-2-propanol; 3-[[3-(3 trifluoromethylbenzyloxy)phenyl] (cyclopentylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3 30 trifluoromethylbenzyloxy)phenyl](cyclopropylmethyl)amino] 1,1,1-trifluoro-2-propanol; 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][(3 trifluoromethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro-2 propanol; 35 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][(3 C:VDocuments ad SettingsahedV" 8 sTmporary Intemel FlesvOLK85VSpecificalion of AU2008201550 (charges tracked) (2).doc pentafluoroethyl)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][[(3 trifluoromethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 5 2-propanol; 3-[[3-(3-trifluoromethylbenzyloxy)phenyl][3-(1,1,2,2 tetrafluoroethoxy)cyclohexylmethyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl](cyclohexyl)amino] 1o 1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](cyclohexyl)amino) 1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl] (cyclohexyl)amino] 1,1,1-trifluoro-2-propanol; 15 3- [[[3- (1,1,2,2 tetrafluoroethoxy)phenyllmethyl](cyclohexyl)amino]-1,1,1 trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyllmethyl] (4 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 20 3-[[[(3-pentafluoroethyl)phenyl]methyl][(4 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl][[4 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](4 25 methylcyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl] (3-trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 30 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 35 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](3 C:Vocuments and SttngsVahedVlf 8s Temporary Intemet FilesOLK85VSpecification of AU2008201550 dangers tracked) (2) doc trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 5 3-[[[(3-pentafluoroethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-([[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-(4 10 chloro-3-ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 15 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 20 3-[[[(3-trifluoromethyl)phenyl]methyl](3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 25 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl] (3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyllmethyl) (3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 30 propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl](3 35 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 C:VDocuments and SetingsahadVLoI off 7 VsVemporary Intemet FilesVOLK85WSpecifleetion of AU2008201550 (changes tracked) (2) doc propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 5 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl] (3 isopropoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 cyclopentyloxycyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 10 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl] (3 phenoxycyclohexyl)amino]-1,1,1-trifluoro-2-propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 trifluoromethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 15 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl][3-(4-chloro-3 ethylphenoxy)cyclohexyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl][3-(1,2,2 tetrafluoroethoxy)cyclohexyl]amino]-1,1,1-trifluoro-2 propanol; 20 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl] (3 pentafluoroethylcyclohexyl)amino]-1,1,1-trifluoro-2 propanol; 3-[[[(2-trifluoromethyl)pyrid-6-yl]methyl](3 trifluoromethoxycyclohexyl)amino]-1,1,1-trifluoro-2 25 propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[((3-pentafluoroethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 30 3-[[[(3-trifluoromethoxy)phenyl]methyl) [3-(4-chloro-3 ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-(4 chloro-3-ethylphenoxy)propyl]amino]-1,1,1-trifluoro-2 propanol; 35 3-[[[(3-trifluoromethyl)phenyl]methyl][3-(4-chloro-3 CVocumemAs a d SattingsaheadVLocf Mg aTemporary Intemae Fils&OLKB5VSpecification of AU2008201550 (changes tracked) (2).doc ethylphenoxy)-2,2-di-fluoropropyl]amino]-1,1,1-trifluoro 2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)-2,2-difluoropropylamino]-1,1,1-trifluoro-2 5 propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl][3-(4-chloro-3 ethylphenoxy)-2,2-difluoropropyl]amino]-1,1,1-trifluoro-2 propanol; 3-[[[(3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3-(4 10 chloro-3-ethylphenoxy)-2,2-difluoropropyl]amino]-1,1,1 trifluoro-2-propanol; 3-[[[(3-trifluoromethyl)phenyl]methyl][3 (isopropoxy)propyl]amino)-1,1,1-trifluoro-2-propanol; 3-[[[(3-pentafluoroethyl)phenyl]methyl][3 15 (isopropoxy)propyllamino]-1,1,1-trifluoro-2-propanol; 3-[[[(3-trifluoromethoxy)phenyl]methyl][3 (isopropoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 (isopropoxy)propyl]amino]-1,1,1-trifluoro-2-propanol; and 20 3-[[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl][3 (phenoxy)propyl]amino]-1,1,1-trifluoro-2-propanol, or a pharmaceutically acceptable salt thereof. The method may also include the compound having a CETP inhibitory activity being cycloalkano-pyridine of the 25 formula (XVIII) A D R (XVIII) E N R wherein A is an aryl having 6 to 10 carbon atoms, which can be optionally substituted up to 5 times in an identical or different manner by halogen, nitro, hydroxyl, 30 trifluoromethyl or trifluoromethoxy, or by linear or branched chain alkyl, acyl, hydroxyalkyl or alkoxy, each having up to 7 carbon atoms, or by a group of the formula C:Documents and Settings~aheadVLoc I RsVTemporary Intemet Fles"OLKB5VSpecificaon of AU2008201550 (changes tracked) (2).doc

-NR

3

R

4 , wherein R 3 and R 4 are identical or different and each is hydrogen, phenyl or linear or branched chain alkyl having up to 6 carbon atoms, D is aryl having 6 to 10 carbon atoms, which is optionally substituted by phenyl, 5 nitro, halogen, trifluoromethyl or trifluoromethoxy, or is a group represented by the formula 7 8 R R

R

5 -L R 6 or R 9

-T-V-X

wherein R 5 , R 6 and R 9 independently of one another denote cycloalkyl having 3 to 6 carbon atoms, or aryl having 6 to lo 10 carbon atoms, or a 5- to 7-membered, optionally benzo fused, saturated or unsaturated, mono-, bi- or tricyclic heterocycle having up to 4 heteroatoms from the series S, N and/or 0, where the cycles are substituted, if appropriate, in the case of a nitrogen-containing rings 15 also via an N functional group, up to 5 times in an identical or different manner by halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, straight-chain or branched acyl, alkyl, alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl, each having up to 6 20 carbon atoms, by aryl- or trifluoromethyl-substituted aryl, each having 6 to 10 carbon atoms, or by an optionally benzo-fused, aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms from the series S, N and/or 0, and/or 10 11 are substituted by a group of the formula -OR , -SR , 12 13 1041 12 25 SO 2 R or -NR R", wherein R1, R" and R independently of one another denote aryl having 6 to 10 carbon atoms, which for its part is substituted up to 2 times in an identical or different manner by phenyl, halogen or by straight chain or branched alkyl having up to 6 carbon atoms, R 13 14 30 and R are identical or different and have the meaning of

R

3 and R 4 indicated above, or R 5 and/or R 6 denote a group of the formula C VDocuments and SettingswahfadV "c sTemnporary Intemet FIlos&OLKB5VSpeIcatin of AU2008201550 (changes tracked) (2) doc X or FF rF 3 C 0

R

7 denotes a hydrogen or halogen, R 8 denotes hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or 5 alkyl each having up to 6 carbon atoms or a group of the 15 16 1516 formula -NR R , wherein R"5 and R are identical or different and have the meaning of R 3 and R 4 indicated above, or R7 and R8 together form a group of the formula =0 or =NR ', wherein R 1 is a hydrogen or linear or 10 branched chain alkyl, alkoxy or acyl, each having up to 6 carbon atoms, L is a linear or branched chain alkylene or alkenylene chain each having up to 8 carbon atoms, each of which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and denote a straight 15 chain or branched alkylene chain having up to 8 carbon atoms, or T or X denotes a bond, V represents an oxygen or sulfur atom or an -NR'B group, wherein R18 is a hydrogen or linear or branched chain alkyl having up to 6 carbon atoms or phenyl, E denotes cycloalkyl having 3 to 8 carbon atoms, 20 or linear or branched chain alkyl having up to 8 carbon atoms, which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, R 1 and R 2 together form linear or 25 branched alkylene chain having up to 7 carbon atoms, which must be substituted by a carbonyl group and/or a group of the formula C:VDocuWents and SettingsvaheadVLoc t ngsUTemporary Intemet Files&OLK85VSpecifiction of AU2008201550 (changes tracked) (2).doc

(CH

2 )a CH 2 1, 30-CH 2 O I I I I 0407, OH -OR or 1, 20 (CR 20R 21)b I I wherein a and b are identical or different and denote a number 1, 2 or 3, R 9 denotes hydrogen, cycloalkyl having 3 to 7 carbon atoms, straight-chain or branched silylalkyl 5 having up to 8 carbon atoms or straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by hydroxyl, straight-chain or branched alkoxy having up to 6 carbon atoms or by phenyl, which for its part can be substituted by halogen, nitro, trifluoromethyl, 10 trifluoromethoxy or by phenyl- or tetrazole-substituted phenyl, and alkyl is optionally substituted by a group of the formula -OR 22 , wherein R 22 is linear or branched chain acyl or benzyl having up to 4 carbon atoms, or R"1 is linear or branched chain acyl having up to 20 carbon atoms, 15 or benzoyl which is optionally substituted by halogen, trifluoromethyl, nitro or trifluoromethoxy, or denotes straight-chain or branched fluoroacyl having up to 8 carbon atoms and up to 9 fluorine atoms, R 20 and R 21 are identical or different, and denote hydrogen, phenyl or 20 straight-chain or branched alkyl having up to 6 carbon atoms, or R20 and R together form a 3 to 6-membered carbocycle, and, if appropriate also geminally, the carbocycles formed are optionally substituted up to 6 times in an identical or different manner by 25 trifluoromethyl, hydroxyl, halogen, carboxyl, nitro, azido, cyano, cycloalkyl or cycloalkyloxy each having 3 to 7 carbon atoms, by straight-chain or branched alkoxycarbonyl, alkoxy or alkylthio each having up to 6 carbon atoms or by straight-chain or branched alkyl having up to 6 carbon 192 *V* ''"'''''''"""'^ of AU2008201550 changee tracked) doc atoms, which for its part is substituted up to 2 times in an identical or different manner by hydroxyl, benzyloxy, trifluoromethyl, benzoyl, straight-chain or branched alkoxy, oxyacyl or carboxyl each having up to 4 carbon 5 atoms and/or phenyl, which for its part can be substituted by halogen, trifluoromethyl or trifluoromethoxy, and/or the carbocycles formed, also geminally, are optionally substituted up to 5 times in an identical or different manner by phenyl, benzoyl, thiophenyl or sulphonylbenzyl, 1o which for their part are optionally substituted by halogen, trifluoromethyl, trifluoromethoxy or nitro, and/or are optionally substituted by a group of the formula 1,I2 (CH2)c , SO2C6H5

-(CO),-NR

2 3

R

24 or =0 wherein c denotes a number 1, 2, 3 or 4, d denotes a 15 number 0 or 1, R 23 and R 24 are identical or different and denote hydrogen, cycloalkyl having 3 to 6 carbon atoms, straight-chain or branched alkyl having up to 6 carbon atoms, benzyl or phenyl, which is optionally substituted up to 2 times in an identical or different manner by 20 halogen, trifluoromethyl, cyano, phenyl or nitro, and/or the carbocycles formed are optionally substituted by a spiro-linked group of the formula R 31 W-Y R2 R 2 6

R

32 I (CR 27R 28 29 30 ~ Ka R3 (C R(CR R O wherein W denotes an oxygen or a sulphur atom, Y and Y' 25 together form a 2- to 6-membered straight-chain or branched alkylene chain, e denotes a number 1, 2, 3, 4, 5, 6 or 7, f denotes a number 1 or 2, R 2 s, R , R , R , R 2 ,

R

30 and R 3 1 are identical or different and denote hydrogen, trifluoromethyl, phenyl, halogen or straight-chain or 30 branched alkyl or alkoxy each having up to 6 carbon atoms, or R and R or R and R in each case together form a 19 3 C *Vpo* * *dVSp*C"On of AU2001201550 (c.ngO. trwOkd) .

straight-chain or branched alkyl chain having up to 6 carbon atoms, or R 25 and R 26 or R 27 and R 28 in each case together form a group of the formula W -CH 2 W

(CH

2 )q 5 wherein W has the meaning indicated above, g denotes a number 1, 2, 3, 4, 5, 6 or 7, R and R 33 together form a 3- to 7-membered heterocycle which contains an oxygen or sulphur atom or a group of the formula SO, SO 2 or -NR 34 , wherein R 34 denotes hydrogen, phenyl, benzyl or straight 10 chain or branched alkyl having up to 4 carbon atoms, a salt thereof or N-oxide thereof, with the exception of 5(6H)-quinolone, 3-benzoyl-7,8-dihydro-2,7,7-trimethyl-4 phenyl. The inhibitor may also include the compound having a 15 CETP inhibitory activity being cycloalkano-pyridine of the formula (XVIII), or a salt thereof or N-oxide thereof. The inhibitor may also be cycloalkano-pyridine of the formula (XVIII), or a salt thereof or N-oxide thereof. The method may also include the compound having a 20 CETP inhibitory activity being substituted quinoline of the formula (XIX) A OR 3 D E N A OR 3 2 (XIX) E N wherein A is aryl having 6 to 10 carbon atoms, which is 25 optionally substituted up to 5 times in an identical or different manner by halogen, hydroxyl, trifluoromethyl, trifluoromethoxy, nitro, or straight chain or branched alkyl, acyl, hydroxyalkyl or alkoxy, each having up to 7 194 C* 'of'VV Spcifcti n of AU2008201550 (hng..e. tracked) ce carbon atoms, or a group of the formula -NR 4 R , wherein R 4 and R 5 are identical or different and denote hydrogen, phenyl or straight chain or branched alkyl having up to 6 carbon atoms, D is aryl having 6 to 10 carbon atoms, which 5 is optionally substituted by phenyl, nitro, halogen, trifluoromethyl or trifluoromethoxy, or denote a group of the formula

R

8

R

9 R 6 -L- or R' 1

-T-V-X

wherein R , R7 and R1 independently of one another denote 10 cycloalkyl having 3 to 6 carbon atoms, or aryl having 6 to 10 carbon atoms, or a 5- to 7-membered, optionally benzo fused, saturated or unsaturated, mono-, bi- or tricyclic heterocycle having up to 4 heteroatoms from the group consisting of S, N and/or 0, where the cycles are 15 optionally substituted in the case of the nitrogen containing rings also via the N functional group, up to 5 times in an identical or different manner by halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, straight-chain or branched acyl, alkyl, 20 alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl, each having up to 6 carbon atoms, by aryl having 6 to 10 carbon atoms, or by an optionally benzo-fused, aromatic 5- to 7 membered heterocycle having up to 3 heteroatoms from the group consisting of S, N and/or 0, and/or are substituted 11 2 13 14 15 25 by a group of the formula -OR", -SR , -SO 2 R or -NR"Ri, wherein R", R' 2 and R 13 independently of one another denote aryl having 6 to 10 carbon atoms, which for its part is substituted up to 2 times in an identical or different manner by phenyl, halogen or by straight-chain or branched 30 alkyl having up to 6 carbon atoms, R 1 4 and R 1 5 are identical or different and have the meaning of R 4 and R 5 indicated above, or R 6 and/or R 7 denote a group of the formula 195 C:pofVrd*Sp '' 'tIo of AU2008201550 changess taked).do F or F 3 C O

R

8 denotes a hydrogen or halogen, R 9 denotes hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or 5 alkyl each having up to 6 carbon atoms or a group of the formula -NR1 6 R, wherein R 6 and R 1 are identical or different and have the meaning of R 4 and R 5 indicated above, or R 8 and R 9 together form a group of the formula =0 or =NR 1 , wherein R1 8 is hydrogen or linear or branched 10 alkyl, alkoxy or acyl, each having up to 6 carbon atoms, L is a linear or branched alkyl or alkenyl each having up to 8 carbon atoms, each of which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and denote straight-chain or branched alkyl having up to 8 15 carbon atoms, or T or X denotes a bond, V represents oxygen or sulfur atom or -NR1 9 group, wherein R 19 is hydrogen or linear or branched alkyl having up to 6 carbon atoms or phenyl, E denotes cycloalkyl having 3 to 8 carbon atoms, or linear or branched alkyl having up to 8 carbon 20 atoms, which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, Ri and R 2 are identical or different and denote cycloalkyl having 3 to 8 carbon atoms, hydrogen, 25 nitro, halogen, trifluoromethyl, trifluoromethoxy, carboxyl, hydroxyl, cyano, or straight chain or branched acyl, alkoxycarbonyl or alkoxy each having up to 6 carbon 20 21 2 0 atoms, or a group of the formula -NR R , wherein R and R are identical or different and denote hydrogen, phenyl, 30 or straight chain or branched alkyl having up to 6 carbon atoms and/or Ri and/or R 2 denote straight chain or branched alkyl having up to 6 carbon atoms, which are optionally substituted by halogen, trifluoromethoxy, 196 C."p''''S ''''o'"o"f * AU20082O1o550 (ch.ngo. tmrce.do c hydroxyl or straight chain or branched alkoxy having up to 4 carbon atoms, and/or aryl having 6 to 10 carbon atoms, which are optionally substituted up to 5 times in an identical or different manner by halogen, cyano, hydroxyl, 5 trifluoromethyl, trifluoromethoxy, nitro, or straight chain or branched alkyl, acyl, hydroxyalkyl or alkoxy each having up to 7 carbon atoms, or a group of the formula NR R , wherein R and R 23 are identical or different and denote hydrogen, phenyl, or straight chain or branched 10 alkyl having up to 6 carbon atoms, and/or R 1 and R 2 together form straight chain or branched alkyl chain or alkenyl chain each having up to 6 carbon atoms, which is optionally substituted by halogen, trifluoromethyl, hydroxyl, or straight chain or branched alkoxy having up 15 to 5 carbon atoms, R 3 denotes hydrogen, straight chain or branched acyl or benzoyl having up to 20 carbon atoms, which is optionally substituted by halogen, trifluoromethyl, nitro or trifluoromethoxy, or straight chain or branched fluoroacyl having up to 8 carbon atoms 20 and up to 7 fluorine atoms, cycloalkyl having 3 to 7 carbon atoms, or straight chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by hydroxyl, straight chain or branched alkoxy having up to 6 carbon atoms, or phenyl, which for its part can be 25 substituted by halogen, nitro, trifluoromethyl, trifluoromethoxy or phenyl or tetrazol-substituted phenyl, and/or alkyl is optionally substituted by a group of the 24 24 formula -OR , wherein R denotes straight chain or branched acyl or benzyl having up to 4 carbon atoms, or a 30 salt thereof. The inhibitor may also include the compound having a CETP inhibitory activity being substituted quinoline of the formula (XIX) or a salt thereof. The inhibitor may also be substituted quinoline of 35 the formula (XIX) or a salt thereof. 197 C:pofworimSpecficaton of AU20082015S0 (changes tracked).doc The method may also include the compound having a CETP inhibitory activity being hetero-tetrahydroquinoline of the formula (XX) A DI R (XX) E N R 5 wherein A represents cycloalkyl having 3 to 8 carbon atoms or, represents a 5- to 7-membered saturated, partially unsaturated or unsaturated, optionally benzo-fused heterocycle having up to 3 heteroatoms from the group consisting of S, N and 0, which, in the case of a io saturated heterocycle with a nitrogen functional group, is optionally also attached via this functional group, and where the abovementioned ring systems are optionally substituted up to 5 times by identical or different substituents from the group consisting of halogen, nitro, 15 hydroxyl, trifluoromethyl, trifluoromethoxy and straight chain or branched alkyl, acyl, hydroxyalkyl or alkoxy having in each case up to 7 carbon atoms, or by a group of the formula

-NR

3

R

4 wherein R 3 and R 4 are identical or different and 20 represent hydrogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, or A represents a group of the formula o 0 D represents aryl having 6 to 10 carbon atoms which is 25 optionally substituted by phenyl, nitro, halogen, trifluoromethyl or trifluoromethoxy, or represents a group of the formula

R

7 Ra R*-L- , Re or R-T-V-X wherein R 5 , R 6 and R 9 independently of one another 198 C"p""' 'rdS' if'tio' o'* AU20082Oisso (cenng.s Irce.Ac represent cycloalkyl having 3 to 6 carbon atoms, or represent aryl having 6 to 10 carbon atoms or represent a 5- to 7-membered optionally benzo-fused saturated or unsaturated mono-, bi- or tricyclic hetreocycle having up 5 to 4 heteroatoms from the group consisting of S, N and 0, where the cycles are optionally substituted, in the case of a nitrogen-containing rings also via an N functional group, up to 5 times by identical or different substituents from the group consisting of halogen, 10 trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, and straight-chain or branched acyl, alkyl, alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, by aryl or trifluoromethyl-substituted aryl having in each case 6 to 15 10 carbon atoms, or by an optionally benzo-fused aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms from the group consisting of S, N and 0 and/or by a group of the formula -OR, -SR' , -SO 2 R1 2 or -NR 1 3 R , wherein R' 0 , R"1 and R1 2 independently of one another represent aryl 20 having 6 to 10 carbon atoms which for its part is substituted up to 2 times by identical or different substituents from the group consisting of phenyl, halogen and straight-chain or branched alkyl having up to 6 carbon atoms, R1 3 and R 14 are identical or different and have the 25 meaning of R3 and R 4 given above, or R 5 and/or R 6 represent(s) a group of the formula XKF or 0 oF

F

3 C o

R

7 is a hydrogen or halogen, R 8 represents hydrogen, 3o halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or alkyl having in each case up to 6 carbon atoms or a group of the formula -NRisR 6, wherein R 1 and R1 are identical 19 9 C"'"""*Spef*"'"ti* n of AU200820550 chargess tckd).oc or different and have the meaning of R 3 and R 4 given above, or R and R8 together form a group of the formula =0 or =NR wherein R represents hydrogen or straight-chain or branched alkyl, alkoxy or acyl having in each case up to 6 5 carbon atoms, L represents a straight-chain or branched alkylene or alkenylene chain having in each case up to 8 carbon atoms, which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and represent a straight-chain or branched alkylene chain 10 having up to 8 carbon atoms, or T or X represents a bond, V represents an oxygen or sulphur atom or represents an NR group wherein R represents hydrogen or straight chain or branched alkyl having up to 6 carbon atoms or phenyl, E represents cycloalkyl having 3 to 8 carbon atoms, 15 or represents straight-chain or branched alkyl having up to 8 carbon atoms which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, R' and R 2 together form a 20 straight-chain or branched alkylene chain having up to 7 carbon atoms, which has to be substituted by a carbonyl group and/or by a group of the formula OH

(CH

2 )a - CH 2

H

2 1,0- (CRR) 1,3 7-C -- OR's or 1.2 0 (R 21 wherein a and b are identical or different and represent a 25 number 1, 2 or 3, R" represents hydrogen, cycloalkyl having 3 to 7 carbon atoms, straight-chain or branched silylalkyl having up to 8 carbon atoms, or straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by hydroxyl, straight-chain or 30 branched alkoxy having up to 6 carbon atoms or by phenyl which for its part may be substituted by halogen, nitro, trifluoromethyl, trifluoromethoxy or by phenyl or tetrazole-substituted phenyl, and alkyl is optionally 2 00 C 'po 'wo 'Spe' 'ca' 'n of AU20082O1s550 rangess tracke.doc 22 2 substituted by a group of the formula -OR , in which R 2 represents straight-chain or branched acyl having up to 4 carbon atoms or benzyl, or R 9 represents straight-chain or branched acyl having up to 20 carbon atoms or benzoyl, 5 which is optionally substituted by halogen, trifluoromethyl, nitro or trifluoromethoxy, or represents straight-chain or branched fluoroacyl having up to 8 carbon atoms and up to 9 fluorine atoms, R20 and R are identical or different, represent hydrogen, phenyl or lo straight-chain or branched alkyl having up to 6 carbon atoms, or R20 and R together form 3 to 6-membered carbocycle and, if appropriate also geminally, the carbocycles formed are optionally substituted up to 6 times by identical or different substituents from the 15 group consisting of trifluoromethyl, hydroxyl, nitrile, halogen, carboxyl, nitro, azido, cyano, cycloalkyl or cycloalkyloxy having in each case 3 to 7 carbon atoms, straight-chain or branched alkoxycarbonyl, alkoxy or alkylthio having in each case up to 6 carbon atoms and 20 straight-chain or branched alkyl having up to 6 carbon atoms, which for its part is substituted up to 2 times by identical or different substituents from the group consisting of hydroxyl, benzyloxy, trifluoromethyl, benzoyl, straight-chain or branched alkoxy, oxyacyl or 25 carboxyl having in each case up to 4 carbon atoms and phenyl, which for its part may be substituted by halogen, trifluoromethyl or trifluoromethoxy, and/or the carbocycles formed are optionally substituted, also geminally, up to 5 times by identical or different 30 substituents from the group consisting of phenyl, benzoyl, thiophenyl and sulphonylbenzyl, which for their part are optionally substituted by halogen, trifluoromethyl, trifluoromethoxy or nitro, and/or are optionally substituted by a group of the formula 35 2 0 1 C *V'r'Spe'fl'*ion of*AU2* 0 201550 (cha2gs s t . cked).dc 1,2 (CH 2 )c , -SO 2 CH,. -(CO),-NR"R" o r wherein c represents a number 1, 2, 3 or 4, d represents a number 0 or 1, R 23 and R 2 4 are identical or different and 5 represent hydrogen, cycloalkyl having 3 to 6 carbon atoms, straight-chain or branched alkyl having up to 6 carbon atoms, benzyl or phenyl which is optionally substituted up to 2 times by identical or different substituents from the group consisting of halogen, trifluoromethyl, cyano, 10 phenyl and nitro, and/or the carbocycles formed are optionally substituted by a spiro-linked group of the formula R 3 R2 2 W-Y R 2 R3 W - Y ' ' ( R R ) ,Co r R (CROR) R wherein W represents either an oxygen or a sulphur atom, Y 15 and Y' together form a 2- to 6-membered straight-chain or branched alkylene chain, e represents a number 1, 2, 3, 4, 5, 6 or 7, f represents a number 1 or 2, R , R , R , R 2 , R , R'0 and R 3 1 are identical or different and represent hydrogen, trifluoromethyl, phenyl, halogen or straight 20 chain or branched alkyl or alkoxy having in each case up to 6 carbon atoms, or R 2 5 and R 26 or R 27 and R 28 in each case together form straight-chain or branched alkyl chain having up to 6 carbon atoms, or R 2 and R 26 or R 27 and R 2 1 in each case together form a group of the formula

W-CH

2 25 W - (CH 2

)

9 wherein W is as defined above, g represents a number 1, 2, 3, 4, 5, 6 or 7, R and R together form 3- to 7-membered heterocycle which contains an oxygen or sulphur atom or a group of the formula SO, SO 2 or -NR , in which R 34 30 represents hydrogen, phenyl, benzyl or straight-chain or 2 02 C:Vpo mr(WSpecJflcton flC AU2003201 550 (changes fakd.o branched alkyl having up to 4 carbon atoms, a salt thereof or N-oxide thereof. The inhibitor may also include the compound having a CETP inhibitory activity being hetero-tetrahydroquinoline 5 of the formula (XX) or a salt thereof or N-oxide thereof. The inhibitor may also be hetero-tetrahydroquinoline of the formula (XX) or a salt thereof or N-oxide thereof. The method may also include the compound having a CETP inhibitory activity being tetrahydroquinoline of the 10 formula (XXI) A R 1

R

2 D R (XXI) E N in which A represents phenyl which is optionally substituted up to 2 times by identical or different substituents from the 15 group consisting of halogen, trifluoromethyl and straight chain or branched alkyl or alkoxy having in each case up to 3 carbon atoms, D represents a group of the formula

R

6

R

5 R or RB-CH 2 -0-CH 2 20 in which

R

5 and R 6 together form a carbonyl group (=0), or

R

5 represents hydrogen and

R

6 represents halogen or hydroxyl, or

R

5 and R 6 represent hydrogen, 25 R and R8 are identical or different and represent phenyl, naphthyl, benzothiazolyl, quinolyl, pyrimidyl or pyridyl which are optionally substituted up to 4 times by identical or different substituents from the group consisting of halogen, trifluoromethyl, nitro, cyano, 30 trifluoromethoxy, or by a group of the formula -S0 2

-CH

3 or 203 C:MporwordUSpecification of AU2008201550 (changes tracked)doc

-NR

9 Rio, in which R 9 and Rio are identical or different and represent hydrogen or straight-chain or branched alkyl having up to 3 carbon atoms, E represents cycloalkyl having 3 to 6 carbon atoms, or 5 represents straight-chain or branched alkyl having up to 8 carbon atoms, Ri represents hydroxyl, and R2 represents hydrogen or represents methyl,

R

3 and R 4 are identical or different and represent io straight-chain or branched alkyl having up to 3 carbon atoms, or

R

3 and R 4 together form a spiro-linked alkyl chain having 2 to 4 carbon atoms, or a salt thereof or N-oxide thereof. 15 The inhibitor may also include the compound having a CETP inhibitory activity being tetrahydroquinoline of the formula (XXI), or a salt thereof or N-oxide thereof. The inhibitor may also be tetrahydroquinoline of the formula (XXI), or a salt thereof or N-oxide thereof. 20 The method may also include the compound having a CETP inhibitory activity being a compound of the formula (XXII) A D R (XXII) 2 E R wherein A is cycloalkyl having 3 to 8 carbon atoms, aryl 25 having 6 to 10 carbon atoms, or 5- to 7-membered saturated, partially unsaturated or unsaturated optionally benzo fused heterocycle having up to 4 hetero atoms from the group consisting of S, N and 0, wherein the ring systems of the aryl and said heterocycle are optionally 30 substituted up to 5 times by identical or different substituents from the group consisting of cyano, halogen, nitro, carboxyl, hydroxyl, trifluoromethyl and 204 C:'po ""mr cmSpadflcautonofAU2082050(changsftrckd).dc trifluoromethoxy, or straight chain or branched alkyl, acyl, hydroxyalkyl, alkylthio, alkoxycarbonyl, oxyalkoxycarbonyl or alkoxy, each having up to 7 carbon atoms, or a group of the formula -NR 3

R

4 , wherein R 3 and R 4 5 are identical or different and denote hydrogen, phenyl or straight chain or branched alkyl having up to 6 carbon atoms, D denotes a group of the formula R7 Ra RR-L- R or R -T-V-X wherein R 5 , R 6 and R 9 independently of one another denote lo aryl having 6 to 10 carbon atoms, or 5- to 7-membered, optionally benzo-fused, saturated or unsaturated, mono-, bi- or tricyclic heterocycle having up to 4 heteroatoms from the group consisting of S, N and 0, where the cycles are optionally substituted, in the case of nitrogen 15 containing rings also via an N functional group, up to 5 times, by identical or different substituents from the group consisting of halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, straight chain or branched acyl, alkyl, alkylthio, alkylalkoxy, 20 alkoxy or alkoxycarbonyl, each having up to 6 carbon atoms, by aryl- or trifluoromethyl-substituted aryl, each having 6 to 10 carbon atoms, or by an optionally benzo-fused, aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms from the group consisting of S, N and 0, 25 and/or by a group of the formula -OR 10 , -SR", -S0 2 R or 13 14 10 11 1 NR R , wherein R1 , R and Ri 2 independently of one another denote aryl having 6 to 10 carbon atoms, which for its part is substituted up to 2 times by identical or different substituents from the group consisting of phenyl 30 and halogen, or by straight-chain or branched alkyl having up to 6 carbon atoms, R' 3 and R1 4 are identical or different and have the meaning of R 3 and R 4 indicated above, or R 5 and/or R 6 denote a group of the formula 2 0 5 C *Vpo dSp f'ctIon of AU20 8201550 changess tra.ed)doc or 3 R denotes a hydrogen, halogen or methyl, R8 denotes hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or 5 alkyl each having up to 6 carbon atoms or a group of the formula -NRi 5

R

16 , wherein R 15 and R 16 are identical or different and have the meaning of R 3 and R 4 indicated above, or R 7 and R 8 together form a group of the formula =0 or =NR , wherein R 17 is hydrogen or linear or branched 1o alkyl, alkoxy or acyl, each having up to 6 carbon atoms, L is a linear or branched alkylene or alkenylene chain each having up to 8 carbon atoms, each of which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and denote straight-chain or 15 branched alkylene chain having up to 8 carbon atoms, or T or X denotes a bond, V represents an oxygen or sulfur atom or -NR' 8 - group, wherein R1 8 is a hydrogen or linear or branched alkyl having up to 6 carbon atoms or phenyl, E denotes cycloalkyl having 3 to 8 carbon atoms, or linear 20 or branched alkyl having up to 8 carbon atoms, which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, R 1 denotes straight chain or branched alkyl having up to 6 25 carbon atoms, which is substituted by hydroxyl or a group of the formula -- OO R2 denotes hydrogen, or straight chain or branched alkyl or alkenyl each having up to 8 carbon atoms, which is 30 optinonally substituted by hydroxy, halogen, phenyl, cycloalkyl having 3 to 6 carbon atoms, or a group of the formula 20 6 C V oI"""''"'''""'AU20082O155O (CIanoes lraexde>.c N0 -0-Rig or wherein R1 9 denotes a group of the formula -Si(CH 3

)

2

C(CH

3

)

3 , or straight chain or branched alkyl having up to 6 carbon 5 atoms, or 5- to 7-membered saturated, partially unsaturated or unsaturated heterocycle having up to 3 hetero atoms from the group consisting of S, N and 0, or phenyl or benzyl, wherein all ring systems for R 9 are optionally substituted up to 2 times by identical or 1o different substituents from the group consisting of trifluoromethyl, fluorine, nitro, hydroxyl, straight chain or branched alkoxy or alkoxycarbonyl having in each case up to 4 carbon atoms, or by straight chain or branched alkyl having up to 4 carbon atoms optionally substituted 15 by hydroxyl, or a salt thereof. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (XXII), or a salt thereof. The inhibitor may also be a compound of the formula 20 (XXII), or a salt thereof. The method may also include the compound having a CETP inhibitory activity being a compound represented by the formula (XXIII) OR'' R' N Ar 1 N1R (XXIII) Ar 2 25 wherein Arl is an aromatic ring group optionally having substituents, Ar 2 is an aromatic ring group having 207 C "p''"*tSp' 'flc'on O'' AU2002O15ss (chang. Ira .doc substituent, OR" is an optionally protected hydroxyl group, R is an acyl group, R' is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof with the exception of tert-butyl benzyl-[2(S)-hydroxy-2 5 thiazol-2-yl-l(S)-(4-trifluoromethyl-benzyl)-ethyl] carbamate. The inhibitor may also include the compound having a CETP inhibitory activity being a compound of the formula (XXIII), or a salt thereof. 10 The inhibitor may also be a compound of the formula (XXIII), or a salt thereof. The method may also include the compound of the formula (XXIII) being a compound selected from the group consisting of 15 N-[(lRS,2SR)-2-(4-fluorophenyl)-2-hydroxy-l-[4 (trifluoromethyl)benzyl]ethyl]-6,7-dihydro-5H benzo[a]cycloheptene-l-carboxamide, 4-fluoro-N-((lR,2S)-2 (4-fluorophenyl)-2-hydroxy-l-((4 (trifluoromethyl)phenyl)methyl)ethyl)-1 20 naphthalenecarboxamide, N-[(lR,2S)-2-(4-fluorophenyl)-2 hydroxy-l-[3-(1,1,2,2-tetrafluoroethoxy)benzyl]ethyl]-6,7 dihydro-5H-benzo[a]cycloheptane-l-carboxamide,

N

[(lRS,2SR)-2-(4-fluorophenyl)-2-hydroxy-l-(3-(1,1,2, 2 tetrafluoroethoxy)benzyl]ethyl]-5,6-dihydronaphthalene-l 25 carboxamide, N-[(lRS,2SR)-2-(4-fluorophenyl)-2-hydroxy-l [3-(1,1,2,2-tetrafluoroethoxy)benzyl]ethyl]-6,7,8,9 tetrahydro-5H-benzo[a]cycloheptene-l-carboxamide, 4 fluoro-N-[(lR,2S)-2-(4-fluorophenyl)-2-hydroxy-l-[3 (1,1,2,2-tetrafluoroethoxy)benzyl]ethyl]naphthalene-l 30 carboxamide, N-[(lRS,2SR)-2-(4-fluorophenyl)-2-hydroxy-l [3-(1,1,2,2-tetrafluoroethoxy)benzyl]ethyl]-5,6,7,8 tetrahydrobenzo[a]cyclooctene-l-carboxamide, N-[(lRS,2SR) 2-(4-fluorophenyl)-2-hydroxy-l-(4-isopropylbenzyl)ethyl] 6,7-dihydro-5H-benzo[a]cycloheptane-1-carboxamide,

N

35 ((lRS,2SR)-2-(3-fluorophenyl)-2-hydroxy-l-((4 208 C"V*''"*'*****''''''''"""'^2008201s50tenhno..Ircked) dc (trifluoromethyl)phenyl)methyl)ethyl)-6,7-dihydro-5H benzo[a]cycloheptane-1-carboxamide, N-((lRS,2SR)-2 hydroxy-2-(4-phenoxyphenyl)-1-((4 (trifluoromethyl)phenyl)methyl)ethyl)-6,7-dihydro-5H 5 benzo[a]cycloheptane-l-carboxamide, N-[(lRS,2SR)-2-(4 chlorophenyl)-2-hydroxy-1-[3-(1,1,2,2 tetrafluoroethoxy)benzyl]ethyl]-6,7-dihydro-5H benzo[a]cycloheptane-1-carboxamide, N-((lRS,2SR)-2 hydroxy-2-(4-(phenyloxy)phenyl)-l-((3-((1,1,2,2 10 tetrafluoroethyl)oxy)phenyl)methyl)ethyl)-6,7-dihydro-5H benzo[a]cycloheptene-1-carboxamide, N-((lRS,2SR)-2-(4-((4 chloro-3-ethylphenyl)oxy)phenyl)-2-hydroxy-l-((3 ((1,1,2,2-tetrafluoroethyl)oxy)phenyl)methyl)ethyl)-6,7 dihydro-5H-benzo[a]cycloheptene-1-carboxamide,

N

15 ((lRS,2SR)-2-(2-fluoropyridin-4-yl)-2-hydroxy-l-((3 (1,1,2,2-tetrafluoroethoxy)phenyl)methyl)ethyl)-6,7 dihydro-5H-benzo[a]cycloheptene-1-carboxamide,

N

((1RS,2RS)-2-(6-fluoropyridin-2-yl)-2-hydroxy-1-((3 (1,1,2,2-tetrafluoroethoxy)phenyl)methyl)ethyl)-6,7 20 dihydro-5H-benzo[a]cycloheptane-1-carboxamide,

N

[(1RS,2SR)-1-(4-tert-butylbenzyl)-2-(3-chlorophenyl)-2 hydroxyethyl]-5-chloro-1-naphthamide and 4-fluoro-N {(1RS,2SR)-2-(4-fluorophenyl)-2-hydroxy-1-[(2,2,3,3 tetrafluoro-2,3-dihydro-1,4-benzodioxyn-6 25 yl)methyl]ethyll-l-naphthamide, or a salt thereof. The inhibitor may also include the compound of the formula (XXIII) being a compound selected from the group consisting of 30 N-[(lRS,2SR)-2-(4-fluorophenyl)-2-hydroxy-l-[4 (trifluoromethyl)benzyl]ethyl]-6,7-dihydro-5H benzo[a]cycloheptene-1-carboxamide, 4-fluoro-N-((lR,2S)-2 (4-fluorophenyl)-2-hydroxy-l-((4 (trifluoromethyl)phenyl)methyl)ethyl)-1 35 naphthalenecarboxamide, N-[(lR,2S)-2-(4-fluorophenyl)-2 20 9 C Vpof'''Spo"Ifi''' 'on of AU20082o155o (changs tr.ckd).oc hyclroxy-1- [3- (1,1,2, 2-tetrafluoroethoxy)benzyl] ethyl] -6,7 dihydro-5H-benzo[a]cycloheptane-1-carboxamide, N (iRS, 2SR) -2- (4-fluorophenyl) -2-hydroxy-1- [3-(l, 1,2,2 tetrafluoroethoxy) benzyl] ethyl] -5, 6-dihycronaphthalene-l 5 carboxamide, N-f (1RS,2SR)-2-(4-fluorophenyl)-2-hyiroxy-1 [3- (1,1,2, 2-tetrafluoroethoxy) benzyl] ethyl] -6, 7,8,9 tetrahydro-SH-benzo[a] cycloheptene-1-carboxamide, 4 fluoro-N-[ (1R,2S)-2-(4-fluorophenyl)-2-hydroxy-l-[3 (1, 1, 2,2-tetrafluoroethoxy) benzyl] ethyl] naphthalene-1 lo carboxamiie, N-[ (1RS,2SR)-2-(4-fluorophenyl)-2-hydroxy-1 [3- (1,1,2, 2-tetrafluoroethoxy) benzyl] ethyl] -5,6,7,8 tetrahycirobenzo[a]cyclooctene-l-carboxamile, N-f (1RS,2SR) 2- (4-fluorophenyl) -2-hyclroxy-1- (4-isopropylbenzyl) ethyl] 6, 7-dihydro-5H-benzo [a] cycloheptane-1-carboxamiie, N 15 ((1RS,2SR)-2-(3-fluorophenyl)-2-hydroxy-1-( (4 (trifluoromethyl) phenyl)methyl) ethyl) -6, 7-dihydro-5H benzo[alcycloheptane-l-carboxamile, N-((1RS,2SR)-2 hydroxy-2- (4-phenoxyphenyl) -1-((4 (trifluoromethyl)phenyl)methyl)ethyl) -6,7-dihyclro-5H 20 benzo[a]cycloheptane-l-carboxanide, N-[(lRS,2SR)-2-(4 chiorophenyl) -2-hyciroxy-l- [3- (1,1,2,2 tetrafluoroethoxy) benzyl] ethyll -6, 7-clihydro-5H benzo~a]cycloheptane-l-carboxamiie, N-( (lRS,2SR) -2 hydroxy-2-(4-(phenyloxy)phenyl)-1-( (3-C (1,1,2,2 25 tetrafluoroethyl)oxy)phenyl)inethyl)ethyl)-6,7-dihydro-5H benzo[a]cycloheptene-1-carboxamide, N-( (1RS,2SR)-2-(4-( (4 chloro-3-ethylphenyl)oxy)phenyl)-2-hyiroxy-1-( (3 ((1,1,2,2-tetrafluoroethyl)oxy)phenyl)methyl)ethyl)-6,7 dihydro-5H-benzo[alcycloheptene--carboxanide, N 30 ((1RS,2SR)-2-(2-fluoropyridin-4-yl)-2-hydroxy-1-((3 (1,1,2, 2-tetrafluoroethoxy) phenyl)methyl) ethyl) -6,7 dihydro-5H-benzo~a]cycloheptene-1-carboxamide, N (1lRS,2RS)-2-(6-fluoropyridin-2-yl)-2-hydroxy-1-((3 (1,1,2, 2-tetrafluoroethoxy)phenyl)methyl) ethyl) -6,7 35 dihycro-5H-benzofajcycloheptane-1-carboxamide, N 2 10 C.VporV~rdWSpCwfiCwtlo of AU2000201550 (cti8oQ. tackd)cDOc [(lRS,2SR)-1-(4-tert-butylbenzyl)-2-(3-chlorophenyl)-2 hydroxyethyl]-5-chloro-l-naphthamide and 4-fluoro-N-{(1RS,2SR) 2-(4-fluorophenyl)-2-hydroxy-l-[(2,2,3,3-tetrafluoro-2,3 dihydro-1,4-benzodioxyn-6-yl)methyl]ethyl}--naphthamide, 5 or a salt thereof. The method may also include the compound having a CEPT inhibitory activity being a compound selected from the group consisting of Code Names: JTT-705, CP-529414, SC-795, SC-744, SC-554, SC-71952, SC-56960, SC-57201, PD-140195, WK-5344A, WK 10 5344B, CETi-l(CETP vaccine), BM99-1 and BM99-2, or a salt thereof. The inhibitor may also include the compound having a CEPT inhibitory activity being a compound selected from the group consisting of Code Names: JTT-705, CP-529414, SC-795, SC-744, 15 SC-554, SC-71952, SC-56960, SC-57201, PD-140195, WK-5344A, WK 5344B, CETi-1(CETP vaccine), BM99-1 and BM99-2, or a salt thereof. The inhibitor may also be a compound selected from the group consisting of Code Names: JTT-705, CP-529414, SC-795, SC-744, 20 SC-554, SC-71952, SC-56960, SC-57201, PD-140195, WK-5344A, WK 5344B, CETi-l(CETP vaccine), BM99-1 and BM99-2, or a salt thereof. In a ninth aspect the present invention relates to an agent for the prophylaxis or treatment of hyper-remnant 25 lipoproteinemia, which comprises an inhibitor of the fifth aspect as an active ingredient. In a tenth aspect the present invention relates to a method for the prophylaxis or treatment of hyper-remnant lipoproteinemia in a patient in need thereof, which comprises 30 administering to said patient an effective amount of an inhibitor of the 211 fifth aspect as an active ingredient or a pharmaceutically acceptable salt thereof. Throughout the description and claims of the specification, the word "comprise" and variations of the 5 word, such as "comprising" and "comprises", is not intended to exclude other additives, components, integers or steps. Detailed Description of the Invention The present invention provides a prophylactic drug or 10 a therapeutic drug of hyperlipidemia, arteriosclerosis or hyper-remnant lipoproteinemia in which a remnant lipoprotein is involved (e.g., hereditary hyper-remnant lipoproteinemia such as familial dysbetalipidemia, familial lipase deficiency, familial combined 15 hyperlipidemia and the like; or secondary hyper-remnant lipoproteinemia that expresses subsequent to diabetic hypertriglyceridemia, hypothyroidism, nephritic syndrome and the like) by selectively inhibiting CETP. 20 Best Mode for Carrying Out the Invention Remnant lipoproteins refer to lipoproteins produced during catabolism of triglyceride-rich lipoproteins (chylomicron, very low density lipoprotein (VLDL)). Remnant lipoproteins are lipoprotein particles which are 25 commonly characterized by being rich in triglyceride, cholesterol and apolipoprotein E (apoE), and having apoB (chylomicron remnant has apoB-48 and a small amount of apoB-100, VLDL remnant has apoB-100) . The metabolism of chylomicron and VLDL starts from hydrolysis of 30 triglyceride by LPL and completes through remnant lipoproteins. The former is called a chylomicron remnant and the latter is called a VLDL remnant. CETP is an abbreviation of cholesteryl ester transfer protein. Due to CETP action, triglyceride in 35 triglyceride-rich lipoproteins is transferred to a high 212 C *pofV* d'Sp'f''c 'n of AU2008201550 (ang"o. trackad).doc density lipoprotein (HDL) and cholesteryl ester in HDL is transferred to a triglyceride-rich lipoproteins. A compound having a CEPT inhibitory action of the present invention (hereinafter to be also referred to as 5 CEPT inhibitor) may be any as long as it has a CEPT inhibitory action, and is exemplified by compounds disclosed in W02003/026672, W02002/088085, W02002/088069, W02002/083128, W02002/064549, W02002/059077, W02002/013797, W02002/011710, W02000/053792, W02000/038726, W02000/038724, 10 W02000/038721, W02000/018724, W02000/018723, W02000/018721, W099/41237, W099/15504, W099/14215, W099/14204, W099/14174, W098/39299, W098/34920, W098/04528, W096/15141, W095/06626, W093/11782, W099/1548, W003/028727, W02004/039453, W099/41237, W003/026672, W095/06626, US patent No. 15 6,727,277, US patent application publication 2003/040545, US patent application publication 2003/032644, US patent application publication 2003/027826, US patent application publication 2002/177708, US patent application publication 2002/165231, US patent application publication 2002/120011, 20 US patent application publication 2001/018446, US patent 6521607, US patent No. 6482862, US patent No. 6476075, US patent No. 6462092, US patent No. 6458849, US patent No. 6458803, US patent No. 6455519, US patent No. 6451823, US patent No. 6207671, US patent No. 6063788, US patent No. 25 5932587, US patent No. 5925645, US patent No. 5519001, JP A-2002-326987, JP patent No. 9059155, AU2002027728, JP-T 516732/2001 (W099/14174), JP-T-510478/2001 (W098/34920), JP-A-10-167967, JP-A-9-255574, JP-A-9-59155, JP-A 293764/2002, JP-A-221376/2003 and the like. 30 Specifically, the compound disclosed in WOOO/17164 (JP-T-2002-526475) can be mentioned: a compound of the formula (I) 213 C:'pof ' '"Spodf' 'on of AU2008201550 (ooch e. ato . d). - .

