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WO2001053267A1 - Compounds exhibiting thrombopoietin receptor agonism - Google Patents

Compounds exhibiting thrombopoietin receptor agonism Download PDF

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Publication number
WO2001053267A1
WO2001053267A1 PCT/JP2001/000411 JP0100411W WO0153267A1 WO 2001053267 A1 WO2001053267 A1 WO 2001053267A1 JP 0100411 W JP0100411 W JP 0100411W WO 0153267 A1 WO0153267 A1 WO 0153267A1
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Prior art keywords
chs
optionally substituted
cfs
substituted
lower alkyl
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PCT/JP2001/000411
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English (en)
French (fr)
Inventor
Hiroshi Takemoto
Takeshi Shiota
Masami Takayama
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Shionogi and Co Ltd
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Shionogi and Co Ltd
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Priority to KR1020027009467A priority Critical patent/KR100563795B1/ko
Priority to US10/169,362 priority patent/US7582665B2/en
Priority to AU27089/01A priority patent/AU777777B2/en
Priority to EP01901511A priority patent/EP1253142A4/en
Priority to CA2397018A priority patent/CA2397018C/en
Priority to JP2001553269A priority patent/JP4136371B2/ja
Publication of WO2001053267A1 publication Critical patent/WO2001053267A1/ja
Anticipated expiration legal-status Critical
Priority to US12/504,604 priority patent/US20100022542A1/en
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Definitions

  • the present invention relates to a compound having a thrombopoietin receptor agonist action.
  • Topopopoetin is a polypeptide cytokine consisting of 332 amino acids, which stimulates the differentiation and proliferation of megakaryocyte cells via receptors to increase platelet production, resulting in thrombocytopenia, etc. It is expected to be used as a drug for the pathological conditions of blood diseases accompanied by abnormal platelet count.
  • the nucleotide sequence of the gene encoding the thrombopoietin receptor is described in Proc. Natl. Acad, Sci. 89: 5640-5644 (1992).
  • low molecular weight peptides having an affinity for the thrombopoietin receptor are also known (Japanese Patent Application Laid-Open No. 10-72,492, WO96 / 40,750), the oral administration of these peptide derivatives Is generally not practical.
  • 1,4-benzothiazepine derivatives are described in JP-A-11-14777 and JP-A-11-152722. .
  • a pharmaceutical composition having a tonpopopoetin receptor agonist action is created to provide an orally administrable platelet production regulator.
  • the present inventors have conducted intensive studies in view of the above points, and as a result, the following compounds have been found to be strong. It has been found to exhibit a high thrombopoietin receptor agonist activity.
  • X 1 is an optionally substituted aryl, an optionally substituted aryl, an optionally substituted heteroaryl, or an optionally substituted heteroarylalkyl;
  • Z 1 is phenylene which may be substituted, monocyclic heteroarylene which may be substituted, monocyclic non-aromatic heterocyclic diyl which may be substituted, or monocyclic cyclo which may be substituted Alkanzir; w 1 is the expression b
  • R, R 2 , R 3 , R 4 , R 7 , and R 8 are each independently a hydrogen atom, a halogen, an optionally substituted lower alkyl, an optionally substituted lower alkyloxy An optionally substituted lower alkylthio, an optionally substituted lower alkenyl, an optionally substituted lower alkynyl, an optionally substituted aryl, an optionally substituted heteroaryl, An optionally substituted cycloalkyl, an optionally substituted aralkyl, an optionally substituted heteroarylalkyl, an optionally substituted non-aromatic heterocyclic group, or an optionally substituted amino;
  • R 5 , R 6 and R 9 are each independently a hydrogen atom, an optionally substituted lower alkyl, an optionally substituted lower alkenyl, an optionally substituted lower alkynyl, Optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted cycloalkyl, optionally substituted
  • a 1 is an optionally substituted aryl or an optionally substituted heteroaryl
  • a dashed line () indicates the presence or absence of a bond) as a compound represented by the formula:, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof. And a thrombopoietin receptor agonist.
  • the present invention relates to the following 2) to 29).
  • X 1 has the formula:
  • R 1 and R 11 are each independently a hydrogen atom, an optionally substituted lower alkyl, carboxy, lower alkyloxycarbonyl, halogen, an optionally substituted aminocarbonyl, Heteroaryl which may be Is an optionally substituted aryl; R 12 is a hydrogen atom or a lower alkyl);
  • X 1 has the formula:
  • a pharmaceutical composition having an agonist action is provided.