0

R

5 N OR4 R 6

R

7 R2 R R R wherein

R

1 is a hydrogen, Y, W-X or W-Y; W is carbonyl, thiocarbonyl, sulfinyl or sulfonyl; 5 X is -0-Y, -S-Y, -N(H)-Y or -N-(Y)2; wherein Y in each case is independently Z or a fully saturated, partially unsaturated or fully unsaturated 1- to 10-membered straight chain or branched carbon chain, wherein the carbons other 10 than a connecting carbons may be replaced with 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen, and the carbon may be independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by hydroxy, the 15 carbon may be mono-substituted by oxo, the sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the carbon chain may be mono-substituted by Z; Z is a partially saturated, fully saturated or 20 fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6 25 membered rings, taken independently, which may have 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen; the Z substituent may be independently mono-, di or tri-substituted by halo, (C 2

-C

6 )alkenyl, (Ci 30 C 6 )alkyl, hydroxy, (C 1

-C

6 )alkoxy, (C 1

-C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci 214 C pof' 'dVS' 'f'cat' o of AU2008201550 (ctrngo. tracked) doc

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, wherein the (Ci-C 6 )alkyl substituent may be independently mono-, di- or tri-substituted by halo, hydroxy, (Ci-C6)alkoxy, (Ci-C4)alkylthio, 5 amino, nitro, cyano, oxo, carboxy, (C 1 C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino and the (Ci-C 6 )alkyl substituent may be substituted by 1 to 9 fluorines; R 2 is a partially saturated, fully saturated or fully 10 unsaturated 1- to 6-membered straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen, the carbon atom may be 15 independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by oxo, the carbon may be mono-substituted by hydroxy, the sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo; or 20 R 2 is a partially saturated, fully saturated or fully unsaturated 3- to 7-membered ring optionally having 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen, wherein the R 2 ring may be bonded via (Ci-C 4 )alkyl; 25 wherein the R 2 ring may be independently mono-, di or tri-substituted by halo, (C 2

-C

6 )alkenyl, (Ci C6)alkyl, hydroxy, (Ci-C)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci 30 C 6 )alkylamino, and the (Ci-C 6 )alkyl substituent may be independently mono-, di- or tri-substituted by halo, hydroxy, (C-C6)alkoxy, (C-C4)alkylthio, oxo or (Ci-C6)alkyloxycarbonyl; provided that R 2 is not methyl; 35 R3 is a hydrogen or Q; 215 C.V"'f'm V ''''""*"'^ of AU2008201550 (oang.. tr.ck.d) do wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be 5 replaced with one heteroatom selected from oxygen, sulfur and nitrogen, the carbon may be independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by hydroxy, the carbon may be mono-substituted by oxo, the sulfur 10 may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the carbon chain may be mono-substituted by V; V is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally 1s having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, which may have 1 to 4 20 heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the V substituent may be independently mono-, di- or tri-substituted by halo, (Ci-C 6 )alkyl,

(C

2

-C

6 )alkenyl, hydroxy, (Ci-Cs)alkoxy, (Cl 25 C 4 )alkylthio, amino, nitro, cyano, oxo, carboxamoyl, mono-N- or di-N,N-(Ci-C 6 )alkylcarboxamoyl, carboxy,

(C

1

-C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, wherein the (Ci-C 6 )alkyl or (C 2 C 6 )alkenyl substituent may be independently mono-, 30 di- or tri-substituted by hydroxy, (Ci-C)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (C-C6)alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, and the (Ci-C 6 )alkyl substituent or

(C

2 -C)alkenyl substituent may be substituted by 1 35 to 9 fluorines; 216C:VpofVwordVSpecfIcatn of AU2008201550 (changes tracked).doc R 4 is Q or V'; wherein Q 1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain, wherein 5 the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen, the carbon may be independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by hydroxy, the 10 carbon may be mono-substituted by oxo, the sulfur may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the carbon chain may be mono-substituted by V';

V

1 is a partially saturated, fully saturated or 15 fully unsaturated 3- to 6-membered ring optionally having 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen; VI substituent may be independently mono-, di-, tri- or tetra-substituted independently by halo, 20 (C 1

-C

6 )alkyl, (Ci-C 6 )alkoxy, amino, nitro, cyano,

(C

1

-C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono-substituted independently by oxo or the (C 1

-C

6 )alkyl substituent is optionally 25 substituted by 1 to 9 fluorines; wherein any R 3 should contain V, or R 4 should contain V'; and

R

5 , R 6 , R 7 and R' are each independently hydrogen, a bond, nitro or 30 halo, wherein the bond is substituted by T or a partially saturated, fully saturated or fully unsaturated straight chain or branched carbon chain having 1 to 12 carbon atoms, wherein the carbons may be replaced with 1 or 2 heteroatoms 35 independently selected from oxygen, sulfur and 217 C:*p*'-"''' e''''''"' '*"'^200820155 o re ngoo..r.cked o nitrogen, wherein the carbon atom may be independently mono-, di- or tri-substituted by halo, the carbon may be mono-substituted by hydroxy, the carbon may be mono-substituted by oxo, the sulfur 5 may be mono or di-substituted by oxo, the nitrogen may be mono or di-substituted by oxo, and the carbon may be mono-substituted by T; T is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally 10 having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6 membered rings, taken independently, which may have 15 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the T substituent is optionally mono-, di or tri-substituted by halo, (Ci-C6) alkyl, (C2 C6)alkenyl, hydroxy, (Ci-C6) alkoxy, (Ci-C 4 ) alkylthio, 20 amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, the (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C 6 )alkoxy, (Ci 25 C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C6)alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, and the (Ci-C)alkyl substituent is optionally substituted by 1 to 9 fluorines; and

R

5 and R 6 , or R 6 and R , and/or R 7 and R 8 30 may be linked to form a partially saturated or fully unsaturated 4- to 8-membered ring optionally having 1 to 3, at least 1, heteroatom independently selected from nitrogen, sulfur and oxygen; wherein the ring (one or plural) formed by R 5 and 35 R 6 , or R 6 and R 7 , and/or R 7 and R 8 may be 218 C odSp'cIf''i'* of AU2008201s550 (ds e d rcOS oc independently mono-, di- or tri-substituted by halo, (Cl-CE)alkyl, (Ci-C 4 )alkylsulfonyl, (C2-CE)alkenyl, hydroxy, (Ci-C6)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cl-CE) alkyloxycarbonyl, 5 mono-N- or di-N, N- (Ci-CE) alkylamino, the (Ci C)alkyl substituent may be independently mono-, di- or tri-substituted by hydroxy, (Ci-C)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cl-C6) alkyloxycarbonyl, mono-N- or di-N, N- (Ci 10 C) alkylamino, and the (Ci-C) alkyl substituent may be substituted by 1 to 9 fluorines; provided that when R 2 is carboxyl or (Ci-C 4 ) alkylcarboxyl,

R

1 is not a hydrogen, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the 15 prodrug. The expression of "prodrug" of the formula (I) refers to a compound which is a drug precursor that releases, following administration, a drug according to a specific chemical or physiological process in vivo (e.g., prodrug 20 is converted to a desired drug form by setting to a physiological pH or by an enzyme action) . An exemplary prodrug releases a corresponding free acid upon cleavage, and examples of such hydrolytic ester forming residue of the compound of the formula (I) includes, but not limited 25 to, those wherein its free hydrogen of carboxyl moiety is substituted by (Ci-C 4 )alkyl, (C 2

-C

7 )alkanoyloxymethyl, 1 (alkanoyloxy)ethyl having 4 to 9 carbon atoms, 1-methyl-l (alkanoyloxy)-ethyl having 5 to 10 carbon atoms, alkoxycarbonyloxymethyl having 3 to 6 carbon atoms, 1 30 (alkoxycarbonyloxy)ethyl having 4 to 7 carbon atoms, 1 methyl-l-(alkoxycarbonyloxy)ethyl having 5 to 8 carbon atoms, N-(alkoxycarbonyl)aminomethyl having 3 to 9 carbon atoms, 1-(N-(alkoxycarbonyl)amino)ethyl having 4 to 10 carbon atoms, 3-phthalidyl, 4-crotonolactonyl, y 35 butyrolacton-4-yl, di-N,N-(Ci-C2)alkylamino(C 2

-C

3 )alkyl 219 C:*po*'*Sp''c'"Io' of'AU20082o15o (chang.. tr.c.d).

(e.g., b-dimethylaminoethyl), carbamoyl-(Cl-C2)alkyl, N,N di(Ci-C 2 )alkylcarbamoyl-(Ci-C 2 )alkyl, piperidino-, pyrrolidino- and morpholino(C2-C3)alkyl. In the following paragraphs, exemplary rings (one 5 kind or plural kinds) are described for the explanation of general rings included herein. An exemplary 5- or 6 membered ring in the formula (I), which may have 1 or 2 heteroatoms independently selected from oxygen, nitrogen and sulfur, includes phenyl, furyl, thienyl, pyrrolyl, 10 oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridiazinyl, pyrimidinyl and pyrazinyl. An exemplary partially saturated, fully saturated or fully unsaturated 5- to 8-membered ring in the formula (I), 15 which may have 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen includes cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl and phenyl. A further exemplary 5-membered ring in the formula (I) includes 2H pyrrolyl, 3H-pyrrolyl, 2-pyrrolinyl, 3-pyrrolinyl, 20 pyrrolidinyl, 1,3-dioxolanyl, oxazolyl, thiazolyl, imidazolyl, 2H-imidazolyl, 2-imidazolinyl, imidazolidinyl, pyrazolyl, 2-pyrazolinyl, pyrazolidinyl, isoxazolyl, isothiazolyl, 1,2-dithiolyl, 1,3-dithiolyl, 3H-1,2 oxathiolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5 25 oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-triazolyl, 1,2,4 triazolyl, 1,3,4-thiadiazolyl, 1,2,3,4-oxatriazolyl, 1,2,3,5-oxatriazolyl, 3H-1,2,3-dioxazolyl, 1,2,4 dioxazolyl, 1,3,2-dioxazolyl, 1,3,4-dioxazolyl, 5H-1,2,5 oxathiazolyl and 1,3-oxathiolyl. 30 A further exemplary 6-membered ring in the formula (I) includes 2H-pyranyl, 4H-pyranyl, pyridinyl, piperidinyl, 1,2-dioxinyl, 1,3-dioxinyl, 1,4-dioxanyl, morpholinyl, 1,4-dithianyl, thiomorpholinyl, pyridazinyl, pyrimidinyl, pyrazinyl, piperazinyl, 1,3,5-triazinyl, 35 1,2,4-triazinyl, 1,2,3-triazinyl, 1,3,5-trithianyl, 4H- 1,2-oxazinyl, 2H-1,3-oxazinyl, 6H-1,3-oxazinyl, 6H-1,2 oxazinyl, 1,4-oxazinyl, 2H-1,2-oxazinyl, 4H-1,4-oxazinyl, 1,2,5-oxathiazinyl, 1,4-oxazinyl, o-isoxadinyl, p isoxadinyl, 1,2,5-oxathiazinyl, 1,2,6-oxathiazinyl, 1,4,2 5 oxadiazinyl and 1,3,5,2-oxadiazinyl. A further exemplary 7-membered ring in the formula (I) includes azepinyl, oxepinyl and thiepinyl. A further exemplary 8-membered ring in the formula (I) includes cyclooctyl, cyclooctenyl and cyclooctadienyl. 10 An exemplary bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 5- or 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen includes indolizinyl, indolyl, 15 isoindolyl, 3H-indolyl, 1H-isoindolyl, indolinyl, cyclopenta(b)pyridinyl, pyrano(3,4-b)pyrrolyl, benzofuryl, isobenzofuryl, benzo(b)thienyl, benzo(c)thienyl, 1H indazolyl, indoxazinyl, benzoxazolyl, benzimidazolyl, benzothiazolyl, purinyl, 4H-quinolizinyl, quinolinyl, 20 isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, 1,8-naphthyridinyl, pteridinyl, indenyl, isoindenyl, naphthyl, tetralinyl, decalinyl, 2H-1 benzopyranyl, pyrido(3,4-b)-pyridinyl, pyrido(3,2-b) pyridinyl, pyrido(4,3-b)-pyridinyl, 2H-1,3-benzoxazinyl, 25 2H-1,4-benzoxazinyl, 1H-2,3-benzoxazinyl, 4H-3,1 benzoxazinyl, 2H-1,2-benzoxazinyl and 4H-1,4-benzoxazinyl. What alkylene in the formula (I) means is a saturated hydrocarbon (straight chain or branched chain) wherein a hydrogen atom has been removed from each 30 terminal carbon. Examples of such group include (assuming that the designated length encompasses specific examples) methylene, ethylene, propylene, butylene, pentylene, hexylene and heptylene. What the halo in the formula (I) means is chloro, 35 bromo, iodo or fluoro. 2 21 C*'Pof' ' 'rdVSpdflc "n o'AU20082O15SO (,Nes tr.wkd).d c What the alkyl in the formula (I) means is a saturated straight chain hydrocarbon or a saturated branched chain hydrocarbon. Examples of such alkyl group (assuming that the designated length encompasses specific 5 examples) include methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, hexyl, isohexyl, heptyl and octyl. What the alkoxy in the formula (I) means is a 10 saturated straight chain alkyl or a saturated branched chain alkyl, each being bonded via oxy. Examples of such alkoxy group (assuming that the designated length encompasses specific examples) include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, 15 pentoxy, isopentoxy, neopentoxy, tert-pentoxy, hexoxy, isohexoxy, heptoxy and octoxy. The terms mono-N- and di-N,N-(Ci-Cx)alkyl ... used for the formula (I) refer to (Ci-C,)alkyl moiety taken independently, when it is di-N,N-(Ci-Cx)alky1 ... (x means 20 an integer). It should be appreciated that, when, in the formula (I), a monocyclic or heterocyclic moiety can be bonded to a designated substrate via a different ring atom, without indicating a specific binding site, or can be linked by a 25 different method, any point with such possibility is intended, whether via a carbon atom, or via, for example, a trivalent nitrogen atom. For example, the term "pyridyl" means 2-, 3- or 4-pyridyl, and "thienyl" means 2-, or 3-thienyl. 30 A reference to a term "the carbon" in the phrases, "the carbon may be independently mono-, di- or tri substituted by halo, the carbon may be mono-substituted by hydroxy, the carbon may be mono-substituted by oxo" in the formula (I) means each carbon in a carbon chain including 35 a connecting carbon. 222 C *pofo"dVSp 'fiCt ^n of AU2008201550 (charges tracked)6oc A reference to "nitrogen may be . .. di-substituted by oxo" in the formula (I) means a terminal nitrogen constituting a nitro functionality. The expression "a pharmaceutically acceptable salt" 5 in the formula (I) means a non-toxic anion salt including anion, which is exemplified by, though not limited to, chloride, bromide, iodide, sulfate, hydrogen sulfate, phosphate, acetate, maleate, fumarate, oxalate, lactate, tartrate, citrate, gluconate, methanesulfonate and 4 10 toluene-sulfonate. This expression also means, but not limited to, non-toxic cation salts such as sodium, potassium, calcium, magnesium, ammonia or protonated benzathine (N,N'-dibenzylethylenediamine), choline, ethanolamine, diethanolamine, ethylenediamine, meglamine 15 (N-methyl-glucamine), benethamine (N-benzylphenethylamine), piperazine and tromethamine (2-amino-2-hydroxymethyl-1,3 propanediol). Specifically, the compound disclosed in WOOO/17166 (JP-T-2002-526477) can be mentioned: 20 a compound of the formula (II): 0 R3

R

5 N OR 4 6 4 (II) R N CH 3 R8 R1 RS RT wherein R 1 is hydrogen, Y, W-X, W-Y; W is carbonyl, thiocarbonyl, sulfinyl or sulfonyl; X is -0-Y, -S-Y, -N(H)-Y or -N-(Y)2; 25 Y in each case is independently, Z or a fully saturated, partially unsaturated or fully unsaturated 1- to 10 membered straight or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently from oxygen, 2 2 3 C*V*o**-*V'*''**''"' of AU2008201550 (..ngo.. .. od),do.

sulfur and nitrogen and aforementioned carbon is optionally mono-, di- or tri-substituted independently by halo, the aforementioned carbon is optionally mono substituted by hydroxy, the aforementioned carbon is 5 optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di-substituted by oxo, the aforementioned nitrogen is optionally mono- or di substituted by oxo, and the aforementioned carbon chain is optionally mono-substituted by Z; 10 Z is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 15 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the aforementioned Z substituent is optionally mono-, di- or tri-substituted independently by halo, (C 2 20 C6)alkenyl, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, (Cl

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino wherein the aforementioned (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by 25 halo, hydroxy, (C 1

-C

6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono N- or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (Cr C6)alkyl is optionally substituted by 1 to 9 fluorines;

R

3 is hydrogen or Q; 30 wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen, the aforementioned carbon is 35 optionally mono-, di- or tri-substituted independently by 224 C.VofNwodVSpaafl aton of AU2008201550 (changes tac~ed( oc halo, the aforementioned carbon is optionally mono substituted by hydroxy, the aforementioned carbon is optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di-substituted by oxo, the 5 aforementioned nitrogen is optionally mono- or di substituted by oxo, and the aforementioned carbon chain is optionally mono-substituted by V; wherein V is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 10 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected 15 independently from nitrogen, sulfur and oxygen; the aforementioned V substituent is optionally mono-, di-, tri- or tetra-substituted independently by halo, (Ci

C

6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Ci-C 6 )alkoxy, (Ci

C

4 )alkylthio,. amino, nitro, cyano, oxo, carboxamoyl, mono 20 N- or di-N,N-(Ci-C 6 )alkylcarboxamoyl, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino wherein the aforementioned (Ct-C 6 )alkyl or (C 2 -C6)alkenyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (C 1

-C

6 )alkoxy, (Ci-C 4 )alkylthio, 25 amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino or the aforementioned (Ci-C 6 )alkyl or (C 2

-C

6 )alkenyl substituent is optionally substituted by 1 to 9 fluorines;

R

4 is Q 1 or V'; 30 wherein Q 1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen and the aforementioned carbon 35 is optionally mono-, di- or tri-substituted independently 225 C*po*V*rd' Sp'df' ' "n oAU200820155O (ch.ngoe track.d),doc by halo, the aforementioned carbon is optionally mono substituted by hydroxy, the aforementioned carbon is optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di-substituted by oxo, the 5 aforementioned nitrogen is optionally mono- or di substituted by oxo, and the aforementioned carbon chain is optionally mono-substituted by V'; wherein V 1 is a partially saturated, fully saturated or fully unsaturated 3- to 6-membered ring optionally having 10 1 or 2 heteroatoms selected from oxygen, sulfur and nitrogen; wherein the aforementioned V 1 substituent is optionally mono-, di-, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Ci-C 6 )alkoxy, amino, nitro, cyano, 15 (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino, the aforementioned (Ci-C 6 )alkyl substituent is optionally mono-substituted by oxo, the aforementioned (Ci-C 6 )alkyl substituent is optionally substituted by 1 to 9 fluorines; 20 wherein either R 3 should contain V or R 4 should contain V'; and R 5 , R 6 , R and R 8 are each independently hydrogen, a bond, nitro or halo wherein the aforementioned bond is substituted by T or a partially saturated, fully saturated or fully unsaturated straight or branched carbon chain 25 having 1 to 12 carbon atoms wherein the carbons may be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen wherein the aforementioned carbon atom is optionally mono- di- or tri substituted independently by halo, the aforementioned 30 carbon is optionally mono-substituted by hydroxy, the aforementioned carbon is optionally mono-substituted by oxo, the aforementioned sulfur is optionally mono- or di substituted by oxo, the aforementioned nitrogen is optionally mono- or di-substituted by oxo, and the 35 aforementioned carbon is optionally mono-substituted by T; 226 C *VpO* rd'Sp'f'o''''"*AU20082O155O (chang.trackd),doc wherein T is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen or a bicyclic ring consisting of two 5 fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the aforementioned T substituent is optionally 10 mono-, di- or tri-substituted independently by halo, (Ci

C

6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Cr-C)alkoxy, (Cl

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cl

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino wherein the aforementioned (Ci-C 6 )alkyl substituent is 15 optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (Ci-C)alkyl substituent is optionally substituted by 1 to 9 fluorines; 20 provided that at least one of substituents R , R, R 7 and R8 is not hydrogen and is not linked to the quinoline moiety through oxy, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. 25 The expression of "prodrug" of the formula (II) refers to a compound of a drug precursor that releases a drug in vivo according to some specific chemical or physiological process after administration (e.g., prodrug is converted to a desired drug form by achieving a 30 physiological pH or by an enzyme action). A typical prodrug cleaves and releases a corresponding free acid. An ester forming residue of a hydrolyzable compound of the formula (II) has a carboxyl moiety, and is exemplified by, but not limited to, those wherein its free hydrogen has 35 been substituted by (Ci-C 4 )alkyl, (C 2

-C

7 )alkanoyloxymethyl, 227 C:po'""dVSpo '' of AU20020 1550 (h.2nes t.. cd) d= 1-(alkanoyloxy)ethyl having 4 to 9 carbon atoms, 1-methyl 1-(alkanoyloxy)ethyl having 5 to 10 carbon atoms, alkoxycarbonyloxymethyl having 3 to 6 carbon atoms, 1 (alkoxycarbonyloxy)ethyl having 4 to 7 carbon atoms, 1 5 methyl-l-(alkoxycarbonyloxy)ethyl having 5 to 8 carbon atoms, N-(alkoxycarbonyl)aminomethyl having 3 to 9 carbon atoms, 1-(N-(alkoxycarbonyl)amino)ethyl having 4 to 10 carbon atoms, 3-phthalidyl, 4-crotonolactonyl, y butyrolacton-4-yl, di-N,N-(Ci-C2)alkylamino(C 2

-C

3 )alkyl 10 (e.g., b-dimethylaminoethyl), carbamoyl-(Cl-C2)alkyl, N,N di(Ci-C 2 )alkylcarbamoyl-(Ci-C2)alkyl, piperidino-, pyrrolidino- or morpholino(C2-C3)alkyl. Examples of the 5- or 6-membered aromatic ring in the formula (II), which has 1 or 2 heteroatoms 15 independently selected from oxygen, nitrogen and sulfur as desired, include phenyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridiazinyl, pyrimidinyl, pyrazinyl and the like. 20 Examples of the partially saturated, fully saturated or fully unsaturated 5- to 8-membered ring in the formula (II), which has 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, include cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, phenyl 25 and the like. Further examples of the 5-membered ring include 2H-pyrrolyl, 3H-pyrrolyl, 2-pyrrolinyl, 3 pyrrolinyl, pyrrolidinyl, 1,3-dioxolanyl, oxazolyl, thiazolyl, imidazolyl, 2H-imidazolyl, 2-imidazolinyl, imidazolidinyl, pyrazolyl, 2-pyrazolinyl, pyrazolidinyl, 30 isoxazolyl, isothiazolyl, 1,2-dithiolyl, 1,3-dithiolyl, 3H-1,2-oxathiolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,3,4-thiadiazolyl, 1,2,3,4-oxatriazolyl, 1,2,3,5-oxatriazolyl, 3H-1,2,3-dioxazolyl, 1,2,4 35 dioxazolyl, 1,3,2-dioxazolyl, 1,3,4-dioxazolyl, 5H-1,2,5 2 28 cpowv rdspeelfication of AU2008201550 (changeS tracd)oc oxathiazolyl, 1,3-oxathiolyl and the like. A further exemplary 6-membered ring includes 2H pyranyl, 4H-pyranyl, pyridinyl, piperidinyl, 1,2-dioxinyl, 1,3-dioxinyl, 1,4-dioxanyl, morpholinyl, 1,4-dithianyl, 5 thiomorpholinyl, pyridazinyl, pyrimidinyl, pyrazinyl, piperazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,3 triazinyl, 1,3,5-trithianyl, 4H-1,2-oxazinyl, 2H-1,3 oxazinyl, 6H-1,3-oxazinyl, 6H-1,2-oxazinyl, 1,4-oxazinyl, 2H-1,2-oxazinyl, 4H-1,4-oxazinyl, 1,2,5-oxathiazinyl, 1,4 10 oxazinyl, o-isoxadinyl, p-isoxadinyl, 1,2,5-oxathiazinyl, 1,2,6-oxathiazinyl, 1,4,2-oxadiazinyl, 1,3,5,2-oxadiazinyl and the like. Further examples of the 7-membered ring include azepinyl, oxepinyl, thiepinyl and the like. 15 Further examples of the 8-membered ring include cyclooctyl, cyclooctenyl, cyclooctadienyl and the like. In the case of the formula (II), examples of a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 5- or 6-membered 20 rings (independently selected) optionally having 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen include indolizinyl, indolyl, isoindolyl, 3H indolyl, 1H-isoindolyl, indolinyl, cyclopenta(b)pyridinyl, pyrano(3,4-b)pyrrolyl, benzofuryl, isobenzofuryl, 25 benzo(b)thienyl, benzo(c)thienyl, 1H-indazolyl, indoxazinyl, benzoxazolyl, benzimidazolyl, benzothiazolyl, purinyl, 4H-quinolizinyl, quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, 1,8 naphthyridinyl, pteridinyl, indenyl, isoindenyl, naphthyl, 30 tetralinyl, decalinyl, 2H-1-benzopyranyl, pyrido(3,4-b) pyridinyl, pyrido(3,2-b)-pyridinyl, pyrido(4,3-b) pyridinyl, 2H-1,3-benzoxazinyl, 2H-1,4-benzoxazinyl, 1H 2,3-benzoxazinyl, 4H-3,1-benzoxazinyl, 2H-1,2-benzoxazinyl, 4H-1,4-benzoxazinyl and the like. 35 The alkylene in the formula (II) means a saturated 2 29 C'"* 'i'Sp*cfica'ton of AU2008201550 (chang. tracked).doc hydrocarbon (straight chain or branched) wherein a hydrogen atom has been removed from each terminal carbon. Examples of such group include (assuming that the designated length encompasses specific examples) methylene, 5 ethylene, propylene, butylene, pentylene, hexylene and heptylene. The halo in the formula (II) means chloro, bromo, iodo or fluoro. The alkyl in the formula (II) means a saturated 10 straight chain hydrocarbon or a saturated branched chain hydrocarbon. Examples of such alkyl group (assuming that the designated length encompasses specific examples) include methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, 1 15 methylbutyl, 2-methylbutyl, 3-methylbutyl, hexyl, isohexyl, heptyl and octyl. The alkoxy in the formula (II) means a saturated straight chain alkyl or a saturated branched chain alkyl, each being bonded via oxy. Examples of such alkoxy group 20 (assuming that the designated length encompasses specific examples) include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, pentoxy, isopentoxy, neopentoxy, tert-pentoxy, hexoxy, isohexoxy, heptoxy and octoxy. 25 The terms mono-N- and di-N,N-(Ci-Cx)alkyl ... used for the formula (II) refer to (Ci-C,)alkyl moiety taken independently, when it is di-N,N-(Ci-Cx)alkyl ... (x means an integer). The "aforementioned carbon" in the "aforementioned 30 carbon may be independently mono-, di- or tri-substituted by halo, the aforementioned carbon may be mono-substituted by hydroxy, the aforementioned carbon may be mono substituted by oxo" in the formula (II) refers to each carbon in the carbon chain containing a connecting carbon. 35 The "nitrogen is ... di-substituted by oxo" in the 2 30 C 'po''V'd*SpefIcatJon of AU2002O155O (change tracked).doc formula (II) refers to the terminal nitrogen constituting the nitro functionality. It should be appreciated that, when a carbon or heterocyclic moiety can be bonded or attached to a 5 designated substrate via a different ring atom, without indicating a specific binding site, any point with such possibility is intended, whether via a carbon atom, or, for example, via a trivalent nitrogen atom. For example, the term "pyridyl" means 2-, 3- or 4-pyridyl, "thienyl" 10 means 2-, or 3-thienyl, and the like. The expression, "a pharmaceutically acceptable salt" in the formula (II) means, but not limited to, non-toxic anion salts including anion such as chloride, bromide, iodide, sulfate, hydrogen sulfate, phosphate, acetate, 15 maleate, fumarate, oxalate, lactate, tartrate, citrate, gluconate, methanesulfonate and 4-toluene-sulfonate. This expression also means, but not limited to, non-toxic cation salts such as sodium, potassium, calcium, magnesium, ammonium or protonated benzathine (N,N' 20 dibenzylethylenediamine), choline, ethanolamine, diethanolamine, ethylenediamine, meglamine (N-methyl glucamine), benethamine (N-benzylphenethylamine), piperazine and tromethamine (2-amino-2-hydroxymethyl-1,3 propanediol). 25 Specifically, the compound disclosed in WOOO/17165 (JP-T-2002-526476) can be mentioned: a compound of the formula (III)

R

3 R4

R

5 N 6 4 (III) 7 R R wherein R' is Y, W-X or W-Y; 30 wherein W is a carbonyl, thiocarbonyl, sulfinyl or 2 31 C 'pof'dSp''f'c''on of AU20082I5 o rc. eo. c sulfonyl; X is -O-Y, -S-Y, -N(H)-Y or -N-(Y)2; Y in each case is independently Z or fully saturated, partially unsaturated or fully unsaturated 1- to 10 5 membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen and the carbon is mono-, di- or tri-substituted independently by halo, the carbon 10 is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is optionally mono or di-substituted by oxo, the nitrogen is optionally mono or di-substituted by oxo, and the carbon chain is optionally mono-substituted by Z; 15 wherein Z is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully 20 unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms from nitrogen, sulfur and oxygen; wherein the Z substituent is optionally mono-, di- or tri substituted independently by halo, (C 2

-C

6 )alkenyl, (C 1 25 C 6 )alkyl, hydroxy, (Cr-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono N- or di-N,N-(Cl-C6)alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by halo, hydroxy, (Ci-C 6 )alkoxy, (Cl 30 C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, the (Ci-C 6 )alkyl substituent is optionally substituted by 1 to 9 fluorines; R2 is a partially saturated, fully saturated or fully 35 unsaturated 1- to 6-membered straight chain or branched 232 C'po '' ''Spd' 'on of AU2002O55o (cha.nge. trk. d).doc carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen wherein the carbon atom is optionally mono-, di- or tri-substituted 5 independently by halo, the carbon is optionally mono substituted by oxo, the carbon is optionally mono substituted by hydroxy, the sulfur is optionally mono or di-substituted by oxo, the nitrogen is optionally mono or di-substituted by oxo; or the R2 is a partially saturated, 10 fully saturated or fully unsaturated 3- to 7-membered ring optionally having 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen, wherein the R 2 ring is optionally bonded via (C 1

-C

4 )alkyl; wherein the R2 ring is optionally mono-, di- or tri 15 substituted by halo, (C2-C6)alkenyl, (Ci-C 6 )alkyl, hydroxy,

(C

1

-C

6 )alkoxy, (C1-C4)alkylthio, amino, nitro, cyano, oxo, carboxy, (C1-C6)alkyloxycarbonyl, mono-N- or di-N,N-(Ci

C

6 )alkylamino wherein the (C 1

-C

6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by 20 halo, hydroxy, (Ci-C 6 )alkoxy, (C 1

-C

4 )alkylthio, oxo or (Ci C6)alkyloxycarbonyl;

R

3 is hydrogen or Q; wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or 25 branched carbon chain wherein the carbons, other than connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono-substituted by 30 hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is mono or di-substituted by oxo, the nitrogen is optionally mono or di-substituted by oxo, and the carbon chain is optionally mono-substituted by V; wherein V is a partially saturated, fully saturated or 35 fully unsaturated 3- to 8-membered ring optionally having 2 33 C '"''rd'Sp*''''n of AU2008201550 (choes ckd) 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, 5 optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the V substituent is optionally mono, di, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (C2

C

6 )alkenyl, hydroxy, (Ci-C 6 ) alkoxy, (C 1 -C4)alkylthio, amino, 10 nitro, cyano, oxo, carboxamoyl, mono-N- or di-N,N-(Ci

C

6 )alkylcarboxamoyl, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Cl-C6)alkylamino wherein the (Ci

C

6 )alkyl substituent or (C 2

-C

6 )alkenyl substituent is optionally mono-, di- or tri-substituted independently by 15 hydroxy, (Cl-C6)alkoxy, (Ci-C4)alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C6)alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino, the (Ci-C 6 )alkyl substituent or

(C

2

-C

6 )alkenyl substituent is optionally substituted by 1 to 9 fluorines; 20 R 4 is cyano, formyl, W Q , W1V1, (Ci-C 4 )alkylene V1 or V2; wherein W 1 is carbonyl, thiocarbonyl, SO or SO 2 ; Q1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain wherein the carbons may be replaced with one 25 heteroatom selected from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono substituted by hydroxy, the carbon is optionally mono substituted by oxo, the sulfur is optionally mono or di 30 substituted by oxo, the nitrogen is optionally mono or di substituted by oxo, and the carbon chain is optionally mono-substituted by V 1 ; wherein V 1 is a partially saturated, fully saturated or fully unsaturated 3- to 6-membered ring optionally having 35 1 or 2 heteroatoms selected independently from oxygen, 234CponsordWspecmcation of AU2008201550 (changes tracked).doc sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected 5 independently from nitrogen, sulfur and oxygen; wherein the V 1 substituent is optionally mono, di, tri- or tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Cr

C

6 )alkoxy, hydroxy, oxo, amino, nitro, cyano, (Cl

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino 10 wherein the (Ci-C 6 )alkyl substituent is optionally mono substituted by oxo, the (Ci-C 6 )alkyl substituent is also optionally substituted by 1 to 9 fluorines; wherein V 2 is a partially saturated, fully saturated or fully unsaturated 5- to 7-membered ring containing 1 to 4 15 heteroatoms independently from oxygen, sulfur and nitrogen; wherein the V 2 substituent is optionally mono-, di- or tri-substituted independently by halo, (Ci-C 2 )alkyl, (Ci

C

2 )alkoxy, hydroxy or oxo, wherein the (Ci-C 2 )alkyl 20 optionally has 1 to 5 fluorines; and wherein R 4 does not include oxycarbonyl bonded directly to the C4 nitrogen; wherein either R 3 should contain V or R 4 should contain V'; 5 6 78 R , R , R and R8 are independently hydrogen, a bond, nitro 25 or halo wherein the bond is substituted by T or a partially saturated, fully saturated or fully unsaturated straight chain or branched carbon chain having 1 to 12 carbon atoms wherein the carbon is replaced with 1 or 2 heteroatoms selected independently from oxygen, sulfur and 30 nitrogen, wherein the carbon atom is optionally mono-, di or tri-substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is optionally mono or di-substituted by oxo, the nitrogen is 35 optionally mono or di-substituted by oxo, and the carbon 235 CW*''w'''"i '''''''''' o"*'^2008'''5'0'"""'"'''''')

*

chain is optionally mono-substituted by T; wherein T is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, 5 sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; 20 wherein the T substituent is optionally mono-, di- or tri substituted by halo, (Ci-C 6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Ci-C)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (C-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci C6)alkylamino wherein the (Ci-C 6 )alkyl substituent is 15 optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, and the (Ci-C 6 )alkyl substituent also optionally has 1 to 9 fluorines; 20 wherein R and R , or R and R , and/or R and R may also be linked to form at least one ring that is a partially saturated or fully unsaturated 4- to 8-membered ring optionally having 1 to 3 heteroatoms independently selected from nitrogen, sulfur and oxygen; 25 wherein the ring formed by R 5 and R 6 , or R 6 and R , and/or R and R8 are optionally mono-, di- or tri-substituted by halo, (Ci-C 6 )alkyl, (Ci-C 4 )alkylsulfonyl, (C2-C6)alkenyl, hydroxy, (Ci-C6)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or 30 di-N,N-(Ci-C 6 )alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino, and the (Ci-C 6 )alkyl 35 substituent also optionally has 1 to 9 fluorines, a 2 3 6 C:VPo"v" 'dSPed'c''' of AU2008201SW (eans trcked).doc prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The expression of "prodrug" of the formula (III) refers to a compound of a drug precursor that releases a 5 drug in vivo due to some specific chemical or physiological process after administration (e.g., prodrug is converted to a desired drug form by achieving a physiological pH or by an enzyme action) . Examples of the prodrug that releases a corresponding free acid upon 10 cleavage and the residue forming hydrolytic ester of the compound of the formula (III) include, but not limited to, those having a carboxyl moiety, wherein its free hydrogen has been substituted by the following groups: (Ci-C 4 )alkyl,

(C

2

-C

7 )alkanoyloxymethyl, 1-(alkanoyloxy)ethyl having 4 to 15 9 carbon atoms, 1-methyl-l-(alkanoyloxy)ethyl having 5 to 10 carbon atoms, alkoxycarbonyloxymethyl having 3 to 6 carbon atoms, 1-(alkoxycarbonyloxy)ethyl having 4 to 7 carbon atoms, 1-methyl-l-(alkoxycarbonyloxy)ethyl having 5 to B carbon atoms, N-(alkoxycarbonyl)aminomethyl having 3 20 to 9 carbon atoms, 1-(N-(alkoxycarbonyl)amino)ethyl having 4 to 10 carbon atoms, 3-phthalidyl, 4-crotonolactonyl, y butyrolacton-4-yl, di-N,N-(Ci-C 2 )alkylamino(C 2

-C

3 )alkyl (e.g., b-dimethylaminoethyl), carbamoyl-(Ci-C 2 )alkyl, N,N di(Ci-C 2 )alkylcarbamoyl-(Ci-C 2 )alkyl, piperidino-, 25 pyrrolidino- or morpholino(C 2