  • composition having a thrombopoietin receptor agonist effect according to any one of 1) to 6), wherein Z 1 is 1,4-phenylene which may be substituted with halogen or lower alkyl.
  • R 2 is a hydrogen atom, a lower alkyl, a halogen, a lower alkyloxy, a lower alkylthio, or an optionally substituted amino 1) having the thrombopoietin receptor agonistic action described in any of 1) to 8) above.
  • W 1 has the formula:,,.
  • R 14 and R 15 are each independently a hydrogen atom, or a lower alkyl which may be substituted by one or more substituents selected from the following Substituent Group A, Lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroarylalkyl;
  • Substituent group A a group represented by halogen, halo-lower alkyl, optionally substituted amino, carboxy, lower alkylthio, lower alkylsilyl, or lower alkyloxy), any of 1) to 9).
  • a pharmaceutical composition having a thrombopoietin receptor agonist action a group represented by halogen, halo-lower alkyl, optionally substituted amino, carboxy, lower alkylthio, lower alkylsilyl, or lower alkyloxy), any of 1) to 9).
  • W 1 is the formula:
  • R 13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthio, or halogen; R 26 is a hydrogen atom or lower alkyl; dashed lines have the same meanings as 1).
  • composition having a thrombopoietin receptor agonist action according to any one of 1) to 11), which is a platelet production regulator.
  • a method for regulating platelet production in a mammal comprising administering a therapeutically effective amount of the compound according to any one of (1) to (11) to a mammal, including a human.
  • X 2 is optionally substituted 5-membered heteroaryl or substituted Good pyridyl
  • Z 2 is an optionally substituted phenylene, an optionally substituted 2,5-pyridinyl, an optionally substituted 2,5-thiophenidyl, or an optionally substituted 2,5-furanyl ;
  • W 2 has the formula:,.
  • R 1 R 2 , R 3 , R 4 , R 7 , and R 8 are each independently a hydrogen atom, a halogen, an optionally substituted lower alkyl, an optionally substituted lower alkyloxy, An optionally substituted lower alkylthio, an optionally substituted lower alkenyl, an optionally substituted lower alkynyl, an optionally substituted aryl, an optionally substituted heteroaryl, a substituted An optionally substituted cycloalkyl, an optionally substituted aralkyl, an optionally substituted heteroarylalkyl, an optionally substituted non-aromatic heterocyclic ring, or an optionally substituted amino;
  • R 5 , R 6 , and R 9 are each independently a hydrogen atom, an optionally substituted low Lower alkyl, lower alkenyl which may be substituted, lower alkynyl which may be substituted, aryl which may be substituted, heteroaryl which may be substituted, cycloalkyl which may be substituted, An optionally substituted aranolalkyl, an optionally substituted heteroarylalkyl, or an optionally substituted non-aromatic heterocyclic group;
  • a 2 is optionally substituted aryl or optionally substituted heteroaryl
  • a dashed line () indicates the presence or absence of a bond), provided that R 2 is not imidazolyl, triazolyl, or tetrazolyl], a compound thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof. Salts or solvates thereof.
  • X 2 is of the formula:
  • R 1 ° and R 11 are each independently a hydrogen atom, an optionally substituted lower alkyl, carboxy, lower alkyloxycarbonyl, so, logen, an optionally substituted aminocarbonyl, 15
  • the compound according to 15 which is a group represented by optionally substituted heteroaryl or optionally substituted aryl), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof.
  • X 2 is the formula:
  • R 16 is a hydrogen atom, an optionally substituted lower alkyl, carboxy, lower alkyloxycarbonyl, halogen, or an optionally substituted aminocarbonyl;
  • R 1 7, R 1 8, R 1 9, R 2 0, R 2 1, R 2 2, and R 2 3 are each independently water atom, 1 or more substituents selected from substituent group B Selected from alkyl, cycloalkyl, alkyloxy, alkylthio, halogen, and substituent group C optionally substituted by one or more substituents selected from substituent group B Huunil optionally substituted by one or more substituents, heteroaryl optionally substituted by one or more substituents selected from substituent group C, or one or more selected from substituent group C A non-aromatic heterocyclic group which may be substituted by a substituent,
  • Substituent group B one or more substituents selected from hydroxy, alkyloxy, halogen, carboxy, lower alkyloxycanolebonyl, aryloxycarbonyl, optionally substituted amino, and substituent group C
  • Substituent group C hydroxy, alkyl, halogen, halo lower alkyl, carboxy, lower alkyloxycarbonyl, alkyloxy, optionally substituted amino, non-aromatic heterocycle, and heteroaryl;
  • R 16 and R 17 together may form — CH 2 —, one CH 2 CH 2 —, —CH 2 CH 2 CH 2 —, one O CH 2 —, or one S CH 2 — 15) or 16), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • 1, 4 -phen, Z 2 may be substituted by halogen or lower alkyl
  • R 1 is a hydrogen atom or lower alkyl, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • R 2 is a hydrogen atom, a lower alkyl, halogen, lower Arukiruokishi, lower ⁇ alkylthio or optionally substituted, a good Amino also 1 5) 1-2 0) compound of any crab description, a prodrug thereof, Or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • W 2 is the formula:
  • R 1 R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and A 2 are 15
  • R 2 is imidazolyl, triazolyl, or tetrazolyl 15
  • a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof is imidazolyl, triazolyl, or tetrazolyl 15
  • W 2 is the formula:
  • R 1 3 is a hydrogen atom, lower alkyl, lower Arukiruokishi, lower alkylthio O or halogen
  • R 1 4 and R 1 5 are each independently hydrogen atom, or its, Lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, heteroaryl, heteroarylalkyl which may be substituted by one or more substituents selected from the following substituent groups A Or a non-aromatic heterocyclic group;
  • Substituent group A a compound according to any one of 15) to 22), which is halogen, halo-lower alkyl, optionally substituted amino, carboxy, lower alkylthio, lower alkylsilyl, or lower alkyloxy) A prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • W 2 is the formula:
  • R 13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthio, or halogen; R 26 is a hydrogen atom or lower alkyl; the broken line is synonymous with 15).
  • 15. The compound according to any one of 5) to 22), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • R 16 is a hydrogen atom, an optionally substituted lower alkyl, carboxy, a lower alkyloxycarbonyl, a halogen, or an optionally substituted aminocarboninole;
  • R 1 7, R 1 S, R 1 9, R 2 °, and R 2 1 are each independently hydrogen atom, alkyl optionally substituted by one or more substituents selected from substituent group B, Cycloalkyl, substituted with one or more substituents selected from substituent group B Alkyloxy, alkylthio, halogen, phenyl optionally substituted by one or more substituents selected from substituent group C, and optionally substituted by one or more substituents selected from substituent group C A good heteroaryl, or a non-aromatic heterocyclic group which may be substituted by one or more substituents selected from substituent group C,
  • Substituent group B substituted by one or more substituents selected from hydroxy, alkyloxy, halogen, carboxy, lower alkyloxycarbonyl, aryloxycarbonyl, optionally substituted amino, substituent group C
  • Substituent group C hydroxy, alkyl, halogen, halo-lower-alkyl, alkoxy, lower-alkyloxycarbonyl, alkyloxy, optionally-substituted amino, non-aromatic heterocycle, and heteroaryl;
  • the R 1 6 Oyopi R 1 7 such together connexion - CH 2 -, - CH 2 CH 2 -, - CH 2 CH 2 C
  • R 3 1 and R 3 2 are each independently a hydrogen atom, a lower alkyl, halogen, Nono port lower alkyl, lower Arukiruokishi, halo-lower Arukiruokishi or inhibit mud, alkoxy;
  • W 3 has the formula:
  • R 13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthio, or nodogen
  • R 14 and R 15 are each independently a hydrogen atom, or a lower alkyl, a lower alkenyl, a lower alkynyl, a cycloanolequinole, an arylene, an aranolequinole, each of which may be substituted by the following substituent group A.