-C

3 )alkyl. Examples of the 5- or 6-membered aromatic ring in the formula (III), which has 1 or 2 heteroatoms as desired, which are independently selected from oxygen, nitrogen and sulfur, include phenyl, furyl, thienyl, pyrrolyl, oxazolyl, 30 thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridiazinyl, pyrimidinyl and pyrazinyl. Examples of the partially saturated, fully saturated or fully unsaturated 5- to 8-membered ring in the formula (III), which has 1 to 4 heteroatoms as desired, which are 35 independently selected from oxygen, sulfur and nitrogen, 237 C pV-d~-lU A20215 -WA include cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, phenyl and the like. Further examples of the 5-membered ring include the following: 2H-pyrrolyl, 3H-pyrrolyl, 2 pyrrolinyl, 3-pyrrolinyl, pyrrolidinyl, 1,3-dioxolanyl, 5 oxazolyl, thiazolyl, imidazolyl, 2H-imidazolyl, 2 imidazolinyl, imidazolidinyl, pyrazolyl, 2-pyrazolinyl, pyrazolidinyl, isoxazolyl, isothiazolyl, 1,2-dithiolyl, 1,3-dithiolyl, 3H-1,2-oxathiolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 10 1,2,3-triazolyl, 1,2,4-triazolyl, 1,3,4-thiadiazolyl, 1,2,3,4-oxatriazolyl, 1,2,3,5-oxatriazolyl, 3H-1,2,3 dioxazolyl, 1,2,4-dioxazolyl, 1,3,2-dioxazolyl, 1,3,4 dioxazolyl, 5H-1,2,5-oxathiazolyl and 1,3-oxathiolyl. Further examples of the 6-membered ring include the 15 following: 2H-pyranyl, 4H-pyranyl, pyridinyl, piperidinyl, 1,2-dioxinyl, 1,3-dioxinyl, 1,4-dioxanyl, morpholinyl, 1,4-dithianyl, thiomorpholinyl, pyridazinyl, pyrimidinyl, pyrazinyl, piperazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,3-triazinyl, 1,3,5-trithianyl, 4H-1,2-oxazinyl, 2H 20 1,3-oxazinyl, 6H-1,3-oxazinyl, 6H-1,2-oxazinyl, 1,4 oxazinyl, 2H-1,2-oxazinyl, 4H-1,4-oxazinyl, 1,2,5 oxathiazinyl, 1,4-oxazinyl, o-isoxadinyl, p-isoxadinyl, 1,2,5-oxathiazinyl, 1,2,6-oxathiazinyl, 1,4,2-oxadiazinyl and 1,3,5,2-oxadiazinyl. 25 Further examples of the 7-membered ring include azepinyl, oxepinyl and thiepinyl. Further examples of the 8-membered ring include cyclooctyl, cyclooctenyl and cyclooctadienyl. In the case of the formula (III), examples of a 30 bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 5- or 6-membered rings, taken independently, having 1 to 4 heteroatoms as desired, which are independently selected from nitrogen, sulfur and oxygen, include the following: indolizinyl, 35 indolyl, isoindolyl, 3H-indolyl, 1H-isoindolyl, indolinyl, 2 38 C"VpofV ' "Spe '"fcabon of AU20082o5o (change troad) doc cyclopenta(b)pyridinyl, pyrano(3,4-b)pyrrolyl, benzofuryl, isobenzofuryl, benzo(b)thienyl, benzo(c)thienyl, 1H indazolyl, indoxazinyl, benzoxazolyl, benzimidazolyl, benzothiazolyl, purinyl, 4H-quinolizinyl, quinolinyl, s isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, 1,8-naphthyridinyl, pteridinyl, indenyl, isoindenyl, naphthyl, tetralinyl, decalinyl, 2H-1 benzopyranyl, pyrido(3,4-b)-pyridinyl, pyrido(3,2-b) pyridinyl, pyrido(4,3-b)-pyridinyl, 2H-1,3-benzoxazinyl, 10 2H-1,4-benzoxazinyl, 1H-2,3-benzoxazinyl, 4H-3,1 benzoxazinyl, 2H-1,2-benzoxazinyl and 4H-1,4-benzoxazinyl. The alkylene in the formula (III) means a saturated hydrocarbon (straight chain or branched chain) wherein a hydrogen atom has been removed from each terminal carbon. 15 Examples of such group include (assuming that the designated length encompasses specific examples) methylene, ethylene, propylene, butylene, pentylene, hexylene and heptylene. The halo in the formula (III) means chloro, bromo, 20 iodo or fluoro. The alkyl in the formula (III) means a saturated straight chain hydrocarbon or a saturated branched chain hydrocarbon. Examples of such alkyl group (assuming that the designated length encompasses specific examples) 25 include methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, isopentyl, neopentyl, t-pentyl, 1 methylbutyl, 2-methylbutyl, 3-methylbutyl, hexyl, isohexyl, heptyl and octyl. The alkoxy in the formula (III) means a saturated 30 straight chain alkyl or a saturated branched chain alkyl bonded via oxy. Examples of such alkoxy group (assuming that the designated length encompasses specific examples) include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, t-butoxy, pentoxy, isopentoxy, neopentoxy, t 35 pentoxy, hexoxy, isohexoxy, heptoxy and octoxy. 239 C:Vo"'d'Sp'd'cao of'AU 202O155O(can.o.trcd).doc The terms mono-N- and di-N,N-(Ci-C,)alkyl ... used for the formula (III) refer to (Ci-C,)alkyl moiety taken independently, when it is di-N,N-(Ci-C,)alkyl ... (x means an integer). 5 The "aforementioned carbon" in the "aforementioned carbon is mono-, di- or tri-substituted as desired by halo, the aforementioned carbon is mono-substituted as desired by hydroxy, the aforementioned carbon is mono-substituted as desired by oxo" in the formula (II) refers to each 10 carbon containing a connecting carbon in the carbon chain. The "nitrogen is ... di-substituted by oxo" in the formula (III) refers to the terminal nitrogen constituting the nitro functional group. It should be appreciated that, in the formula (III), 15 when a carbon ring or heterocyclic moiety is bonded to a designated substrate via various ring atoms, or attached thereto in a different form, without indicating a specific binding site, any point with such possibility is intended, whether via a carbon atom, or, for example, via a 20 trivalent nitrogen atom. For example, the term "pyridyl" means 2-, 3- or 4-pyridyl, "thienyl" means 2-, or 3 thienyl, and the like, and hereinafter the same. The expression "a pharmaceutically acceptable salt" in the formula (III) means, but not limited to, a non 25 toxic anion salt including anion such as chloride, bromide, iodide, sulfate, hydrogen sulfate, phosphate, acetate, maleate, fumarate, oxalate, lactate, tartrate, citrate, gluconate, methanesulfonate and 4-toluene-sulfonate. This expression also means, but not limited to, non-toxic 30 cation salts such as sodium, potassium, calcium, magnesium, ammonium or protonated benzathine (N,N' dibenzylethylenediamine), choline, ethanolamine, diethanolamine, ethylenediamine, meglamine (N-methyl glucamine), benethamine (N-benzylphenethylamine), 35 piperazine and tromethamine (2-amino-2-hydroxymethyl-1,3 2 4 QC~por#%rdVSpecdflctof of AU2008201550 (changes trackd).doc propanediol). Specifically, the compound disclosed in JP-A-2000 95764 can be mentioned: a compound of the formula (IV): 0 R3

R

5 N OR 4 5 R6 6 4 (IV) R7

CH

3 R8 R1 R R wherein R' is hydrogen, Y, W-X, W-Y; wherein W is a carbonyl, thiocarbonyl, sulfinyl or sulfonyl; X is -O-Y, -S-Y, -N(H)-Y or -N-(Y)2; 10 Y in each case is independently Z or a fully saturated, partially unsaturated or fully unsaturated 1- to 10 membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with 1 or 2 heteroatoms selected independently 15 from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is optionally mono- or di-substituted by oxo, the 20 nitrogen is optionally mono- or di-substituted by oxo, and the carbon chain is optionally mono-substituted by Z; wherein Z is a partially saturated, fully saturated or fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, 25 sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; 2 41 C"pof' d'Sp f'c'ton of AU2008201550 ( -e. trackad)oc wherein Z substituent is optionally mono-, di- or tri substituted independently by halo, (C 2

-C

6 )alkenyl, (Ci

C

6 )alkyl, hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono 5 N- or di-N,N-(Ci-C6)alkylamino wherein (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by halo, hydroxy, (Ci-C 6 )alkoxy, (Ci

C

4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(C 1

-C

6 )alkylamino, 10 the (Ci-C 6 )alkyl is optionally substituted by 1 to 9 fluorines;

R

3 is hydrogen or Q; wherein Q is a fully saturated, partially unsaturated or fully unsaturated 1- to 6-membered straight chain or 15 branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri-substituted independently by halo, the carbon is optionally mono-substituted by 20 hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is optionally mono- or di-substituted by oxo, the nitrogen is optionally mono- or di-substituted by oxo, the carbon chain is optionally mono-substituted by V; wherein V is a partially saturated, fully saturated or 25 fully unsaturated 3- to 12-membered ring optionally having 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, 30 optionally having 1 to 4 heteroatoms selected independently from nitrogen, sulfur and oxygen; wherein the V substituent is optionally mono-, di-, tri or tetra-substituted independently by halo, (Ci-Cs)alkyl,

(C

2

-C

6 )alkenyl, hydroxy, (Ci-C6)alkoxy, (Cr-C 4 )alkylthio, 35 amino, nitro, cyano, oxo, carboxamoyl, mono-N- or di-N,N 2 4 2C p" 'dVSp 'fi''.' ' ' A' 2008201550<.O.1 0.. . .o.d (Ci-C 6 )alkylcarboxamoyl, carboxy, (Ci-C)alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the (Cr

C

6 )alkyl or (C 2

-C

6 )alkenyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (Cr 5 C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(C

C

6 )alkylamino, the (Ci-C 6 )alkyl or (C 2 -C)alkenyl is optionally substituted by 1 to 9 fluorines;

R

4 is Q1 or V'; wherein Q1 is a fully saturated, partially 10 unsaturated or fully unsaturated 1- to 6-membered straight chain or branched carbon chain wherein the carbons other than the connecting carbon, may be replaced with one heteroatom selected independently from oxygen, sulfur and nitrogen and the carbon is optionally mono-, di- or tri 15 substituted independently by halo, the carbon is optionally mono-substituted by hydroxy, the carbon is optionally mono-substituted by oxo, the sulfur is mono- or di-substituted by oxo, the nitrogen is optionally mono- or di-substituted by oxo, the carbon chain is optionally 20 mono-substituted by Vi; wherein V 1 is a partially saturated, fully saturated or fully unsaturated 3- to 6 membered ring optionally having 1 or 2 heteroatoms selected independently from oxygen, sulfur and nitrogen; the V 1 substituent is optionally mono-, di-, tri- or 25 tetra-substituted independently by halo, (Ci-C 6 )alkyl, (Cl

C

6 )alkoxy, amino, nitro, cyano, (Ci-C 6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C6)alkylamino wherein the (Cl

C

6 )alkyl substituent is optionally mono-substituted by oxo, the (Ci-C 6 )alkyl substituent optionally has 1 to 9 30 fluorines; either R 3 should contain V or R 4 should contain V'; and

R

5 and R , or R 6 and R 7 , and/or R 7 and R 8 are linked to form at least one partially saturated or fully unsaturated 4 to 8-membered ring optionally having 1 to 3 heteroatoms 35 independently selected from nitrogen, sulfur and oxygen; 2 4 3 C*po ''Sp'fl''t'"l 0AU20082O155o changess trcad).doc the rings (one or more) formed by R 5 and R 6 , or R 6 and R, and/or R" and R 8 are optionally mono-, di- or tri substituted independently by halo, (C 1

-C

6 )alkyl, (Cr

C

6 )alkylsulfonyl, (C 2

-C

6 )alkenyl, hydroxy, (C1-C)alkoxy, 5 (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Cr

C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Ci-C 6 )alkylamino wherein the (Ci-C 6 )alkyl substituent is optionally mono-, di- or tri-substituted independently by hydroxy, (Cr

C

6 )alkoxy, (C 1

-C

4 )alkylthio, amino, nitro, cyano, oxo, 10 carboxy, (C 1

-C

6 )alkyloxycarbonyl, mono-N- or di-N,N-(Cl

C

6 )alkylamino, and the (C 1

-C

6 )alkyl substituent optionally has 1 to 9 fluorines; provided that when the R , R 6 , R 7 and/or R 8 do not form at least one ring, they are each independently hydrogen, halo, (C 1

-C

6 )alkoxy or (Ci-C 6 )alkyl, 15 wherein the (Ci-C 6 )alkyl optionally has 1 to 9 fluorines, a prodrug thereof or a pharmaceutically acceptable salt of the compound or the prodrug. The expression of "prodrug" of the formula (IV) refers to a compound of a drug precursor that releases a 20 drug in vivo according to some specific chemical or physiological process after administration (e.g., prodrug becomes an object drug form by achieving a physiological pH or by an enzyme action) . Examples of the prodrug that releases a corresponding free acid upon cleavage and the 25 residue forming hydrolytic ester of the compound of the formula (IV) include, but not limited to, those having a carboxy moiety, wherein its free hydrogen has been substituted by the following groups: (Ci-C 4 )alkyl, (C2

C

7 )alkanoyloxymethyl, 1-(alkanoyloxy)ethyl having 4 to 9 30 carbon atoms, 1-methyl-l-(alkanoyloxy)ethyl having S to 10 carbon atoms, alkoxycarbonyloxymethyl having 3 to 6 carbon atoms, 1-(alkoxycarbonyloxy)ethyl having 4 to 7 carbon atoms, 1-methyl-l-(alkoxycarbonyloxy)ethyl having 5 to 8 carbon atoms, N-(alkoxycarbonyl)aminomethyl having 3 to 9 35 carbon atoms, 1-(N-(alkoxycarbonyl)amino)ethyl having 4 to 24 4 C:VpofW rdVSpdfcction of AU2082O01550 (changes traked)doc 10 carbon atoms, 3-phthalidyl, 4-crotonolactonyl, y butyrolacton-4-yl, di-N,N-(Ci-C 2 )alkylamino(C 2

-C

3 )alkyl (e.g., b-dimethylaminoethyl), carbamoyl-(C1-C 2 )alkyl, N,N di(Ci-C 2 )alkylcarbamoyl-(Ci-C 2 )alkyl, piperidino-, 5 pyrrolidino- or morpholino(C 2

-C

3 )alkyl. Examples of the 5- or 6-membered aromatic ring in the formula (IV), which may have 1 or 2 heteroatoms independently selected from oxygen, nitrogen and sulfur include phenyl, furyl, thienyl, pyrrolyl, oxazolyl, 10 thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridiazinyl, pyrimidinyl and pyrazinyl. Examples of the partially saturated, fully saturated or fully unsaturated 5- to 8-membered ring in the formula (IV), which may have 1 to 4 heteroatoms independently 15 selected from oxygen, sulfur and nitrogen, include cyclohexyl, cycloheptyl, cyclooctyl and phenyl. Examples of other 5-membered ring include the following: 2H pyrrolyl, 3H-pyrrolyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolidinyl, 1,3-dioxolanyl, oxazolyl, thiazolyl, 20 imidazolyl, 2H-imidazolyl, 2-imidazolinyl, imidazolidinyl, pyrazolyl, 2-pyrazolinyl, pyrazolidinyl, isoxazolyl, isothiazolyl, 1,2-dithiolyl, 1,3-dithiolyl, 3H-1,2 oxathiolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5 oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiazolyl, 1,2,4 25 thiazolyl, 1,3,4-thiazolyl, 1,2,3,4-oxatriazolyl, 1,2,3,5 oxatriazolyl, 3H-1,2,3-dioxazolyl, 1,2,4-dioxazolyl, 1,3,2-dioxazolyl, 1,3,4-dioxazolyl, 5H-1,2,5-oxathiazolyl and 1,3-oxathiolyl. Examples of other 6-membered ring in the formula 30 (IV) include the following: 2H-pyranyl, 4H-pyranyl, pyridinyl, piperidinyl, 1,2-dioxinyl, 1,3-dioxinyl, 1,4 dioxanyl, morpholinyl, 1,4-dithianyl, thiomorpholinyl, pyridazinyl, pyrimidinyl, pyrazinyl, piperazinyl, 1,3,5 triazinyl, 1,2,4-triazinyl, 1,2,3-triazinyl, 1,3,5 35 trithianyl, 4H-1,2-oxazinyl, 2H-1,3-oxazinyl, 6H-1,3 245 CV"'*"'rdVSp"c"'''on'ofAU2008201550(changa tracked).doc oxazinyl, 6H-1,2-oxazinyl, 1,4-oxazinyl, 2H-1,2-oxazinyl, 4H-1,4-oxazinyl, 1,2,5-oxathiazinyl, 1,4-oxazinyl, o isoxadinyl, p-isoxadinyl, 1,2,5-oxathiazinyl, 1,2,6 oxathiazinyl, 1,4,2-oxadiazinyl and 1,3,5,2-oxadiazinyl. 5 Further examples of the 7-membered ring include azetidinyl, oxepinyl and thiepinyl. Further examples of the 8-membered ring include cyclooctyl, cyclooctenyl and cyclooctadienyl. Examples of the two fused partially saturated, fully 10 saturated or fully unsaturated 5- or 6-membered rings, which independently optionally have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen, include the following: indolizinyl, indolyl, isoindolyl, 3H-indolyl, 1H-isoindolyl, indolinyl, 15 cyclopenta(b)pyridinyl, pyrano(3,4-b)pyrrolyl, benzofuryl, isobenzofuryl, benzo(b)thienyl, benzo(c)thienyl, 1H indazolyl, indoxazinyl, benzoxazolyl, benzimidazolyl, benzothiazolyl, purinyl, 4H-quinolizinyl, quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, 20 quinoxalinyl, 1,8-naphthyridinyl, pteridinyl, indenyl, isoindenyl, naphthyl, tetralinyl, decalinyl, 2H-1 benzopyranyl, pyrido(3,4-b)-pyridinyl, pyrido(3,2-b) pyridinyl, pyrido(4,3-b)-pyridinyl, 2H-1,3-benzoxazinyl, 2H-1,4-benzoxazinyl, 1H-2,3-benzoxazinyl, 4H-3,1 25 benzoxazinyl, 2H-1,2-benzoxazinyl and 4H-1,4-benzoxazinyl. The alkylene in the formula (IV) means a saturated hydrocarbon (straight chain or branched chain) wherein a hydrogen atom has been removed from each terminal carbon. Examples of such group include (assuming that the 30 designated length encompasses specific examples) methylene, ethylene, propylene, butylene, pentylene, hexylene and heptylene. The halo in the formula (IV) means chloro, bromo, iodo or fluoro. The alkyl in the formula (IV) means a 35 saturated straight chain hydrocarbon or a saturated 24 6 C *r'''' f'''''''**A^200 O201 (eang..traediADC branched chain hydrocarbon. Examples of such alkyl group (assuming that the designated length encompasses specific examples) include methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, isopentyl, neopentyl, t-pentyl, 5 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, hexyl, isohexyl, heptyl and octyl. The alkoxy in the formula (IV) means a saturated straight chain alkyl or a saturated branched chain alkyl bonded via oxy. Examples of such alkoxy group (assuming 10 that the designated length encompasses specific examples) include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, t-butoxy, pentoxy, isopentoxy, neopentoxy, t pentoxy, hexoxy, isohexoxy, heptoxy and octoxy. The terms mono-N- and di-N,N-(Ci-C,)alkyl ... used 15 for the formula (IV) refer to (Ci-C,)alkyl moiety taken independently, when it is di-N,N-(Ci-Cx)alkyl ... (x means an integer). It should be appreciated that, in the formula (IV), when a carbon ring or heterocyclic moiety is bonded to a 20 designated substrate via various ring atoms, or attached thereto in a different form, without indicating a specific binding site, any point with such possibility is intended, whether via a carbon, or via, for example, a trivalent nitrogen atom. For example, the term "pyridyl" means 2-, 25 3- or 4-pyridyl, "thienyl" means 2- or 3-thienyl, and hereinafter the same. The "aforementioned carbon" in the "aforementioned carbon may be independently mono-, di- or tri-substituted by halo, the aforementioned carbon may be mono-substituted 30 by hydroxy, the aforementioned carbon may be mono substituted by oxo" in the formula (IV) refers to each carbon containing a connecting carbon in the carbon chain. The "nitrogen may be ... di-substituted by oxo" in the formula (IV) refers to the terminal nitrogen 35 constituting the nitro functional group. The expression 247 C **o*'''V'p"'""'"' of AU200820o550 (cang s rckd).i c "a pharmaceutically acceptable salt" in the formula (IV) means, but not limited to, non-toxic anion salts including anion such as chloride, bromide, iodide, sulfate, hydrogen sulfate, phosphate, acetate, maleate, fumarate, oxalate, 5 lactate, tartrate, citrate, gluconate, methanesulfonate and 4-toluene-sulfonate. This expression also means, but not limited to, non-toxic cation salts such as sodium, potassium, calcium, magnesium, ammonia or protonated benzathine (N,N'-dibenzylethylenediamine), choline, 10 ethanolamine, diethanolamine, ethylenediamine, meglamine (N-methyl-glucamine), benethamine (N-benzylphenethylamine), piperazine and tromethamine (2-amino-2-hydroxymethyl-1,3 propanediol). Specifically, the compound disclosed in JP-A-2000 15 191645 can be mentioned: a compound of the formula (V) 0

R

3

R

5 N OR 4 6 4 (V)

R

7

CH

3

R

8 R wherein Ri is a hydrogen, Y, W-X or W-Y; 20 wherein W is carbonyl, thiocarbonyl, sulfinyl or sulfonyl; X is -O-Y, -S-Y, -N (H) -Y or -N- (Y) 2; Y for each bond is independently Z or a fully saturated, partially unsaturated or fully 25 unsaturated 1- to 10-membered straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with 1 or 2 heteroatoms selected from oxygen, sulfur and nitrogen as desired, the aforementioned carbon is 248 C Vpof dVSpecfication of AU2008201550 changess tracked)doc independently mono-substituted, di-substituted or tri-substituted by halogen as desired, the aforementioned carbon is mono-substituted by hydroxy as desired, the aforementioned carbon is 5 mono-substituted by oxo as desired, the aforementioned sulfur is mono-substituted or di substituted by oxo as desired, the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain 10 is mono-substituted by Z as desired; wherein Z is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, or a bicyclic ring 15 consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, to have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen as desired; the aforementioned Z 20 substituent is independently mono-substituted, di substituted or tri-substituted as desired by halogen, (C 2

-C

6 )alkenyl, (Ci-C 6 )alkyl, hydroxy, (Ci

C

6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxyl, (Ci-C 6 )alkyloxycarbonyl, mono-N-(Ci 25 C 6 )alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (Ci-C 6 )alkyl substituent is independently mono-substituted, di-substituted or tri-substituted as desired by halogen, hydroxy,

(C

1

-C

6 ) alkoxy, (C 1

-C

4 ) alkylthio, amino, nitro, cyano, 30 oxo, carboxyl, (C 1

-C

6 )alkyloxycarbonyl, mono-N-(Ci

C

6 )alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (C 1

-C

6 )alkyl substituent is further substituted by 1 to 9 fluorines as desired; R3 is a hydrogen or Q; wherein Q is a fully saturated, 35 partially unsaturated or fully unsaturated 1- to 6 2 4 9 C'po"fV' ''dVSpodf'" of AU20082o1550 (chang s t,ckod).doc membered straight chain or branched carbon chain wherein the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen as desired, the 5 aforementioned carbon is independently mono substituted, di-substituted or tri-substituted by halogen as desired, the aforementioned carbon is mono-substituted by hydroxy as desired, the aforementioned carbon is mono-substituted by oxo as 10 desired, the aforementioned sulfur is mono substituted or di-substituted by oxo as desired, the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono-substituted by 15 V as desired; wherein V is a partially saturated, fully saturated or fully unsaturated 3- to 8-membered ring having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, or a bicyclic ring 20 consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken independently, to have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen as desired; the aforementioned V 25 substituent is independently mono-substituted, di substituted, tri-substituted or tetra-substituted as desired by halogen, (C 1

-C

6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Ci-C 6 )alkoxy, (C 1

-C

4 )alkylthio, amino, nitro, cyano, oxo, carbamoyl, mono-N-(Ci 30 C 6 )alkylcarbamoyl, di-N,N-(C 1

-C

6 )alkylcarbamoyl, carboxyl, (Ci-C 6 )alkyloxycarbonyl, mono-N-(Cl

C

6 )alkylamino or di-N,N-(C 1

-C

6 )alkylamino, the aforementioned (C 1

-C

6 )alkyl substituent or (C 2 C6)alkenyl substituent is independently mono 35 substituted, di-substituted or tri-substituted as 250 C*'of'''Sp fct"on of AU200201550 changess 'ackd)D c desired by hydroxy, (Ci-C 6 )alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxyl, (Ci

C

6 )alkyloxycarbonyl, mono-N-(Ci-C 6 )alkylamino or di N,N-(Ci-C 6 )alkylamino, the aforementioned (Ci 5 C 6 )alkyl substituent or (C 2

-C

6 )alkenyl substituent is further substituted by 1 to 9 fluorines as desired;

R

4 is Q1 or V'; wherein Q1 is a fully saturated, partially unsaturated or fully unsaturated 1- to 6 10 membered straight chain or branched carbon chain, wherein the carbons other than a connecting carbons may be replaced with one heteroatom selected from oxygen, sulfur and nitrogen as desired, the aforementioned carbon is independently mono 15 substituted, di-substituted or tri-substituted by halogen as desired, the aforementioned carbon is mono-substituted by hydroxy as desired, the aforementioned carbon is mono-substituted by oxo as desired, the aforementioned sulfur is mono 20 substituted or di-substituted by oxo as desired, the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono-substituted by V' as desired; wherein V1 is a partially saturated, 25 fully saturated or fully unsaturated 3- to 6 membered ring having, as desired, 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen; the aforementioned V 1 substituent is independently mono-substituted, di 30 substituted, tri-substituted or tetra-substituted as desired by halogen, (Ci-C 6 )alkyl, (CI-C 6 )alkoxy, amino, nitro, cyano, (Ci-C 6 )alkyloxycarbonyl, mono N-(Ci-C 6 )alkylamino or di-N,N-(Ci-C 6 )alkylamino, the aforementioned (Ci-C 6 )alkyl substituent is mono 35 substituted as desired by oxo, and the 251 C'V' 'rd'Sp'ci'tIon"of'AU 20012O5so (eangeostracked),doc aforementioned (Ci-C 6 )alkyl substituent is further substituted by 1 to 9 fluorines as desired; R 3 should contain V or R 4 should contain V'; and R , R , R 7 , and R 8 5 are each independently hydrogen, hydroxy or oxy, wherein the aforementioned oxy is substituted by T or a partially saturated, fully saturated or fully unsaturated 1- to 12-membered straight chain or branched carbon chain, the carbons other than a 10 connecting carbons may be replaced with 1 or 2 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, the aforementioned carbon is independently mono-substituted, di substituted or tri-substituted by halogen as 15 desired, the aforementioned carbon is mono substituted by hydroxy as desired, the aforementioned carbon is mono-substituted by oxo as desired, the aforementioned sulfur is mono substituted or di-substituted by oxo as desired, 20 the aforementioned nitrogen is mono-substituted or di-substituted by oxo as desired, and the aforementioned carbon chain is mono-substituted as desired by T; wherein T is a partially saturated, fully saturated or fully unsaturated 3- to 8 25 membered ring having 1 to 4 heteroatoms independently selected from oxygen, sulfur and nitrogen as desired, or a bicyclic ring consisting of two fused partially saturated, fully saturated or fully unsaturated 3- to 6-membered rings, taken 30 independently, to have 1 to 4 heteroatoms independently selected from nitrogen, sulfur and oxygen as desired; the aforementioned T substituent is independently mono-substituted, di-substituted or tri-substituted as desired by halogen, (Ci 35 C 6 )alkyl, (C 2

-C

6 )alkenyl, hydroxy, (Ci-C 6 )alkoxy, 252 CVpo *"dVSp'c"i'o of AU20082O1550 (ng. trced).doc (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci-C)alkyloxycarbonyl, mono-N-(Ci-C 6 )alkylamino or di-N,N-(Ci-C 6 )alkylamino, the aforementioned (Ci C6)alkyl substituent is independently mono 5 substituted, di-substituted or tri-substituted as desired by hydroxy, (Cl-CE)alkoxy, (Ci-C 4 )alkylthio, amino, nitro, cyano, oxo, carboxy, (Ci C6) alkyloxycarbonyl, mono-N- (Cl-C6) alkylamino or di N,N-(Ci-C)alkylamino, and the aforementioned (Ci 10 Cd)alkyl substituent is further substituted as desired by 1 to 9 fluorines, a prodrug thereof, a pharmaceutically acceptable salt of the compound or a pharmaceutically acceptable salt of the prodrug. 15 The "prodrug" of the formula (V) refers to a compound which is a drug precursor that releases a drug in vivo via some specific chemical or physiological process after administration (e.g., prodrug is converted to a desired drug form by achieving a physiological pH or by an 20 enzyme action). A typicalprodrug produces a corresponding free acid upon cleavage and the residue forming such hydrolytic ester of the compound of the formula (V) includes, but not limited to, a residue having a carboxyl moiety, in which a free hydrogen is substituted by the 25 following groups: (CI-C4) alkyl, (C 2

-C

7 ) alkanoyloxymethyl, 1-(alkanoyloxy)ethyl having 4 to 9 carbon atoms, 1-methyl 1-(alkanoyloxy)ethyl having 5 to 10 carbon atoms, alkoxycarbonyloxymethyl having 3 to 6 carbon atoms, 1 (alkoxycarbonyloxy)ethyl having 4 to 7 carbon atoms, 1 30 methyl-1-(alkoxycarbonyloxy)ethyl having 5 to 8 carbon atoms, N-(alkoxycarbonyl)aminomethyl having 3 to 9 carbon atoms, 1-(N-(alkoxycarbonyl)amino)ethyl having 4 to 10 carbon atoms, 3-phthalidyl, 4-crotonolactonyl, y butyrolacton-4-yl, di-N,N-(Ci-C 2 )alkylamino(C 2

-C

3 )alkyl 35 (e.g., B-dimethylaminoethyl), carbamoyl-(Ci-C 2 )alkyl, N,N 253 C *pof''""SP"c"fic"'n of AU2008201SO (chang.. tr.ckd).ioc di(C 1

-C

2 )alkylcarbamoyl-(C 1

-C

2 )alkyl, piperidino(C 2

-C

3 alkyl), pyrrolidino(C 2

-C

3 )alkyl or morpholino(C 2

-C

3 )alkyl. The following paragraphs describe representative rings relative to the general ring names contained in the 5 formula (V). Examples of the representative 5- or 6-membered aromatic ring in the formula (V), which has 1 or 2 heteroatoms as desired, which are independently selected from oxygen, nitrogen and sulfur, include phenyl, furyl, 10 thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridiazinyl, pyrimidinyl, pyrazinyl and the like. Representative examples of the partially saturated, fully saturated or fully unsaturated 5- to 8-membered ring 15 in the formula (V), which has 1 to 4 heteroatoms, which are independently selected from oxygen, sulfur and nitrogen, include cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, phenyl and the like. Further examples of the representative 5-membered ring in the formula (V) include 20 the following: 2H-pyrrolyl, 3H-pyrrolyl, 2-pyrrolinyl, 3 pyrrolinyl, pyrrolidinyl, 1,3-dioxolanyl, oxazolyl, thiazolyl, imidazolyl, 2H-imidazolyl, 2-imidazolinyl, imidazolidinyl, pyrazolyl, 2-pyrazolinyl, pyrazolidinyl, isoxazolyl, isothiazolyl, 1,2-dithiolyl, 1,3-dithiolyl, 25 3H-1,2-oxathiolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,3,4-thiadiazolyl, 1,2,3,4-oxatriazolyl, 1,2,3,5-oxatriazolyl, 3H-1,2,3-dioxazolyl, 1,2,4 dioxazolyl, 1,3,2-dioxazolyl, 1,3,4-dioxazolyl, 5H-1,2,5 30 oxathiazolyl, 1,3-oxathiolyl and the like. Further examples of representative 6-membered ring in the formula (V) include the following: 2H-pyranyl, 4H pyranyl, pyridinyl, piperidinyl, 1,2-dioxinyl, 1,3 dioxinyl, 1,4-dioxanyl, morpholinyl, 1,4-dithianyl, 35 thiomorpholinyl, pyridazinyl, pyrimidinyl, pyrazinyl, 254 C:pf~Opd~to fA2OB050(hnmtakd.o piperazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,3 triazinyl, 1,3,5-trithianyl, 4H-1,2-oxazinyl, 2H-1,3 oxazinyl, 6H-1,3-oxazinyl, 6H-1,2-oxazinyl, 1,4-oxazinyl, 2H-1,2-oxazinyl, 4H-1,4-oxazinyl, 1,2,5-oxathiazinyl, 1,4 5 oxazinyl, o-isoxadinyl, p-isoxadinyl, 1,2,5-oxathiazinyl, 1,2,6-oxathiazinyl, 1,4,2-oxadiazinyl, 1,3,5,2-oxadiazinyl and the like. Further examples of the representative 7-membered ring in the formula (V) include azepinyl, oxepinyl, 10 thiepinyl and the like. Further examples of the representative 8-membered ring in the formula (V) include cyclooctyl, cyclooctenyl, cyclooctadienyl and the like. Examples of the representative bicyclic ring in the formula (V), consisting of two fused partially saturated, 15 fully saturated or fully unsaturated 5- or 6-membered rings, taken independently, optionally having 1 to 4 heteroatoms as desired, which are independently selected from nitrogen, sulfur and oxygen, include the following: indolizinyl, indolyl, isoindolyl, 3H-indolyl, 1H 20 isoindolyl, indolinyl, cyclopenta(b)pyridinyl, pyrano(3,4 b)pyrrolyl, benzofuryl, isobenzofuryl, benzo(b)thienyl, benzo(c)thienyl, 1H-indazolyl, indoxazinyl, benzoxazolyl, benzimidazolyl, benzothiazolyl, purinyl, 4H-quinolizinyl, quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, 25 quinazolinyl, quinoxalinyl, 1,8-naphthyridinyl, pteridinyl, indenyl, isoindenyl, naphthyl, tetralinyl, decalinyl, 2H 1-benzopyranyl, pyrido(3,4-b)-pyridinyl, pyrido(3,2-b) pyridinyl, pyrido(4,3-b)-pyridinyl, 2H-1,3-benzoxazinyl, 2H-1,4-benzoxazinyl, 1H-2,3-benzoxazinyl, 4H-3,1 30 benzoxazinyl, 2H-1,2-benzoxazinyl, 4H-1,4-benzoxazinyl and the like. The alkylene in the formula (V) means a saturated hydrocarbon (straight chain or branched chain) wherein hydrogen atom has been removed from each terminal carbon. 35 Examples of such group include (assuming that the 2 55 C""po"' ''Sp' 'V'o' ' of AU2o2315o (c .gs Ircod) doc designated length encompasses specific examples) methylene, ethylene, propylene, butylene, pentylene, hexylene and heptylene. The halo in the formula (V) means chloro, bromo, 5 iodo or fluoro. The alkyl in the formula (V) means a saturated straight chain hydrocarbon or a saturated branched chain hydrocarbon. Examples of such alkyl group (assuming that the designated length encompasses specific examples) include methyl, ethyl, propyl, isopropyl, butyl, 10 sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, hexyl, isohexyl, heptyl and octyl. The alkoxy in the formula (V) means a saturated straight chain alkyl or a saturated branched chain alkyl 15 bonded via oxy. Examples of such alkoxy group (assuming that the designated length encompasses specific examples) include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, pentoxy, isopentoxy, neopentoxy, tert-pentoxy, hexoxy, isohexoxy, heptoxy and octoxy. 20 The terms mono-N- and di-N,N-(Ci-Cx)alkyl ... used for the formula (V) refer to (Ci-Cx)alkyl moiety taken independently, when it is di-N,N-(Ci-Cx)alkyl ... (x means an integer). It should be appreciated that, in the formula (V), 25 when a carbon ring moiety or heterocyclic moiety is bonded or attached to a designated substrate via a different ring atom, without indicating a specific binding site, any point with such possibility is intended, whether via a carbon atom, or via, for example, a trivalent nitrogen 30 atom. For example, the term "pyridyl" means 2-, 3- or 4 pyridyl, "thienyl" means 2-, or 3-thienyl, and the like. The "aforementioned carbon" in the "aforementioned carbon is independently mono-substituted, di-substituted or tri-substituted as desired by halogen, the 35 aforementioned carbon is mono-substituted as desired by 256 C 'p"'"""''pa'''''''''""*'^2008201 5 e(hne. track.doc hydroxy, the aforementioned carbon is mono-substituted as desired by oxo" in the formula (V) refers to each carbon in the carbon chain containing binding carbons. The "nitrogen di-substituted by oxo" in the formula 5 (V) refers to the terminal nitrogen constituting the nitro functionality. The expression, "a pharmaceutically acceptable salt" in the formula (V) means, but not limited to, non-toxic anion salts including anion, such as chloride ion, bromide ion, iodide ion, sulfate ion, 10 hydrogen sulfate ion, phosphate ion, acetate ion, maleate ion, fumarate ion, oxalate ion, lactate ion, tartrate ion, citrate ion, gluconate ion, methanesulfonate ion and 4 toluene-sulfonate ion. This expression also means, but not limited to, non-toxic cation salts including cation, 15 such as sodium ion, potassium ion, calcium ion, magnesium ion, ammonium or protonated benzathine (N,N' dibenzylethylenediamine), choline, ethanolamine, diethanolamine, ethylenediamine, meglamine (N-methyl glucamine), benethamine (N-benzylphenethylamine), 20 piperazine and tromethamine (2-amino-2-hydroxymethyl-1,3 propanediol). Specifically, the compound disclosed in W098/35937 and JP-A-Hll-49743 can be mentioned: a compound represented by the formula (VII) R-YN X1 ,-~ NZ X2: X4 25 3 wherein R is a straight chain or branched C1-1 0 alkyl group, a straight chain or branched C 2

-

10 alkenyl group, a halogenated C 1 4 lower alkyl group, an optionally 30 substituted C 3

-

10 cycloalkyl group, an optionally substituted C 5

-

8 cycloalkenyl group, an optionally 257 C*pof' 'd'S' ''f on of AU2008201550 (cang. racked).oc substituted C3- 10 cycloalkyl C1- 10 alkyl group, an optionally substituted aryl group, an optionally substituted aralkyl group or an optionally substituted 5- or 6-membered heterocyclic group 5 having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom;

X

1 , X 2 , X 3 and X 4 are the same or different and each is a hydrogen atom, a halogen atom, a C 1

-

4 lower alkyl group, a 10 halogenated C 1

-

4 lower alkyl group, a C 1

-

4 lower alkoxy group, a cyano group, a nitro group, an acyl group or an aryl group; Y is -CO- or -SO 2 -; and Z is a hydrogen atom or a mercapto protecting group, 15 a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. The "straight chain or branched C 1

-

10 alkyl group" in the formula (VII) means a straight chain or branched alkyl group having 1 to 10 carbon atoms, which is specifically 20 methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, sec-butyl group, tert-butyl group, pentyl group, isopentyl group, neopentyl group, tert-pentyl group, 1-ethylbutyl group, 2-ethylbutyl group, 1-propylbutyl group, 1,1-dimethylbutyl group, 1-isobutyl 25 3-methylbutyl group, 1-ethylpentyl group, 1-propylpentyl group, 1-isobutylpentyl group, 2-ethylpentyl group, 2 isopropylpentyl group, 2-tert-butylpentyl group, 3 ethylpentyl group, 3-isopropylpentyl group, 4-methylpentyl group, 1,4-dimethylpentyl group, 2,4-dimethylpentyl group, 30 1-ethyl-4-methylpentyl group, hexyl group, 1-ethylhexyl group, 1-propylhexyl group, 2-ethylhexyl group, 2 isopropylhexyl group, 2-tert-butylhexyl group, 3 ethylhexyl group, 3-isopropylhexyl group, 3-tert butylhexyl group, 4-ethylhexyl group, 5-methylhexyl group, 35 heptyl group, 1-ethylheptyl group, 1-isopropylheptyl group, 2 5 8 C'po'vrdVSp'd'c" 'o" of AU200820 10 ( wgOe t.r~ex.Asc e 2-ethylheptyl group, 2-isopropylheptyl group, 3 propylheptyl group, 4-propylheptyl group, 5-ethylheptyl group, 6-methylheptyl group, octyl group, 1-ethyloctyl group, 2-ethyloctyl group, nonyl group, 1-methylnonyl 5 group, 2-methylnonyl group, decyl group and the like, with preference given to a straight chain or branched alkyl group having 1 to 8 carbon atoms. The "C1-4 lower alkyl group" in the formula (VII) means a straight chain or branched alkyl group having 1 to 10 4 carbon atoms, which is specifically methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, sec-butyl group, tert-butyl group and the like. The "straight chain or branched C 2

-

1 o alkenyl group" 15 in the formula (VII) means a straight chain or branched alkenyl group having 2 to 10 carbon atoms and at least one double bond, which is specifically allyl group, vinyl group, isopropenyl group, 1-propenyl group, 1-methyl-2 propenyl group, 2-methyl-2-propenyl group, 1-methyl-l 20 butenyl group, crotyl group, 1-methyl-3-butenyl group, 3 methyl-2-butenyl group, 1,3-dimethyl-2-butenyl group, 1 pentenyl group, 1-methyl-2-pentenyl group, 1-ethyl-3 pentenyl group, 4-pentenyl group, 1,3-pentadienyl group, 2,4-pentadienyl group, 1-hexenyl group, 1-methyl-2-hexenyl 25 group, 3-hexenyl group, 4-hexenyl group, 1-butyl-5-hexenyl group, 1,3-hexadienyl group, 2,4-hexadienyl group, 1 heptenyl group, 2-heptenyl group, 3-heptenyl group, 4 heptenyl group, 5-heptenyl group, 6-heptenyl group, 1,3 heptadienyl group, 2,4-heptadienyl group, 1-octenyl group, 30 2-octenyl group, 3-octenyl group, 4-octenyl group, 5 octenyl group, 6-octenyl group, 7-octenyl group, 1-nonenyl group, 2-nonenyl group, 3-nonenyl group, 4-nonenyl group, 5-nonenyl group, 6-nonenyl group, 7-nonenyl group, 8 nonenyl group, 9-decenyl group and the like, with 35 preference given to a straight chain or branched alkenyl 259 C.WoordS pasfIcabon of AU200820155o Chs .. ,ck.ioc group having 2 to 8 carbon atoms. The "halogen atom" in the formula (VII) means fluorine atom, chlorine atom, bromine atom and the like. The "halogenated Ci4 alkyl group" in the formula 5 (VII) means the aforementioned Ci-4 lower alkyl group substituted by 1 to 3 the same or different halogen atoms, which is specifically fluoromethyl group, chloromethyl group, bromomethyl group, difluoromethyl group, dichloromethyl group, trifluoromethyl group, 10 trichloromethyl group, chloroethyl group, difluoroethyl group, trifluoroethyl group, pentachloroethyl group, bromopropyl group, dichloropropyl group, trifluorobutyl group and the like, with preference given to trifluoromethyl group and chloroethyl group. 15 The "C-4 lower alkoxy group" in the formula (VII) means an alkoxy group having the aforementioned Ci-4 lower alkyl group, which is specifically methoxy group, ethoxy group, propoxy group, isopropoxy group, butoxy group, isobutoxy group, sec-butoxy group, tert-butoxy group and 20 the like. The "C4 lower alkylthio group" in the formula (VII) means an alkylthio group having the aforementioned C1-4 lower alkyl group, which is specifically methylthio group, ethylthio group, propylthio group, isopropylthio group, 25 butylthio group, isobutylthio group, sec-butylthio group, tert-butylthio group and the like. The "C3-10 cycloalkyl group" in the formula (VII) means a monocyclic or polycyclic cycloalkyl group having 3 to 10 carbon atoms, which is specifically cyclopropyl 30 group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclooctyl group, octahydroindenyl group, decahydronaphthyl group, bicyclo[2.2.1]heptyl group, adamantyl group and the like, with preference given to cyclopentyl group, cyclohexyl 35 group and cycloheptyl group, each of which having 5 to 7 2 6 0 Cpf'dSp f''o" of AU20082oSSO (ca.ng. trackd).doc carbon atoms. The "C 5

-

8 cycloalkenyl group" in the formula (VII) means a cycloalkenyl group having 5 to 8 carbon atoms and one or more double bonds on the ring, which is 5 specifically cyclopentenyl group, cyclohexenyl group, cycloheptenyl group, cyclooctenyl group, cyclopentadienyl group, cyclohexadienyl group, cycloheptadienyl group, cyclooctadienyl group and the like, with preference given to cyclopentenyl group, cyclohexenyl group and 20 cycloheptenyl group, each of which having 5 to 7 carbon atoms. The "C 3 10 cycloalkyl Ci-1o alkyl group" in the formula (VII) means the aforementioned straight chain or branched Ci- 10 alkyl group substituted by the aforementioned C 3