  • Substituent group A halogen, halo-lower alkyl, optionally substituted Amino, Cal Bokishi, lower alkylthio, lower alkyl silyl or lower Arukiruokishi,;
  • R 2 4 is hydrogen atom or lower alkyl;
  • R 25 is lower alkyl, optionally substituted aryl, or optionally substituted non-aromatic heterocycle
  • a 3 is a group represented by heteroaryl)], a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • R 2 7 is a hydrogen atom, C 1-3 alkyl, triflumizole Ruo Russia methyl or halo gen;
  • R 28 , R 29 , and R 3 ° each independently represent a hydrogen atom, alkyl optionally substituted by one or more substituents selected from substituent group B, cycloalkyl, substituent group B From alkynolexy, alkylthio, halogen, and substituents selected from one or more substituents selected from among substituents C.
  • a heteroaryl optionally substituted by one or more substituents selected, or a non-aromatic heterocyclic group optionally substituted by one or more substituents selected from substituent group C;
  • Substituent group B one or more substituents selected from hydroxy, alkyloxy, halogen, carboxy, lower alkyloxycanoleponyl, aryloxycarbonyl, optionally substituted amino, and substituent group C
  • Substituent group C hydroxy, alkyl, halogen, halo-lower-alkyl, carboxy, lower-alkyloxycarbonyl, alkyloxy, optionally substituted amino, non-aromatic heterocycle, and heteroaryl;
  • R 3 1 and R 3 2 are each independently a hydrogen atom, a lower alkyl, halogen, C port lower alkyl, lower Arukiruokishi, halo-lower Arukiruokishi or inhibit mud, alkoxy;
  • W 4 has the formula:
  • R 13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthio, or halogen
  • R 14 and R 15 are each independently a hydrogen atom, or lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, heteroaryl, heteroaryl which may be each substituted by the following substituent group A.
  • R 2 4 is represented by a hydrogen atom or a lower alkyl)]; halogen, halo-lower alkyl, optionally substituted Amino, Cal Bokishi, lower alkylthio, lower alkyl silyl or lower Arukiruokishi: substituent group A Or a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
  • R 2 8, R 2 9 , and R 3 respectively ° is independently a hydrogen atom, an alkyl optionally substituted by one or more substituents selected et or Substituent Group B, Shikuroa alkyl, Alkyloxy, alkylthio, halogen optionally substituted by one or more substituents selected from Substituent Group B, fuunyl optionally substituted by one or more substituents selected from Substituent Group C, substituted Heteroaryl optionally substituted by one or more substituents selected from group C, or non-aromatic heterocyclic group optionally substituted by one or more substituents selected from substituent group C- Substituent group B: hydroxy, alkyloxy, halogen, carboxy, lower alkyloxycarbonyl, aryloxycarbonyl, optionally substituted amino, substituent 1 or more which may be phenylene-substituted by substituents selected from C, non-aromatic heterocyclic group, and
  • Substituent group C hydroxy, alkynole, halogen, halo lower alkyl, carboxy, lower alkyloxycarbonyl, alkyloxy, optionally substituted amino, non-aromatic heterocycle, and heteroaryl;
  • R 3 1 and R 3 2 are each independently a hydrogen atom, a lower alkyl, halogen, C port lower alkyl, lower Arukiruokishi, halo-lower Arukiruokishi or inhibit mud, alkoxy;
  • W 4 has the formula: (In the formula, R 13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthio, or lactone;
  • R 14 and R 15 are each independently a hydrogen atom, or lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, heteroaryl, heteroaryl which may be each substituted by the following substituent group A.
  • Substituent group A halogen, halo-lower alkyl, optionally substituted amino, carboxy, lower alkylthio, lower alkylsilyl, or lower alkyloxy;
  • R 24 represents a hydrogen atom or lower alkyl);
  • T is a compound represented by one CH 2 —, one CH 2 CH 2 —, one CH 2 CH 2 CH 2 —, one OCH 2 — or one S CH 2 —], a prodrug thereof, or a pharmaceutically acceptable salt thereof. Acceptable salts or solvates thereof.
  • a pharmaceutical composition comprising the compound according to any one of 15) to 27) as an active ingredient.
  • a pharmaceutical composition having a thrombopoietin receptor agonist effect comprising as an active ingredient the compound according to any one of 15) to 27).
  • a platelet production regulator comprising the compound according to any one of 15) to 27) as an active ingredient.
  • halogen means fluorine, chlorine, bromine, and iodine. Fluorine, chlorine, and bromine are preferred.
  • Alkyl as used herein, alone or in combination with other terms.
  • the term includes a linear or branched monovalent hydrocarbon group having 1 to 15 carbon atoms.