-

10 15 cycloalkyl group, which is specifically cyclopropylmethyl group, cyclopentylmethyl group, cyclohexylmethyl group, cyclohexylcyclopentylmethyl group, dicyclohexylmethyl group, 1-cyclopentylethyl group, 1-cyclohexylethyl group, 2-cyclopropylethyl group, 2-cyclopentylethyl group, 2 20 cyclohexylethyl group, 2-cycloheptylethyl group, 1 cyclohexyl-1-methylethyl group, 1-cyclohexylpropyl group, 2-cyclopentylpropyl group, 3-cyclobutylpropyl group, 3 cyclopentylpropyl group, 3-cyclohexylpropyl group, 3 cycloheptylpropyl group, 1-cyclopropyl-l-methylpropyl 25 group, 1-cyclohexyl-2-methylpropyl group, 1 cyclopentylbutyl group, 1-cyclohexylbutyl group, 3 cyclohexylbutyl group, 4-cyclopropylbutyl group, 4 cyclobutylbutyl group, 4-cyclopentylbutyl group, 1 cyclohexyl-1-methylbutyl group, 1-cyclopentyl-2-ethylbutyl 30 group, 1-cyclohexyl-3-methylbutyl group, 1 cyclopentylpentyl group, 1-cyclohexylpentyl group, 1 cyclohexylmethylpentyl group, 2-cyclohexylpentyl group, 2 cyclohexylmethylpentyl group, 3-cyclopentylpentyl group, 1-cyclohexyl-4-methylpentyl group, 5-cyclopentylpentyl 35 group, 1-cyclopentylhexyl group, 1-cyclohexylhexyl group, 2 61 C po 'rd"S"'c' ' tIo' ' of AU2008201S50 (c.fg. tracked)doc 1-cyclopentylmethylhexyl group, 2-cyclopentylhexyl group, 2-cyclopropylethylhexyl group, 3-cyclopentylhexyl group, 1-cyclohexylheptyl group, 1-cyclopentyl-l-methylheptyl group, 1-cyclohexyl-1,6-dimethylheptyl group, 1 5 cycloheptyloctyl group, 2-cyclopentyloctyl group, 3 cyclohexyloctyl group, 2-cyclopentylmethyloctyl group, 1 cyclopentylnonyl group, 1-cyclohexylnonyl group, 3 cyclopropylnonyl group, 1-cyclopentyldecyl group, 1 cyclohexylundecyl group, 1-cyclopentyltridecyl group, 2 10 cyclohexyltridecyl group and the like. The "aryl group" in the formula (VII) means phenyl group, naphthyl group, anthryl group, phenanthryl group, biphenyl group and the like, with preference given to phenyl group, naphthyl group and biphenyl group. 15 The "aralkyl group" in the formula (VII) means the aforementioned C1-4 lower alkyl group substituted by one or more the aforementioned aryl groups, which is specifically benzyl group, benzhydryl group, trityl group, phenethyl group, 3-phenylpropyl group, 2-phenylpropyl group, 4 20 phenylbutyl group, naphthylmethyl group, 2-naphthylethyl group, 4-biphenylmethyl group, 3-(4-biphenyl)propyl group and the like. The "arylalkenyl group" in the formula (VII) means alkenyl group having 2 to 4 carbon atoms substituted by 25 the aforementioned aryl group, which is specifically 2 phenylvinyl group, 3-phenyl-2-propenyl group, 3-phenyl-2 methyl-2-propenyl group, 4-phenyl-3-butenyl group, 2-(l naphthyl)vinyl group, 2-(2-naphthyl)vinyl group, 2-(4 biphenyl)vinyl group and the like. 30 The "arylthio group" in the formula (VII) means arylthio group having the aforementioned aryl group, which is specifically phenylthio group, naphthylthio group and the like. The "heterocyclic group" in the formula (VII) means 35 a 5- or 6-membered aromatic or nonaromatic heterocyclic 262 C* o e' f''' ' '*" U20o8201550 (hengeotrcka.doc group having one or more, specifically 1 to 4, preferably 1 to 3, heteroatoms selected from nitrogen atom, oxygen atom and sulfur atom, which is specifically aromatic heterocyclic groups such as thiatriazolyl group, 5 tetrazolyl group, dithiazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, oxazolyl group, pyrazolyl group, pyrrolyl group, furyl group, thienyl group, tetrazinyl group, triazinyl group, pyrazinyl group, pyridazinyl group, pyrimidinyl group, pyridyl group and 10 the like and nonaromatic heterocyclic groups such as dioxolanyl group, pyrrolidinyl group, tetrahydrofuryl group, tetrahydrothienyl group, dithiadiazinyl group, thiadiazinyl group, morpholino group, morpholinyl group, oxazinyl group, thiazinyl group, piperazinyl group, 15 piperidyl group, piperidino group, pyranyl group, thiopyranyl group and the like. Preferred are an aromatic heterocyclic (heteroaryl) group such as furyl group, thienyl group, pyrrolyl group, pyridyl group and the like and a nonaromatic heterocyclic group having at least one 20 nitrogen atom, such as pyrrolidinyl group, tetrahydrofuryl group, piperazinyl group, piperidyl group, piperidino group and the like. The "heteroarylalkyl group" in the formula (VII) means the aforementioned C1-4 lower alkyl substituted by 25 the above-mentioned 5- or 6-membered aromatic heterocyclic (heteroaryl) group, which is specifically 2-thienylmethyl group, 2-furylmethyl group, 2-pyridylmethyl group, 3 pyridylmethyl group, 2-thienyl-2-ethyl group, 3-furyl-1 ethyl group, 2-pyridyl-3-propyl group and the like. 30 The "acyl group" in the formula (VII) specifically means formyl group, acetyl group, propionyl group, butyryl group, isobutyryl group, valeryl group, isovaleryl group, pivaloyl group, hexanoyl group, acryloyl group, propioloyl group, metacryloyl group, crotonoyl group, benzoyl group, 35 naphthoyl group, toluoyl group, hydroatropoyl group, 2 63 C'pordSpfcio of AU20s2O155o (change.o..rkei.dic atropoyl group, cinnamoyl group, furoyl group, thenoyl group, nicotinoyl group, isonicotinoyl group, glycoloyl group, lactoyl group, glyceroyl group, tropoyl group, benziloyl group, salicyloyl group, anisoyl group, 5 vanilloyl group, veratroyl group, piperonyloyl group, protocatechuoyl group, galloyl group, cyclopentanecarbonyl group, cyclohexanecarbonyl group, cycloheptanecarbonyl group, 1-methylcyclohexanecarbonyl group, 1 isopentylcyclopentanecarbonyl group, 1 10 isopentylcyclohexanecarbonyl group, tert-butoxycarbonyl group, methoxycarbonyl group, ethoxycarbonyl group, 2-(l isopentylcyclohexanecarbonylamino)phenylthiocarbonyl group and the like. Preferred are acetyl group, tert butoxycarbonyl group, benzoyl group, 1 15 methylcyclohexanecarbonyl group, 1 isopentylcyclopentanecarbonyl group, 1 isopentylcyclohexanecarbonyl group and 2-(l isopentylcyclohexanecarbonylamino)phenylthiocarbonyl group. In the formula (VII), the "optionally substituted" 20 of the "optionally substituted C3-10 cycloalkyl group", "optionally substituted C5-8 cycloalkenyl group" and "optionally substituted C3-10 cycloalkyl C1-10 alkyl group" for R and the like means being optionally substituted by 1 to 4 substituents. The substituent may be the same or 25 different and the position of substituent is optional and free of any particular limitation. Specifically, the aforementioned straight chain or branched Ci-1o alkyl group; the aforementioned straight chain or branched C2-10 alkenyl group; the aforementioned C3-10 cycloalkyl group; 30 the aforementioned C5-8 cycloalkenyl group; the aforementioned C3-10 cycloalkyl C1-10 alkyl group; the aforementioned aryl group; amino group; C1-4 lower alkylamino group such as methylamino group, ethylamino group and the like; acylamino group such as acetylamino 35 group, propionylamino group, benzylamino group and the 2 64 C:'pof ''rdSp ''"t1on of AU2 201550 (cange. tracked)doc like; oxo group; the aforementioned aralkyl group; the aforementioned arylalkenyl group and the like can be mentioned. The above substituents are recommended mainly as the substituent for R. 5 In the formula (VII), the "optionally substituted" of the "optionally substituted aryl group", "optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom" and "optionally substituted aralkyl group" for R and the like 10 means being optionally substituted by 1 to 4, preferably 1 to 3, substituents. The substituent may be the same or different and the position of substituent is optional and free of any particular limitation. Specifically, the aforementioned straight chain or branched CI-10 alkyl group, 15 preferably straight chain or branched C1-6 alkyl group; the aforementioned straight chain or branched C2- 10 alkenyl group, preferably straight chain or branched C2-6 alkenyl group; the aforementioned halogen atom; nitro group; the aforementioned C1-4 lower alkyl group or amino group 20 optionally substituted by the aforementioned acyl group; hydroxyl group; the aforementioned Ci-4 lower alkoxy group; the aforementioned C1-4 lower alkylthio group; the aforementioned halogenated C1-4 lower alkyl group; the aforementioned acyl group; oxo group and the like can be 25 mentioned. Of these, the aforementioned straight chain or branched C1-6 alkyl group, the aforementioned halogen atom, and nitro group are particularly preferable. In the formula (VII), the "mercapto-protecting group" for Z means a conventionally used mercapto 30 protecting group, and is free of any particular limitation as long as it is an organic residue liberated in living organisms. It may also form a disulfide form, which is a dimer. Specifically, those such as the following C1-4 lower alkoxymethyl group; C1-4 lower alkylthiomethyl group; 35 aralkyloxymethyl group; aralkylthiomethyl group; C310 2 65 C'pof 'rd'SpocJf'ca'on of AU20082o5o (eang.s tracked).doc cycloalkyloxymethyl group; C5-8 cycloalkenyloxymethyl group; C3-10 cycloalkyl Ci-o alkoxymethyl group; aryloxymethyl group; arylthiomethyl group; acyl group; acyloxy group; aminocarbonyloxymethyl group; thiocarbonyl 5 group; and thio group can be mentioned. More specifically, C1-4 lower alkoxymethyl group having the aforementioned C1-4 lower alkoxy group; C1-4 lower alkylthiomethyl group having the aforementioned C1-4 lower alkylthio group; aralkyloxymethyl group having the aforementioned aralkyl 10 group; aralkylthiomethyl group having the aforementioned aralkyl group; C3-10 cycloalkyloxymethyl group having the aforementioned C3-10 cycloalkyl group; C-8 cycloalkenyloxymethyl group having the aforementioned C5-8 cycloalkenyl group; C3-10 cycloalkyl Cl-10 alkoxymethyl 15 group having the aforementioned C3-10 cycloalkyl Ci-io alkyl group; aryloxymethyl group having the aforementioned aryl group; arylthiomethyl group having the aforementioned arylthio group; acyl group having the aforementioned optionally substituted straight chain or branched Ci-10 20 alkyl group, the aforementioned halogenated C1-4 lower alkyl group, the aforementioned C1-4 lower alkoxy group, the aforementioned C1-4 lower alkylthio group, the aforementioned optionally substituted amino group, the aforementioned optionally substituted ureido group, the 25 aforementioned optionally substituted C3-10 cycloalkyl group, the aforementioned optionally substituted C3-10 cycloalkyl Ci-1o alkyl group, the aforementioned optionally substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally 30 substituted arylalkenyl group, the aforementioned optionally substituted arylthio group, the aforementioned optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6 35 membered heteroarylalkyl group; acyloxy group having the 266 C'V*'''''''''''''""* o"*AU200820155D (changes tracked).doc aforementioned optionally substituted straight chain or branched C1-10 alkyl group, the aforementioned halogenated Ci-4 lower alkyl group, the aforementioned C1-4 lower alkoxy group, the aforementioned C1-4 lower alkylthio group, the 5 aforementioned optionally substituted amino group, the aforementioned optionally substituted ureido group, the aforementioned optionally substituted C3-10 cycloalkyl group, the aforementioned optionally substituted C3-10 cycloalkyl Ci-1o alkyl group, the aforementioned optionally 10 substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally substituted arylalkenyl group, the aforementioned optionally substituted arylthio group, the aforementioned optionally substituted 5- or 6-membered heterocyclic group 15 having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6 membered heteroarylalkyl group; aminocarbonyloxymethyl group optionally substituted by the aforementioned optionally substituted straight chain or branched C1-10 20 alkyl group, the aforementioned halogenated Ci4 alkyl group, the aforementioned C1-4 lower alkoxy group, the aforementioned C1-4 lower alkylthio group, the aforementioned optionally substituted C3-10 cycloalkyl group, the aforementioned optionally substituted C3-10 25 cycloalkyl CI-10 alkyl group, the aforementioned optionally substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally substituted arylalkenyl group, the aforementioned optionally substituted 5- or 6-membered heterocyclic group 30 having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6 membered heteroarylalkyl group; thiocarbonyl group having the aforementioned optionally substituted straight chain or branched C1-10 alkyl group, the aforementioned 35 halogenated C1-4 lower alkyl group, the aforementioned C1-4 2 67 C"'''' '''d ''"icaton of AU2008201550 (chans tracked) doc lower alkoxy group, the aforementioned C1-4 lower alkylthio group, the aforementioned optionally substituted amino group, the aforementioned optionally substituted ureido group, the aforementioned optionally substituted C3-10 5 cycloalkyl group, the aforementioned optionally substituted C3-10 cycloalkyl C1-1o alkyl group, the aforementioned optionally substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally substituted arylalkenyl group, 10 the aforementioned optionally substituted arylthio group, the aforementioned optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6-membered heteroarylalkyl 15 group; and thio group having the aforementioned optionally substituted C1-4 lower alkyl group or aryl group can be mentioned. To be more concrete, as the "straight chain or branched C1-10 alkyl group" for R of the formula (VII), 20 methyl group, ethyl group, isopropyl group, butyl group, isobutyl group, tert-butyl group, heptyl group, 1 propylbutyl group and 1-isobutyl-3-methylbutyl group are preferable. As the "straight chain or branched C2-10 alkenyl 25 group" for R of the formula (VII), allyl group, vinyl group, isopropenyl group, 1-methyl-2-propenyl group, 2 methyl-2-propenyl group, 1-methyl-l-butenyl group, crotyl group, 1,3-dimethyl-2-butenyl group, 1-pentenyl group and 1-methyl-2-pentenyl group are preferable. 30 The "halogenated C1-4 lower alkyl group" for R of the formula (VII) means C1-4 lower alkyl group (particularly preferably methyl group) substituted by the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom), with preference given to trifluoromethyl 35 group. 268 C:VpofwordVSpecifIctfon of AU2008201550 (changes tracked) doc The "optionally substituted C 3 o 10 cycloalkyl group" for R of the formula (VII) is C3 1 0 cycloalkyl group (particularly preferably cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl 5 group, octahydroindenyl group, decahydronaphthyl group, adamantyl group, bicyclo[2.2.1]heptyl group) optionally substituted by 1 to 4 substituents selected from the aforementioned straight chain or branched CI-10 alkyl group (particularly preferably C1-8 alkyl group such as methyl 10 group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, tert-butyl group, pentyl group, isopentyl group, 2,2-dimethylpropyl group, 4-methylpentyl group, 2-ethylbutyl group etc.), the aforementioned straight chain or branched C2-10 alkenyl group 15 (particularly preferably C2-8 alkenyl group such as 1 methylvinyl group, 2-methylvinyl group, 3-methyl-3 propenyl group etc.), the aforementioned C3-10 cycloalkyl group (particularly preferably C7 cycloalkyl group such as cyclopropyl group, cyclopentyl group, cyclohexyl group 20 etc.), the aforementioned C5-8 cycloalkenyl group (particularly preferably C5-6 cycloalkenyl group such as cyclopentenyl group, cyclohexenyl group etc.), the aforementioned C3-10 cycloalkyl C1-10 alkyl group (particularly preferably C3-7 cycloalkyl C1-4 alkyl group 25 such as cyclopropylmethyl group, 2-cyclopropylethyl group, 2-cyclopentylethyl group, cyclohexylmethyl group, 2 cyclohexylethyl group etc.), the aforementioned aryl group (particularly preferably phenyl group), oxo group, the aforementioned aralkyl group (particularly preferably 30 phenyl C1-4 lower alkyl group such as benzyl group, phenethyl group etc.) and the aforementioned arylalkenyl group (particularly preferably 2-phenylvinyl group). Preferred are 2,2,3,3-tetramethylcyclopropyl group, 1 isopentylcyclobutyl group, 1-isopropylcyclopentyl group, 35 1-isobutylcyclopentyl group, 1-isopentylcyclopentyl group, 269 C:pofodVSpecification of AU2008201550 (dwanges tracked).doc 1-cyclohexylmethylcyclopentyl group, cyclohexyl group, 1 methylcyclohexyl group, 1-ethylcyclohexyl group, 1 propylcyclohexyl group, 1-isopropylcyclohexyl group, 1 butylcyclohexyl group, 1-isobutylcyclohexyl group, 1 5 pentylcyclohexyl group, 1-isopentylcyclohexyl group, 1 (2,2-dimethylpropyl)cyclohexyl group, 1-(4 methylpentyl)cyclohexyl group, 1-(2-ethylbutyl)cyclohexyl group, 4-tert-butyl-1-isopentylcyclohexyl group, 1 cyclopropylcyclohexyl group, 1-bicyclohexyl group, 1 10 phenylcyclohexyl group, 1-cyclopropylmethylcyclohexyl group, 1-cyclohexylmethylcyclohexyl group, 1-(2 cyclopropylethyl)cyclohexyl group, 1-(2 cyclopentylethyl)cyclohexyl group, 1-(2 cyclohexylethyl)cyclohexyl group, 4-methylcyclohexyl group, 15 4-propylcyclohexyl group, 4-isopropylcyclohexyl group, 4 tert-butylcyclohexyl group, 4-pentylcyclohexyl group, 4 bicyclohexyl group, 1-isopentylcycloheptyl group, 3a octahydroindenyl group, 4a-decahydronaphthyl group, 1 adamantyl group and 7,7-dimethyl-1-(2 20 oxo)bicyclo[2.2.1]heptyl group. While the position of substitution is not particularly limited, it is particularly preferably the 1-position. While the substituent may be any of the above-mentioned substituents, it is particularly preferably straight chain or branched 25 C1- 1 0 alkyl group. The substituent of the "optionally substituted C5-8 cycloalkenyl group" for R of the formula (VII) is completely the same as in the case of the aforementioned "optionally substituted C3-10 cycloalkyl group". Specific 30 examples thereof include cycloalkenyl group (particularly cyclopentenyl group, cyclohexenyl group) optionally substituted by 1 to 4 substituents selected from the aforementioned straight chain or branched CI-10 alkyl group (particularly preferably C1-8 alkyl group such as methyl 35 group, ethyl group, propyl group, isopropyl group, butyl 270 C'V"'''"'**"''' of AU20020O1550o (c... tr.cked) oc group, isobutyl group, pentyl group, isopentyl group, 2,2 dimethylpropyl group, 4-methylpentyl group etc.), the aforementioned straight chain or branched C2-10 alkenyl group (particularly preferably C2-8 alkenyl group such as 5 1-methylvinyl group, 2-methylvinyl group, 3-methyl-3 propenyl group etc.), the aforementioned C3-10 cycloalkyl group (particularly preferably C3-7 cycloalkyl group such as cyclopropyl group, cyclopentyl group, cyclohexyl group etc.), the aforementioned C 5

-

8 cycloalkenyl group 10 (particularly preferably C5-6 cycloalkenyl group such as cyclopentenyl group, cyclohexenyl group etc.), the aforementioned C3-10 cycloalkyl C1-10 alkyl group (particularly preferably C37 cycloalkyl C1-4 lower alkyl group such as cyclopropylmethyl group, 2-cyclopropylethyl 15 group, 2-cyclopentylethyl group, cyclohexylmethyl group, 2-cyclohexylethyl group etc.), the aforementioned aryl group (particularly preferably phenyl group), oxo group, the aforementioned aralkyl group (particularly preferably phenyl C1-4 lower alkyl group such as benzyl group, 20 phenethyl group etc.) and the aforementioned arylalkenyl group (particularly preferably 2-phenylvinyl group). Preferred are 1-isopropyl-2-cyclopentenyl group, 1 isopropyl-3-cyclopentenyl group, 1-isobutyl-2 cyclopentenyl group, 1-isobutyl-3-cyclopentenyl group, 1 25 isopentyl-2-cyclopentenyl group, 1-isopentyl-3 cyclopentenyl group, 1-cyclohexylmethyl-2-cyclopentenyl group, 1-cyclohexylmethyl-3-cyclopentenyl group, 1 cyclohexenyl group, 2-cyclohexenyl group, 3-cyclohexenyl group, 1-methyl-2-cyclohexenyl group, 1-methyl-3 30 cyclohexenyl group, 1-ethyl-2-cyclohexenyl group, 1-ethyl 3-cyclohexenyl group, 1-propyl-2-cyclohexenyl group, 1 propyl-3-cyclohexenyl group, 1-isopropyl-2-cyclohexenyl group, 1-isopropyl-3-cyclohexenyl group, 1-butyl-2 cyclohexenyl group, 1-butyl-3-cyclohexenyl group, 1 35 isobutyl-2-cyclohexenyl group, 1-isobutyl-3-cyclohexenyl 271 C "pof' 'VS'fl'"'Ion o AU2002 550 (c20 oes.goa.. e group, 1-pentyl-2-cyclohexenyl group, 1-pentyl-3 cyclohexenyl group, 1-isopentyl-2-cyclohexenyl group, 1 isopentyl-3-cyclohexenyl group, 1-(2,2-dimethylpropyl)-2 cyclohexenyl group, 1-(2,2-dimethylpropyl)-3-cyclohexenyl 5 group, 1-(4-methylpentyl)-2-cyclohexenyl group, 1-(4 methylpentyl)-3-cyclohexenyl group, 1-cyclopropyl-2 cyclohexenyl group, 1-cyclopropyl-3-cyclohexenyl group, 1 cyclohexyl-2-cyclohexenyl group, 1-cyclohexyl-3 cyclohexenyl group, 1-phenyl-2-cyclohexenyl group, 1 10 phenyl-3-cyclohexenyl group, 1-cyclopropylmethyl-2 cyclohexenyl group, 1-cyclopropylmethyl-3-cyclohexenyl group, 1-cyclohexylmethyl-2-cyclohexenyl group, 1 cyclohexylmethyl-3-cyclohexenyl group, 1-(2 cyclopropylethyl)-2-cyclohexenyl group, 1-(2 15 cyclopropylethyl)-3-cyclohexenyl group, 1-(2 cyclopentylethyl)-2-cyclohexenyl group, 1-(2 cyclopentylethyl)-3-cyclohexenyl group, 1-(2 cyclohexylethyl)-2-cyclohexenyl group and 1-(2 cyclohexylethyl)-3-cyclohexenyl group. While the position 20 of substitution is not particularly limited, it is particularly preferably the 1-position. While the substituent may be any of the above-mentioned substituents, it is particularly preferably straight chain or branched Cio alkyl group or C310 cycloalkyl C14 alkyl group. 25 The "optionally substituted C310 cycloalkyl Ci-1o alkyl group" for R of the formula (VII) means C3-10 cycloalkyl C1-1o alkyl group (particularly preferably cyclohexylmethyl group, 1-cyclohexylethyl group, 1 cyclohexyl-l-methylethyl group, 1-cyclohexyl-2 30 methylpropyl group, 1-cyclohexyl-3-methylbutyl group, 1 cyclohexylhexyl group, 1-cyclohexyl-4-methylpentyl group, 1-cyclohexylheptyl group) optionally substituted by 1 to 4 substituents selected from the aforementioned C3-10 cycloalkyl group (particularly preferably C37 cycloalkyl 35 group such as cyclopentyl group, cyclohexyl group etc.), 27 2 C'V"''**' ''''''''"" of AU2o82O155o changess tracke)oc the aforementioned C5-8 cycloalkenyl group (particularly preferably C57 cycloalkenyl group such as cyclopentenyl group and cyclohexenyl group) and the aforementioned aryl group (particularly preferably phenyl group), wherein Ci-1o 5 alkyl group is straight chain or branched. The position of substitution is not particularly limited, and the straight chain or branched C1-10 alkyl group moiety may have a substituent. Preferred are cyclohexylmethyl group, 1-cyclohexylethyl group, cyclohexylcyclopentylmethyl group, 10 dicyclohexylmethyl group, 1-cyclohexyl-l-methylethyl group, 1-cyclohexyl-2-methylpropyl group, 1-cyclohexyl-3 methylbutyl group, 1-cyclohexyl-4-methylpentyl group, 1 cyclohexylhexyl group and 1-cyclohexylheptyl group. The "optionally substituted aryl group" for R of the 15 formula (VII) means aryl group (particularly preferably phenyl group) optionally substituted by 1 to 4 substituents selected from the aforementioned straight chain or branched C1-6 alkyl group (particularly preferably tert-butyl group), the aforementioned halogen atom 20 (particularly preferably fluorine atom, chlorine atom) and nitro group. Preferred are phenyl group, 2-chlorophenyl group, 4-nitrophenyl group and 3,5-di-tert-butylphenyl group. The "optionally substituted aralkyl group" for R of 25 the formula (VII) means aralkyl group (particularly preferably benzyl group, benzhydryl group, trityl group) optionally substituted by the substituent selected from the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom), nitro group and hydroxyl 30 group, wherein the C1-4 lower alkyl group is straight chain or branched. The position of substitution is not particularly limited and the straight chain or branched C1-4 lower alkyl group moiety may have said substituent. Preferred are benzyl group and trityl group. 35 The "optionally substituted 5- or 6-membered 2 7 3 C po' ' *''SpocJf*ca*' n of AU200S2o1S5o changee tck.. , oc heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom" for R of the formula (VII) means the aforementioned heterocyclic group optionally substituted by 1 to 4 substituents selected from the 5 aforementioned straight chain or branched C 1

-

6 alkyl group (particularly preferably tert-butyl group), the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom) and nitro group, with preference given to aromatic heterocyclic group. 10 Particularly preferred are furyl group, thienyl group and pyridyl group. The "halogen atom" for X 1 , X 2 , X 3 , X 4 in the formula (VII) means halogen atom such as fluorine atom, chlorine atom, bromine atom and the like, with preference given to 15 fluorine atom and chlorine atom. The "C 1

-

4 lower alkyl group" for X 1 , X 2 , X 3 , X 4 in the formula (VII) is preferably methyl group. The "halogenated C 1 4 lower alkyl group" for X 1 , X 2 ,

X

3 , X 4 in the formula (VII) is C1-4 lower alkyl group 20 (particularly preferably methyl group) substituted by the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom), with preference given to trifluoromethyl group. The "Ci- 4 lower alkoxy group" for X 1 , X 2 , X 3 , X 4 in 25 the formula (VII) is preferably methoxy group. In the formula (VII), the "acyl group" for Xi, X 2 , X 3 ,

X

4 is preferably benzoyl group. In the formula (VII), the "aryl group" for X 1 , X 2 , X 3 ,

X

4 is preferably phenyl group. 30 The "prodrug compound" of the formula (VII) is a derivative of the compound of the formula (VII), which has a chemically or metabolically degradable group and shows pharmaceutical activity by hydrolysis or solvent decomposition, or by degradation under physiological 35 conditions. 2 74 C:pof1wdSpefCabof of AU2008201550 (chang.. traed).doc The "pharmaceutically acceptable salt" of the formula (VII) may be any as long as it forms a nontoxic salt with a compound represented by the above-mentioned formula (VII). For example, inorganic acid salts such as 5 hydrochloride, hydrobromide, hydroiodide, sulfate, nitrate, phosphate, carbonate, hydrogen carbonate, perchlorate etc.; organic acid salts such as formate, acetate, trifluoroacetate, propionate, oxalate, glycolate, succinate, lactate, maleate, hydroxymaleate, methylmaleate, 10 fumarate, adipate, tartrate, malate, citrate, benzoate, cinnamate, ascorbate, salicylate, 2-acetoxybenzoate, nicotinate, isonicotinate etc.; sulfonates such as methanesulfonate, ethanesulfonate, isethionate, benzenesulfonate, p-toluenesulfonate, naphthalenesulfonate 15 etc.; acidic amino acid salts such as aspartate, glutamate etc.; alkali metal salts such as sodium salt, potassium salt etc.; alkaline earth metal salts such as magnesium salt, calcium salt etc.; ammonium salt; organic base salts such as trimethylamine salt, triethylamine salt, pyridine 20 salt, picoline salt, dicyclohexylamine salt, N,N' dibenzylethylenediamine salt etc.; and amino acid salts such as lysin salt, arginine salt etc. can be mentioned. In some cases, it may be a hydrate or a solvate with alcohol and the like. 25 Specifically, the compound disclosed in JP-A-Hll 222428 can be mentioned: a compound represented by the formula (VIII) R-YN X1 I l~l z(V III) X2:I X4

X

3 wherein 3o R is a straight chain or branched Ciio alkyl group, a straight chain or branched C2_10 alkenyl group, a 27 5 CVpo''"dS''c'''ton of AU2O8201550 changess tracked)doc halogenated C1-4 lower alkyl group, a C3-10 cycloalkyl group, a C5-8 cycloalkenyl group, a C3-10 cycloalkyl C1-10 alkyl group (wherein these cycloalkyl group, cycloalkenyl group and 5 cycloalkylalkyl group are each optionally substituted by a group selected from straight chain or branched C1-io alkyl group, straight chain or branched C2-10 alkenyl group, C3-10 cycloalkyl group, C5-8 cycloalkenyl group, C3-10 cycloalkyl C1-10 alkyl 10 group, aryl group, amino group, C1-4 lower alkylamino group, acylamino group, oxo group, aralkyl group and arylalkenyl group), an aryl group, an aralkyl group or a 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom 15 and sulfur atom (wherein these aryl group, aralkyl group and heterocyclic group are each optionally substituted by a group selected from straight chain or branched C1-10 alkyl group, straight chain or branched C2-10 alkenyl group, halogen atom, nitro 20 group, amino group optionally substituted by C1-4 lower alkyl group or acyl group, hydroxyl group, C1-4 lower alkoxy group, C-4 lower alkylthio group, halogenated C1-4 lower alkyl group, acyl group and oxo group); 25 X 1 , X 2 , X 3 and X 4 may be the same or different and each is a hydrogen atom, a halogen atom, a C1-4 lower alkyl group, a halogenated C1-4 lower alkyl group, a C1-4 lower alkoxy group, a cyano group, a nitro group, an acyl 30 group or an aryl group; Y is -CO- or -SO 2 -; Z is a hydrogen atom or a mercapto-protecting group selected from a group that forms a disulfide form, which is a dimer, C1-4 lower alkoxymethyl group, C1-4 35 lower alkylthiomethyl group, aralkyloxymethyl group, 276 C'p*''''''''''''''''' ""''^2008201 sWo(cw~eo..rcked) oc aralkylthiomethyl group, C3-10 cycloalkyloxymethyl group, Cs-8 cycloalkenyloxymethyl group, C3-10 cycloalkyl C1-10 alkoxymethyl group, aryloxymethyl group, arylthiomethyl group, acyl 5 group, acyloxy group, aminocarbonyloxymethyl group, thiocarbonyl group and thio group, a prodrug compound thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof or a solvate thereof. The "straight chain or branched CIo alkyl group" in 10 the formula (VIII) means a straight chain or branched alkyl group having 1 to 10 carbon atoms, which is specifically methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, sec-butyl group, tert-butyl group, pentyl group, isopentyl group, 15 neopentyl group, tert-pentyl group, 1-ethylbutyl group, 2 ethylbutyl group, 1-propylbutyl group, 1,1-dimethylbutyl group, 1-isobutyl-3-methylbutyl group, 1-ethylpentyl group, 1-propylpentyl group, 1-isobutylpentyl group, 2 ethylpentyl group, 2-isopropylpentyl group, 2-tert 20 butylpentyl group, 3-ethylpentyl group, 3-isopropylpentyl group, 4-methylpentyl group, 1,4-dimethylpentyl group, 2,4-dimethylpentyl group, 1-ethyl-4-methylpentyl group, hexyl group, 1-ethylhexyl group, 1-propylhexyl group, 2 ethylhexyl group, 2-isopropylhexyl group, 2-tert 25 butylhexyl group, 3-ethylhexyl group, 3-isopropylhexyl group, 3-tert-butylhexyl group, 4-ethylhexyl group, 5 methylhexyl group, heptyl group, 1-ethylheptyl group, 1 isopropylheptyl group, 2-ethylheptyl group, 2 isopropylheptyl group, 3-propylheptyl group, 4 30 propylheptyl group, 5-ethylheptyl group, 6-methylheptyl group, octyl group, 1-ethyloctyl group, 2-ethyloctyl group, nonyl group, 1-methylnonyl group, 2-methylnonyl group, decyl group and the like, with preference given to a straight chain or branched alkyl group having 1 to 8 35 carbon atoms. 277 C "V*''""'"'e'''''''*"*'^A20082015o .rchari . c The "C-4 lower alkyl group" in the formula (VIII) means a straight or branched alkyl group having 1 to 4 carbon atoms, which is specifically methyl group, ethyl group, propyl group, isopropyl group, butyl group, 5 isobutyl group, sec-butyl group, tert-butyl group and the like. The "straight chain or branched C2-10 alkenyl group" in the formula (VIII) means a straight chain or branched alkenyl group having 2 to 10 carbon atoms and at least one 10 double bond, which is specifically allyl group, vinyl group, isopropenyl group, 1-propenyl group, 1-methyl-2 propenyl group, 2-methyl-2-propenyl group, 1-methyl-1 butenyl group, crotyl group, 1-methyl-3-butenyl group, 3 methyl-2-butenyl group, 1,3-dimethyl-2-butenyl group, 1 15 pentenyl group, 1-methyl-2-pentenyl group, 1-ethyl-3 pentenyl group, 4-pentenyl group, 1,3-pentadienyl group, 2,4-pentadienyl group, 1-hexenyl group, 1-methyl-2-hexenyl group, 3-hexenyl group, 4-hexenyl group, 1-butyl-5-hexenyl group, 1,3-hexadienyl group, 2,4-hexadienyl group, 1 20 heptenyl group, 2-heptenyl group, 3-heptenyl group, 4 heptenyl group, 5-heptenyl group, 6-heptenyl group, 1,3 heptadienyl group, 2,4-heptadienyl group, 1-octenyl group, 2-octenyl group, 3-octenyl group, 4-octenyl group, 5 octenyl group, 6-octenyl group, 7-octenyl group, 1-nonenyl 25 group, 2-nonenyl group, 3-nonenyl group, 4-nonenyl group, 5-nonenyl group, 6-nonenyl group, 7-nonenyl group, 8 nonenyl group, 9-decenyl group and the like, with preference given to a straight chain or branched alkenyl group having 2 to 8 carbon atoms. 30 The "halogen atom" in the formula (VIII) means fluorine atom, chlorine atom, bromine atom and the like. The "halogenated C1-4 alkyl group" in the formula (VIII) means the aforementioned C1-4 lower alkyl group substituted by 1 to 3 the same or different halogen atoms, 35 which is specifically fluoromethyl group, chloromethyl 2 7 8 C:Vo"'" *Sp*c"f'c 'on of AU20082O155o (ct.ngo.. tra d).do group, bromomethyl group, difluoromethyl group, dichloromethyl group, trifluoromethyl group, trichloromethyl group, chloroethyl group, difluoroethyl group, trifluoroethyl group, pentachloroethyl group, 5 bromopropyl group, dichloropropyl group, trifluorobutyl group and the like, with preference given to trifluoromethyl group and chloroethyl group. The "C1-4 lower alkoxy group" in the formula (VIII) means an alkoxy group having the aforementioned C1-4 lower 10 alkyl group, which is specifically methoxy group, ethoxy group, propoxy group, isopropoxy group, butoxy group, isobutoxy group, sec-butoxy group, tert-butoxy group and the like. The "C1-4 lower alkylthio group" in the formula (VIII) 15 means an alkylthio group having the aforementioned C1-4 lower alkyl group, which is specifically methylthio group, ethylthio group, propylthio group, isopropylthio group, butylthio group, isobutylthio group, sec-butylthio group, tert-butylthio group and the like. 20 The "C3-10 cycloalkyl group" in the formula (VIII) means a monocyclic or polycyclic cycloalkyl group having 3 to 10 carbon atoms, which is specifically cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclooctyl group, 25 octahydroindenyl group, decahydronaphthyl group, bicyclo[2.2.1]heptyl group, adamantyl group and the like, with preference given to cyclopentyl group, cyclohexyl group and cycloheptyl group, each having 5 to 7 carbon atoms. 30 The "C5-8 cycloalkenyl group" in the formula (VIII) means a cycloalkenyl group having 5 to 8 carbon atoms and one or more double bonds on the ring, which is specifically cyclopentenyl group, cyclohexenyl group, cycloheptenyl group, cyclooctenyl group, cyclopentadienyl 35 group, cyclohexadienyl group, cycloheptadienyl group, 279 C:p"'**''V*p**f''''' '*"'^2008201 (s c ed).c.

cyclooctadienyl group and the like, with preference given to cyclopentenyl group, cyclohexenyl group and cycloheptenyl group, each having 5 to 7 carbon atoms. The "C 3

-

1 0 cycloalkyl C1-10 alkyl group" in the formula 5 (VIII) means the aforementioned straight chain or branched Cj-io alkyl group substituted by the aforementioned C3-10 cycloalkyl group, which is specifically cyclopropylmethyl group, cyclopentylmethyl group, cyclohexylmethyl group, cyclohexylcyclopentylmethyl group, dicyclohexylmethyl 10 group, 1-cyclopentylethyl group, 1-cyclohexylethyl group, 2-cyclopropylethyl group, 2-cyclopentylethyl group, 2 cyclohexylethyl group, 2-cycloheptylethyl group, 1 cyclohexyl-l-methylethyl group, 1-cyclohexylpropyl group, 2-cyclopentylpropyl group, 3-cyclobutylpropyl group, 3 15 cyclopentylpropyl group, 3-cyclohexylpropyl group, 3 cycloheptylpropyl group, 1-cyclopropyl-l-methylpropyl group, 1-cyclohexyl-2-methylpropyl group, 1 cyclopentylbutyl group, 1-cyclohexylbutyl group, 3 cyclohexylbutyl group, 4-cyclopropylbutyl group, 4 20 cyclobutylbutyl group, 4-cyclopentylbutyl group, 1 cyclohexyl-l-methylbutyl group, 1-cyclopentyl-2-ethylbutyl group, 1-cyclohexyl-3-methylbutyl group, 1 cyclopentylpentyl group, 1-cyclohexylpentyl group, 1 cyclohexylmethylpentyl group, 2-cyclohexylpentyl group, 2 25 cyclohexylmethylpentyl group, 3-cyclopentylpentyl group, 1-cyclohexyl-4-methylpentyl group, 5-cyclopentylpentyl group, l-cyclopentylhexyl group, 1-cyclohexylhexyl group, 1-cyclopentylmethylhexyl group, 2-cyclopentylhexyl group, 2-cyclopropylethylhexyl group, 3-cyclopentylhexyl group, 30 1-cyclohexylheptyl group, 1-cyclopentyl-l-methylheptyl group, 1-cyclohexyl-1,6-dimethylheptyl group, 1 cycloheptyloctyl group, 2-cyclopentyloctyl group, 3 cyclohexyloctyl group, 2-cyclopentylmethyloctyl group, 1 cyclopentylnonyl group, 1-cyclohexylnonyl group, 3 35 cyclopropylnonyl group, 1-cyclopentyldecyl group, 1 28 0C V V'rd'Spo'fI''t' o of AU2008201550 (dlem. tracked).doc cyclohexylundecyl group, 1-cyclopentyltridecyl group, 2 cyclohexyltridecyl group and the like. The "aryl group" in the formula (VIII) means phenyl group, naphthyl group, anthryl group, phenanthryl group, 5 biphenyl group and the like, with preference given to phenyl group, naphthyl group and biphenyl group. The "aralkyl group" in the formula (VIII) means the aforementioned C 1 4 lower alkyl group substituted by one or more aryl groups mentioned above, which is specifically 10 benzyl group, benzhydryl group, trityl group, phenethyl group, 3-phenylpropyl group, 2-phenylpropyl group, 4 phenylbutyl group, naphthylmethyl group, 2-naphthylethyl group, 4-biphenylmethyl group, 3-(4-biphenyl)propyl group and the like. 15 The "arylalkenyl group" in the formula (VIII) means alkenyl group having 2 to 4 carbon atoms substituted by aryl group mentioned above, which is specifically 2 phenylvinyl group, 3-phenyl-2-propenyl group, 3-phenyl-2 methyl-2-propenyl group, 4-phenyl-3-butenyl group, 2-(1 20 naphthyl)vinyl group, 2-(2-naphthyl)vinyl group, 2-(4 biphenyl)vinyl group and the like. The "arylthio group" in the formula (VIII) means arylthio group having the aforementioned aryl group, which is specifically phenylthio group, naphthylthio group and 25 the like. The "heterocyclic group" in the formula (VIII) means a 5- or 6-membered aromatic or nonaromatic heterocyclic group having one or more, specifically 1 to 4, preferably 1 to 3, heteroatoms selected from nitrogen atom, oxygen 30 atom and sulfur atom, which is specifically aromatic heterocyclic groups such as thiatriazolyl group, tetrazolyl group, dithiazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, oxazolyl group, pyrazolyl group, pyrrolyl group, furyl group, thienyl 35 group, tetrazinyl group, triazinyl group, pyrazinyl group, 2 8 1 C:"po'V'd*Spf* ''on ofAU2008201550 (chang.. .r.e.d).doc pyridazinyl group, pyrimidinyl group, pyridyl group and the like and nonaromatic heterocyclic groups such as dioxolanyl group, pyrrolidinyl group, tetrahydrofuryl group, tetrahydrothienyl group, dithiadiazinyl group, 5 thiadiazinyl group, morpholino group, morpholinyl group, oxazinyl group, thiazinyl group, piperazinyl group, piperidyl group, piperidino group, pyranyl group, thiopyranyl group and the like. Preferred are an aromatic heterocyclic (heteroaryl) group such as furyl group, 10 thienyl group, pyrrolyl group, pyridyl group and the like and a nonaromatic heterocyclic group having at least one nitrogen atom, such as pyrrolidinyl group, tetrahydrofuryl group, piperazinyl group, piperidyl group, piperidino group and the like. 15 The "acyl group" in the formula (VIII) specifically means formyl group, acetyl group, propionyl group, butyryl group, isobutyryl group, valeryl group, isovaleryl group, pivaloyl group, hexanoyl group, acryloyl group, propioloyl group, metacryloyl group, crotonoyl group, benzoyl group, 20 naphthoyl group, toluoyl group, hydroatropoyl group, atropoyl group, cinnamoyl group, furoyl group, thenoyl group, nicotinoyl group, isonicotinoyl group, glycoloyl group, lactoyl group, glyceroyl group, tropoyl group, benziloyl group, salicyloyl group, anisoyl group, 25 vanilloyl group, veratroyl group, piperonyloyl group, protocatechuoyl group, galloyl group, cyclopentanecarbonyl group, cyclohexanecarbonyl group, cycloheptanecarbonyl group, 1-methylcyclohexanecarbonyl group, 1 isopentylcyclopentanecarbonyl group, 1 30 isopentylcyclohexanecarbonyl group, tert-butoxycarbonyl group, methoxycarbonyl group, ethoxycarbonyl group, 2-(l isopentylcyclohexanecarbonylamino)phenylthiocarbonyl group and the like. Preferred are acetyl group, tert butoxycarbonyl group, benzoyl group, 1 35 methylcyclohexanecarbonyl group, 1 2 82 C 'Vpof''rd' Sp' dfl'o' ' of AU20020 50 (i n...ir.cr.d) c isopentylcyclopentanecarbonyl group, 1 isopentylcyclohexanecarbonyl group and 2-(1 isopentylcyclohexanecarbonylamino)phenylthiocarbonyl group. In the formula (VIII), the "optionally substituted" 5 of the "optionally substituted C3-10 cycloalkyl group", "optionally substituted C 5

-

8 cycloalkenyl group" and "optionally substituted C3-10 cycloalkyl C1-10 alkyl group" for R and the like means being optionally substituted by 1 to 4 substituents. The substituent may be the same or 10 different and the position of substituent is optional and free of any particular limitation. Specifically, the aforementioned straight chain or branched C1-10 alkyl group; the aforementioned straight chain or branched C2-10 alkenyl group; the aforementioned C 3

-

10 cycloalkyl group; 15 the aforementioned C5-8 cycloalkenyl group; the aforementioned C3-10 cycloalkyl C1-10 alkyl group; the aforementioned aryl group; amino group; C1-4 lower alkylamino group such as methylamino group, ethylamino group and the like; acylamino group such as acetylamino 20 group, propionylamino group, benzylamino group and the like; oxo group; the aforementioned aralkyl group; the aforementioned arylalkenyl group and the like can be mentioned. The above substituents are recommended mainly as the substituent for R. 25 In the formula (VIII), the "optionally substituted" of the "optionally substituted aryl group", "optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom", "optionally substituted aralkyl group", "optionally 30 substituted arylalkenyl group", "optionally substituted arylthio group" and "optionally substituted 5- or 6 membered heteroarylalkyl group" for R and the like means being optionally substituted by 1 to 4, preferably 1 to 3, substituents. The substituent may be the same or 35 different and the position of substituent is optional and 2 8 3 C:VpoNorSpecificaton of AU2008201550 (changes tracked).doc free of any particular limitation. Specifically, the aforementioned straight chain or branched Ci-jo alkyl group, preferably straight chain or branched C1-6 alkyl group; the aforementioned straight chain or branched C2-10 alkenyl 5 group, preferably straight chain or branched C2-6 alkenyl group; the aforementioned halogen atom; nitro group; the aforementioned C1-4 lower alkyl group or amino group optionally substituted by the aforementioned acyl group; hydroxyl group; the aforementioned C1-4 lower alkoxy group; 10 the aforementioned C1-4 lower alkylthio group; the aforementioned halogenated C1-4 lower alkyl group; the aforementioned acyl group; oxo group and the like can be mentioned. Of these, the aforementioned straight chain or branched C1-6 alkyl group; the aforementioned halogen atom; 15 and nitro group are particularly preferable . In the formula (VIII), the "optionally substituted" of the "optionally substituted amino group" means being optionally substituted by one or more, preferably 1 or 2, substituents. The substituents may be the same or 20 different and the position of substitution is optional and is not particularly limited. Specific examples thereof include the aforementioned aryl group optionally substituted by the aforementioned C1-4 lower alkyl group, and the like; hydroxyl group; the aforementioned acyl 25 group; and the aforementioned C1-4 lower alkoxy group. In the formula (VIII), the "mercapto-protecting group" for Z means a conventionally used mercapto protecting group, and is free of any particular limitation as long as it is an organic residue liberated in living 30 organisms. It may also form a disulfide form, which is a dimer. Specifically, those such as the following C1-4 lower alkoxymethyl group; C1-4 lower alkylthiomethyl group; aralkyloxymethyl group; aralkylthiomethyl group; C3-1a cycloalkyloxymethyl group; C5-8 cycloalkenyloxymethyl 35 group; C3-10 cycloalkyl C1-10 alkoxymethyl group; 2 8 4 C 'po 'ordVSpc'f'caon of AU2008201550 (cang s tracked).dc aryloxymethyl group; arylthiomethyl group; acyl group; acyloxy group; aminocarbonyloxymethyl group; thiocarbonyl group; and thio group can be mentioned. More specifically, C1-4 lower alkoxymethyl group having the aforementioned C1-4 5 lower alkoxy group; C1-4 lower alkylthiomethyl group having the aforementioned C1-4 lower alkylthio group; aralkyloxymethyl group having the aforementioned aralkyl group; aralkylthiomethyl group having the aforementioned aralkyl group; C 3

-

10 cycloalkyloxymethyl group having the 10 aforementioned C3-10 cycloalkyl group; C5-8 cycloalkenyloxymethyl group having the aforementioned C5-8 cycloalkenyl group; C3-10 cycloalkyl Cl-a alkoxymethyl group having the aforementioned C3-10 cycloalkyl C1-10 alkyl group; aryloxymethyl group having the aforementioned aryl 15 group; arylthiomethyl group having the aforementioned arylthio group; acyl group having the aforementioned optionally substituted straight chain or branched C1-10 alkyl group, the aforementioned halogenated C4 lower alkyl group, the aforementioned C1-4 lower alkoxy group, 20 the aforementioned C1-4 lower alkylthio group, the aforementioned optionally substituted amino group, the aforementioned optionally substituted ureido group, the aforementioned optionally substituted C3-10 cycloalkyl group, the aforementioned optionally substituted C3-10 25 cycloalkyl Ci-1o alkyl group, the aforementioned optionally substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally substituted arylalkenyl group, the aforementioned optionally substituted arylthio group, the aforementioned 30 optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6 membered heteroarylalkyl group; acyloxy group having the aforementioned optionally substituted straight chain or 35 branched Ci-1o alkyl group, the aforementioned halogenated 2 8 5 C "'pofV'"dSp ''t' o of AU20DB20155O (Co.ge. trk.od) oc C1-4 lower alkyl group, the aforementioned C14 lower alkoxy group, the aforementioned C1-4 lower alkylthio group, the aforementioned optionally substituted amino group, the aforementioned optionally substituted ureido group, the 5 aforementioned optionally substituted C 3

-

10 cycloalkyl group, the aforementioned optionally substituted C 3

-

10 cycloalkyl C1-1o alkyl group, the aforementioned optionally substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally 10 substituted arylalkenyl group, the aforementioned optionally substituted arylthio group, the aforementioned optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6 15 membered heteroarylalkyl group; aminocarbonyloxymethyl group optionally substituted by the aforementioned optionally substituted straight chain or branched C 1

-

10 alkyl group, the aforementioned halogenated C1- 4 alkyl group, the aforementioned C1-4 lower alkoxy group, the 20 aforementioned Ci-4 lower alkylthio group, the aforementioned optionally substituted C 3

-

10 cycloalkyl group, the aforementioned optionally substituted C3-10 cycloalkyl Ci-1o alkyl group, the aforementioned optionally substituted aryl group, the aforementioned optionally 25 substituted aralkyl group, the aforementioned optionally substituted arylalkenyl group, the aforementioned optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6 30 membered heteroarylalkyl group; thiocarbonyl group having the aforementioned optionally substituted straight chain or branched Ci-10 alkyl group, the aforementioned halogenated C1-4 lower alkyl group, the aforementioned Ci-4 lower alkoxy group, the aforementioned C1-4 lower alkylthio 35 group, the aforementioned optionally substituted amino 28C6 :VpofordSpecfictIon of AU2008201550 (change tracked).doc group, the aforementioned optionally substituted ureido group, the aforementioned optionally substituted C3-10 cycloalkyl group, the aforementioned optionally substituted C 3 -10cycloalkyl Ci-10 alkyl group, the 5 aforementioned optionally substituted aryl group, the aforementioned optionally substituted aralkyl group, the aforementioned optionally substituted arylalkenyl group, the aforementioned optionally substituted arylthio group, the aforementioned optionally substituted 5- or 6-membered 10 heterocyclic group having 1 to 3 from nitrogen atom, oxygen atom and sulfur atom or the aforementioned optionally substituted 5- or 6-membered heteroarylalkyl group; and thio group having the aforementioned optionally substituted Ci-4 lower alkyl group or aryl group can be 15 mentioned. To be more concrete, as the "straight chain or branched Cl-10 alkyl group" for R of the formula (VIII), methyl group, ethyl group, isopropyl group, butyl group, isobutyl group, tert-butyl group, heptyl group, 1 20 propylbutyl group and 1-isobutyl-3-methylbutyl group are preferable. As the "straight chain or branched C2-10 alkenyl group" for R of the formula (VIII), allyl group, vinyl group, isopropenyl group, 1-methyl-2-propenyl group, 2 25 methyl-2-propenyl group, 1-methyl-1-butenyl group, crotyl group, 1,3-dimethyl-2-butenyl group, 1-pentenyl group and 1-methyl-2-pentenyl group are preferable. The "halogenated C1-4 lower alkyl group" for R of the formula (VIII) means C1-4 lower alkyl group (particularly 30 preferably methyl group) substituted by the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom), with preference given to trifluoromethyl group. The "optionally substituted C3-10 cycloalkyl group" 35 for R of the formula (VIII) is C310 cycloalkyl group 2 8 7 C "p *"r*VS*'"fic'Von of AU2008201550 (ang"o..t,.cko).doc (particularly preferably cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, octahydroindenyl group, decahydronaphthyl group, adamantyl group, bicyclo[2.2.1]heptyl group) optionally 5 substituted by 1 to 4 substituents selected from the aforementioned straight chain or branched C 1

-

10 alkyl group (particularly preferably C1-8 alkyl group such as methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, tert-butyl group, pentyl group, 10 isopentyl group, 2,2-dimethylpropyl group, 4-methylpentyl group, 2-ethylbutyl group etc.), the aforementioned straight chain or branched C 2

-

1 0 alkenyl group (particularly preferably C2-8 alkenyl group such as 1 methylvinyl group, 2-methylvinyl group, 3-methyl-3 15 propenyl group etc.), the aforementioned C3-10 cycloalkyl group (particularly preferably C3-7 cycloalkyl group such as cyclopropyl group, cyclopentyl group, cyclohexyl group etc.), the aforementioned C5-8 cycloalkenyl group (particularly preferably C5-6 cycloalkenyl group such as 20 cyclopentenyl group, cyclohexenyl group etc.), the aforementioned C3-10 cycloalkyl C1-10 alkyl group (particularly preferably C3-7 cycloalkyl C14 alkyl group such as cyclopropylmethyl group, 2-cyclopropylethyl group, 2-cyclopentylethyl group, cyclohexylmethyl group, 2 25 cyclohexylethyl group etc.), the aforementioned aryl group (particularly preferably phenyl group), oxo group, the aforementioned aralkyl group (particularly preferably phenyl C14 lower alkyl group such as benzyl group, phenethyl group etc.) and the aforementioned arylalkenyl 30 group (particularly preferably 2-phenylvinyl group). Preferred are 2,2,3,3-tetramethylcyclopropyl group, 1 isopentylcyclobutyl group, 1-isopropylcyclopentyl group, 1-isobutylcyclopentyl group, 1-isopentylcyclopentyl group, 1-cyclohexylmethylcyclopentyl group, cyclohexyl group, 1 35 methylcyclohexyl group, 1-ethylcyclohexyl group, 1 288 C r* ordVSpcmficmon of AU2DO82O155O (c .. anges trac oed)doc propylcyclohexyl group, 1-isopropylcyclohexyl group, 1 butylcyclohexyl group, 1-isobutylcyclohexyl group, 1 pentylcyclohexyl group, 1-isopentylcyclohexyl group, 1 (2,2-dimethylpropyl)cyclohexyl group, 1-(4 5 methylpentyl)cyclohexyl group, 1-(2-ethylbutyl)cyclohexyl group, 4-tert-butyl-1-isopentylcyclohexyl group, 1 cyclopropylcyclohexyl group, 1-bicyclohexyl group, 1 phenylcyclohexyl group, 1-cyclopropylmethylcyclohexyl group, 1-cyclohexylmethylcyclohexyl group, 1-(2 10 cyclopropylethyl)cyclohexyl group, 1-(2 cyclopentylethyl)cyclohexyl group, 1-(2 cyclohexylethyl)cyclohexyl group, 4-methylcyclohexyl group, 4-propylcyclohexyl group, 4-isopropylcyclohexyl group, 4 tert-butylcyclohexyl group, 4-pentylcyclohexyl group, 4 15 bicyclohexyl group, 1-isopentylcycloheptyl group, 3a octahydroindenyl group, 4a-decahydronaphthyl group, 1 adamantyl group and 7,7-dimethyl-l-(2 oxo)bicyclo[2.2.1]heptyl group. While the position of substitution is not particularly limited, it is 20 particularly preferably the 1-position. While the substituent may be any of the above-mentioned substituents, it is particularly preferably straight chain or branched C1-10 alkyl group. The substituent of the "optionally substituted C5-8 25 cycloalkenyl group" for R of the formula (VIII) is completely the same as in the case of the aforementioned "optionally substituted C3-10 cycloalkyl group". Specific examples thereof include cycloalkenyl group (particularly cyclopentenyl group, cyclohexenyl group) optionally 30 substituted by 1 to 4 substituents selected from the aforementioned straight chain or branched Ci-io alkyl group (particularly preferably C1-8 alkyl group such as methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2,2 35 dimethylpropyl group, 4-methylpentyl group etc.), the 2 8 9 C:Vof'dVSpc''^tIon of AU2008201550 ( gsnt..r,.cked) dm aforementioned straight chain or branched C 2

-

10 alkenyl group (particularly preferably C2-8 alkenyl group such as 1-methylvinyl group, 2-methylvinyl group, 3-methyl-3 propenyl group etc.), the aforementioned C 3

-

1 0 cycloalkyl 5 group (particularly preferably C3-7 cycloalkyl group such as cyclopropyl group, cyclopentyl group, cyclohexyl group etc.), the aforementioned C5-8 cycloalkenyl group (particularly preferably C 5

-

6 cycloalkenyl group such as cyclopentenyl group, cyclohexenyl group etc.), the 10 aforementioned C3-10 cycloalkyl C1-10 alkyl group (particularly preferably C3-7 cycloalkyl C1-4 lower alkyl group such as cyclopropylmethyl group, 2-cyclopropylethyl group, 2-cyclopentylethyl group, cyclohexylmethyl group, 2-cyclohexylethyl group etc.), the aforementioned aryl 25 group (particularly preferably phenyl group), oxo group, the aforementioned aralkyl group (particularly preferably phenyl C1-4 lower alkyl group such as benzyl group, phenethyl group etc.) and the aforementioned arylalkenyl group (particularly preferably 2-phenylvinyl group). 20 Preferred are 1-isopropyl-2-cyclopentenyl group, 1 isopropyl-3-cyclopentenyl group, 1-isobutyl-2 cyclopentenyl group, 1-isobutyl-3-cyclopentenyl group, 1 isopentyl-2-cyclopentenyl group, 1-isopentyl-3 cyclopentenyl group, 1-cyclohexylmethyl-2-cyclopentenyl 25 group, 1-cyclohexylmethyl-3-cyclopentenyl group, 1 cyclohexenyl group, 2-cyclohexenyl group, 3-cyclohexenyl group, 1-methyl-2-cyclohexenyl group, 1-methyl-3 cyclohexenyl group, 1-ethyl-2-cyclohexenyl group, 1-ethyl 3-cyclohexenyl group, 1-propyl-2-cyclohexenyl group, 1 30 propyl-3-cyclohexenyl group, 1-isopropyl-2-cyclohexenyl group, 1-isopropyl-3-cyclohexenyl group, 1-butyl-2 cyclohexenyl group, 1-butyl-3-cyclohexenyl group, 1 isobutyl-2-cyclohexenyl group, 1-isobutyl-3-cyclohexenyl group, 1-pentyl-2-cyclohexenyl group, 1-pentyl-3 35 cyclohexenyl group, 1-isopentyl-2-cyclohexenyl group, 1 2 9 0 C'" *rd'S'f'''c''' of AU2'" 8201550 ( g" rn. ed).dc isopentyl-3-cyclohexenyl group, 1-(2,2-dimethylpropyl)-2 cyclohexenyl group, 1-(2,2-dimethylpropyl)-3-cyclohexenyl group, 1-(4-methylpentyl)-2-cyclohexenyl group, 1-(4 methylpentyl)-3-cyclohexenyl group, 1-cyclopropyl-2 5 cyclohexenyl group, 1-cyclopropyl-3-cyclohexenyl group, 1 cyclohexyl-2-cyclohexenyl group, 1-cyclohexyl-3 cyclohexenyl group, 1-phenyl-2-cyclohexenyl group, 1 phenyl-3-cyclohexenyl group, 1-cyclopropylmethyl-2 cyclohexenyl group, 1-cyclopropylmethyl-3-cyclohexenyl 10 group, 1-cyclohexylmethyl-2-cyclohexenyl group, 1 cyclohexylmethyl-3-cyclohexenyl group, 1-(2 cyclopropylethyl)-2-cyclohexenyl group, 1-(2 cyclopropylethyl)-3-cyclohexenyl group, 1-(2 cyclopentylethyl)-2-cyclohexenyl group, 1-(2 15 cyclopentylethyl)-3-cyclohexenyl group, 1-(2 cyclohexylethyl)-2-cyclohexenyl group and 1-(2 cyclohexylethyl)-3-cyclohexenyl group. While the position of substitution is not particularly limited, it is particularly preferably the 1-position. While the 20 substituent may be any of the above-mentioned substituents, it is particularly preferably straight chain or branched CI-10 alkyl group or C3-10 cycloalkyl C1-4 alkyl group. The "optionally substituted C3-10 cycloalkyl CI-10 alkyl group" for R of the formula (VIII) means C3-10 25 cycloalkyl C1-1a alkyl group (particularly preferably cyclohexylmethyl group, 1-cyclohexylethyl group, 1 cyclohexyl-1-methylethyl group, 1-cyclohexyl-2 methylpropyl group, 1-cyclohexyl-3-methylbutyl group, 1 cyclohexylhexyl group, 1-cyclohexyl-4-methylpentyl group, 30 1-cyclohexylheptyl group) optionally substituted by 1 to 4 substituents selected from the aforementioned C3-10 cycloalkyl group (particularly preferably C3-7 cycloalkyl group such as cyclopentyl group, cyclohexyl group etc.), the aforementioned C5-8 cycloalkenyl group (particularly 35 preferably C5-7 cycloalkenyl group such as cyclopentenyl 2 91 C.po' 'rd ''Spedf'c't'on of AU2008201550 (chang. .,.cked) c group and cyclohexenyl group) and the aforementioned aryl group (particularly preferably phenyl group), wherein Ci-i alkyl group is straight chain or branched. The position of substitution is not particularly limited, and the 5 straight chain or branched C1-10 alkyl group moiety may have a substituent. Preferred are cyclohexylmethyl group, 1-cyclohexylethyl group, cyclohexylcyclopentylmethyl group, dicyclohexylmethyl group, 1-cyclohexyl-l-methylethyl group, 1-cyclohexyl-2-methylpropyl group, 1-cyclohexyl-3 10 methylbutyl group, 1-cyclohexyl-4-methylpentyl group, 1 cyclohexylhexyl group and 1-cyclohexylheptyl group. The "optionally substituted aryl group" for R of the formula (VIII) means aryl group (particularly preferably phenyl group) optionally substituted by 1 to 4 15 substituents selected from the aforementioned straight chain or branched Ci-6 alkyl group (particularly preferably tert-butyl group), the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom) and nitro group. Preferred are phenyl group, 2-chlorophenyl 20 group, 4-nitrophenyl group and 3,5-di-tert-butylphenyl group. The "optionally substituted aralkyl group" for R of the formula (VIII) means aralkyl group (particularly preferably benzyl group, benzhydryl group, trityl group) 25 optionally substituted by the substituent selected from the aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom), nitro group and hydroxyl group, wherein the Ci 4 lower alkyl group is straight chain or branched. The position of substitution is not 30 particularly limited and the straight chain or branched C14 lower alkyl group moiety may have said substituent. Preferred are benzyl group and trityl group. The "optionally substituted 5- or 6-membered heterocyclic group having 1 to 3 from nitrogen atom, 35 oxygen atom and sulfur atom" for R of the formula (VIII) 292 C:VpofV'dVSp'oflcaton of AU200201550 (.g... tr.. d).do means the aforementioned heterocyclic group optionally substituted by 1 to 4 substituents selected from the aforementioned straight chain or branched C1-6 alkyl group (particularly preferably tert-butyl group), the 5 aforementioned halogen atom (particularly preferably fluorine atom, chlorine atom) and nitro group, with preference given to aromatic heterocyclic group. Particularly preferred are furyl group, thienyl group and pyridyl group. 10 The "halogen atom" for X 1 , X 2 , X 3 , X 4 in the formula (VIII) means halogen atom such as fluorine atom, chlorine atom, bromine atom and the like, with preference given to fluorine atom and chlorine atom. The "Ci-4 lower alkyl group" for X 1 , X 2 , X 3 , X 4 in the 15 formula (VIII) is preferably methyl group. The "halogenated C1-4 lower alkyl group" for X 1 , X 2 ,

X

3 , X 4 in the formula (VIII) is C1_4 lower alkyl group (particularly preferably methyl group) substituted by the aforementioned halogen atom (particularly preferably 20 fluorine atom, chlorine atom), with preference given to trifluoromethyl group. The "group" of the "C1-4 lower alkoxy group" for X 1 ,

X

2 , X 3 , X 4 in the formula (VIII) is preferably methoxy group. 25 In the formula (VIII), the "acyl group" for X 1 , X 2 , X3, X 4 is preferably benzoyl group. In the formula (VIII), the "aryl group" for X 1 , X 2 ,

X

3 , X 4 is preferably phenyl group. The "prodrug compound" of the formula (VIII) is a 30 derivative of the compound of the formula (VIII), which has a chemically or metabolically degradable group and shows pharmaceutical activity by hydrolysis or solvent decomposition, or by degradation under physiological conditions. 35 The "pharmaceutically acceptable salt" of the 2 9 3 C"pof" d"Spo"'fi' "o of AU2008201O550 (c.c. c ek) formula (VIII) may be any as long as it forms a nontoxic salt with a compound represented by the above-mentioned formula (VIII). For example, inorganic acid salts such as hydrochloride, hydrobromide, hydroiodide, sulfate, nitrate, 5 phosphate, carbonate, hydrogen carbonate, perchlorate etc.; organic acid salts such as formate, acetate, trifluoroacetate, propionate, oxalate, glycolate, succinate, lactate, maleate, hydroxymaleate, methylmaleate, fumarate, adipate, tartrate, malate, citrate, benzoate, 20 cinnamate, ascorbate, salicylate, 2-acetoxybenzoate, nicotinate, isonicotinate etc.; sulfonates such as methanesulfonate, ethanesulfonate, isethionate, benzenesulfonate, p-toluenesulfonate, naphthalenesulfonate etc.; acidic amino acid salts such as aspartate, glutamate 15 etc.; alkali metal salts such as sodium salt, potassium salt etc.; alkaline earth metal salts such as magnesium salt, calcium salt etc.; ammonium salt; organic base salts such as trimethylamine salt, triethylamine salt, pyridine salt, picoline salt, dicyclohexylamine salt, N,N' 20 dibenzylethylenediamine salt etc.; and amino acid salts such as lysin salt, arginine salt etc. can be mentioned. In some cases, it may be a hydrate or a solvate with alcohol and the like. In addition, the compounds disclosed in W02004/020393 25 and Patent Application No. 2003-308156 can be mentioned. A dibenzylamine compound represented by the formula (IX) (M)n B R N (IX) A R R 5 R4 2 94 **'po *'"'''''"""*'"*** of"'208 "05 "'""***'**wed)d wherein R' and R 2 are the same or different and each is a halogen atom, a nitro group, a cyano group or a C16 alkyl 5 group optionally substituted by halogen atom;

R

3 , R 4 and R 5 are the same or different and each is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen atom, a C1- alkylthio group 10 optionally substituted by halogen atom or a C1-6 alkoxy group optionally substituted by halogen atom, or R 3 and R 4 or R 4 and R 5 may form, together with a carbon atom they are bonded to, a homocyclic ring optionally having substituent(s) or a heterocyclic 15 ring optionally having substituent(s); A is -N(R 7 ) (R 8 ) (wherein R7 and R 8 are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein C 1

-

6 alkyl group is optionally substituted by phenyl group or 20 -(CH 2 )n-COOR 9 (wherein R 9 is a hydrogen atom or a Ci 6 alkyl group and m is 0 or an integer of 1 to 5)) or a C4-10 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, 25 amino group, hydroxyl group, cyano group, acyl group, Ci- alkoxy group, CI-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group, Ci-6 alkoxy group or phosphono group) , - (CH2) q-CON (R 2) (R ) (wherein R20 and R are 30 the same or different and each is hydrogen atom or C1-6 alkyl group and q is 0 or an integer of 1 to 5) or -(CH 2 )r-COOR 10 (wherein R1 0 is hydrogen atom or C1-6 alkyl group and r is 0 or an integer of 1 to 5) ) , -C (R11) (R12 (R 13) (wherein R", R and R1 are 35 the same or different and each is a hydrogen atom, 2 95 c:Vpor*-,eVSp.efcaio of AU2008201550 (oenfo...rckod).doc a Ci-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by phenyl group or -COOR 9 (wherein R 9 is as defined above) ) or a C4-10 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl 5 group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C1-6 alkoxy group, C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group, 10 C1-6 alkoxy group or phosphono group) , - (CH2) q

CON(R

2 1) (R 21 ) (wherein R 2 0 , R 21 and q are as defined above) or -(CH2)r-COOR 10 (wherein R 10 and r are as defined above))) or -0-C(R1 ) (R ) (R ) (wherein R , R1 2 and R1 3 are as defined above); 15 ring B is an aryl group or a heterocyclic residue;

R

6 is a hydrogen atom, a halogen atom, a nitro group, an amino group, a hydroxyl group, a cyano group, an acyl group, a C1-6 alkoxy group, a C2-6 alkenyl group or a C1-6 alkyl group (wherein C-6 alkyl group is 20 optionally substituted by hydroxyl group or -COOR 4 (wherein R 4 is hydrogen atom or C1-6 alkyl group)); and n is an integer of 1 to 3 or a prodrug thereof or a pharmaceutically acceptable salt 25 thereof. The "halogen atom" in the formula (IX) is a chlorine atom, a bromine atom, a fluorine atom and the like. The halogen atom for R1, R 2, R 3, R4, R5 or R6 is preferably a chlorine atom or a fluorine atom and preferable halogen 30 atom as a substituent of C4-10 cycloalkylalkyl group for R 7 , 8 11 12 13 R , R , R or R1 is a chlorine atom or a fluorine atom. The "C2-6 alkenyl group" in the formula (IX) is a straight chain or branched alkenyl group having 2 to 6 carbon atoms. Examples thereof include ethenyl group 35 (vinyl group), 1-propenyl group, 2-propenyl group (allyl 2 9 6 C* 'dVSpf'"io" ^ of AU2008201550 (Sso.e tracked) doDc group), isopropenyl group, 1-butenyl group, 2-butenyl group, 3-butenyl group, 1-methyl-1-propenyl group, 1 methyl-2-propenyl group, 2-methyl-2-propenyl group, 1 ethylvinyl group, 1-pentenyl group, 2-pentenyl group, 3 5 pentenyl group, 4-pentenyl group, 1,2-dimethyl-1-propenyl group, 1,2-dimethyl-2-propenyl group, 1-ethyl-1-propenyl group, 1-ethyl-2-propenyl group, 1-methyl-1-butenyl group, 1-methyl-2-butenyl group, 2-methyl-1-butenyl group, 1 isopropylvinyl group, 2,4-pentadienyl group, 1-hexenyl 10 group, 2-hexenyl group, 3-hexenyl group, 4-hexenyl group, 5-hexenyl group, 2,4-hexadienyl group and 1-methyl-1 pentenyl group and the like, with preference given to alkenyl group having 2 to 4 carbon atoms, which may be a straight chain or branched. Particularly preferred are 15 ethenyl group, isopropenyl group and 2-methyl-2-propenyl group. The "C 1

-

6 alkyl group" in the formula (IX) is a straight chain or branched alkyl group having 1 to 6 carbon atoms. Examples thereof include methyl group, 20 ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, sec-butyl group, tert-butyl group, pentyl group, isopentyl group, neopentyl group, tert-pentyl group, hexyl group and the like, with preference given to straight chain and branched alkyl group having 1 to 4 25 carbon atoms. Particularly preferred are methyl group, ethyl group and isopropyl group. For R20 or R , it is 6 preferably methyl group. For R , it is preferably methyl 7 8 11 12 13 group or ethyl group, for R , R , R , R or R , it is preferably ethyl group, propyl group or butyl group, and 30 for R 9 or R1 0 , it is preferably methyl group or ethyl group. Preferable C1-6 alkyl group as a substituent of C 4 1 0 cycloalkylalkyl group for R 7, R , R , R12 or R is methyl group or ethyl group. For R', it is preferably methyl group or ethyl group. 35 The "Ci-6 alkyl group optionally substituted by 2 97 C.'*'"'d'Sp'''''""n ' AU2008201550 changess tracked)doc halogen atom" in the formula (IX) is the aforementioned C1-6 alkyl group optionally substituted by the aforementioned halogen atom. Examples thereof include methyl group, ethyl group, propyl group, isopropyl group, 5 butyl group, isobutyl group, sec-butyl group, tert-butyl group, pentyl group, isopentyl group, neopentyl group, tert-pentyl group, hexyl group, trifluoromethyl group, 1 or 2-chloroethyl group, 1- or 2-bromoethyl group, 1- or 2 fluoroethyl group, 1-, 2- or 3-chloropropyl group, 1-, 2 10 or 3-bromopropyl group, 1-, 2- or 3-fluoropropyl group, 1-, 2-, 3- or 4-chlorobutyl group, 1-, 2-, 3- or 4-bromobutyl group, 1-, 2-, 3- or 4-fluorobutyl group and the like, with preference given to methyl group, ethyl group and trifluoromethyl group. For R , R 2, R', R4 or R', it is 15 preferably methyl group, ethyl group or trifluoromethyl group. The "C16 alkoxy group" in the formula (IX) is a straight chain or branched alkoxy group having 1 to 6 carbon atoms. Examples thereof include methoxy group, 20 ethoxy group, propoxy group, isopropoxy group, butoxy group, tert-butoxy group, pentyloxy group, tert-pentyloxy group and hexyloxy group, with preference given to methoxy group, ethoxy group, isopropoxy group, butoxy group and tert-butoxy group, all having 1 to 4 carbon atoms. 25 Particularly preferred are methoxy group and ethoxy group. For R , it is preferably methoxy group. Preferable C1-6 alkoxy group as a substituent of C4-i0 cycloalkylalkyl 7 8 11 12 13 group for R , R , R , R or R is methoxy group or ethoxy group. 30 The "C-6 alkoxy group optionally substituted by halogen atom" in the formula (IX) is the aforementioned C1-6 alkoxy group optionally substituted by the aforementioned halogen atom. Examples thereof include methoxy group, ethoxy group, propoxy group, isopropoxy 35 group, butoxy group, tert-butoxy group, pentyloxy group, 298 C oVp'r'rdVSpe' Ic'"''of'' AU2o8201o550(r geso. raked) doc tert-pentyloxy group, hexyloxy group, trifluoromethoxy group, 1- or 2-chloroethoxy group, 1- or 2-bromoethoxy group, 1- or 2-fluoroethoxy group, 1-, 2- or 3 chloropropoxy group, 1-, 2- or 3-bromopropoxy group, 1-, 5 2- or 3-fluoropropoxy group, 1-, 2-, 3- or 4-chlorobutoxy group, 1-, 2-, 3- or 4-bromobutoxy group, 1-, 2-, 3- or 4 fluorobutoxy group and the like, with preference given to methoxy group, ethoxy group and trifluoromethoxy group. For R , R 4 or R , it is preferably methoxy group, ethoxy 10 group or trifluoromethoxy group. The "C1-6 alkylthio group optionally substituted by halogen atom" in the formula (IX) is Ci- 6 alkylthio group optionally substituted by the aforementioned halogen atom. Examples thereof include methylthio group, ethylthio group, 15 propylthio group, isopropylthio group, butylthio group, tert-butylthio group, pentylthio group, tert-pentylthio group, hexylthio group, trifluoromethylthic group, 1- or 2-chloroethylthio group, 1- or 2-bromoethylthio group, 1 or 2-fluoroethylthio group, 1-, 2- or 3-chloropropylthio 20 group, 1-, 2- or 3-bromopropylthio group, 1-, 2- or 3 fluoropropylthio group, 1-, 2-, 3- or 4-chlorobutylthio group, 1-, 2-, 3- or 4-bromobutylthio group, 1-, 2-, 3- or 4-fluorobutylthio group and the like, with preference given to methylthio group, ethylthio group and 25 trifluoromethylthio group. For R 3 , R 4 or R', it is preferably methylthio group, ethylthio group or trifluoromethylthio group. The "C 4

-

10 cycloalkylalkyl group" in the formula (IX) is C1-3 alkyl group substituted by C3-7 cycloalkyl group. 30 As used herein, the "C3-7 cycloalkyl group" means a cycloalkyl group having 3 to 7 carbon atoms. Specific examples thereof include cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group and cycloheptyl group, with preference given to cycloalkyl group having 3 3s to 6 carbon atoms. Specific examples thereof include 299 C'poV*W'Sp'cifi" on'o'AU020 550 (changesO tr.ckod)doc cyclopropyl group, cyclobutyl group, cyclopentyl group and cyclohexyl group. The "Cim alkyl group" is a straight chain or branched alkyl group having 1 to 3 carbon atoms. Examples thereof include methyl group, ethyl group, propyl 5 group and isopropyl group, with preference given to methyl group, ethyl group and propyl group. Specific examples of the "C 4

-

1 0 cycloalkylalkyl group" in the formula (IX) include cyclopropylmethyl group, cyclobutylmethyl group, cyclopentylmethyl group, 10 cyclohexylmethyl group, cycloheptylmethyl group, cyclopentylethyl group (1- or 2-(cyclopentyl)ethyl group), cyclohexylethyl group (1- or 2-(cyclohexyl)ethyl group), cyclopentylpropyl group (1-, 2- or 3-(cyclopentyl)propyl group) and cyclohexylpropyl group (1-, 2- or 3 15 (cyclohexyl)propyl group) . Preferred is cycloalkylalkyl group having 3 to 7 carbon atoms. Specific examples thereof include cyclopropylmethyl group, cyclobutylmethyl group, cyclopentylmethyl group and cyclohexylmethyl group. 7 8 11 12 Preferable C 4

-

1 0 cycloalkylalkyl group for R , R , R , R 20 or R 13 is cyclopentylmethyl group, cyclohexylmethyl group or 2-(cyclopentyl)ethyl group. The "acyl group" in the formula (IX) is an alkylcarbonyl group such as acetyl group, propionyl group, butyryl group, pivaloyl group and the like; or an 25 arylcarbonyl group such as benzoyl group, naphthoyl and 6 the like, with preference given to acetyl group. For R it is preferably acetyl group. Preferable acyl group as a 7 8 11 substituent of C 4 -10 cycloalkylalkyl group for R , R , R R or R is acetyl group. 30 The "aryl group" in the formula (IX) is phenyl group, naphthyl group, biphenyl group and the like, with preference given to phenyl group. The "heterocyclic residue" in the formula (IX) is a 5- to 8-membered aromatic heterocyclic group having 1 to 4 35 heteroatoms selected from oxygen atom, sulfur atom and 3 00 C'of'rdVSp'fl't'on of AU2008201550 (cha.n. tracked) do nitrogen atom, and the like other than carbon atom, and bicyclic or tricyclic condensed heterocyclic group fused thereto and the like. Examples thereof include pyrrolyl group (1-, 2- or 3-pyrrolyl group), furyl group (2- or 3 5 furyl group), thienyl group (2- or 3-thienyl group), imidazolyl group (1-, 2-, 4- or 5-imidazolyl group), oxazolyl group (2-, 4- or 5-oxazolyl group), thiazolyl group (2-, 4- or 5-thiazolyl group), pyrazolyl group (1-, 3-, 4- or 5-pyrazolyl group), isoxazolyl group (3-, 4- or 10 5-isoxazolyl group), isothiazolyl group (3-, 4- or 5 isothiazolyl group), oxadiazolyl group (1,2,4-oxadiazol-3 or 5-yl group, 1,3,4-oxadiazol-2-yl group, 1,2,5 oxadiazol-3-yl group), thiadiazolyl group (1,2,4 thiadiazol-3 or 5-yl group, 1,3,4-thiadiazol-2-yl group, 15 1,2,5-thiadiazol-3-yl group), triazolyl group (1,2,4 triazol-1, 3, 4 or 5-yl group, 1,2,3-triazol-1, 2 or 4-yl group), indolyl group (1-, 2-, 3-, 4-, 5-, 6- or 7-indolyl group), benzofuryl group (2-, 3-, 4-, 5-, 6- or 7 benzofuryl group), benzothienyl group (2-, 3-, 4-, 5-, 6 20 or 7-benzothienyl group), benzimidazolyl group (1-, 2-, 4-, 5-, 6- or 7-benzimidazolyl group), benzoxazolyl group (2-, 4-, 5-, 6- or 7-benzoxazolyl group), benzothiazolyl group (2-, 4-, 5-, 6- or 7-benzothiazolyl group), pyridyl group (2-, 3- or 4-pyridyl group), pyridine-1-oxide group (2-, 25 3- or 4-pyridine-l-oxide group), pyrimidinyl group (2-, 4 or 5-pyrimidinyl group), tetrazolyl group (lH-tetrazol-1 or 5-yl group, 2H-tetrazol-2 or 5-yl group), quinolyl group (2-, 3-, 4-, 5-, 6-, 7- or 8-quinolyl group), isoquinolyl group (1-, 3-, 4-, 5-, 6-, 7- or 8-isoquinolyl 30 group) and the like. As the "homocyclic ring" in the formula (IX), optionally condensed 3- to 7-membered carbocyclic ring and the like can be used. Examples thereof include C 6

-

10 arene

(C

6 -jo aryl) (e.g., benzene (phenyl), naphthalene 35 (naphthyl) etc.), C3-, cycloalkane (C3-7 cycloalkyl) (e.g., 301 C:pof 'd' Sp'' '' '"^on of AU2008201550 ( ngeo. tr.ckid) c cyclopropane (cyclopropyl), cyclobutane (cyclobutyl), cyclopentane (cyclopentyl), cyclohexane (cyclohexyl), cycloheptane (cycloheptyl) etc.), C3-7 cycloalkene (C3-7 cycloalkenyl) (e.g., cyclopropene (cyclopropenyl), 5 cyclobutene (cyclobutenyl), cyclopentene (cyclopentenyl), cyclohexene (cyclohexenyl), cycloheptane (cycloheptenyl) etc.) and the like. The parenthesis attached to each homocyclic ring shows a homocyclic group corresponding to the homocyclic ring. 10 As the substituent that the above-mentioned homocyclic ring may have, for example, (1) C1-6 alkyl group optionally substituted by halogen (of which C1-6 alkyl group substituted by halogen is preferable.), (2) C 3

-

10 cycloalkyl group, (3) C2-10 alkenyl group, (4) C2-10 alkynyl 15 group, (5) C6-10 aryl group, (6) C7-20 aralkyl group, (7) nitro group, (8) hydroxy group, (9) mercapto group, (10) oxo group, (11) thioxo group, (12) cyano group, (13) carbamoyl group, (14) carboxyl group, (15) C1-6 alkoxycarbonyl group (e.g., methoxycarbonyl group, 20 ethoxycarbonyl group etc.), (16) sulfo, (17) halogen atom, (18) C1.6 alkoxy group, (19) C6-10 aryloxy group (e.g., phenoxy group etc.), (20) C-6 acyloxy group (e.g., acetoxy, propionyloxy), (21) Ci-6 alkylthio group (e.g., methylthio group, ethylthio group, n-propylthio group, isopropylthio 25 group, n-butylthio group, tert-butylthio group etc.), (22) C6-10 arylthio group (e.g., phenylthio group etc.), (23) Ci 6 alkylsulfinyl group (e.g., methylsulfinyl group, ethylsulfinyl group etc.), (24) C-10 arylsulfinyl group (e.g., phenylsulfinyl group etc.), (25) C1-6 alkylsulfonyl 30 group (e.g., methylsulfonyl group, ethylsulfonyl group etc.), (26) C6-io arylsulfonyl group (e.g., phenylsulfonyl group etc.), (27) amino group, (28) C1-6 acylamino group (e.g., acetylamino group, propionylamino group etc.), (29) mono- or di-C- 4 alkylamino group (e.g., methylamino group, 35 ethylamino group, n-propylamino group, isopropylamino 30 2 CVpo "'VSpd"'' '^n of AU20012O15 (hes t.a.cd) .

group, n-butylamino group, dimethylamino group, diethylamino group etc.), (30) C3-8 cycloalkylamino group (e.g., cyclopropylamino group, cyclobutylamino group, cyclopentylamino group, cyclohexylamino group etc.), (31) 5 C6-io arylamino group (e.g., anilino etc.), (32) C1-6 alkanoyl group (e.g., formyl group, acetyl group, hexanoyl group etc.), (33) C 6

-

10 arylcarbonyl group (e.g., benzoyl group etc.), (34) 5- or 6-membered heterocyclic group (e.g., 2- or 3-thienyl group, 2- or 3-furyl group, 3-, 4 10 or 5-pyrazolyl group, 2-, 4- or 5-thiazolyl group, 3-, 4 or 5-isothiazolyl group, 2-, 4- or 5-oxazolyl group, 3-, 4- or 5-isoxazolyl group, 2-, 4- or 5-imidazolyl group, 1,2,3- or 1,2,4-triazolyl (1,2,4-triazol-1,3,4 or 5-yl group, 1,2,3-triazol-1, 2 or 4-yl group), 1H or 2H 15 tetrazolyl (lH-tetrazol-1 or 5-yl group, 2H-tetrazol-2 or 5-yl group), 2-, 3- or 4-pyridyl group, 2-, 4- or 5 pyrimidyl group, 3- or 4-pyridazinyl group, quinolyl group (2-, 3-, 4-, 5-, 6-, 7- or 8-quinolyl group), isoquinolyl group (1-, 3-, 4-, 5-, 6-, 7- or 8-isoquinolyl group), 20 indolyl group (1-, 2-, 3-, 4-, 5-, 6- or 7-indolyl group) etc.) having 1 to 4 heteroatoms selected from oxygen, sulfur, nitrogen and the like other than carbon atom, and the like can be mentioned. The number of substitutions is 1 to 6, preferably 1 to 3, more preferably 1 or 2. 25 Preferable examples of the "homocyclic ring optionally having substituents" in the formula (IX), which may be formed by R 3 and R 4 or R 4 and R 5 together with a carbon atom bonded thereto is C3-7 cycloalkane and benzene, more preferably cyclopentane and cyclohexane. 30 As the "heterocyclic ring" in the formula (IX), a 5 to 8-membered heterocyclic ring having 1 to 4 heteroatoms selected from oxygen atom, sulfur atom and nitrogen atom and the like other than carbon atom, and bicyclic or tricyclic condensed heterocyclic ring fused thereto and 35 the like can be mentioned. Specific examples of the 30 3 C "Vpo"V 'Sp 'fi'ton of AU20082O1s5o chargess t ckd).io heterocyclic ring include (1) 5-membered heterocyclic ring having 1 to 4 heteroatoms selected from oxygen atom, sulfur atom, nitrogen atom and the like other than carbon atom, such as thiophene (thienyl group), furan (furyl 5 group), pyrrole (pyrrolyl group), pyrroline (pyrrolinyl group), pyrrolidine (pyrrolidinyl group), 1,3-dioxole (1,3-dioxolyl group), oxazole (oxazolyl group), thiazole (thiazolyl group), pyrazole (pyrazolyl group), imidazole (imidazolyl group), imidazoline (imidazolinyl group), 10 isoxazole (isoxazolyl group), isothiazole (isothiazolyl group), furazan (furazanyl group), 1,2,3-thiadiazole (1,2,3-thiadiazolyl group), 1,2,5-thiadiazole (1,2,5 thiadiazolyl group), 1,2,3-triazole (1,2,3-triazolyl group), 1,2,3-triazolidine (triazolidinyl group) and the 15 like; (2) 6-membered heterocyclic ring having 1 to 4 heteroatoms selected from oxygen atom, sulfur atom, nitrogen atom and the like other than carbon atom, such as pyridine (pyridyl group), pyrimidine (pyrimidinyl group), thiomorpholine 20 (thiomorpholinyl group), morpholine (morpholinyl group), 1,2,3-triazine, 1,2,4-triazine (triazinyl group), piperidine (piperidinyl group), pyran (pyranyl group), thiopyran (thiopyranyl group), 1,4-oxazine (1,4-oxazinyl group), 1,4-dioxane (1,4-dioxanyl group), 1,4-thiazine 25 (1,4-thiazinyl group), 1,3-thiazine (1,3-thiazinyl group), piperazine (piperazinyl group), oxotriazine (oxotriazinyl group), pyridazine (pyridazinyl group), pyrazine (pyrazinyl group) and the like can be mentioned. As the bicyclic or tricyclic condensed heterocyclic ring, a 30 bicyclic or tricyclic condensed heterocyclic ring having 1 to 4 heteroatoms selected from oxygen atom, sulfur atom, nitrogen atom and the like other than carbon atom can be mentioned. Examples thereof include benzofuran (benzofuryl group), benzothiazole (benzothiazolyl group), 35 benzoxazole (benzoxazolyl group), tetrazolo[1,5 30 4 C:*pof*V Sp'df''ca"on of AU2o2Q15W (changes tracked) doc b]pyridazine (tetrazolo[1,5-b]pyridazinyl group), triazolo[4,5-b]pyridazine (triazolo[4,5-b]pyridazinyl group), benzimidazole (benzimidazolyl group), quinoline (quinolyl group), isoquinoline (isoquinolyl group), 5 cinnoline (cinnolinyl group), phthalazine (phthalazinyl group), quinazoline (quinazolinyl group), quinoxaline (quinoxalinyl group), indolizine (indolizinyl group), indole (indolyl group), quinolizidine (quinolizinyl group), 1,8-naphthyridine (1,8-naphthyridinyl group), pteridine 10 (pteridinyl group), dibenzofuran (dibenzofuranyl group), carbazole (carbazolyl group), acridine (acrydinyl group), phenanthridine (phenanthridinyl group), chromane (chromanyl group), benzoxazine (benzoxazinyl group), phenazine (phenazinyl group), phenothiazine 15 (phenothiazinyl group), phenoxazine (phenoxazinyl group) and the like. The parenthesis attached to each heterocyclic ring shows a heterocyclic group corresponding to the heterocyclic ring. As the substituent that the above-mentioned 20 heterocyclic ring may have, for example, (1) C 1 _ alkyl group, (2) C 2 -6 alkenyl group, (3) C 2