  • Examples include heptyl, n-octynole, n-nonanyl, n-decanyl, n-ndendyl, n-dodecanyl, n-tridecanyl, II-tetradecanyl, n-pentadeyl and the like.
  • the “lower alkyl” used alone or in combination with another term includes a linear or branched monovalent hydrocarbon group having 1 to 8 carbon atoms.
  • C1-C6 alkyl is chosen. More preferably, a C1-C3 alkyl is mentioned.
  • C 1-3 anoalkylene used alone or in combination with other terms, includes methylene, ethylene, and propylene.
  • cycloalkane used alone or in combination with other terms includes a monocyclic cycloalkane having 3 to 8 carbon atoms. Examples include cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane, and cyclooctane. Preferably, a C3-C6 cycloalkane is used.
  • cycloalkyl used alone or in combination with other terms includes a monocyclic cycloalkyl having 3 to 8 carbon atoms.
  • cyclinol propynole cyclopentinole, cyclopentinole, cyclohexinole, cyclin heptyl, and cyclooctyl.
  • C3-C6 cycloalkyl Le Preferably C3-C6 cycloalkyl Le.
  • lower alkenyl refers to a straight-chain or branched-chain monovalent hydrocarbon having 2 to 8 carbon atoms and having one or more double bonds. Include groups. For example, butyl, aryl, 1-propenyl, 2-propenyl, various butynyl isomers and the like can be mentioned. Preferably, a C2-C6 alkynyl is mentioned. More preferably, a C2-C4 alkynyl is mentioned.
  • lower alkynyl j refers to a linear or branched monovalent hydrocarbon group having 2 to 8 carbon atoms and having one or more triple bonds. Examples thereof include ethininole, 1-propyl, 2-propynyl, 1-propenyl, 2-propenyl, crotonyl, isopentenyl, various butyr isomers, etc.
  • C 2 To C 6 alkenyl More preferably, C 2 to C 4 alkenyl is used.
  • aryl used alone or in combination with other terms, includes a monocyclic or condensed cyclic aromatic hydrocarbon.
  • aryl used alone or in combination with other terms, includes a monocyclic or condensed cyclic aromatic hydrocarbon.
  • phenyl, 1.1-naphthyl, 2-naphthyl, anthryl and the like can be mentioned.
  • aralkyl includes those in which the above “lower alkyl” is substituted by one or more of the above “aryl”, and these are substituted at all possible positions.
  • benzyl, phenylethyl for example, 2-phenylethyl
  • phenylpropyl for example, 3-phenylpropyl
  • naphthylmethyl for example, 1-naphthylmethyl, 2-naphthylmethyl, etc.
  • anthrylmethyl for example, , 9 -anthrylmethyl, etc.
  • benzyl and phenyl are mentioned.
  • non-aromatic complex ring group used alone or in combination with other terms includes one or more arbitrarily selected oxygen, sulfur or nitrogen atoms in the ring. It includes non-aromatic 5- to 7-membered rings or rings obtained by condensing two or more of them.
  • pyrrolidinyl eg, 1-pyrrolidinyl, 2-pyrrolidinyl
  • imidazolidinyl eg, 2-imidazolidinyl
  • imidazolinyl eg, imidazolinyl
  • pyrazolidinyl eg, 1-pyrazolidinyl, 2-pyrazolidinyl
  • pyrazolinyl eg, birazopinyl
  • piperazinyl eg, 1-piperazinyl
  • indolinyl eg, 1-indolinyl
  • isoindolinyl eg, isoindolinyl
  • morpholinyl eg, morpholino, 3-morpholinyl
  • tetrahydrofuranyl Tetrahidrobiral
  • morpholino, piperazino, pyrrolidino, tetrahydrofurael, tetrahydrobilanyl and the like are preferable.
  • non-aromatic heterocyclic group in the substituent group B, morpholino, piperazino, piperidino, tetrahydrofuranyl, tetrahydrobilanyl and the like are preferable.
  • non-aromatic heterocyclic group in the substituent group C, morpholino, piperazino, piperidino, pyrrolidino, tetrahydrofuranyl, tetrahydroviranyl and the like are preferable.