-

6 alkynyl group, (4)

C

3 6 cycloalkyl group, (5) cycloalkenyl group, (6) C 7

-

11 aralkyl group, (7) C6- 14 aryl group, (8) Ci-6 alkoxy group, (9) C 6

-

14 aryloxy group (e.g., phenoxy group etc.), (10) Ci_ 25 6 alkanoyl group (e.g., formyl group, acetyl group, propionyl group, n-butyryl group, iso-butyryl group etc.), (11) C 6

-

14 arylcarbonyl group (e.g., benzoyl group etc.), (12) C 1

-

6 alkanoyloxy group (e.g., formyloxy group, acetyloxy group, propionyloxy group, n-butyryloxy group, 30 iso-butyryloxy group etc.), (13) C6-14 arylcarbonyloxy group (e.g., benzoyloxy group etc.), (14) carboxyl group, (15) C1-6 alkoxycarbonyl group (e.g., methoxycarbonyl group, ethoxycarbonyl group, n-propoxycarbonyl group, iso propoxycarbonyl group, n-butoxycarbonyl group, 35 isobutoxycarbonyl group, tert-butoxycarbonyl group etc.), 305 C *Vpo*V*rd Spc f* of AU2 201550 (h ngoe tracked) doc (16) carbamoyl group, (17) N-mono-C- 4 alkylcarbamoyl group (e.g., N-methylcarbamoyl group, N-ethylcarbamoyl group, N propylcarbamoyl group, N-isopropylcarbamoyl group, N butylcarbamoyl group etc.), (18) N,N-di-Cl- 4 alkylcarbamoyl 5 group (e.g., N,N-dimethylcarbamoyl group, N,N diethylcarbamoyl group, N,N-dipropylcarbamoyl group, N,N dibutylcarbamoyl group etc.), (19) cyclic aminocarbonyl group (e.g., 1-aziridinylcarbonyl group, 1 azetidinylcarbonyl group, 1-pyrrolidinylcarbonyl group, 1 10 piperidinylcarbonyl group, N-methylpiperazinylcarbonyl group, morpholinocarbonyl group etc.), (20) halogen atom, (21) C 1 s alkyl group optionally substituted by halogen atom (e.g., chloromethyl group, dichloromethyl group, trifluoromethyl group, trifluoroethyl group etc.), (22) 15 oxo group, (23) amidino group, (24) imino group, (25) amino group, (26) mono- or di-C 1 4 alkylamino group (e.g., methylamino group, ethylamino group, propylamino group, isopropylamino group, butylamino group, dimethylamino group, diethylamino group, dipropylamino group, 20 diisopropylamino group, dibutylamino group etc.), (27) 3 to 6-membered cyclic amino group (e.g., aziridinyl group, azetidinyl group, pyrrolidinyl group, pyrrolinyl group, pyrrolyl group, imidazolyl group, pyrazolyl group, imidazolidinyl group, piperidino group, morpholino group, 25 dihydropyridyl group, pyridyl group, N-methylpiperazinyl group, N-ethylpiperazinyl group etc.) which may have 1 to 3 heteroatoms selected from oxygen atom, sulfur atom, nitrogen atom and the like other than carbon atom and one nitrogen atom, (28) C 1

-

6 alkanoylamino group (e.g., 30 formamide group, acetamide group, trifluoroacetamide group, propionyl amide group, butyryl amide group, isobutyryl amide group etc.), (29) benzamide group, (30) carbamoylamino group, (31) N-C- 4 alkylcarbamoylamino group (e.g., N-methylcarbamoylamino group, N-ethylcarbamoylamino 35 group, N-propylcarbamoylamino group, N 3 0 6 V*'**''''''''"'''" o AU20D201550 (c nge. traco d). oc isopropylcarbamoylamino group, N-butylcarbamoylamino group etc.), (32) N,N-di-C 1 4 alkylcarbamoylamino group (e.g., N,N-dimethylcarbamoylamino group, N,N diethylcarbamoylamino group, N,N-dipropylcarbamoylamino 5 group, N,N-dibutylcarbamoylamino group etc.), (33) C1-3 alkylenedioxy group (e.g., methylenedioxy group, ethylenedioxy group etc.), (34) -B(OH) 2 , (35) hydroxy group, (36) epoxy group (-0-), (37) nitro group, (38) cyano group, (39) mercapto group, (40) sulfo group, (41) 10 sulfino group, (42) phosphono group, (43) sulfamoyl group, (44) C1- alkylsulfamoyl group (e.g., N-methylsulfamoyl group, N-ethylsulfamoyl group, N-propylsulfamoyl group, N isopropylsulfamoyl group, N-butylsulfamoyl group etc.), (45) di-C- 6 alkylsulfamoyl group (e.g., N,N 15 dimethylsulfamoyl group, N,N-diethylsulfamoyl group, N,N dipropylsulfamoyl group, N,N-dibutylsulfamoyl group etc.), (46) C1s alkylthio group (e.g., methylthio group, ethylthio group, propylthio group, isopropylthio group, n butylthio group, sec-butylthio group, tert-butylthio group 20 etc.), (47) phenylthio group, (48) C1-6 alkylsulfinyl group (e.g., methylsulfinyl group, ethylsulfinyl group, propylsulfinyl group, butylsulfinyl group etc.), (49) phenylsulfinyl group, (50) C1-6 alkylsulfonyl group (e.g., methylsulfonyl group, ethylsulfonyl group, propylsulfonyl 25 group, butylsulfonyl group etc.), (51) phenylsulfonyl group and the like can be mentioned. The number of substitutions is 1 to 6, preferably 1 to 3, more preferably 1 to 2. Preferable examples of the "heterocyclic ring 30 optionally having substituents" in the formula (IX), which may be formed by R 3 and R 4 or R 4 and R 5 together with a carbon atom bonded thereto, include thiophene, furan, pyrrole, pyrroline, oxazole, thiazole, pyrazole, imidazole, imidazoline, isoxazole, isothiazole, furazan, 1,2,3 35 thiadiazole, 1,2,5-thiadiazole, 1,2,3-triazole, 1,2,3 307 C:Vpof 'rd Spo'f''' on of A 2008201550 (eango. tr.cked).doc triazine, 1,2,4-triazine, 1,2,3-triazolidine, 2,2 difluoro-1,3-dioxole and 2,2,3,3-tetrafluoro-1,4-dioxane. In the above-mentioned embodiment of the formula (IX), it is preferable that the substituent in the 5 "homocyclic ring optionally having substituents" and the substituent in the "heterocyclic ring optionally having substituents" are selected from the group consisting of (1) C 1 6 alkyl group optionally substituted by halogen atom, (2) nitro group, (3) hydroxy group, (4) mercapto group, l0 (5) cyano group, (6) carbamoyl group, (7) carboxyl group, (8) C 1 6 alkoxycarbonyl group, (9) sulfo group, (10) halogen atom, (11) C 1 6 alkoxy group, (12) C 1 - alkylthio group, (13) C 1 6 alkylsulfinyl group, (14) C 1

-

6 alkylsulfonyl group, (15) amino group, (16) mono- or di 15 C 1

-

4 alkylamino group, (17) C 1

-

6 alkanoyl group and (18) C1-6 alkanoyloxy group. The "pharmaceutically acceptable salt" of the formula (IX) may be any as long as it forms a nontoxic salt with a compound represented by the above-mentioned 20 formula (IX). Examples thereof include, but not limited to, inorganic acid salts such as hydrochloride, hydrobromide, hydroiodide, sulfate, nitrate, phosphate, carbonate, hydrogen carbonate, perchlorate etc.; organic acid salts such as formate, acetate, trifluoroacetate, 25 propionate, oxalate, glycolate, succinate, lactate, maleate, hydroxymaleate, methylmaleate, fumarate, adipate, tartrate, malate, citrate, benzoate, cinnamate, ascorbate, salicylate, 2-acetoxybenzoate, nicotinate, isonicotinate etc.; sulfonates such as methanesulfonate, ethanesulfonate, 30 isethionate, benzenesulfonate, p-toluenesulfonate, naphthalenesulfonate etc.; acidic amino acid salts such as aspartate, glutamate etc.; alkali metal salts such as sodium salt, potassium salt etc.; alkaline earth metal salts such as magnesium salt, calcium salt etc.; ammonium 35 salt; organic base salts such as trimethylamine salt, 3 0 8 C:Vpo*r**oSp ' *Von of AU2008201550 (changes trcAed)doc triethylamine salt, pyridine salt, picoline salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt etc.; and amino acid salts such as lysin salt, arginine salt etc. In some cases, it may be a water-containing 5 product, a hydrate or a solvate with alcohol and the like. In the compound represented by the above-mentioned formula (IX), various isomers can be present. Examples thereof include E form and Z form as geometric isomers, and, when an asymmetric carbon atom exists, enantiomer and 10 diastereomer are present as stereoisomers based thereon, and tautomer can be present. Accordingly, the compound of the formula (IX) encompasses all these isomers and a mixture thereof. Here, the compound of the formula (IX) also 15 encompasses prodrug compounds and metabolites. The "prodrug compound" of the formula (IX) is a derivative of the compound of the formula (IX), which has a chemically or metabolically degradable group and restores to the original compound to show an intrinsic 20 efficacy after administration to a living organism. It includes a complex and a salt not based on a covalent bond. As a prodrug compound of the compound represented by the formula (IX) of the present invention, a compound represented by the formula (IX) wherein a carboxyl group 25 has been modified by ethyl group, pivaloyloxymethyl group, 1-(acetyloxy)ethyl group, 1-(ethoxycarbonyloxy)ethyl group, 1-(cyclohexyloxycarbonyloxy)ethyl group, carboxylmethyl group, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl group, phenyl group, o-tolyl group and the like; a compound 30 represented by the formula (IX), wherein a hydroxyl group has been modified by acetyl group, propionyl group, isobutyryl group, pivaloyl group, benzoyl group, 4 methylbenzoyl group, dimethylcarbamoyl group or sulfo group; a compound represented by the formula (IX), wherein 35 an amino group has been modified by hexylcarbamoyl group, 309 C "f"''V*'O""''''''''"*A^2008201550 Chag...raedi.dco 3-methylthio-l-(acetylamino)propylcarbonyl group, 1-sulfo 1-(3-ethoxy-4-hydroxyphenyl)methyl group, (5-methyl-2-oxo 1,3-dioxol-4-yl)methyl group and the like, and the like can be mentioned. 5 Specifically, the following compound disclosed in JP-A-2003-221376 can be mentioned: a compound represented by the formula (X) Y 2 N (X)

Y

5 X 1 - A

X

2 X4

X

3 wherein X 1

-X

4 and Y 1

-Y

5 are the same or different and each 1o is a hydrogen atom or any substituent, Z is the formula (XI); -Z 1

-Z

2 wherein Zi is -CO-, -CS- or -SO 2 -, Z 2 is a hydrogen atom, an optionally substituted hydrocarbon group having 1 to 20 carbon atoms, an optionally substituted amino group, an optionally substituted alkoxy group or an 15 optionally substituted alkylthio group, A is a disubstituted amino group, an optionally substituted alkoxy group, an optionally substituted alkylthio group or an optionally substituted hydrocarbon group having 1 to 20 carbon atoms, or X 2 and X 3 , X 3 and X 4 or X 4 and A may be 20 taken together to form a homocyclic ring group optionally having substituents or a heterocyclic group optionally having substituents, or a salt thereof. Each term used for the formulas (X) and (XI) is as described in the above-mentioned publication. 25 Specifically, the following compound disclosed in WOOO/18724 (JP-T-2002-525351) can be mentioned: a compound having the formula (XII): 310 C "Vpof 'Sp'fIca'on'of'AU20082155O (cha.ngesraced)doc K Di D2,. R R4 Rg R16 8 Z R 9

R

1 0 Ri''( H R2 n 2-Rlii R3

R

1 4 R13

R

1 2 (XII) or a pharmaceutically acceptable salt thereof, wherein n is an integer selected from 1 through 4: 5 X is oxy; Ri is selected from the group consisting of haloalkyl, haloalkenyl, haloalkoxymethyl, and haloalkenyloxymethyl with the proviso that R 1 has a higher Cahn-Ingold-Prelog stereochemical system ranking than both R 2 and (CHR 3 )n 1o N(A)Q wherein A is the formula (XIII) and Q is the formula (XIV); R6 I ' R9 Rio

R

5 7 D /Y

K

2

-R

1 1

R

4 D R R 14

D

4 -J( / -1

-

(XIV ) Z (XIII) 13 R 12

R

1 5

R

16 is selected from the group consisting of hydrido; alkyl; acyl; aroyl; heteroaroyl; trialkylsilyl; and a 25 spacer selected from the group consisting of a covalent single bond and a linear spacer moiety having a chain length of 1 to 4 atoms linked to the point of bonding of any aromatic substituent selected from the group consisting of R 4 , R 8 , R 9 and R 13 to form a heterocyclyl 20 ring having from 5 through 10 continuous members: 311 C:po 'rd'Sp''*tIon of AU2008201550 (changes tracaed)doc

D

1 , D 2 , Ji, J 2 and Ki are independently selected from the group consisting of C, N, 0, S and a covalent bond with the proviso that no more than one of D 1 , D 2 , J 1 , J 2 and Ki is a covalent bond; no more than one of D 1 , D 2 , J 1 , J 2 and 5 Ki is 0; no more than one of D 1 , D 2 , J 1 , J 2 and Ki is S; one of

D

1 , D 2 , J 1 , J 2 and Ki must be a covalent bond when two of D 1 ,

D

2 , J 1 , J 2 and Ki are 0 and S; and no more than four of Di , D 2 , J 1 , J 2 and Ki are N; 10 D 3 , D 4 , J 3 , J 4 and K 2 are independently selected from the group consisting of C, N, 0, S and a covalent bond with the proviso that no more than one of D 3 , D 4 , J 3 , J 4 and K2 is a covalent bond; no more than one of D 3 , D 4 , J 3 , J 4 and

K

2 is 0; no more than one of D 3 , D 4 , J 3 , J 4 and K 2 is S; no 15 more than two of D 3 , D 4 , J 3 , J 4 and K2 are 0 and S; one of

D

3 , D 4 , J 3 , J 4 and K 2 must be a covalent bond when two of D 3 ,

D

4 , J 3 , J 4 and K 2 are 0 and S; and no more than four of D 3 ,

D

4 , J 3 , J 4 and K2 are N;

R

2 is selected from the group consisting of hydrido, aryl, 20 aralkyl, alkyl, alkenyl, alkenyloxyalkyl, haloalkyl, haloalkenyl, halocycloalkyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, dicyanoalkyl, and carboalkoxycyanoalkyl with 25 the proviso that R 2 has a lower Cahn-Ingold-Prelog system ranking than both Ri and (CHR 3 ),-N(A)Q;

R

3 is selected from the group consisting of hydrido, hydroxy, cyano, aryl, aralkyl, acyl, alkoxy, alkyl, alkenyl, alkoxyalkyl, heteroaryl, alkenyloxyalkyl, 30 haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, monocyanoalkyl, dicyanoalkyl, carboxamide, and carboxamidoalkyl with the provisos that

(CHR

3 ),-N(A)Q has a lower Cahn Ingold-Prelog stereochemical system ranking than Ri and a higher Cahn 35 Ingold-Prelog stereochemical system ranking than R 2 ; 312 C *Vpof''dSpo*f*c*" ^ of AU2008201550 (chnes tracked)oc Y is selected from a group consisting of a covalent single bond, (C(R14)2)q wherein q is an integer selected from 1 and 2 and (CH(R 14 ) )g-W-(CH(R 14 ))p wherein g and p are integers independently selected from 0 and 1; 5 R 1 4 is selected from the group consisting of hydrido, hydroxy, cyano, hydroxyalkyl, acyl, alkoxy, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, monocarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, 10 carboalkoxy, carboxamide, and carboxamidoalkyl; Z is selected from the group consisting of a covalent single bond, (C(Ri5)2)q wherein q is an integer selected from 1 and 2, and (CH(R 15 ))j-W-(CH(R 15 ))k wherein j and k are integers independently selected from 0 and 1: 15 W is selected from the group consisting of 0, C(O), C(S),

C(O)N(R

14 ), C(S)N(R 14 ), (R 1 4 )NC(O), (R 1 4 )NC(S), S, S(O), S (0) 2, S(0) 2 N (R 14 ) , (R 1 4 ) NC (0)2, and N (R 1 4 ) with the proviso that R 1 4 is other than cyano;

R

15 is selected from the group consisting of hydrido, 20 cyano, hydroxyalkyl, acyl, alkoxy, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, monocarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, carboalkoxy, carboxamide, and carboxamidoalkyl; 25 R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 1 2 , and R 13 are independently selected from the group consisting of hydrido, carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aroylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, 30 aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, 35 heteroarylamino, N-heteroarylamino-N-alkylamino, 313 C *po''' S'cJfIc'o ^ of AU2008201550 changess trcki)oc heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, 5 halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl, hydroxy, amino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, 10 arylsulfonylalkyl, heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkyl-amidosulfonyl, dialkyl-amidosulfonyl, 15 monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl-monoaryl-amidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, 20 aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, 25 haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, heteroaralkynyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, 30 heteroaralkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylaminodocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, 35 phosphono, phosphonoalkyl, diaralkoxyphosphono, and 312.4 C:WpfVrdVSpCaflc8iOfl of AU2008201550 (changes tracked) dc diaralkoxyphosphonoalkyl with the proviso that R 4 , R 5 , R 6 ,

R

7 , Re, R9, Rio, R 11 , R 12 , and R 13 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of 5 sulfur, and the divalent nature of oxygen;

R

4 and R 5 , R 5 and R 6 , R 6 and R 7 , R 7 and Re, R 9 and Rio, Rio and

R

11 , R 11 and R 1 2 , and R 12 and R 13 are independently selected to form spacer pairs wherein a spacer pair is taken io together to form a linear moiety having from 3 through 6 continuous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 continuous members, a partially saturated heterocyclyl 15 ring having 5 through 8 continuous members, a heteroaryl ring having 5 through 6 continuous members, and an aryl with the provisos that no more than one of the group consisting of spacer pairs R 4 and R 5 , R 5 and R 6 , R 6 and R 7 , and R 7 and Re, is used at the same time and that no more 20 than one of the group consisting of spacer pairs R 9 and Rio, Rio and

R

11 , Rii and R 12 , and R 1 2 and R 13 is used at the same time;

R

4 and R 9 , R 4 and R 13 , Re and R 9 , and Re and R 1 3 are independently selected to form a spacer pair wherein said 25 spacer pair is taken together to form a linear moiety wherein said linear moiety forms a ring selected from the group consisting of a partially saturated heterocyclyl ring having from 5 through 8 continuous members and a heteroaryl ring having from 5 through 6 continuous members 30 with the proviso that no more than one of the group consisting of spacer pairs R 4 and R9, R 4 and R 13 , Re and R 9 , and Re and R 13 is used at the same time. Each term used for the formulas (XII), (XIII) and (XIV) is as described in the above-mentioned publication. 35 Specifically, the following compound disclosed in 315 C'*'o ''rd "Spcl*l2l 2 of AU 2 S c01550 (ang.. tr.cked).c WOOO/18721 (JP-T-2002-525348) can be mentioned: a compound represented by the formula (XV):

R

6

R

5 , K 6 R 7

R

16 D DI 2(CR 3 H) -N R I1 R9 R

D

3 R13-D4

J

3

-R

1 O

J

4

-K

2 / \ R12

R

11 or a pharmaceutically acceptable salt thereof, wherein; 5 n is an integer selected from 0 through 5; Ri is selected from the group consisting of haloalkyl, haloalkenyl, haloalkoxyalkyl and haloalkenyloxyalkyl; X is selected from the group consisting of 0, H, F, S, S(0), NH, N(OH), N(alkyl), and N(alkoxy); l0 Ri 6 is selected from the group consisting of hydrido, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, 15 cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, 20 monocarboalkoxyalkyl, monocarboalkoxy, dicarboalkoxyalkyl, monocarboxamido, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, dialkoxyphosphonoalkyl, trialklylsilyl, 31c6 Vporv rdVSpmcation of AU200a201550 (Ohan tracked).doc and a spacer selected from the group consisting of a covalent single bond and a linear spacer moiety having from 1 through 4 continuous atoms linked to the point of bonding of an aromatic substituent selected from the group 5 consisting of R 4 , R 8 , R 9 , and R 13 to form a heterocyclyl ring having from 5 through 10 continuous members with the provisos that said spacer moiety is other than a covalent single bond when R 2 is alkyl and there is no R 16 wherein X is H or F; 10 D 1 , D 2 , J1, J2 and Ki are independently selected from the group consisting of C, N, 0, S and a covalent bond with the provisos that no more than one of D 1 , D 2 , Ji, J2 and Ki is a covalent bond, no more than one of D 1 , D 2 , Ji, J2 and Ki is 0, no more than one of D 1 , D 2 , J1, J2 and Ki is S, one 15 of D 1 , D 2 , J1, J2 and Ki must be a covalent bond when two of

D

1 , D 2 , Ji, J2 and Ki are 0 and S, and no more than four of

D

1 , D 2 , J1, J2 and Ki are N;

D

3 , D 4 , J3, J4 and K 2 are independently selected from the group consisting of C, N, 0, S and a covalent bond with 20 the provisos that no more than one of D 3 , D 4 , J3, J4 and K 2 is a covalent bond, no more than one of D 3 , D 4 , J3, J4 and

K

2 is 0, no more than one of D 3 , D 4 , J3, J4 and K 2 is S, one of D 3 , D 4 , J3, J4 and K 2 must be a covalent bond when two of

D

3 , D 4 , J3, J4 and K 2 are 0 and S, and no more than four of 25 D 3 , D 4 , J3, J4 and K 2 are N;

R

2 is independently selected from the group consisting of hydrido, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkoxyalkyl, aryloxyalkyl, alkoxyalkyl, 30 heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, aralkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, 35 haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, 317 C:""*''**''' e**'''''''* o'AU20082O155O (e.ngo. . t.oked)do halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, 5 dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, alkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, 10 cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, 15 carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl and diaralkoxyphosphonoalkyl;

R

2 and R 3 are taken together to form a linear spacer moiety selected from the group consisting of a covalent 20 single bond and a moiety having from 1 through 6 continuous atoms to form a ring selected from the group consisting of a cycloalkyl having from 3 through 8 continuous members, a cycloalkenyl having from 5 through 8 continuous members, and a heterocyclyl having from 4 through 8 continuous 25 members;

R

3 is selected from the group consisting of hydrido, hydroxy, halo, cyano, aryloxy, hydroxyalkyl, amino, alkylamino, dialkylamino, acyl, sulfhydryl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, 30 aralkyl, aryloxyalkyl, alkoxyalkyl, heteroarylthio, aralkylthio, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aroyl, heteroaroyl, aralkylthioalkyl, heteroaralkylthioalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, 35 cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, 318 C"po *dVSpe f*tIo^ of AU2008201550 (dwgea tracked). oc haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, 5 perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, 10 arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, 15 heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl and diaralkoxyphosphonoalkyl; 20 Y is selected from a group consisting of a covalent single bond, (C(R14)2)q wherein q is an integer selected from 1 and 2, and (CH(R 4 ))g-W- CH(R1 4 ))p wherein g and p are integers independently selected from 0 and 1;

R

14 is independently selected from the group consisting 25 of hydrido, hydroxy, halo, cyano, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkylalkoxy, 30 alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, 35 halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, 319 C.""o" 'dVSp'f' " "on of AU20D8201550 change . trk.ed) do haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, 5 monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, 10 cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, 15 carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, a spacer selected from a moiety having a chain length of 3 to 6 atoms connected to the point of bonding selected from the 20 group consisting of R9 and R 13 to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 continuous members and a heterocyclyl ring having from 5 through 8 continuous members, and a spacer selected from a moiety having a chain length of 2 to 5 atoms 25 connected to the point of bonding selected from the group consisting of R 4 and R 8 to form a heterocyclyl having from 5 through 8 continuous members with the proviso that, when Y is a covalent bond, R 14 substituent is not attached to Y;

R

14 and R 14 , when bonded to the different atoms, are 30 taken together to form a group selected from the group consisting of a covalent bond, alkylene, haloalkylene, and a spacer selected from a group consisting of a moiety having a chain length of 2 to 5 atoms connected to form a ring selected from the group of a saturated cycloalkyl 35 having from 5 through 8 continuous members, a cycloalkenyl 3 2 0 C *po*V*rdSp*d'*caon of AU2008201550 (ch** * tra*k*d)*do having from 5 through 8 continuous members, and a heterocyclyl having from 5 through 8 continuous members;

R

14 and R 14 , when bonded to the same atom, are taken together to form a group selected from the group consisting 5 of oxo, thiono, alkylene, haloalkylene, and a spacer selected from the group consisting of a moiety having a chain length of 3 to 7 atoms connected to form a ring selected from the group consisting of a cycloalkyl having from 4 through 8 continuous members, a cycloalkenyl having 10 from 4 through 8 continuous members, and a heterocyclyl having from 4 through 8 continuous members; W is selected from the group consisting of 0, C(0), C(S), C(0)N(R 14 ) , C (S)N(R 14 ), (R 14 )NC(0), (R 14 )NC(S), S, S (O), S(0) 2 , S(0) 2

N(R

14 ), (R 14 )NS(0) 2 , and N(R 14 ) with the proviso 15 that R 14 is selected from other than halo and cyano; Z is independently selected from a group consisting of a covalent single bond, (C(Ri5)2)q wherein q is an integer selected from 1 and 2, and (CH(Rls))j-W-(CH(Ri 5 ))k wherein j and k are integers independently selected from 0 and 1 with 20 the proviso that, when Z is a covalent single bond, R 15 substituent is not attached to Z;

R

15 is independently selected, when Z is (C(Ri5)2)q wherein q is an integer selected from 1 and 2, from the group consisting of hydrido, hydroxy, halo, cyano, aryloxy, 25 amino, alkylamino, dialkylamino, hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, 30 heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenlyl, haloalkoxy, haloalkoxyalkyl, 35 haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, 321 C*p*''*"''' ec'''''''' ''**^20082o155o(cha~ng..racka.>.e halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, 5 dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, 10 cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, 15 carboaralkoxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, a spacer selected from a moiety having a chain length of 3 to 6 atoms connected to the point of bonding selected from the group consisting of R 4 and R 8 to form a ring selected from 20 the group consisting of a cycloalkenyl ring having from 5 through 8 continuous members and a heterocyclyl ring having from 5 through 8 continuous members, and a spacer selected from a moiety having a chain length of 2 to 5 atoms connected to the point of bonding selected from the group 25 consisting of R 9 and R 13 , to form a heterocyclyl having from 5 through 8 continuous members;

R

15 and R 15 , when bonded to the different atoms, are taken together to form a group selected from the group consisting of a covalent bond, alkylene, haloalkylene, and 30 a spacer selected from a group consisting of a moiety having a chain length of 2 to 5 atoms connected to form a ring selected from the group consisting of a saturated cycloalkyl having from 5 through 8 continuous members, a cycloalkenyl having from 5 through 8 continuous members, 35 and a heterocyclyl having from 5 through 8 continuous 32 2 C'VpoV'r"VSpo"fcatIon of AU2oD20155o (ch ne. trcked).doc members;

R

15 and R 15 , when bonded to the same atom, are taken together to form a group selected from the group consisting of oxo, thiono, alkylene, haloalkylene, and a spacer 5 selected from the group consisting of a moiety having a chain length of 3 to 7 atoms connected to form a ring selected from the group consisting of a cycloalkyl having from 4 through 8 continuous members, a cycloalkenyl having from 4 through 8 continuous members, and a heterocyclyl lo having from 4 through 8 continuous members;

R

15 is independently selected, when Z is (CH(Ri 5 ))j-W (CH(R15))k wherein j and k are integers independently selected from 0 and 1, from the group consisting of hydrido, halo, cyano, aryloxy, carboxyl, acyl, aroyl, heteroaroyl, 15 hydroxyalkyl, heteroaryloxyalkyl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl, heteroaryloxyalkyl, aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfonylalkyl, alkylsulfinylalkyl, alkenyloxyalkyl, alkylthioalkyl, 20 arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, 25 halocycloalkenyloxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, 30 alkylsulfonyl, haloalkylsulfinyl, haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, 35 heteroarylsulfonylalkyl, heteroarylsulfinyl, 323 3'*f' S''fic 'o ^ of AU2008201550 (cch.ngo .red) doe heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, a spacer 5 selected from a linear moiety having a chain length of 3 to 6 atoms connected to the point of bonding selected from the group consisting of R 4 and R 8 to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 continuous members and a heterocyclyl ring having 10 from 5 through 8 continuous members, and a spacer selected from a linear moiety having a chain length of 2 to 5 atoms connected to the point of bonding selected from the group consisting of R 9 and R 13 to form a heterocyclyl ring having from 5 through 8 continuous members; 15 R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , RIO, R 11 , R 12 , and R 13 are independently selected from the group consisting of perhaloaryloxy, alkanoylalkyl, alkanoylalkoxy, alkanoyloxy, N-aryl-N-alkylamino, heterocyclylalkoxy, heterocyclylthio, hydroxyalkoxy, carboxamidoalkoxy, alkoxycarbonylalkoxy, 20 alkoxycarbonylalkenyloxy, aralkanoylalkoxy, aralkenoyl, N alkylcarboxamido, N-haloalkylcarboxamido, N cycloalkylcarboxamido, N-arylcarboxamidoalkoxy, cycloalkylcarbonyl, cyanoalkoxy, heterocyclylcarbonyl, hydrido, carboxy, heteroaralkylthio, heteroaralkoxy, 25 cycloalkylamino, acylalkyl, acylalkoxy, aroylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, 30 cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, heteroarylamino, N heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, 35 cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, 3 2 4 C *' 'ordVSp'a'cto of AU2008201550 (chages tracked) doc cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl, hydroxy, amino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, 5 aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, 10 alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkylamidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkylmonoarylamidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, 15 heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloaralkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower 20 cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, heteroaralkynyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, 25 heteroaryloxy, heteroaryloxyalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, 30 carboxamidoalkyl, cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl with the proviso that there are one to five non-hydrido ring substituents R 4 , R 5 , R 6 , R 7 , and R 8 present, that there are one to five non-hydrido ring 35 substituents R 9 , R 10 , R 11 , R 12 , and R 13 present, and R 4 , R 5 , 325 C 'pof' ''Sp'ci'' 'on'of'AU2008201550 (changes tr.ckid)doc

R

6 , R 7 , R 8 , R 9 , RIO, R 11 , R 12 , and R 13 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; 5 R 4 and R 5 , R 5 and R 6 , R 6 and R7, R 7 and R 8 , R 9 and Rio, RIO and R 11 , R 11 and R1 2 , and R 1 2 and R 1 3 are independently selected to form spacer pairs wherein a spacer pair is taken together to form a linear moiety having from 3 through 6 continuous atoms connecting the points of bonding 10 of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 continuous members, a partially saturated heterocyclyl ring having 5 through 8 continuous members, a heteroaryl ring having 5 through 6 continuous members, and 15 an aryl with the provisos that no more than one of the group consisting of spacer pairs R 4 and R 5 , R 5 and R 6 , R 6 and R7, and R 7 and R 8 , is used at the same time and that no more than one of the group consisting of spacer pairs R9 and Rio, Rio and R 11 , R 11 and R 12 , and R 12 and R 13 is used at 20 the same time;

R

4 and R 9 , R 4 and R 1 3 , R 8 and R 9 , and R 8 and R 13 are independently selected to form a spacer pair wherein said spacer pair is taken together to form a linear moiety wherein said linear moiety forms a ring selected from the 25 group consisting of a partially saturated heterocyclyl ring having from 5 through 8 continuous members and a heteroaryl ring having from 5 through 6 continuous members with the proviso that no more than one of the group consisting of spacer pairs R 4 and R 9 , R 4 and R 13 , R 8 and R 9 , 30 and R 8 and R 1 3 is used at the same time. Each term used for the formula (XV) is as described in the above-mentioned publication. Specifically, the following compound disclosed in WOOO/18723 (JP-T-2002-525350) can be mentioned: 35 a compound having the formula (XVI): 32 6 C'V"'''''r''''''''"''o*AU20o820155oren.v... ,.ca.ice / A R2

R

3 (XVI) or a pharmaceutically acceptable salt thereof, wherein n is an integer selected from 1 through 2; 5 A and Q are independently selected from the group consisting of -CH 2

(CR

3 7R 38 ) v- (CR 33

R

34 ) u-T- (CR 35

R

36 ) w-H, R6 R11 R31 AQ-1 AQ-2 \ / R J 3

-K

2 Rio R R32 R4 -- R. and R B12

R

13 with the provisos that one of A and Q must be AQ-1 and that one of A and Q must be selected from the group 1o consisting of AQ-2 and -CH 2

(CR

37

R

3 8 ) v- (CR 3 3

R

34 ) u-T- (CR 35 R3 6 ) w H; T is selected from the group consisting of a single covalent bond, 0, S, S (0) , S (0) 2, C (R 33 ) =C (R 35 ) , and C=C; v is an integer selected from 0 through 1 with the proviso 15 that v is 1 when any one of R 3 3 , R 34 , R 35 , and R 3 6 is aryl or heteroaryl; u and w are integers independently selected from 0 through 6;

A

1 is C (R 30 ); 20 D 1 , D 2 , J 1 , J 2 and Ki are independently selected from the group consisting of C, N, 0, S and a covalent bond with the provisos that no more than one of D 1 , D 2 , J 1 , J 2 and K 1 is a covalent bond, no more than one of Di, D 2 , J 1 , J 2 and 327 C:VpotVwordvSpecitfcaon of AU2008201550 changess tracked).doc

K

1 is 0, no more than one of D 1 , D 2 , J 1 , J 2 and Ki is S, one of D 1 , D 2 , J 1 , J 2 and K 1 must be a covalent bond when two of D 1 , D 2 , J 1 , J 2 and Ki are 0 and S, and no more than four of D 1 , D 2 , Ji, J 2 and K 1 are N; 5 B 1 , B 2 , D 3 , D 4 , J3, J 4 and K 2 are independently selected from the group consisting of C, C(R 3 0 ), N, 0, S and a covalent bond with the provisos that no more than 5 of B 1 ,

B

2 , D 3 , D4, J 3 , J 4 and K 2 are a covalent bond, no more than two of B 1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are 0, no more than two lo of B 1 , B 2 , D 3 , D 4 , J 3 , J 4 and K 2 are S, no more than two of

B

1 , B 2 , D3, D4, J 3 , J 4 and K 2 are simultaneously 0 and S, and no more than two of B 1 , B 2 , D3, D4, J 3 , J 4 and K 2 are N;

B

1 and D3, D3 and J 3 , J 3 and K 2 , K 2 and J 4 , J 4 and D4, and D 4 and B 2 are independently selected to form an in-ring 15 spacer pair wherein said spacer pair is selected from the group consisting of C(R 3 3

)=C(R

3 5 ) and N=N with the provisos that AQ-2 must be a ring of at least five continuous members, that no more than two of the group of said spacer pairs are simultaneously C (R 3 3 )=C (R 3 5 ) , and that no more 20 than one of the group of said spacer pairs are N=N unless the other spacer pairs are other than C (R 3 3 )=C (R 3 5 ) , 0, N, and S; Ri is selected from the group consisting of haloalkyl and haloalkoxymethyl; 25 R 2 is selected from the group consisting of hydrido, aryl, alkyl, alkenyl, haloalkyl, haloalkoxy, haloalkoxyalkyl, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl and heteroaryl;

R

3 is selected from the group consisting of hydrido, aryl, 30 alkyl, alkenyl, haloalkyl and haloalkoxyalkyl; Y is selected from a group consisting of a covalent single bond, (CH2)q wherein q is an integer selected from 1 through 2, and (CH 2 ) j-0-(CH2)k wherein j and k are integers independently selected from 0 through 1; 35 Z is selected from the group consisting of a covalent 3 2 8 C."o ''rdVSp'c'IcIo of AU20082O15O (cangos tracked).doc single bond, (CH2)q wherein q is an integer selected from 1 through 2, and (CH 2 )j-O-(CH2)k wherein j and k are integers independently selected from 0 through 1;

R

4 , R 8 , R 9 and R 1 3 are independently selected from the 5 group consisting of hydrido, halo, haloalkyl and alkyl;

R

30 is selected from the group consisting of hydrido, alkoxy, alkoxyalkyl, halo, haloalkyl, alkylamino, alkylthio, alkylthioalkyl, alkyl, alkenyl, haloalkoxy, and haloalkoxyalkyl with the proviso that R 30 is selected to 10 maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R

3 0 , when bonded to Ai, is taken together to form an intra ring linear spacer connecting the Ai-carbon at the point 15 of attachment of R 30 to the point of bonding of a group selected from the group consisting of R 10 , R 11 , R 1 2 , R 31 , and R 32 wherein said intra-ring linear spacer is selected from the group consisting of a covalent single bond and a spacer moiety having from 1 through 6 continuous atoms to 20 form a ring selected from the group consisting of a cycloalkyl having from 3 through 10 continuous members, a cycloalkenyl having from 5 through 10 continuous members, and a heterocyclyl having from 5 through 10 continuous members; 25 R 30 , when bonded to Ai, is taken together to form an intra ring branched spacer connecting the Ai-carbon at the point of attachment of R 30 to the points of bonding of each member of any one of substituent pairs selected from the group consisting of subsitituent pairs Rio and R 11 , Rio and 30 R 31 , Rio and R 32 , Rio and R 12 , R 11 and R 31 , R 11 and R 32 , R 11 and

R

12 , R 31 and R 32 , R 31 and R 12 , and R 32 and R 12 and wherein said intra-ring branched spacer is selected to form two rings selected from the group consisting of cycloalkyl having from 3 through 10 continuous members, cycloalkenyl 35 having from 5 through 10 continuous members, and 329 C:VpofVodVSpcfIcalIon of AU2008201550 (changes tracked) doc heterocyclyl having from 5 through 10 continuous members;

R

4 , R 5 , R 6 , R7, R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 31 , R 32 , R 33 , R 3 4 ,

R

3 5 , and R 36 are independently selected from the group consisting of hydrido, carboxy, heteroaralkylthio, 5 heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aroylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, 10 cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, 15 cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl, hydroxy, amino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, 20 aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, 25 alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl-monoaryl-amidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, 30 heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, 35 cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower 33 0 C:p,dWS cdflcvto of AU200L2O155o (ce...i trmo.d) c cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, heteroaralkynyl, aryloxy, aralkoxy, aryloxyalkyl, 5 saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, 10 carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl with the provisos that R 4 , R 5 , R 6 ,

R

7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 31 , R 3 2 , R 3 3 , R 3 4 , R 35 , and R 36 15 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen, that no more than three of the R 33 and

R

34 substituents are simultaneously selected from other 20 than the group consisting of of hydrido and halo, and that no more than three of the R 35 and R 3 6 substituents are simultaneously selected from other than the group consisting of of hydrido and halo:

R

9 , R 10 , R 11 , R 12 , R 13 , R 31 , and R 32 are independently 25 selected to be oxo with the provisos that B 1 , B 2 , D 3 , D 4 ,

J

3 , J 4 and K 2 are independently selected from the group consisting of C and S, no more than two of R 9 , RIO, R 1 1 , R 1 2 ,

R

13 , R 3 1 , and R 32 are simultaneously oxo, and that R 9 , R 10 ,

R

11 , R 12 , R 13 , R 31 , and R 32 are each independently selected 30 to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R

4 and R 5 , R 5 and R 6 , R 6 and R 7 , R 7 and R 8 , R 9 and R 10 , R 10 and R 11 , R 11 and R 3 1 , R 3 1 and R 32 , R 32 and R 12 , and R 12 and R 13 35 are independently selected to form spacer pairs wherein a 331 C *Vpo' 'rd''Sp fct"on of AU2 2O1o55 . (...ges acked).dc spacer pair is taken together to form a linear moiety having from 3 through 6 continuous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl 5 ring having 5 through 8 continuous members, a partially saturated heterocyclyl ring having 5 through 8 continuous members, a heteroaryl ring having 5 through 6 continuous members, and an aryl with the provisos that no more than one of the group consisting of spacer pairs R 4 and R 5 , R 5 lo and R 6 , R 6 and R 7 , and R 7 and R8, are used at the same time and that no more than one of the group consisting of spacer pairs R 9 and Rio, Rio and R 11 , R 11 and R 31 , R 3 1 and R 32 ,

R

32 and R 12 , and R 12 and R 13 are used at the same time;

R

9 and R 11 , R 9 and R 12 , R 9 and R 13 , R 9 and R 3 1 , Rg and R 32 , Rio 15 and R 12 , Rio and R 13 , Rio and R 31 , Rio and R 32 , R 11 and R 12 , R 11 and R 13 , R 11 and R 32 , R 12 and R 31 , R 13 and R 31 , and R 13 and R 32 are independently selected to form a spacer pair wherein said spacer pair is taken together to form a linear spacer moiety selected from the group consisting of a covalent 20 single bond and a moiety having from 1 through 3 continuous atoms to form a ring selected from the group consisting of a cycloalkyl having from 3 through 8 continuous members, a cycloalkenyl having from 5 through 8 continuous members, a saturated heterocyclyl having from 5 25 through 8 continuous members and a partially saturated heterocyclyl having from 5 through 8 continuous members with the provisos that no more than one of said group of spacer pairs is used at the same time;

R

37 and R 38 are independently selected from the group 30 consisting of hydrido, alkoxy, alkoxyalkyl, hydroxy, amino, thio, halo, haloalkyl, alkylamino, alkylthio, alkylthioalkyl, cyano, alkyl, alkenyl, haloalkoxy, and haloalkoxyalkyl. Each term used for the formula (XVI) is as described 35 in the above-mentioned publication. 3 3 2 C 'po ''dVSpf''ot'o' ^ of AU20002O150o (e.o.es ,.cked), Specifically, the compound designated with Code Name PD-140195 [Compound (XVII)], which is disclosed in W099/14204, and the like can be mentioned. Specifically, the compound disclosed in JP-A-10 5 67746 can be mentioned: Cycloalkano-pyridine of the formula (XVIII) A D R (XVIII) 2 E N R wherein A is an aryl having 6 to 10 carbon atoms, which can be optionally substituted up to 5 times in an 10 identical or different manner by halogen, nitro, hydroxyl, trifluoromethyl or trifluoromethoxy, or by linear or branched chain alkyl, acyl, hydroxyalkyl or alkoxy, each having up to 7 carbon atoms, or by a group of the formula

-NR

3

R

4 , wherein R 3 and R' are identical or different and 15 each is hydrogen, phenyl or linear or branched chain alkyl having up to 6 carbon atoms, D is aryl having 6 to 10 carbon atoms, which is optionally substituted by phenyl, nitro, halogen, trifluoromethyl or trifluoromethoxy, or is a group represented by the formula 7 8 R R Rs--L R 6 or R 9