  • heteroaryl used alone or in combination with other terms refers to an arbitrarily selected 5- to 6-membered ring containing at least one oxygen, sulfur or nitrogen atom. Which includes an aromatic ring. This may be condensed with the above-mentioned “cycloalkyl j”, the “aryl”, the “non-aromatic heterocyclic group”, or another heteroaryl at all possible positions. Whether the heteroaryl is a single ring or a condensed ring, it can be bonded at all possible positions.
  • pyrrolyl for example, 1-pyrrolinol, 2-pyrrolinol, 3-pyrrolyl
  • furinole for example, 2-furinole, 31-furyl
  • chenyl for example, 2-phenyl, 3-phenyl
  • imidazolyl eg, 2-imidazolyl, 4-imidazolyl
  • pyrazolyl eg, 1-pyrazolyl, 3-pyrazolyl
  • isothiazolyl eg, 3-isothiazolyl
  • Isoxazolinole eg, 3-isoxazolyl
  • oxazolyl eg, 2-oxazolyl
  • thiazolyl eg, 2-thiazolyl
  • pyridyl eg, 2-pyridyl, 3-pyridyl, 4-pyridyl
  • pyrazinyl eg, 2- Virazinyl
  • pyrimidinyl eg, 2-pyrimidinyl
  • R 1 , R 2 , R 3 , R 4 , R 7 and R s pyridyl, thiazolyl, benzothiazolyl and the like are preferable.
  • heteroaryl in A 1 , A 2 and A 3 , imidazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidinyl and the like are preferable.
  • R 1 7, R 1 8, R 1 9, R 2 0, R 2 1, R 2 2, R 2 3, R 2 8, R 2 9, and R 3 pyridyl , Phenyl, pyrenyl, pyrimidinyl, imidazolyl, thiazolyl, oxazolyl, triazolyl and the like.
  • the ⁇ heteroaryl in the substituent group B '' includes pyridyl, pyrazolyl, pyrimidyl, imidazolyl, oxazolyl, thiazolyl, furyl, Chenil is preferred.
  • heteroaryl in the substituent group C, pyridyl, pyrazolyl, imidazolyl and the like are preferable.
  • the “5-membered heteroaryl” includes an optionally selected 5-membered aromatic ring containing at least one oxygen atom, sulfur atom or nitrogen atom in the ring.
  • Thiazolyl is preferred.
  • heteroarylalkyl includes those in which any one or more of the above “heteroaryl” is substituted by one or more of the above “lower alkyl”, and these are substituted at all possible positions.
  • chenylmethyl for example, 2-phenylmethylinole
  • chenylethyl for example, 2- (thiophen-2-ethyl) ethyl
  • furylmethyl for example, 2-furylmethyl
  • furylethyl for example, 2- (furan-12) —Yl) ethyl
  • pyrrolylmethyl eg, 2-pyrrolinolemethyl
  • pyrrolylethyl eg, 2- (pyrrole-2-yl) ethyl
  • imidazolyl methyl eg, 2-imidazolylmethyl, 4-imidazolylmethyl
  • Imidazolylethyl eg, 2- (imidazole-2-yl) ethyl
  • 2-thiazolylmethyl 2- (thiazol-2-yl) ethyl
  • isothiazolylmethyl for example, 3-isothiazolylmethyl
  • isoxazolylmethyl for example, 3-isoxazolylmethyl
  • oxazolylmethyl for example, 2 —Oxazolylmethyl
  • oxazolylethyl eg, 2- (oxazole-1-2-yl) ethyl
  • pyridylmethyl eg, 2-pyridylmethyl, 3-pyridylmethyl, 4-pyridylmethyl
  • Pyridylethyl for example, 2-pyridylethyl and the like.
  • heteroarylalkyl, kill J in R 1 N R 2 , R 3 , R 4 , R 7 , and R 8 include 2-phenylmethyl, 2-furylmethyl and the like.
  • phenylene means a divalent group such as phenyl.
  • 1,4-phenylene Preferable is 1,4-phenylene.
  • monocyclic heteroarylene means a monocyclic heteroaryl divalent group of the above “heteroaryl”. For example, thiofenzil, frangyl, pyridinezyl and the like can be mentioned.
  • 2,5—Cofenzyl, 2,5—Franzyl, 2,5—Pyridine are preferred.
  • “monocyclic non-aromatic double-ringed diyl” means a divalent monocyclic non-aromatic heterocyclic group of the “non-aromatic heterocyclic group”.
  • pyrrolidinediyl, piperidinediyl, pyrazinediyl and the like can be mentioned.
  • monocyclic cycloalkanediyl means a divalent group of a monocyclic cycloalkane in the “cycloalkane”.
  • 1,4-cyclopentanzyl, 1,4-cyclohexanezil and the like can be mentioned.
  • alkyloxy includes methyloxy, ethyloxy, n-propyloxy, isopropyloxy, n-butyloxy, isobutyloxy, sec-butynoleoxy, tert-butynoleoxy, 1-pentynoleoxy, n-hexynoleoxy, and n-heptinoleoxy , N-butinoreoxy, n-nonaninoleoxy, n -decanyloxy and the like.
  • methyloxy, ethyloxy, n-propyloxy, isopropyloxy, and n-butyloxy are used.
  • lower alkyloxy J includes methyloxy, ethyloxy, n-propyloxy, isopropyloxy, n-butyloxy, isoptyloxy, sec-butyloxy, tert-butyloxy, and the like.
  • methyloxy examples include ethyloxy, n-propyloxy, isopropyloxy, and n-butyloxy.
  • lower alkylthio refers to methylthio, ethylthio, etc. I can do it. ⁇
  • lower alkyloxycarbonyl includes methyloxycarbonyl, ethyloxycarbonyl, n-propyloxycarbonyl, isopropionoleoxycarbonyl, n-butyloxycarbonyl, t-butyloxycarbonyl And n-pentyloxycarbonyl.
  • aryloxycarbonyl includes phenyloxycarbonyl, 1-naphthyloxycarbonyl, 2-naphthyloxycarbonyl and the like.
  • acyl used alone or in combination with other terms refers to an alkylcarbonyl wherein the alkyl moiety is the above “lower alkyl” or the aryl moiety is the above “aryl”.
  • Arylcarbonyl For example, acetyl, propionyl, ptiroyl, benzoyl and the like can be mentioned. “Lower alkyl” and “aryl” may be substituted by the respective substituents described below.
  • halo lower alkyl used alone or in combination with other terms includes the above “lower alkyl” substituted with 1 to 8, preferably 1 to 5 positions by the halogen. I do.
  • trifluoromethyl, trichloromethylinole, diphneoleolochinole, triflinoleolotine, dichloroethynole, trichloroethyl, and the like can be mentioned.
  • trifluoromethyl is used.
  • halo-lower alkyloxy includes trifluoromethyloxy, trichloromethinoleoxy, difnorooletinoleoxy, trifnorolenothinoleoxy, dichloroethyloxy, and trichloro mouth Ethyloxy and the like.
  • trif.fluoromethyloxy is used.
  • examples of "asyloxy” include acetyloxy, propionoxy, benzoyloxy and the like.
  • lower alkylsilyl includes triethylsilyl, t-petit Dimethylsilyl and the like.
  • the term “optionally substituted amino” used alone or in combination with other terms includes the above “lower alkyl”, the above “aryl”, the above “aralkyl”, the above “heteroaryl” , The above-mentioned “heteroarylalkyl”, or the above-mentioned “acyl” which may be substituted one or two times.
  • amino, methylamino, dimethylamino, ethylmethylamino, methylamino, ethylmethylamino, benzylamino, acetylamino, benzoylamino and the like can be mentioned.
  • amino, methylamino, dimethylamino, ethylmethylamino, getylamino, and acetylamino are exemplified.
  • the “optionally substituted aminocarbonyl” includes aminocarbonyl, methylaminocarbonyl, dimethylaminopropyl, ethylmethylaminocarbonyl, getylaminocarbonyl and the like. Preferred are aminocarbonyl, methylaminocarbonyl and dimethylaminocarbonyl.
  • the term “optionally substituted ureido” refers to the “lower alkyl”, the “aralkyl”, the “aralkyl”, the “heteroaryl”, the aforementioned “heteroarylalkyl”, Alternatively, the above-mentioned “includes a ureid which may be substituted at one or more positions with acyl J.
  • Examples of the substituent of “optionally substituted lower alkyl” in R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 include hydroxy and carboxy. And halogen, alkyloxy, alkylthio, alkylsilyl, and optionally substituted amino, cyano, and acyl.
  • examples of the substituent in “optionally substituted lower alkyloxy” and “optionally substituted lower alkylthio” include cycloalkyl, lower alkenyl, lower alkylidene, hydroxy, lower alkyloxy, and mercapto.