-T-V-X

20 wherein R , R 6 and R 9 independently of one another denote cycloalkyl having 3 to 6 carbon atoms, or aryl having 6 to 10 carbon atoms, or a 5- to 7-membered, optionally benzo fused, saturated or unsaturated, mono-, bi- or tricyclic 25 heterocycle having up to 4 heteroatoms from the series S, N and/or 0, where the cycles are substituted, if appropriate, in the case of a nitrogen-containing rings also via an N functional group, up to 5 times in an identical or different manner by halogen, trifluoromethyl, 30 nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, 3 3 3 C"''*'VSp' fi'c 'on ofAU20D2O155o changeo tracked),doc straight-chain or branched acyl, alkyl, alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl, each having up to 6 carbon atoms, by aryl- or trifluoromethyl-substituted aryl, each having 6 to 10 carbon atoms, or by an optionally 5 benzo-fused, aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms from the series S, N and/or 0, and/or are substituted by a group of the formula -OR I, -SR , 12 13 14 10 11 12

SO

2 R or -NR R , wherein R", R and R independently of one another denote aryl having 6 to 10 carbon atoms, which 10 for its part is substituted up to 2 times in an identical or different manner by phenyl, halogen or by straight chain or branched alkyl having up to 6 carbon atoms, R 13 and R 14 are identical or different and have the meaning of

R

3 and R 4 indicated above, or R 5 and/or R 6 denote a group 15 of the formula X or

F

3 0 O: F r 3C O

R

7 denotes a hydrogen or halogen, R 8 denotes hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or 20 alkyl each having up to 6 carbon atoms or a group of the 15 16 15 1 formula -NR1 R , wherein R and R' are identical or different and have the meaning of R 3 and R 4 indicated above, or R and R8 together form a group of the formula =0 or =NR', wherein R 1 is a hydrogen or linear or 25 branched chain alkyl, alkoxy or acyl, each having up to 6 carbon atoms, L is a linear or branched chain alkylene or alkenylene chain each having up to 8 carbon atoms, each of which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and denote a straight 30 chain or branched alkylene chain having up to 8 carbon atoms, or T or X denotes a bond, V represents an oxygen or sulfur atom or an -NR 18 group, wherein R1 8 is a hydrogen or linear or branched chain alkyl having up to 6 carbon atoms 334 C:VpofV-dVSpeifcation of AU2008201550 (changes tracked) doc or phenyl, E denotes cycloalkyl having 3 to 8 carbon atoms, or linear or branched chain alkyl having up to 8 carbon atoms, which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents 5 phenyl which is optionally substituted by halogen or trifluoromethyl, RI and R 2 together form linear or branched alkylene chain having up to 7 carbon atoms, which must be substituted by a carbonyl group and/or a group of the formula 10

(CH

2 )a

CH

2 1, 30-CH 2 I I 1 107 OH -OR19 or 1, 2 0 (CR20 R2 ) b I I wherein a and b are identical or different and denote a number 1, 2 or 3, R 9 denotes hydrogen, cycloalkyl having 15 3 to 7 carbon atoms, straight-chain or branched silylalkyl having up to 8 carbon atoms or straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by hydroxyl, straight-chain or branched alkoxy having up to 6 carbon atoms or by phenyl, which for its 20 part can be substituted by halogen, nitro, trifluoromethyl, trifluoromethoxy or by phenyl- or tetrazole-substituted phenyl, and alkyl is optionally substituted by a group of the formula -OR 22 , wherein R 22 is linear or branched chain acyl or benzyl having up to 4 carbon atoms, or R' 9 is 25 linear or branched chain acyl having up to 20 carbon atoms, or benzoyl which is optionally substituted by halogen, trifluoromethyl, nitro or trifluoromethoxy, or denotes straight-chain or branched fluoroacyl having up to 8 carbon atoms and up to 9 fluorine atoms, R 20 and R 2 1 are 30 identical or different, and denote hydrogen, phenyl or 3 35 C** 'Spoif'c''io' * of AU20082O155o (changes tr.c.ed)do straight-chain or branched alkyl having up to 6 carbon atoms, or R20 and R together form a 3 to 6-membered carbocycle, and, if appropriate also geminally, the carbocycles formed are optionally substituted up to 6 5 times in an identical or different manner by trifluoromethyl, hydroxyl, halogen, carboxyl, nitro, azido, cyano, cycloalkyl or cycloalkyloxy each having 3 to 7 carbon atoms, by straight-chain or branched alkoxycarbonyl, alkoxy or alkylthio each having up to 6 carbon atoms or by lo straight-chain or branched alkyl having up to 6 carbon atoms, which for its part is substituted up to 2 times in an identical or different manner by hydroxyl, benzyloxy, trifluoromethyl, benzoyl, straight-chain or branched alkoxy, oxyacyl or carboxyl each having up to 4 carbon 15 atoms and/or phenyl, which for its part can be substituted by halogen, trifluoromethyl or trifluoromethoxy, and/or the carbocycles formed, also geminally, are optionally substituted up to 5 times in an identical or different manner by phenyl, benzoyl, thiophenyl or sulphonylbenzyl, 20 which for their part are optionally substituted by halogen, trifluoromethyl, trifluoromethoxy or nitro, and/or are optionally substituted by a group of the formula 1, 2 (CH 2 ) c-S0 2

-C

6

H

5 -(CO)d-NR 2 3

R

24 or =0 wherein c denotes a number 1, 2, 3 or 4, d denotes a 25 number 0 or 1, R 23 and R 24 are identical or different and denote hydrogen, cycloalkyl having 3 to 6 carbon atoms, straight-chain or branched alkyl having up to 6 carbon atoms, benzyl or phenyl, which is optionally substituted up to 2 times in an identical or different manner by 3o halogen, trifluoromethyl, cyano, phenyl or nitro, and/or the carbocycles formed are optionally substituted by a spiro-linked group of the formula 3 3 6 CVpo ''VSp'' c'''o of AU20082O155o (es.. trckad) c

R

3 1 W-Y R 25 R 26 R 3 Z(CR 27R) 28e2001 oR3 W-Y'' ' CR29R30) '& K or wherein W denotes an oxygen or a sulphur atom, Y and Y' together form a 2- to 6-membered straight-chain or branched alkylene chain, e denotes a number 1, 2, 3, 4, 5, 25 26 27 28 29 5 6 or 7, f denotes a number 1 or 2, R , R , R , R , R

R

30 and R 3 1 are identical or different and denote hydrogen, trifluoromethyl, phenyl, halogen or straight-chain or branched alkyl or alkoxy each having up to 6 carbon atoms, or R and R or R and R in each case together form a lo straight-chain or branched alkyl chain having up to 6 carbon atoms, or R25 and R or R and R 28 in each case together form a group of the formula

W-CH

2 W (CH2)g wherein W has the meaning indicated above, g denotes a 15 number 1, 2, 3, 4, 5, 6 or 7, R 32 and R 33 together form a 3- to 7-membered heterocycle which contains an oxygen or sulphur atom or a group of the formula SO, SO 2 or -NR34, wherein R 34 denotes hydrogen, phenyl, benzyl or straight chain or branched alkyl having up to 4 carbon atoms, a 20 salt thereof or N-oxide thereof, with the exception of 5(6H)-quinolone, 3-benzoyl-7,8-dihydro-2,7,7-trimethyl-4 phenyl. Each term used for the formula (XVIII) is as described in the above-mentioned publication. 25 Specifically, the following compound disclosed in W098/39299 (JP-T-2001-513790) can be mentioned: Substituted quinoline of the formula (XIX) 3 37 C'V"'""''''''''"''"" of AU2 82002O55 (cones..,ckdi dc A OR 3 D

I-R

2 (XIX) E N wherein A is aryl having 6 to 10 carbon atoms, which is optionally substituted up to 5 times in an identical or different manner by halogen, hydroxyl, trifluoromethyl, 5 trifluoromethoxy, nitro, or straight chain or branched alkyl, acyl, hydroxyalkyl or alkoxy, each having up to 7 carbon atoms, or a group of the formula -NR 4 R , wherein R 4 and R 5 are identical or different and denote hydrogen, phenyl or straight chain or branched alkyl having up to 6 1o carbon atoms, D is aryl having 6 to 10 carbon atoms, which is optionally substituted by phenyl, nitro, halogen, trifluoromethyl or trifluoromethoxy, or denote a group of the formula

R

8 R9 R 6 -L- , 7 or R' 1

-T-V-X

15 wherein R6, R 7 and R1 0 independently of one another denote cycloalkyl having 3 to 6 carbon atoms, or aryl having 6 to 10 carbon atoms, or a 5- to 7-membered, optionally benzo fused, saturated or unsaturated, mono-, bi- or tricyclic heterocycle having up to 4 heteroatoms from the group 20 consisting of S, N and/or 0, where the cycles are optionally substituted in the case of the nitrogen containing rings also via the N functional group, up to 5 times in an identical or different manner by halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, 25 trifluoromethoxy, straight-chain or branched acyl, alkyl, alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl, each having up to 6 carbon atoms, by aryl having 6 to 10 carbon atoms, or by an optionally benzo-fused, aromatic 5- to 7 membered heterocycle having up to 3 heteroatoms from the 30 group consisting of S, N and/or 0, and/or are substituted 338 C "po"'' 'Spec''catilon of AU2O0820155 (changes rtcked.doc by a group of the formula -OR", -SR", -SO 2 R1 3 or -NR"R, wherein R", R' and R' independently of one another denote aryl having 6 to 10 carbon atoms, which for its part is substituted up to 2 times in an identical or different 5 manner by phenyl, halogen or by straight-chain or branched alkyl having up to 6 carbon atoms, R 4 and R1 5 are identical or different and have the meaning of R 4 and R 5 indicated above, or R 6 and/or R7 denote a group of the formula F or 100 3

R

8 denotes a hydrogen or halogen, R 9 denotes hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or alkyl each having up to 6 carbon atoms or a group of the 16 17 16 17 15 formula -NR R , wherein R and R are identical or different and have the meaning of R 4 and R 5 indicated above, or R 8 and R 9 together form a group of the formula =0 or =NR , wherein R' is hydrogen or linear or branched alkyl, alkoxy or acyl, each having up to 6 carbon atoms, L 20 is a linear or branched alkyl or alkenyl each having up to 8 carbon atoms, each of which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and denote straight-chain or branched alkyl having up to 8 carbon atoms, or T or X denotes a bond, V represents 25 oxygen or sulfur atom or -NR" group, wherein R" is hydrogen or linear or branched alkyl having up to 6 carbon atoms or phenyl, E denotes cycloalkyl having 3 to 8 carbon atoms, or linear or branched alkyl having up to 8 carbon atoms, which is optionally substituted by cycloalkyl 30 having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, R1 and R2 are identical or different and denote cycloalkyl having 3 to 8 carbon atoms, hydrogen, 3 39 C "po" 'Spec'f'caon ofAU200820,55O (chnges traced) doc nitro, halogen, trifluoromethyl, trifluoromethoxy, carboxyl, hydroxyl, cyano, or straight chain or branched acyl, alkoxycarbonyl or alkoxy each having up to 6 carbon atoms, or a group of the formula -NR 2 0

R

21 , wherein R 2 0 and 5 R are identical or different and denote hydrogen, phenyl, or straight chain or branched alkyl having up to 6 carbon atoms and/or R1 and/or R 2 denote straight chain or branched alkyl having up to 6 carbon atoms, which are optionally substituted by halogen, trifluoromethoxy, lo hydroxyl or straight chain or branched alkoxy having up to 4 carbon atoms, and/or aryl having 6 to 10 carbon atoms, which are optionally substituted up to 5 times in an identical or different manner by halogen, cyano, hydroxyl, trifluoromethyl, trifluoromethoxy, nitro, or straight 15 chain or branched alkyl, acyl, hydroxyalkyl or alkoxy each having up to 7 carbon atoms, or a group of the formula 22 23 22 23 NR R , wherein R and R are identical or different and denote hydrogen, phenyl, or straight chain or branched alkyl having up to 6 carbon atoms, and/or R1 and R2 20 together form straight chain or branched alkyl chain or alkenyl chain each having up to 6 carbon atoms, which is optionally substituted by halogen, trifluoromethyl, hydroxyl, or straight chain or branched alkoxy having up to 5 carbon atoms, R 3 denotes hydrogen, straight chain or 25 branched acyl or benzoyl having up to 20 carbon atoms, which is optionally substituted by halogen, trifluoromethyl, nitro or trifluoromethoxy, or straight chain or branched fluoroacyl having up to 8 carbon atoms and up to 7 fluorine atoms, cycloalkyl having 3 to 7 30 carbon atoms, or straight chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by hydroxyl, straight chain or branched alkoxy having up to 6 carbon atoms, or phenyl, which for its part can be substituted by halogen, nitro, trifluoromethyl, 35 trifluoromethoxy or phenyl or tetrazol-substituted phenyl, 3 4 0 " " *''dVS*'"f" '"on of AU200*201550 (" es tc*d) * and/or alkyl is optionally substituted by a group of the formula -OR 24 , wherein R 24 denotes straight chain or branched acyl or benzyl having up to 4 carbon atoms, or a salt thereof. 5 Each term used for the formula (XIX) is as described in the above-mentioned publication. Specifically, the following compound disclosed in W099/14215 (JP-T-2001-516757) can be mentioned: Hetero-tetrahydroquinoline of the formula (XX) A D R (XX) 2 10 E N R wherein A represents cycloalkyl having 3 to 8 carbon atoms or, represents a 5- to 7-membered saturated, partially unsaturated or unsaturated, optionally benzo-fused heterocycle having up to 3 heteroatoms from the group 15 consisting of S, N and 0, which, in the case of a saturated heterocycle with a nitrogen functional group, is optionally also attached via this functional group, and where the abovementioned ring systems are optionally substituted up to 5 times by identical or different 20 substituents from the group consisting of halogen, nitro, hydroxyl, trifluoromethyl, trifluoromethoxy and straight chain or branched alkyl, acyl, hydroxyalkyl or alkoxy having in each case up to 7 carbon atoms, or by a group of the formula 25 -NR 3

R

4 wherein R 3 and R 4 are identical or different and represent hydrogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, or A represents a group of the formula 3 41 C:Vpo 'dSp 'fic 'on of AU20082O5o (changes tracked).idoc l I 0 0 D represents aryl having 6 to 10 carbon atoms which is optionally substituted by phenyl, nitro, halogen, trifluoromethyl or trifluoromethoxy, or represents a group 5 of the formula

R

7 Ra

R

6 -L- , RG or R'-T-V-X wherein R 5 , R 6 and R 9 independently of one another represent cycloalkyl having 3 to 6 carbon atoms, or lo represent aryl having 6 to 10 carbon atoms, or represent a 5- to 7-membered optionally benzo-fused saturated or unsaturated mono-, bi- or tricyclic hetreocycle having up to 4 heteroatoms from the group consisting of S, N and 0, where the cycles are optionally substituted, in the case 15 of nitrogen-containing rings also via an N functional group, up to 5 times by identical or different substituents from the group consisting of halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, and straight-chain or branched acyl, 20 alkyl, alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, by aryl or trifluoromethyl-substituted aryl having in each case 6 to 10 carbon atoms, or by an optionally benzo-fused aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms 25 from the group consisting of S, N and 0 and/or by a group 10 11 1213 14 1 of the formula -OR10, -SR", -SO 2 R" or -NR R , wherein R10,

R

11 and R 12 independently of one another represent aryl having 6 to 10 carbon atoms which for its part is substituted up to 2 times by identical or different 30 substituents from the group consisting of phenyl, halogen and straight-chain or branched alkyl having up to 6 carbon 342 C Vpo V r"Spc~fIcaUofl of AU2008201550 (Cflafgas Imcke2dAC atoms, R 13 and R1 4 are identical or different and have the meaning of R 3 and R4 given above, or R 5 and/or R 6 represent(s) a group of the formula s OForFCO 5 < :iuCO X F or F 3 C 0:) R' is a hydrogen or halogen, R 8 represents hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or 10 alkyl having in each case up to 6 carbon atoms or a group of the formula -NR 5 R ", wherein R 15 and R' 6 are identical or different and have the meaning of R 3 and R 4 given above, or R7 and R 8 together form a group of the formula =0 or

=NR"

7 wherein R" 7 represents hydrogen or straight-chain or 15 branched alkyl, alkoxy or acyl having in each case up to 6 carbon atoms, L represents a straight-chain or branched alkylene or alkenylene chain having in each case up to 8 carbon atoms, which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and 20 represent a straight-chain or branched alkylene chain having up to 8 carbon atoms, or T or X represents a bond, V represents an oxygen or sulphur atom or represents an NR group wherein R represents hydrogen or straight chain or branched alkyl having up to 6 carbon atoms or 25 phenyl, E represents cycloalkyl having 3 to 8 carbon atoms, or represents straight-chain or branched alkyl having up to 8 carbon atoms which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by 3o halogen or trifluoromethyl, R and R2 together form a straight-chain or branched alkylene chain having up to 7 carbon atoms, which has to be substituted by a carbonyl group and/or by a group of the formula 34 3 C Up'''' '' "'Sp'ifl'ion of AU2002o15so (changes. .c.d)doc

(CH

2 )A - CH 2 H 2 OH 01,3 O-C 0 -OR" or 1,2 0 (CRNR), v . I I .

I 1 . wherein a and b are identical or different and represent a number 1, 2 or 3, R 19 represents hydrogen, cycloalkyl having 3 to 7 carbon atoms, straight-chain or branched 5 silylalkyl having up to 8 carbon atoms, or straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by hydroxyl, straight-chain or branched alkoxy having up to 6 carbon atoms or by phenyl which for its part may be substituted by halogen, nitro, 10 trifluoromethyl, trifluoromethoxy or by phenyl or tetrazole-substituted phenyl, and alkyl is optionally substituted by a group of the formula -OR 22 , in which R 22 represents straight-chain or branched acyl having up to 4 carbon atoms or benzyl, or R 19 represents straight-chain 15 or branched acyl having up to 20 carbon atoms or benzoyl, which is optionally substituted by halogen, trifluoromethyl, nitro or trifluoromethoxy, or represents straight-chain or branched fluoroacyl having up to 8 carbon atoms and up to 9 fluorine atoms, R 20 and R 21 are 20 identical or different, represent hydrogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, or R 20 and R 21 together form 3 to 6-membered carbocycle and, if appropriate also geminally, the carbocycles formed are optionally substituted up to 6 25 times by identical or different substituents from the group consisting of trifluoromethyl, hydroxyl, nitrile, halogen, carboxyl, nitro, azido, cyano, cycloalkyl or cycloalkyloxy having in each case 3 to 7 carbon atoms, straight-chain or branched alkoxycarbonyl, alkoxy or 30 alkylthio having in each case up to 6 carbon atoms and straight-chain or branched alkyl having up to 6 carbon atoms, which for its part is substituted up to 2 times by identical or different substituents from the group 3 44 C h~owodSeficIon of AU2008201550 (changes tracked).o consisting of hydroxyl, benzyloxy, trifluoromethyl, benzoyl, straight-chain or branched alkoxy, oxyacyl or carboxyl having in each case up to 4 carbon atoms and phenyl, which for its part may be substituted by halogen, 5 trifluoromethyl or trifluoromethoxy, and/or the carbocycles formed are optionally substituted, also geminally, up to 5 times by identical or different substituents from the group consisting of phenyl, benzoyl, thiophenyl and sulphonylbenzyl, which for their part are lo optionally substituted by halogen, trifluoromethyl, trifluoromethoxy or nitro, and/or are optionally substituted by a group of the formula 1,2 1(CH 2 ) ' -S0 2 -C,H,, -(CO),-NR2 R or =0, wherein c represents a number 1, 2, 3 or 4, d represents a number 0 or 1, R 23 and R 24 are identical or different and represent hydrogen, cycloalkyl having 3 to 6 carbon atoms, 20 straight-chain or branched alkyl having up to 6 carbon atoms, benzyl or phenyl which is optionally substituted up to 2 times by identical or different substituents from the group consisting of halogen, trifluoromethyl, cyano, phenyl and nitro, and/or the carbocycles formed are 25 optionally substituted by a spiro-linked group of the formula R 3 W~Y RR RR W-Y' ' (CRERM), , K%~(CR2RX or wherein W represents either an oxygen or a sulphur atom, Y and Y' together form a 2- to 6-membered straight-chain or 30 branched alkylene chain, e represents a number 1, 2, 3, 4, 25 26 27 28 5, 6 or 7, f represents a number 1 or 2, R , R , R , R 34 5 C:powordSpecification of AU2008201550 (changes tracked).doc 29 30 31 R , R and R are identical or different and represent hydrogen, trifluoromethyl, phenyl, halogen or straight chain or branched alkyl or alkoxy having in each case up to 6 carbon atoms, or R 25 and R 26 or R 27 and R 28 in each 5 case together form straight-chain or branched alkyl chain having up to 6 carbon atoms, or R 25 and R 26 or R 27 and R 28 in each case together form a group of the formula W -

CH

2 W -- (CH 2 ) , wherein W is as defined above, g represents a number 1, 2, 10 3, 4, 5, 6 or 7, R and R 33 together form 3- to 7-membered heterocycle which contains an oxygen or sulphur atom or a group of the formula SO, SO 2 or -NR 34 , in which R 34 represents hydrogen, phenyl, benzyl or straight-chain or branched alkyl having up to 4 carbon atoms, a salt thereof 15 or N-oxide thereof. Each term used for the formula (XX) is as described in the above-mentioned publication. Specifically, the following compound disclosed in W099/155504 (JP-T-2001-517655) can be mentioned: 20 Tetrahydro-quinoline of the formula (XXI) A R 1

R

2 D R (XXI) E N R 4 in which A represents phenyl which is optionally substituted up to 2 times by identical or different substituents from the 25 group consisting of halogen, trifluoromethyl and straight chain or branched alkyl or alkoxy having in each case up to 3 carbon atoms, D represents a group of the formula

R

6

R

5 R or R 8

-CH

2

-O-CH

2 3 4 6 C.'"'r'So"f''on o'AU20082O155o (chwagt r.cs t .doc in which

R

5 and R 6 together form a carbonyl group (=0), or

R

5 represents hydrogen and

R

6 represents halogen or hydroxyl, or 5 R 5 and R 6 represent hydrogen,

R

7 and R 8 are identical or different and represent phenyl, naphthyl, benzothiazolyl, quinolyl, pyrimidyl or pyridyl which are optionally substituted up to 4 times by identical or different substituents from the group lo consisting of halogen, trifluoromethyl, nitro, cyano, trifluoromethoxy, or by a group of the formula -S0 2

-CH

3 or

-NR

9

R

10 , in which R 9 and R' 0 are identical or different and represent hydrogen or straight-chain or branched alkyl having up to 3 carbon atoms, 25 E represents cycloalkyl having 3 to 6 carbon atoms, or represents straight-chain or branched alkyl having up to 8 carbon atoms, Ri represents hydroxyl, and

R

2 represents hydrogen or represents methyl, 20 R 3 and R 4 are identical or different and represent straight-chain or branched alkyl having up to 3 carbon atoms, or

R

3 and R 4 together form a spiro-linked alkyl chain having 2 to 4 carbon atoms, 25 or a salt thereof or N-oxide thereof. Each term used for the formula (XXI) is as described in the above-mentioned publication. Specifically, the following compound disclosed in W099/15487 (JP-T-2001-517646) can be mentioned: 30 a compound of the formula (XXII) A D R (XXII) E : R 34 7 C 'V*'*dSp'f'c n of AU2 820O55O cargo. t,.ckd).doc wherein A is cycloalkyl having 3 to 8 carbon atoms, aryl having 6 to 10 carbon atoms, or 5- to 7-membered saturated, partially unsaturated or unsaturated optionally benzo fused heterocycle having up to 4 hetero atoms from the 5 group consisting of S, N and 0, wherein the ring systems of the aryl and said heterocycle are optionally substituted up to 5 times by identical or different substituents from the group consisting of cyano, halogen, nitro, carboxyl, hydroxyl, trifluoromethyl and 20 trifluoromethoxy, or straight chain or branched alkyl, acyl, hydroxyalkyl, alkylthio, alkoxycarbonyl, oxyalkoxycarbonyl or alkoxy, each having up to 7 carbon atoms, or a group of the formula -NR 3

R

4 , wherein R 3 and R 4 are identical or different and denote hydrogen, phenyl or 15 straight chain or branched alkyl having up to 6 carbon atoms, D denotes a group of the formula 7 Ra

R

5 -L- , Ro R -T-V-X wherein R 5 , R 6 and R 9 independently of one another denote aryl having 6 to 10 carbon atoms, or 5- to 7-membered, 20 optionally benzo-fused, saturated or unsaturated, mono-, bi- or tricyclic heterocycle having up to 4 heteroatoms from the group consisting of S, N and 0, where the cycles are optionally substituted, in the case of nitrogen containing rings also via an N functional group, up to 5 25 times, by identical or different substituents from the group consisting of halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, straight chain or branched acyl, alkyl, alkylthio, alkylalkoxy, alkoxy or alkoxycarbonyl, each having up to 6 carbon atoms, 30 by aryl- or trifluoromethyl-substituted aryl, each having 6 to 10 carbon atoms, or by an optionally benzo-fused, aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms from the group consisting of S, N and 0, 34 8 C"PON *SP* df'""''fl"' ' AU200821550 chargess ticked) doc and/or by a group of the formula -OR , -SR", -SO 2 R" or 13 14 10 112 NR R , wherein R , R" and R 12 independently of one another denote aryl having 6 to 10 carbon atoms, which for its part is substituted up to 2 times by identical or 5 different substituents from the group consisting of phenyl and halogen, or by straight-chain or branched alkyl having up to 6 carbon atoms, R1 3 and R 4 are identical or different and have the meaning of R 3 and R 4 indicated above, or R 5 and/or R 6 denote a group of the formula or FF 10 -_ajIIo>: o F3C 0'

R

7 denotes a hydrogen, halogen or methyl, R8 denotes hydrogen, halogen, azido, trifluoromethyl, hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy or alkyl each having up to 6 carbon atoms or a group of the 15 formula -NRR1 6 , wherein R' 5 and R 16 are identical or different and have the meaning of R 3 and R 4 indicated above, or R 7 and R 8 together form a group of the formula =0 or =NR , wherein R' is hydrogen or linear or branched alkyl, alkoxy or acyl, each having up to 6 carbon atoms, L 20 is a linear or branched alkylene or alkenylene chain each having up to 8 carbon atoms, each of which is optionally substituted up to 2 times by hydroxyl, T and X are identical or different and denote straight-chain or branched alkylene chain having up to 8 carbon atoms, or T 25 or X denotes a bond, V represents an oxygen or sulfur atom or -NR' 8 - group, wherein R' 8 is a hydrogen or linear or branched alkyl having up to 6 carbon atoms or phenyl, E denotes cycloalkyl having 3 to 8 carbon atoms, or linear or branched alkyl having up to 8 carbon atoms, which is 30 optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, Ri denotes straight chain or branched alkyl having up to 6 carbon atoms, which is substituted by hydroxyl or a group 34 9 C**o'r'SpecIflcaon o AU2082O1S5O (cngos Ircked)dc of the formula R2 denotes hydrogen, or straight chain or branched alkyl or alkenyl each having up to 8 carbon atoms, which is 5 optinonally substituted by hydroxyl, halogen, phenyl, cycloalkyl having 3 to 6 carbon atoms, or a group of the formula 00

-O-R

19 or 1o wherein R1 9 denotes a group of the formula -Si(CH 3

)

2

C(CH

3

)

3 , or straight chain or branched alkyl having up to 6 carbon atoms, or 5- to 7-membered saturated, partially unsaturated or unsaturated heterocycle having up to 3 hetero atoms from the group consisting of S, N and 0, or 15 phenyl or benzyl, wherein all ring systems for R1 are optionally substituted up to 2 times by identical or different substituents from the group consisting of trifluoromethyl, fluorine, nitro, hydroxyl, straight chain or branched alkoxy or alkoxycarbonyl having in each case 20 up to 4 carbon atoms, or by straight chain or branched alkyl having up to 4 carbon atoms optionally substituted by hydroxyl, or a salt thereof. Each term used for the formula (XXII) is as described in the above-mentioned publication. 25 Specifically, the compound disclosed in WO00/53792 (Code Names WK-5344A and WK-5344B) can be mentioned. Specifically, the following compound disclosed in 3 50 C MpoW "Sp" "fl''on '" AU20082O155 (Canges tckd).ic JP-A-2002-293764 can be mentioned: a compound represented by the formula (XXIII) OR'' R' N ArN R (XXIII) Ar 2 wherein Ar 1 is an aromatic ring group optionally having 5 substituents, Ar2 is an aromatic ring group having substituent, OR" is an optionally protected hydroxyl group, R is an acyl group, R' is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof with the exception of tert-butyl benzyl-[2(S)-hydroxy-2 10 thiazol-2-yl-1(S)-(4-trifluoromethyl-benzyl)-ethyl] carbamate. Each term used for the formula (XXIII) is as described in the above-mentioned publication. Specifically, CETi-l (CETP vaccine) disclosed in 15 W099/20302 (JP-T-2001-520204) can be mentioned. Furthermore, as a compound having a CETP inhibitory activity in the present invention, a compound selected from the group consisting of Code Names: JTT-705, CP 529414, SC-795, SC-744, SC-554, SC-71952, SC-56960, SC 20 57201, PD-140195, WK-5344A, WK-5344B, CETi-1 (CETP vaccine), BM99-1 and BM99-2, and the like can be mentioned. Of these, as a CETP inhibitor, S-{2-([[l-(2 ethylbutyl)cyclohexyl]carbonyl]amino)phenyl} 2 methylpropanethioate, as well as ethyl (2R,4S)-4-[[3,5 25 bis(trifluoromethyl)benzyl](methoxycarbonyl)amino]-2 ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2H) carboxylate, an anhydride thereof, an ethanolate thereof, crystals thereof (JP-T-2003-515592), methyl (3-cyano-5 trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N 30 ethylamino)indan-5-ylmethyl]-carbamate (JP-A-221376/2003) and trans-(4-{(N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 3 51 C U"o*''**'" ''''''*" o' AU200201550 (changes r.cked) oc trifluoromethylphenyl)-N-ethylamino]methyllcyclohexyl) acetic acid methanesulfonate (W02004/020393) are particularly preferable. The above-mentioned compounds having a CETP 5 inhibitory activity can be used for (1) a remnant lipoprotein production inhibitor comprising a compound having a CETP inhibitory activity as an active ingredient, (2) an inhibitor of transfer of cholesteryl ester in HDL lo to chylomicron and/or VLDL, which comprises a compound having a CETP inhibitory activity as an active ingredient, (3) a CETP inhibitor having an inhibitory activity on the transfer of cholesteryl ester in HDL to chylomicron and/or VLDL, 25 (4) the inhibitor of the above-mentioned (1), wherein the compound having a CETP inhibitory activity inhibits transfer of cholesteryl ester in HDL to chylomicron and/or VLDL due to a CETP inhibitory activity thereof and (5) a CETP inhibitor that inhibits transfer of cholesteryl 20 ester in HDL to chylomicron and/or VLDL and has a remnant lipoprotein production inhibitory activity. Moreover, the present invention relates to a commercial package comprising at least one of the inhibitors of the above-mentioned (1) to (5) and a written 25 matter relating to the use thereof. Each inhibitor (remnant lipoprotein production inhibitor, inhibitor of transfer of cholesteryl ester in HDL to chylomicron and/or VLDL, CETP inhibitor) in the present invention can be generally admixed with 30 pharmacologically acceptable carrier, excipient, diluent, extender, disintegrant, stabilizer, preservative, buffer, emulsifier, aromatic, coloring agent, sweetening agent, thickener, corrigent, dissolution aids, and other additives concretely exemplified by water, vegetable oil, 35 alcohol such as ethanol and benzyl alcohol, polyethylene 3 52 C Vpo 'dVS''e'f'con of AU20B2O1o550 (hranos tracked) oc glycol, glycerol triacetate gelatin, carbohydrates such as lactose, starch and the like, magnesium stearate, talc, lanolin, vaseline and the like, which are known per se, and systemically or topically, orally or parenterally 5 administered to an administration subject (mammals such as human, bovine, horse, dog, cat, rat, mouse, hamster etc.) in the form of tablet, pill, powder, granule, suppository, injection, eye drop, liquid, capsule, troche, aerozol, elixir, suspension, emulsion, syrup and the like. While 10 the dose varies depending on various factors such as the kind of inhibitor, age and body weight of the administration subject, disease, symptoms, treatment effect and the like, and determined appropriately upon consideration of these factors and administered once or 15 several times a day. In addition, the inhibitor of the present invention can be used concurrently with other one or more pharmaceutical agents by a method generally employed for pharmaceutical agents. The compound having the CEPT inhibitory activity 20 encompasses "pharmaceutically acceptable salt". The "pharmaceutically acceptable salt" may be any as long as it forms a nontoxic salt with the compound. Examples thereof include, but not limited to, inorganic acid salts such as hydrochloride, hydrobromide, 25 hydroiodide, sulfate, nitrate, phosphate, carbonate, hydrogen carbonate, perchlorate etc.; organic acid salts such as formate, acetate, trifluoroacetate, propionate, oxalate, glycolate, succinate, lactate, maleate, hydroxymaleate, methylmaleate, fumarate, adipate, tartrate, 30 malate, citrate, benzoate, cinnamate, ascorbate, salicylate, 2-acetoxybenzoate, nicotinate, isonicotinate etc.; sulfonates such as methanesulfonate, ethanesulfonate, isethionate, benzenesulfonate, p-toluenesulfonate, naphthalenesulfonate etc.; acidic amino acid salts such as 35 aspartate, glutamate etc.; alkali metal salts such as 353 C 'f* '''Spodf'^Uon of AU20082O1550 (chng.. .. cd).doec sodium salt, potassium salt etc.; alkaline earth metal salts such as magnesium salt, calcium salt etc.; ammonium salt; organic base salts such as trimethylamine salt, triethylamine salt, pyridine salt, picoline salt, 5 dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt etc.; and amino acid salts such as lysin salt, arginine salt etc. In some cases, it may be a water-containing product, a hydrate or a solvate with alcohol and the like. In the compound, various isomers can be present. 10 Examples thereof include E form and Z form as geometric isomers, and, when an asymmetric carbon atom exists, enantiomer and diastereomer are present as stereoisomers based thereon, and tautomer can be present. Accordingly, the compound encompasses all these isomers and a mixture 15 thereof. Here, the compound having the CEPT inhibitory activity also encompasses prodrug compounds and metabolites. The "prodrug compound" of the compound having the 20 CEPT inhibitory activity is a derivative of the compound, which has a chemically or metabolically degradable group and restores to the original compound to show an intrinsic efficacy after administration to a living organism. It includes a complex and a salt not based on a covalent bond. 25 As the prodrug compound, a compound represented by the above formula wherein a carboxyl group has been modified by ethyl group, pivaloyloxymethyl group, 1 (acetyloxy)ethyl group, 1-(ethoxycarbonyloxy)ethyl group, 1-(cyclohexyloxycarbonyloxy)ethyl group, carboxyimethyl 30 group, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl group, phenyl group, o-tolyl group and the like; a compound represented by the above formula, wherein a hydroxyl group has been modified by acetyl group, propionyl group, isobutyryl group, pivaloyl group, benzoyl group, 4 35 methylbenzoyl group, dimethylcarbamoyl group or sulfo 3 5 4 C 'o''dSp'' '''''"n ofAU2008201550 (di.o . trackau)A.

group; a compound represented by the above formula, wherein an amino group has been modified by hexylcarbamoyl group, 3-methylthio-l-(acetylamino)propylcarbonyi group, 1-sulfo-l-(3-ethoxy-4-hydroxyphenyl)methyl group, (5 5 methyl-2-oxo-1,3-dioxol-4-yl)methyl group and the like, and the like can be mentioned. The present invention is useful for the prophylaxis or treatment of diseases such as hyperlipidemia, arteriosclerosis and hyper-remnant lipoproteinemia (e.g., 10 hereditary hyper-remnant lipoproteinemia such as familial dysbetalipidemia, familial lipase deficiency, familial combined hyperlipidemia etc.; and secondary hyper-remnant lipoproteinemia that expresses subsequent to diabetic hypertriglyceridemia, hypothyroidism, nephritic syndrome 15 etc.) and the like. The present invention is more specifically explained in the following by referring to Examples. The present invention is not limited at all by the Examples. Compound A used in the following experiments refers to S-{2-([[1 20 (2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl} 2 methylpropanethioate; Compound B refers trans-(4-{[N-(2 {[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N 25 ethylamino]methyl}cyclohexyl)acetic acid methanesulfonate, Compound C refers methyl (3-cyano-5 trifluoromethylbenzyl)-[6-(N-cyclopentylmethyl-N ethylamino)indan-5-ylmethyl]-carbamate [i.e., methyl N-(3 cyano-5-trifluoromethylbenzyl)-[6-(N'-cyclopentylmethyl 30 N'-ethylamino)indan-5-ylmethyl]carbamate], Compound D refers ethyl (2R,4S)-4-[[3,5 bis(trifluoromethyl)benzyl](methoxycarbonyl)amino]-2 ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2H) carboxylic acid ester [i.e., ethyl (2R,4S)-4-[N-[3,5 35 bis(trifluoromethyl)benzyl]-N-(methoxycarbonyl)amino]-2 3 55 C *Vpo' rd''Sp'f 'cation of AU2008201550 (changes tac. d).dc ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2H) carboxylic acid ester]. Examples Preparation of Donor Lipoprotein 5 Potassium bromide (KBr) was added to plasma (40 mL) of healthy subject and the mixture was adjusted to have a specific density d=1.125 g/mL. The mixture was subjected to density gradient centrifugation (227,000xg, 40C, 17 hr) and a fraction showing a specific density of d>1.125 g/mL 10 (HDL 3 fraction) was harvested. The obtained fraction was dialyzed against PBS solution [10 mmol/L Na 2

HPO

4 ; 10 mmol/L NaH 2

PO

4 ; 0.15 mol/L NaCl; 1 mmol/L EDTA (pH 7.4)]. Then, tritium-labeled cholesterol (37 MBq) was dissolved in 95% ethanol, gradually added to the above-mentioned 15 HDL 3 fraction with stirring and incubated at 370C for 18 hr. [By this operation, tritium-labeled cholesterol was esterified by the action of lecithin cholesterol acyl transferase (LCAT) present on the HDL 3 surface and taken up into HDL3 as tritium-labeled cholesteryl ester 20 ([ 3 H]CE)]. After incubation, KBr was added, the mixture was adjusted to have a specific density d=1.21 g/mL, subjected to density gradient centrifugation (227,000xg, 40C, 17 hr) and a fraction of specific density d>1.21 g/mL was harvested. The obtained fraction was dialyzed against 25 the aforementioned PBS solution to give HDL 3 incorporating

[

3 H]CE ([3H]CE-HDL 3 , specific density: 1.125<d<1.21, specific activity: 22,000 - 33,000 dpm/pL), which was used as a donor lipoprotein. Experimental Example 1: in vitro effect on remnant 30 lipoprotein production in plasma Compound A, Compound B, Compound C and Compound D were previously dissolved in dimethyl sulfoxide (DMSO). Plasma (200 ptL) of healthy subject, and a solution (2 pL) of each compound in DMSO or DMSO (2 pL) were added into a 35 microtube. On the other hand, a monoclonal antibody 356 C" o*''**''''e'''"**'' """'^20082015so ( e so.raed) doe against human CETP was diluted with physiological saline and added into a microtube together with plasma (190 ptL) of healthy subject and a diluted solution (10 pL) of the monoclonal antibody or physiological saline (10 pL). These 5 were incubated at 37*C or 40C for 6 hr (Compound A) or 4 hr (Compound B, Compound C, Compound D, the monoclonal antibody). After ice-cooling, the cholesterol amount in the remnant fraction was measured using "RLP-cholesterol "JIMRO II"" (manufactured by Japan Immunoresearch 10 Laboratories Co., Ltd.). The difference in the measured values from incubation of solvent alone at 4*C and 37*C, namely, an increase in the remnant cholesterol was taken as a 100% production amount of remnant lipoprotein, and the percent of decrease in the measured values of 15 incubation at 37*C with the addition of each compound or the antibody was taken as percent inhibition of remnant lipoprotein production. The results are shown in the following. 357 C'V*''""'V**O**'''''''*"*'^200820150o es.,cke)dc Table 1 Compound A Inhibition (%) concentration of remnant cnet i lipoprotein (pM) production 0 0 3 25 10 54 30 77 5 Table 2 Compound B Inhibition (%) concentration of remnant lipoprotein (pM) production 0 0 0.01 29 0.03 36 0.1 42 0.3 52 1 84 Table 3 Compound C Inhibition (%) concentration of remnant lipoprotein ( pM) production 0 0 0.1 21 0.3 34 1 41 3 93 10 15 3 58 C:4Of 'dVSP'C'f' n Of AU2008201550 (dwt~e s trnced).doc Table 4 Compound D Inhibition (%) concentration of remnant lipoprotein (piM) production 0 0 0.01 38 0.03 32 0.1 44 0.3 59 1 62 5 Table 5 Monoclonal Inhibition (%) antibody of remnant concentration lipoprotein (ptg/mL) production 0 0 3 32 10 49 30 91 100 84 Experimental Example 2: effect on cholesteryl ester lo transfer from donor lipoprotein to remnant lipoprotein The donor lipoprotein obtained above was added to the plasma of healthy subject to prepare a [ 3

H]CE-HDL

3 containing plasma (2,000 - 4,000 dpm/pL) . Compound A, Compound B, Compound C and Compound D were dissolved in 15 dimethyl sulfoxide (DMSO). A solution of each compound in DMSO (1 pL) or DMSO (1 pL), and the [ 3 H]CE- HDL 3 -containing plasma (100 pL) were added into a microtube. On the other hand, the monoclonal antibody was diluted with physiological saline and added into a microtube together 20 with a diluted solution (5 pL) of the monoclonal antibody or physiological saline (5 pL), and [ 3

H]CE-HDL

3 containing plasma (95 pL) . These were incubated at 37 0 C or 4 0 C for 6 359 C Vo'VSp'dfcatJo*f"AU2Oa2155O(chgStes.irced).doc hr (Compound A) or 4 hr (Compound B, Compound C, Compound D and the monoclonal antibody) . After ice-cooling, a remnant fraction was harvested using "RLP-cholesterol "JIMRO II"" (manufactured by Japan Immunoresearch 5 Laboratories Co., Ltd.), and the radioactivity in the fraction was measured with a liquid scintillation counter. The difference in the measured values from incubation of solvent alone at 4'C and 37*C was taken as a 100% cholesteryl ester transfer activity, and the percent of 1o decrease in the measured values of incubation at 37*C with the addition of each compound or the antibody was taken as percent inhibition of cholesteryl ester transfer. The CETP activity was measured according to the method shown below using a part of the same plasma after 15 incubation. After ice-cooling, plasma (80 tL) was separated and a TBS solution [80 pL, 20 mmol/L Tris; 0.15 mol/L NaCi (pH 7.4)] containing 50 mmol/L magnesium chloride and 0.1% dextran sulfate was added to each microtube and thoroughly stirred. After standing at 4*C 20 for 30 min, the mixture was centrifuged (10,000xg, 4*C, 10 min.),. and the radioactivity in the obtained supernatant (HDL fraction) was measured with a scintillation counter. The difference in the measured values from incubation of solvent alone at 4*C and 37*C was taken as a 100% CETP 25 activity, and the percent of decrease in the measured values of incubation at 37'C with the addition of each compound or the antibody was taken as percent inhibition of CETP activity. The above results are shown in the following. 30 35 3 6 0 Cpof 'dVSp'f'c'Uo' of AU2002o55o (ceres.. tracked) doc Table 6 Compound A Inhibition (%) of Inhibition (%) concentration cholesteryl ester of CETP ( M) transfer to remnant activity fraction 0 0 0 3 21 3 10 29 34 30 92 75 Table 7 Compound B Inhibition (%) of Inhibition (%) concentration cholesteryl ester of CETP ( M) transfer to remnant activity fraction 0 0 0 0.01 15 10 0.03 26 25 0.1 55 53 0.3 89 74 1 100 86 5 Table 8 Compound C Inhibition (%) of Inhibition (%) concentration cholesteryl ester of CETP (pM) transfer to remnant activity fraction 0 0 0 0.1 -25 6 0.3 9 12 1 35 31 3 92 57 Table 9 Compound D Inhibition (%) of Inhibition (%) concentration cholesteryl ester of CETP ( M) transfer to remnant activity fraction 0 0 0 0.01 12 9 0.03 28 24 0.1 54 53 0.3 78 73 1 94 83 10 361 C *VpofVd' Sp'ci'c''on of A 20 2 1550 (changes tracked) doc Table 10 Monoclonal Inhibition (%) of antibody cholesteryl ester Inhibition (%) concentration transfer to remnant of CETP activity (pg/mL) fraction 0 0 0 3 19 18 10 57 47 30 67 68 100 90 80 From the foregoing test results and the like, it is considered that CETP promotes remnant lipoprotein production, 5 and a CETP inhibitor and an anti-CETP antibody can suppress production of remnant lipoprotein by inhibiting cholesteryl ester transfer from HDL. It is clear that the remnant cholesterol is a risk factor of promotion of arteriosclerosis, and a CETP inhibitor and an anti-CETP antibody are useful for 10 the prophylaxis or treatment of hyper-remnant lipoproteinemia, as well as for the prophylaxis or treatment of arteriosclerotic diseases (e.g., atherosclerosis, myocardial infarction, cerebral infarction, angina pectoris, peripheral vascular disease, cardiovascular disorder, ischemia, cardiac ischemia, 15 stroke, Ischemia-reperfusion injury, restenosis after angioplasty, vascular complication of diabetes and the like) and the like, because they can decrease remnant cholesterol in plasma. 20 INDUSTRIAL APPLICABILITY The present invention provides a prophylactic drug or a therapeutic drug of hyper-remnant lipoproteinemia (hyper remnant-emia) in which a remnant lipoprotein is involved (e.g., hereditary hyper-remnant lipoproteinemia such as familial 25 dysbetalipidemia, familial lipase deficiency, familial 362 combined hyperlipidemia and the like; or secondary hyper remnant lipoproteinemia that expresses subsequent to diabetic hypertriglyceridemia, hypothyroidism, nephritic syndrome and the like) by selectively inhibiting CETP. 363 C*p*'''''' p***'''''' ''"'^2008201550(cha o.. c, . c c

Claims (12)

1. A method for treating or preventing hyper-remnant lipoproteinemia in a patient, which method comprises administering an effective amount of a compound having a CETP 5 inhibitory activity, wherein said compound is trans-(4-{[N-(2 {[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol

5-yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, together with a pharmaceutically 10 acceptable carrier to the patient. 2. Use of an effective amount of trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically 15 acceptable salt thereof, together with a pharmaceutically acceptable carrier in the preparation of a medicament for the treatment or prevention of hyper-remnant lipoproteinemia in a patient. 3. The method of claim 1, wherein the trans-(4-{ [N-(2-{[N' 20 [3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyll-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, inhibits the production of chylomicron remnant. 25 4. The method of claim 1, wherein the trans-(4-{[N-(2-{[N' [3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyll-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, inhibits the production of VLDL 30 remnant. 5. The use of claim 2, wherein the trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl)-N'-(2-methyl-2H-tetrazol-5 364 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylaminolmethyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, inhibits the production of chylomicron remnant. 5 6. The use of claim 2, wherein the trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof, inhibits the production of VLDL 10 remnant.

7. A method for treating or preventing hyper-remnant lipoproteinemia in a patient, which method comprises administering to the patient an effective amount of a compound having a CETP inhibitory activity, wherein said compound is 15 represented by the formula (IX) R1 (R 6 )n B R2 N (X) A R* R5 4 wherein R and R2 are the same or different and each is a halogen atom, a nitro group, a cyano group or a C1-6 alkyl group 20 optionally substituted by halogen atom; R 3 , R 4 and R 5 are the same or different and each is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen atom, a C1-6 alkylthio group optionally substituted by halogen atom or a C1-6 alkoxy group optionally 365 substituted by halogen atom, or R 3 and R 4 or R 4 and R 5 may form, together with a carbon atom they are bonded to, a homocyclic ring optionally having substituent(s) or a heterocyclic ring optionally having substituent(s); 5 A is -N(R ) (R8) (wherein R and R are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by phenyl group or -(CH 2 )m-COOR 9 (wherein R 9 is a hydrogen atom or a C1-6 10 alkyl group and m is 0 or an integer of 1 to 5)) or a C4-10 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C 1 - 6 alkoxy group, C1-6 alkyl group (wherein C1-6 15 alkyl group is optionally substituted by hydroxyl group, C1-6 alkoxy group or phosphono group), -(CH 2 )q-CON(R 20 ) (R 21 ) (wherein R 20 and R 21 are the same or different and each is hydrogen atom or C1-6 alkyl group and q is 0 or an integer of 1 to 5) or (CH 2 ) r-COOR (wherein Rio is hydrogen atom or C1-6 alkyl group 20 and r is 0 or an integer of 1 to 5)), -C(R") (R ) (R ) (wherein R", R' 2 and R 13 are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by phenyl group or -COOR 9 (wherein R 9 is as defined above) ) or a C4-10 25 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C1-6 alkoxy group, C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group, C1-6 30 alkoxy group or phosphono group), - (CH2)q-CON(R 2 1) (R 21 ) (wherein R , R and q are as defined above) or -(CH 2 )r-COOR' 0 (wherein Rio and r are as defined above))) or -O-C(R 1 1 ) (R 12 ) (R 13 ) (wherein 366 11 123 R , R and R' are as defined above); ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, an amino group, a hydroxyl group, a cyano group, an acyl group, a 5 C1-6 alkoxy group, a C2-6 alkenyl group or a C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group or -COOR1 4 (wherein R1 4 is a hydrogen atom or a C 1 -6 alkyl group)); and n is an integer of 1 to 3 10 or a prodrug thereof or a pharmaceutically acceptable salt thereof.

8. The method of claim 7, wherein the compound of the formula (IX) is a compound selected from a group consisting of N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 15 tetrahydronaphthalen-2-ylmethyl]-N-[3,5 bis(trifluoromethyl)benzyl]-(2-methyl-2H-tetrazol-5-yl)amine, 3-{[N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-trifluoromethylbenzonitrile, 20 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2-methyl-2H tetrazol-5-yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2-methyl-2H 25 tetrazol-5-yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(2H-tetrazol-5-yl)-[3,5 bis(trifluoromethyl)benzyl]amine, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 367 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl)-(pyrimidin-2 yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl]-(5-methyl-lH 5 pyrazol-3-yl)amine, 5-{N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyllindan-5-yl)-N ethylamino}pentanoic acid hydrochloride, methyl trans-4-{ [N-(2-{ [N'-(3,5 10 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl cyclohexanecarboxylate, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-5 15 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2-ethyl-2H tetrazol-5-yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 20 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1-methyl-1H [1,2,4]triazol-3-yl)amine, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl)-N-phenylamino}methyl)-5-trifluoromethylbenzonitrile, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 25 ylmethyl]-N-(4,5-dimethylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(thiazol-2 yl)amine hydrochloride, 368 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(thiazol-2-yl)aminoImethyl)-5 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 5 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(oxazol-2 yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methylthiazol-2-yl)amine hydrochloride, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4,5 15 dimethylthiazol-2-yl)amine hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(5-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 20 ylmethyl]-N-(4-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 methyloxazol-2-yl)amine hydrochloride, 25 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-(3 methylisothiazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 30 methylisoxazol-3-yl)amine hydrochloride, 369 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 methylisoxazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 5 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyll-(1-methyl-1H pyrazol-3-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(l-methyl-lH pyrazol-4-yl)amine hydrochloride, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5-methyl [1,3,4]thiadiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5-methyl 15 [1,3,4]oxadiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-pyridin-3 ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 20 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-pyridin-2 ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[2-(N' cyclopentylmethyl-N'-ethylamino)-5-trifluoromethylbenzyl]-(2 methyl-2H-tetrazol-5-yl)amine hydrochloride, 25 3-{[N-[2-(N'-cyclopentylmethyl-N'-ethylamino)-5 trifluoromethylbenzyl]-N-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-trifluoromethylbenzonitrile hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 30 ethylamino]pentanoate hydrochloride, 370 methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-ylmethyl)-N ethylamino]pentanoate hydrochloride, methyl 5-[N-(6-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N' 5 (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoate hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoic acid hydrochloride, 10 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyllindan-5-yl)-N 15 ethylaminolpentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoic acid hydrochloride, methyl trans-4-{[N-(3-{[N'-[3,5 20 bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylaminolmethylicyclohexanecarboxylate hydrochloride, methyl trans-4-{ [N-(3-{[N'-(3-cyano-5 trifluoromethylbenzyl)-N'-(l-methyl-lH-pyrazol-3 25 yl)amino]methyll-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 371 trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5-methyl [1,2,4]oxadiazol-3-yl)amine hydrochloride, methyl trans-4-{[N-(6-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH-pyrazol-3 10 yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 15 methyl trans-4-{[N-(6-{[N'-(3-cyano-5 trifluoromethylbenzyl)-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylate, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 20 (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 25 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl)cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 372 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 5 (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methyl-isoxazol-5-yl)amino]methyljindan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 10 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N 15 ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 20 (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylaminolmethylIcyclohexanecarboxylic acid, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3-methyl [1,2,4]thiadiazol-5-yl)amine, 25 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 30 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate 373 hydrochloride, methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate 5 hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 10 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 15 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-5,6,7,8 20 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methyl)-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, 30 trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 374 (3-methylisoxazol-5-yl)amino]methyll-5,6, 7 ,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 5 (3-methylisoxazol-5-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 2-(5-{N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5 10 ylmethyl]amino}tetrazol-2-yl)ethanol hydrochloride, methyl 5-(N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 15 methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 20 methyl-lH-[1,2,4]triazol-3-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyll-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 30 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 375 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-5,6,7,8 5 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid 10 hydrochloride, trans-4-{ [N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyllindan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 15 methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethoxyphenyl) N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]pentanoic acid hydrochloride, 20 5-[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl)-4-trifluoromethylphenyl) N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) 25 N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 ethyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-{N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 30 hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5-yl]-N 376 ethylaminolpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]pentanoic acid 5 hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino] 2,2-dimethylpentanoic acid hydrochloride, 6-[N-(6-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] hexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino] 3,3-dimethylpentanoic acid hydrochloride, 15 trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl)cyclohexanecarboxylic acid hydrochloride, (1-{2-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 20 ethylamino]ethyl}cyclopentyl)acetic acid hydrochloride, trans-4-({N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]aminolmethyl)indan-5-yl] N-ethylamino}methyl)cyclohexanecarboxylic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 25 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N ethylamino)methyl}cyclohexanecarboxylic acid hydrochloride, (1-{2-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 30 tetrahydronaphthalen-2-yl)-N 377 ethylamino]ethyl cyclopentyl)acetic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N 5 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 10 trans-4-({N-[3-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]aminolmethyl)-5,6,7,8 tetrahydronaphthalen-2-yl]-N ethylaminolmethyl)cyclohexanecarboxylic acid hydrochloride, 1-{3-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 15 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]propyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-lH-pyrazol-3-yl)aminolmethyl}indan-5-yl)-N-ethylamino] 3,3-dimethylpentanoic acid, 20 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 25 trifluoromethoxyphenyl)-N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 30 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 378 (1-methyl-1H-pyrazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 5 methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethoxyphenyl) N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3-dimethylpentanoic 10 acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 15 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]hexanoic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino] 4,4-dimethylhexanoic acid hydrochloride, 25 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 3,3-dimethylhexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 30 4,4-dimethylpentanoic acid hydrochloride, 379 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 5 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]-4,4-dimethylhexanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 15 acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl cyclohexyl)methanol hydrochloride, 20 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino] 5,5-dimethylhexanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 25 trifluoromethoxyphenyl)-N propylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 30 isobutylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 380 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid amide, 5 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid methylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid dimethylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-chlorophenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N 15 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (m-tolyl)amino]methyll-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3,5-dichlorobenzyl)-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylaminolmethyllcyclohexanecarboxylic acid hydrochloride, 25 trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) N'-(3-methyl-5-trifluoromethylbenzyl)amino]methyl)-4 trifluoromethoxyphenyl)amino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3-chloro-5-trifluoromethylbenzyl) 30 N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 381 trifluoromethoxyphenyl)-N ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) N'-(3-nitro-5-trifluoromethylbenzyl)amino]methyll-4 5 trifluoromethoxyphenyl)aminolmethyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-2,2 difluorobenzo[l,3]dioxol-5-yl)-N 10 ethylamino]methyl cyclohexyl)methanol hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 difluorobenzo(1,3]dioxol-5-yl)-N ethylaminolmethyllcyclohexyl)acetic acid hydrochloride, 15 trans-3-(4-{(N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)propionic acid hydrochloride, trans-(4-{ [N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3-tetrafluoro 2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{ [N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3-tetrafluoro 25 2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-2-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3 tetrafluoro-2,3-dihydrobenzo[l,4]dioxin-6-yl)-N 30 ethylamino]methyl cyclohexyl)acetamide hydrochloride, 382 trans-N-[3,5-bis(trifluoromethyl)benzyl]-N-{2-[N'-ethyl N'-(4-(methoxymethyl)cyclohexylmethyl)amino]-5 trifluoromethoxybenzyl}-(2-methyl-2H-tetrazol-5-yl)amine hydrochloride, 5 trans-2-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylaminolmethyllcyclohexyl)ethanol hydrochloride, trans-(4-{[N-(2-{{N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 15 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 20 acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyllcyclohexylmethyl)phosphonic acid, 25 trans-4-{[N-(2-{[N'-(3-bromo-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 30 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-bromophenyl)-N 383 ethylamino methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-bromophenyl)-N ethylamino]methyllcyclohexyl)acetic acid hydrochloride, 5 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (4-methoxyphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol 15 hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4,5-dimethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethylthiophenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 25 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic 30 acid hydrochloride, 384 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 5 trans-4-({N-[2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-(2,2,2 trifluoroethyl)phenyl]-N ethylamino}methyl)cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyl)-5-methyl-4 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 15 trifluoromethoxyphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-ethylphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 20 trans-4-{[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl)-4 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 25 (4-isopropenylphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl)cyclohexanecarboxylic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid dihydrochloride, 30 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 385 (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 5 (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 10 trifluoromethylphenyl)-N-propylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic 15 acid, trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid, 20 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid methanesulfonate, ethyl trans-(4-{[N-(2-{[N'-[3,5 25 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetate, and trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 30 trifluoromethyiphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid, a prodrug thereof or a pharmaceutically acceptable salt 386 thereof.

9. Use of an effective amount of a compound having a CETP inhibitory activity in the preparation of a medicament for the treatment or prevention of hyper-remnant lipoproteinemia in a 5 patient, wherein said compound is represented by the formula (IX) R1 (R 6 )n B "NN R2N (X) A R*R5 4 wherein R and R2 are the same or different and each is a halogen 10 atom, a nitro group, a cyano group or a C16 alkyl group optionally substituted by halogen atom; R 3 , R 4 and R 5 are the same or different and each is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen atom, a C1-6 alkylthio group optionally 15 substituted by halogen atom or a C 1 - 6 alkoxy group optionally substituted by halogen atom, or R 3 and R 4 or R 4 and R 5 may form, together with a carbon atom they are bonded to, a homocyclic ring optionally having substituent(s) or a heterocyclic ring optionally having substituent(s); 20 A is -N(R ) (R ) (wherein R7 and R8 are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by phenyl group or -(CH 2 )m-COOR 9 (wherein R 9 is a hydrogen atom or a Ci-6 387 alkyl group and m is 0 or an integer of 1 to 5)) or a C 4 - 10 cycloalkylalkyl group (wherein C 4 -10 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, 5 acyl group, Ci-6 alkoxy group, Ci-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl group, C1-6 alkoxy group or phosphono group), -(CH2)q-CON(R 20 ) (R 21 ) (wherein R20 and R 21 are the same or different and each is hydrogen atom or C1-6 alkyl group and q is 0 or an integer of 1 to 5) or 10 (CH 2 )r-COOR 1 0 (wherein R 10 is hydrogen atom or C1-6 alkyl group and r is 0 or an integer of 1 to 5)), 11 12) 13)1 12 13 -C(R ) (R2) (R ) (wherein R", R and R are the same or different and each is a hydrogen atom, a C1-6 alkyl group (wherein Ci-6 alkyl group is optionally substituted by phenyl 15 group or -COOR 9 (wherein R 9 is as defined above) ) or a C4-10 cycloalkylalkyl group (wherein C4-10 cycloalkylalkyl group is optionally substituted by 1 to 3 substituents from halogen atom, nitro group, amino group, hydroxyl group, cyano group, acyl group, C-6 alkoxy group, C1-6 alkyl group (wherein Ci-6 20 alkyl group is optionally substituted by hydroxyl group, C1-6 alkoxy group or phosphono group), -(CH 2 )q-CON(R20) (R ) (wherein R 20, R and q are as defined above) or -(CH 2 )r-COOR 1 0 (wherein Rio and r are as defined above))) or -0-C(R ) (R ) (R 1) (wherein 11 12 13 R , R and R are as defined above); 25 ring B is an aryl group or a heterocyclic residue; R is a hydrogen atom, a halogen atom, a nitro group, an amino group, a hydroxyl group, a cyano group, an acyl group, a C1-6 alkoxy group, a C2-6 alkenyl group or a Ci-6 alkyl group (wherein C1-6 alkyl group is optionally substituted by hydroxyl 30 group or -COOR 4 (wherein R 14 is a hydrogen atom or a Ci-6 alkyl group)); and n is an integer of 1 to 3 388 or a prodrug thereof or a pharmaceutically acceptable salt thereof.

10. The use of claim 9, wherein the compound of the formula (IX) is a compound selected from a group consisting of 5 N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl)-N-[3,5 bis(trifluoromethyl)benzyl]-(2-methyl-2H-tetrazol-5-yl)amine, 3-{[N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-(2-methyl-2H-tetrazol-5 10 yl)amino]methyl}-5-trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl)-(2-methyl-2H tetrazol-5-yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 15 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2-methyl-2H tetrazol-5-yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(2H-tetrazol-5-yl)-[3,5 bis(trifluoromethyl)benzyl]amine, 20 N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl]-(pyrimidin-2 yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-[3,5-bis(trifluoromethyl)benzyl]-(5-methyl-lH 25 pyrazol-3-yl)amine, 5-{N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino}pentanoic acid hydrochloride, methyl trans-4-{[N-(2-{[N'-[3,5 389 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyll-4-trifluoromethoxyphenyl)-N ethylaminolmethyl cyclohexanecarboxylate, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 5 ylmethyl]-N-(2-methyl-2H-tetrazol-5-yl)amino]methyll-5 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(2-ethyl-2H tetrazol-5-yl)amine, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1-methyl-lH [1,2,4]triazol-3-yl)amine, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-phenylamino}methyl)-5-trifluoromethylbenzonitrile, 15 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(4,5-dimethylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(thiazol-2 20 yl)amine hydrochloride, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(thiazol-2-yl)amino}methyl)-5 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 25 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(oxazol-2 yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methylthiazol-2-yl)amine hydrochloride, 390 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 5 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4,5 dimethylthiazol-2-yl)amine hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(5-methylthiazol-2-yl)amino]methyl)-5 trifluoromethylbenzonitrile hydrochloride, 10 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]-N-(4-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(4 15 methyloxazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 methylisothiazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 20 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5 methylisoxazol-3-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3 methylisoxazol-5-yl)amine hydrochloride, 25 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1-methyl-lH pyrazol-3-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(1-methyl-1H 30 pyrazol-4-yl)amine hydrochloride, 391 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5-methyl (1,3,4]thiadiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 5 cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5-methyl [1,3,4]oxadiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-pyridin-3 ylamine hydrochloride, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-pyridin-2 ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[2-(N' cyclopentylmethyl-N'-ethylamino)-5-trifluoromethylbenzyl)-(2 15 methyl-2H-tetrazol-5-yl)amine hydrochloride, 3-{[N-[2-(N'-cyclopentylmethyl-N'-ethylamino)-5 trifluoromethylbenzyl]-N-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-trifluoromethylbenzonitrile hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-ylmethyl)-N ethylamino]pentanoate hydrochloride, 25 methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 30 ethylamino]pentanoic acid hydrochloride, 392 5-[N-(6-{ [N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 5 methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 10 methyl trans-4-{[N-(3-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(1-methyl-1H-pyrazol-3 yl)amino]methyll-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylate hydrochloride, methyl trans-4-{[N-(3-{[N'-(3-cyano-5 15 trifluoromethylbenzyl)-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen-2-yl)-N ethylamino]methyl cyclohexanecarboxylate hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 20 tetrahydronaphthalen-2-yl)-N ethylaminomethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(5-methyl [1,2,4]oxadiazol-3-yl)amine hydrochloride, methyl trans-4-{ [N-(6-{([N'-[3,5 30 bis(trifluoromethyl)benzyl]-N'-(1-methyl-1H-pyrazol-3 393 yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N 5 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, methyl trans-4-{[N-(6-{[N'-(3-cyano-5 trifluoromethylbenzyl)-N'-(l-methyl-lH-pyrazol-3 yl)amino]methyl}indan-5-yl)-N ethylamino]methyl cyclohexanecarboxylate, 10 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 15 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (3-methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, 25 methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)aminolmethyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methyl-isoxazol-5-yl)amino]methyl}indan-5-yl)-N 30 ethylamino]pentanoic acid hydrochloride, 394 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylaminolpentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 5 methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 10 trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-(3-methyl 15 [1,2,4]thiadiazol-5-yl)amine, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-[1,2,4]triazol-3-yl)amino]methylindan-5-yl)-N ethylamino]pentanoic acid hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (1-methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylaminolpentanoate hydrochloride, methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N-ethylaminolpentanoate hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid 30 hydrochloride, 395 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5 trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylaminomethyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl)-5,6,7,8 15 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 20 ethylamino]methyl}cyclohexanecarboxylic acid, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (3-methylisoxazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl cyclohexanecarboxylic acid hydrochloride, 25 trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (3-methylisoxazol-5-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylaminolmethyl}cyclohexanecarboxylic acid hydrochloride, 2-(5-{N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' 30 cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]amino}tetrazol-2-yl)ethanol hydrochloride, 396 methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl)-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentancate hydrochloride, 5 methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (1-methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 10 methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 15 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 20 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoic acid 30 hydrochloride, 397 trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 5 methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethoxyphenyl) N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]pentanoic acid hydrochloride, 10 5-[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) 15 N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 ethyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, 5-{N-[6-((N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 20 hydroxyethyl)-2H-tetrazol-5-yl]aminolmethyl)indan-5-yl]-N ethylamino}pentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N-ethylamino]pentanoic acid 25 hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 2,2-dimethylpentanoic acid hydrochloride, 6-[N-(6-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N'-(2 30 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 398 hexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 3,3-dimethylpentanoic acid hydrochloride, 5 trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, (1-{2-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 10 ethylamino]ethyl}cyclopentyl)acetic acid hydrochloride, trans-4-({N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5-yl] N-ethylaminolmethyl)cyclohexanecarboxylic acid, trans-4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 15 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, (1-{2-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 20 tetrahydronaphthalen-2-yl)-N ethylamino]ethyl}cyclopentyl)acetic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-ethyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl cyclohexanecarboxylic acid hydrochloride, 30 trans-4-({N-[3-({N'-[3,5-bis(trifluoromethyl)benzyl]-N' 399 [2-(2-hydroxyethyl)-2H-tetrazol-5-yl]aminolmethyl)-5,6,7,8 tetrahydronaphthalen-2-yl]-N ethylaminolmethyl)cyclohexanecarboxylic acid hydrochloride, 1-{3-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 5 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]propyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N-ethylamino] 3,3-dimethylpentanoic acid, 10 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 15 trifluoromethoxyphenyl)-N-ethylamino)-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)aminolmethyll-4-trifluoromethylphenyl) N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 20 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-lH-pyrazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(1 25 methyl-lH-pyrazol-3-yl)amino]methyl}-4-trifluoromethoxyphenyl) N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]-3,3-dimethylpentanoic 30 acid hydrochloride, 400 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl)-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]hexanoic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino] 4,4-dimethylhexanoic acid hydrochloride, 15 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 3,3-dimethylhexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino] 20 4,4-dimethylpentanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 25 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N-ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 30 methyl-2H-tetrazol-5-yl)amino]methyll-4-trifluoromethylphenyl) 401 N-ethylamino]-4,4-dimethylhexanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 5 acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino)methyllcyclohexyl)methanol hydrochloride, 10 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino] 5,5-dimethylhexanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 15 trifluoromethoxyphenyl)-N propylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl)-4 trifluoromethoxyphenyl)-N 20 isobutylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid amide, 25 trans-4-{([N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexanecarboxylic acid methylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 30 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 402 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid dimethylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-chlorophenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N 5 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (m-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3,5-dichlorobenzyl)-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 15 trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) N'-(3-methyl-5-trifluoromethylbenzyl)aminolmethyll-4 trifluoromethoxyphenyl)amino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3-chloro-5-trifluoromethylbenzyl) 20 N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl) N'-(3-nitro-5-trifluoromethylbenzyl)amino]methyl}-4 25 trifluoromethoxyphenyl)amino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 difluorobenzo[1,3]dioxol-5-yl)-N 30 ethylamino]methyl}cyclohexyl)methanol hydrochloride, 403 trans-(4-{ [N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 difluorobenzo[1,3]dioxol-5-yl)-N ethylamino]methyllcyclohexyl)acetic acid hydrochloride, 5 trans-3-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)propionic acid hydrochloride, trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 10 (2-methyl-2H-tetrazol-5-yl)amino]methyl)-2,2,3,3-tetrafluoro 2,3-dihydrobenzo[l,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(7-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-2,2,3,3-tetrafluoro 15 2,3-dihydrobenzo[1,4]dioxin-6-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-2-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3 tetrafluoro-2,3-dihydrobenzo[1,4]dioxin-6-yl)-N 20 ethylamino]methyl}cyclohexyl)acetamide hydrochloride, trans-N-[3,5-bis(trifluoromethyl)benzyl]-N-{2-[N'-ethyl N'-(4-(methoxymethyl)cyclohexylmethyl)amino]-5 trifluoromethoxybenzyl}-(2-methyl-2H-tetrazol-5-yl)amine hydrochloride, 25 trans-2-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl] N'-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)ethanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 30 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl)cyclohexyl)methanol 404 hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 5 acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 10 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexylmethyl)phosphonic acid, trans-4-{[N-(2-{[N'-(3-bromo-5-trifluoromethylbenzyl)-N' 15 (2-methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-bromophenyl)-N 20 ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{([N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyll-4-bromophenyl)-N ethylaminolmethylicyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 25 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-4-{ (N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-methoxyphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 405 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)aminolmethyl)-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, 5 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4,5-dimethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 10 trifluoromethylthiophenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{ ([N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5 ethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid 15 hydrochloride, trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylphenyl)-N-propylamino]methyllcyclohexyl)acetic acid hydrochloride, 20 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-4-({N-[2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 25 (2-methyl-2H-tetrazol-5-yl)amino]methyi}-4-(2,2,2 trifluoroethyl)phenyl)-N ethylaminomethyl)cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{ [N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 30 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, 406 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, 5 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-ethylphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 10 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (4-isopropenylphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylaminolmethyl}cyclohexanecarboxylic acid, 15 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (p-tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid dihydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 20 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 25 acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (5-methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, 30 trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 407 (2-methyl-2H-tetrazol-5-yl)aminojmethyl}-5-methyl-4 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 5 (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyllcyclohexyl)acetic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 10 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid methanesulfonate, ethyl trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N 15 ethylamino]methyl}cyclohexyl)acetate, and trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid, a prodrug thereof or a pharmaceutically acceptable salt 20 thereof.

11. An agent when used for the treatment or prophylaxis of hyper-remnant lipoproteinemia in a patient, which comprises a compound of trans-(4-{[N-(2-{[N'-[3,5 bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 25 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylaminolmethyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof having a CETP inhibitory activity as an active ingredient.

12. The agent of claim 11, wherein the trans-(4-{[N-(2-{[N' 30 [3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 408 yl)amino]methyll-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof inhibits the production of chylomicron remnant. 5 13. The agent of claim 11, wherein the trans-(4-{[N-(2-{[N' [3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-methyl-4-trifluoromethylphenyl)-N ethylamino]methyl}cyclohexyl)acetic acid or a pharmaceutically acceptable salt thereof inhibits the production ofremnant 10 lipoprotein is a VLDL remnant.

14. An agent when used for the treatment of prophylaxis of hyper-remnant lipoproteinemia in a patient, which comprises a compound having CETP inhibitory activity and is selected from a group consisting of 15 N-[3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-[3,5 bis(trifluoromethyl)benzyl]-(2-methyl-2H-tetrazol-5-yl)amine, 3-{[N-(3-(N'-cyclopentylmethyl-N'-ethylamino)-5,6,7,8 tetrahydronaphthalen-2-ylmethyl]-N-(2-methyl-2H-tetrazol-5 20 yl)amino]methyl}-5-trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl)-(2-methyl-2H-tetrazol-5 yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl 25 N'-ethylamino)indan-5-ylmethyl]-(2-methyl-2H-tetrazol-5 yl)amine hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-N (2H-tetrazol-5-yl)-[3,5-bis(trifluoromethyl)benzyl]amine, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-N 30 [3,5-bis(trifluoromethyl)benzyl]-(pyrimidin-2-yl)amine 409 hydrochloride, N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl]-N [3,5-bis(trifluoromethyl)benzyl]-(5-methyl-lH-pyrazol-3 yl)amine, 5 5-{N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5-methyl [1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino}pentanoic acid hydrochloride, methyl trans-4-{[N-(2-{ [N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl}-4 10 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylate, 3-{([N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyll N-(2-methyl-2H-tetrazol-5-yl)amino]methyl}-5 trifluoromethylbenzonitrile, 15 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(2-ethyl-2H-tetrazol-5 yl)amine, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(1-methyl-lH-[1,2,4]triazol-3 20 yl)amine, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl) N-phenylamino}methyl)-5-trifluoromethylbenzonitrile, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyll N-(4,5-dimethylthiazol-2-yl)amino]methyl}-5 25 trifluoromethylbenzonitrile, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(thiazol-2-yl)amine hydrochloride, 3-({N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl] 410 N-(thiazol-2-yl)amino}methyl)-5-trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(oxazol-2-yl)amine 5 hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(5-methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl 10 N'-ethylamino)indan-5-ylmethyl]-(4-methylthiazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(4,5-dimethylthiazol-2-yl)amine hydrochloride, 15 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl] N-(5-methylthiazol-2-yl)amino]methyl}-5 trifluoromethylbenzonitrile hydrochloride, 3-{[N-[6-(N'-cyclopentylmethyl-N'-ethylamino)indan-5-ylmethyl] N-(4-methylthiazol-2-yl)amino]methyl}-5 20 trifluoromethylbenzonitrile hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(4-methyloxazol-2-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl 25 N'-ethylamino)indan-5-ylmethyl]-(3-methylisothiazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(5-methylisoxazol-3-yl)amine hydrochloride, 411 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(3-methylisoxazol-5-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl 5 N'-ethylamino)indan-5-ylmethyl]-(1-methyl-1H-pyrazol-3-yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(1-methyl-1H-pyrazol-4-yl)amine hydrochloride, 10 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(5-methyl-[1,3,4]thiadiazol-2 yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(5-methyl-[1,3,4]oxadiazol-2 15 yl)amine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-pyridin-3-ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl)-N-[6-(N'-cyclopentylmethyl 20 N'-ethylamino)indan-5-ylmethyl]-pyridin-2-ylamine hydrochloride, N-[3,5-bis(trifluoromethyl)benzyl]-N-[2-(N'-cyclopentylmethyl N'-ethylamino)-5-trifluoromethylbenzyl]-(2-methyl-2H-tetrazol 5-yl)amine hydrochloride, 25 3-{[N-[2-(N'-cyclopentylmethyl-N'-ethylamino)-5 trifluoromethylbenzyl]-N-(2-methyl-2H-tetrazol-5 yl)amino]methyl}-5-trifluoromethylbenzonitrile hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyllindan-5-yl)-N 30 ethylamino]pentanoate hydrochloride, 412 methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-ylmethyl)-N ethylamino]pentanoate hydrochloride, methyl 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 5 methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoate hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino]pentanoic acid hydrochloride, 10 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2-methyl-2H tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)aminolmethyllindan-5-yl)-N 15 ethylaminolpentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l-methyl-1H pyrazol-3-yl)amino]methyl}indan-5-yl)-N-ethylamino]pentanoic acid hydrochloride, methyl trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' 20 (1-methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyllcyclohexanecarboxylate hydrochloride, methyl trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl) N'-(l-methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N ethylamino]methyl cyclohexanecarboxylate hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-1H-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 413 trans-4-{[N-(3-{ [N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(1 methyl-lH-pyrazol-3-yl)amino]methyll-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(5-methyl-[1,2,4]oxadiazol- 3 yl)amine hydrochloride, methyl trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (1-methyl-1H-pyrazol-3-yl)amino]methyl}indan-5-yl)-N 10 ethylaminolmethyl}cyclohexanecarboxylate hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyllindan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, methyl trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl) 15 N'-(l-methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylate, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 20 trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 30 methylisoxazol-5-yl)amino]methyl}indan-5-yl)-N 414 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, methyl 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyllindan-5-yl)-N ethylamino]pentanoate hydrochloride, 5 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3-methyl isoxazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l-methyl-lH pyrazol-3-yl)amino]methyl}indan-5-yl)-N-ethylamino]pentanoic 10 acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH [1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 15 methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, 20 N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N'-cyclopentylmethyl N'-ethylamino)indan-5-ylmethyl]-(3-methyl-[1,2,4]thiadiazol-5 yl)amine, 5-[N-(6-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l-methyl-lH [1,2,4]triazol-3-yl)amino]methyl}indan-5-yl)-N 25 ethylamino]pentanoic acid hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl)-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylaminolpentanoate hydrochloride, 415 methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-pyrazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate hydrochloride, 5 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH pyrazol-3-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen-2-yl) N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l-methyl-lH pyrazol-3-yl)amino]methyll-5,6,7,8-tetrahydronaphthalen-2-yl) 10 N-ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(3-([N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 15 trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l 20 methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{ [N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 25 tetrahydronaphthalen-2-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, trans-4-{ [N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]methyl}cyclohexanecarboxylic acid 30 hydrochloride, 416 trans-4-{[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5 2-(5-{N-[3,5-bis(trifluoromethyl)benzyl]-N-[6-(N' cyclopentylmethyl-N'-ethylamino)indan-5 ylmethyl]amino}tetrazol-2-yl)ethanol hydrochloride, methyl 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l methyl-1H-[1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8 10 tetrahydronaphthalen-2-yl)-N-ethylamino]pentancate hydrochloride, methyl 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l methyl-lH-[1,2,4]triazol-3-yl)amino]methyl)-5,6,7,8 tetrahydronaphthalen-2-yl)-N-ethylamino]pentanoate 15 hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l-methyl-lH [1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l-methyl-lH 20 [1,2,4]triazol-3-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 25 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(3 methylisoxazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen 2-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-5,6,7,8-tetrahydronaphthalen-2-yl) 30 N-ethylamino]pentanoic acid hydrochloride, 417 5-[N-(3-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2-methyl-2H tetrazol-5-yl)amino]methyll-5,6,7,8-tetrahydronaphthalen-2-yl) N-ethylamino]pentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexanecarboxylic acid, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(-methyl-1H pyrazol-3-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]pentanoic acid hydrochloride, 10 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(l-methyl-1H pyrazol-3-yl)amino]methyl}-4-trifluoromethylphenyl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(l-methyl-lH pyrazol-3-yl)amino]methyl}-4-trifluoromethylphenyl)-N 15 ethylaminolpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-ethyl-2H 20 tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino]pentanoic acid hydrochloride, 5-{N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)indan-5-yl]-N ethylaminolpentanoic acid hydrochloride, 25 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]pentanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino]-2,2 30 dimethylpentanoic acid hydrochloride, 418 6-[N-(6-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino]-hexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2-methyl-2H 5 tetrazol-5-yl)aminolmethyllindan-5-yl)-N-ethylamino]-3,3 dimethylpentanoic acid hydrochloride, trans-4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 ethyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyllcyclohexanecarboxylic acid hydrochloride, 10 (1-{2-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl 2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]ethyl}cyclopentyl)acetic acid hydrochloride, trans-4-({N-[6-({N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 hydroxyethyl)-2H-tetrazol-5-yl]aminolmethyl)indan-5-yl]-N 15 ethylamino}methyl)cyclohexanecarboxylic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, (l-{2-[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl 20 2H-tetrazol-5-yl)amino]methyll-5,6,7,8-tetrahydronaphthalen-2 yl)-N-ethylamino]ethyl}cyclopentyl)acetic acid, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N 25 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(3-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 ethyl-2H-tetrazol-5-yl)amino]methyl}-5,6,7,8 tetrahydronaphthalen-2-yl)-N ethylaminolmethyllcyclohexanecarboxylic acid hydrochloride, 30 trans-4-({N-[3-({N'-[3,5-bis(trifluoromethyl)benzyl]-N'-[2-(2 419 hydroxyethyl)-2H-tetrazol-5-yl]amino}methyl)-5,6,7,8 tetrahydronaphthalen-2-yl]-N ethylamino}methyl)cyclohexanecarboxylic acid hydrochloride, 1-{3-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl 5 2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]propyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(l-methyl-lH pyrazol-3-yl)amino]methyllindan-5-yl)-N-ethylamino]-3,3 dimethylpentanoic acid, 10 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5-methyl [1,2,4]oxadiazol-3-yl)amino]methyllindan-5-yl)-N-ethylamino) 3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N 15 ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, trans-4-([N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(l 20 methyl-lH-pyrazol-3-yl)amino]methyll-4-trifluoromethoxyphenyl) N-ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(l-methyl-lH pyrazol-3-yl)amino]methyll-4-trifluoromethoxyphenyl)-N ethylamino]-3,3-dimethylpentanoic acid hydrochloride, 25 5-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5-methyl [1,2,4]oxadiazol-3-yl)amino]methyl}-4-trifluoromethoxyphenyl) N-ethylamino]-3,3-dimethylpentanoic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[l,2,4]oxadiazol-3-yl)amino]methyl}-4 30 trifluoromethoxyphenyl)-N 420 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]hexanoic acid hydrochloride, 5 trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}indan-5-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino]-4,4 10 dimethylhexanoic acid hydrochloride, 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyllindan-5-yl)-N-ethylamino]-3,3 dimethylhexanoic acid hydrochloride, 5-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H 15 tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino]-4,4 dimethylpentanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 20 acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]-4,4-dimethylhexanoic acid hydrochloride, 6-[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H 25 tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl)-N ethylamino]-4,4-dimethylhexanoic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 421 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl cyclohexyl)methanol hydrochloride, 5 6-[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}indan-5-yl)-N-ethylamino]-5,5 dimethylhexanoic acid hydrochloride, trans-4-{[N-(2-{(N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 10 trifluoromethoxyphenyl)-N propylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N 15 isobutylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid amide, 20 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid methylamide, trans-4-{[N-(2-{[N'-(3,5-bis(trifluoromethyl)benzyl]-N'-(2 25 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid dimethylamide, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(4 chlorophenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 422 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(p tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(m 5 tolyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3,5-dichlorobenzyl)-N'-(2-methyl-2H tetrazol-5-yl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 10 trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl)-N'-(3 methyl-5-trifluoromethylbenzyl)amino]methyl}-4 trifluoromethoxyphenyl)amino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-(2-{[N'-(3-chloro-5-trifluoromethylbenzyl)-N'-(2 15 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl)cyclohexanecarboxylic acid hydrochloride, trans-4-{[N-ethyl-N-(2-{[N'-(2-methyl-2H-tetrazol-5-yl)-N'-(3 nitro-5-trifluoromethylbenzyl)amino]methyl}-4 20 trifluoromethoxyphenyl)amino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 difluorobenzo[1,3]dioxol-5-yl)-N 25 ethylamino]methyl cyclohexyl)methanol hydrochloride, trans-(4-{[N-(6-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-2,2 difluorobenzo[1,3]dioxol-5-yl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 30 trans-3-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 423 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexyl)propionic acid hydrochloride, trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 5 methyl-2H-tetrazol-5-yl)amino]methyll-2,2,3,3-tetrafluoro-2,3 dihydrobenzo[1,4]dioxin-6-yl)-N ethylaminomethyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-2,2,3,3-tetrafluoro-2,3 10 dihydrobenzo[l,4]dioxin-6-yl)-N ethylaminolmethyl}cyclohexyl)acetic acid hydrochloride, trans-2-(4-{[N-(7-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-2,2,3,3-tetrafluoro-2,3 dihydrobenzo[1,4]dioxin-6-yl)-N 15 ethylamino]methyl}cyclohexyl)acetamide hydrochloride, trans-N-[3,5-bis(trifluoromethyl)benzyl]-N-{2-[N'-ethyl-N'-(4 (methoxymethyl)cyclohexylmethyl)amino]-5 trifluoromethoxybenzyl}-(2-methyl-2H-tetrazol-5-yl)amine hydrochloride, 20 trans-2-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)ethanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 25 methyl-2H-tetrazol-5-yl)amino]methyll-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 30 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 424 trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyllcyclohexyl)acetic acid hydrochloride, 5 trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexylmethyl)phosphonic acid, trans-4-{[N-(2-{[N'-(3-bromo-5-trifluoromethylbenzyl)-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyll-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-bromophenyl)-N 15 ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-bromophenyl)-N ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 20 methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5-ethylphenyl) N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(4 methoxyphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 25 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)methanol hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 30 methyl-2H-tetrazol-5-yl)amino]methyl}-4,5-dimethylphenyl)-N 425 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethylthiophenyl)-N 5 ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-chloro-5-ethylphenyl) N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyl}-4-trifluoromethylphenyl) N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methoxy-4 methylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid 15 hydrochloride, trans-4-({N-[2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-(2,2,2 trifluoroethyl)phenyl]-N ethylaminolmethyl)cyclohexanecarboxylic acid hydrochloride, 20 trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-propylamino]methyllcyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{ [N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 25 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-propylamino]methyl)cyclohexyl)acetic acid hydrochloride, trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(4 ethylphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N 30 ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 426 trans-4-{[N-(2-{[N'-(3-cyano-5-trifluoromethylbenzyl)-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid hydrochloride, 5 trans-4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(4 isopropenylphenyl)amino]methyl}-4-trifluoromethoxyphenyl)-N ethylamino]methyl}cyclohexanecarboxylic acid, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(p tolyl)amino]methyll-4-trifluoromethoxyphenyl)-N 10 ethylamino]methyl}cyclohexyl)acetic acid dihydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-4 trifluoromethoxyphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, 15 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(5 20 methyl-[1,2,4]oxadiazol-3-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid hydrochloride, trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 25 trifluoromethylphenyl)-N-propylamino]methyl}cyclohexyl)acetic acid, trans-(4-{ [N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyl}-4-methyl-5 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic 30 acid, 427 trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 methyl-2H-tetrazol-5-yl)amino]methyll-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl}cyclohexyl)acetic acid methanesulfonate, 5 ethyl trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N' (2-methyl-2H-tetrazol-5-yl)amino]methyl)-5-methyl-4 trifluoromethylphenyl)-N-ethylamino)methyl}cyclohexyl)acetate, and trans-(4-{[N-(2-{[N'-[3,5-bis(trifluoromethyl)benzyl]-N'-(2 10 methyl-2H-tetrazol-5-yl)amino]methyl}-5-methyl-4 trifluoromethylphenyl)-N-ethylamino]methyl cyclohexyl)acetic acid, or a pharmaceutically acceptable salt thereof.

15. A method of any one of claims 1, 3, 4, 7 or 8 which method is substantially as herein described with reference to any one 15 of the Examples.

16. Use of any one of claims 2, 5, 6, 9 or 10 substantially as herein described with reference to any one of the Examples.

17. An agent of any one of claims 11 to 14, substantially as herein described with reference to any one of the Examples. 428