  • Lower alkylthio, halogen, nitro, cyano, carboxy, lower alkyloxycarbonyl, halo-lower alkyl, halo-lower alkyloxy, substituted or unsubstituted aminocarbonyl, optionally substituted aminocarbonyl, asil, acyloxy, Optionally substituted non-aromatic heterocyclic group, aryloxy (e.g., phenyloxy), aranorecheloxy (e.g., benzyloxy), lower alkylsulfonyl, guanidino, azo group, optionally substituted Ward, N—O— (asil) and the like. These may be substituted one or more times in all possible positions. Preferably, halogen and the like are used.
  • examples of the substituent in “optionally substituted lower alkenyl” and “optionally substituted lower alkynyl” include cycloalkyl, lower alkylidene, hydroxy, lower alkyloxy, mercapto, lower Alkylthio, Halogen, nitro, cyano, carboxy, lower alkyloxycarbonyl, halo-lower alkyl, halo-lower alkyloxy, optionally substituted amino, optionally substituted aminocarbonyl, acyl, acyloxy, substituted Non-aromatic heterocyclic group, aryl, aryloxy (for example, phenyloxy), aralkyl, aralkyloxy (for example, benzyloxy), lower alkylsulfonyl, guanidino, azo, optionally substituted ureido And the like. These may be substituted one or more times in all possible positions.
  • Optionally substituted phenylene "optionally substituted monocyclic heteroarylene”, “optionally substituted 2,5-pyridinediyl”, “optionally substituted 2, 5-thiophenzyl “,” optionally substituted 2,5-furanzyl “,” optionally substituted monocyclic non-aromatic heterocyclic diyl “, and” optionally substituted monocyclic cycloalkanediyl "
  • substituent for " halogen, nitro, cyano, lower alkyl, lower alkyloxy and the like are preferable. Unsubstituted ones are preferred.
  • Is a substituent of the "optionally substituted Ariru" and "good substituted I Ararukiru” in X 1, lower alkyl, human Dorokishi lower alkyl, human Dorokishi, lower Arukiruokishi, lower alkylthio, halogen, Nitro, cyano, carboxy, phenyl, lower alkyl, halo lower alkyloxy, aralkyloxy, optionally substituted amino, optionally substituted aminocarbonyl, aryl, heteroaryl, non-aromatic heterocyclic group, 1 N N— (phenyl) and the like.
  • Preferred substituents include lower alkyl, hydroxy, lower alkyloxy, lower alkylthio, halogen, halo-lower alkyl, aralkyloxy, 1N-N- (phenyl), alkylenedioxy and the like.
  • Examples of the "aryl which may be substituted" in X 1 include phenyl, 3-methylphenyl, 4-methylphenyl, 3,4-dimethylphenyl, 4-ethynolepheninole, 4-t-pentynolepheninole, 4-n-butyl phenyl, 4-II hexinole, 4-n-octynole fenole, 3, 5-g-t-butinole 4-hydroxy feninole, 4-ethynoleoxyphenine, 4-Funolelov ninole, 3,5-Dichlorophenol, 4-Fedophenyl, 4-Trifluoromethylphenyl, 4-Methylenolethiophenyl, 4-Pheninoleoxymethylphenyl, Azobenzene-1 Hey Benzodioxolyl (for example, 1,3-benzodioxolyl) and the like.
  • aryl optionally substituted heteroaryl (eg, pyridyl, imidazolyl), non-aromatic heterocycl
  • alkyl or cycloalkyl optionally substituted by one or more substituents selected from substituent group B may be substituted by one or more substituents selected from substituent group B Alkyloxy, alkylthio, halogen, phenyl optionally substituted by one or more substituents selected from substituent group C, and optionally substituted by one or more substituents selected from substituent group C
  • a non-aromatic heterocyclic group which may be substituted by teloaryl or one or more substituents selected from substituent group C (Substituent group
  • Substituent group C hydroxy, alkyl, halogen, halo-lower-alkyl, carboxy, lower-alkyloxycarbonyl, alkyloxy, optionally-substituted amino, non-aromatic heterocycle, and heteroaryl).
  • the aryl may be a C5-C7 cyclohexane ring (eg, cyclopentane, cyclohexane, etc.) or a non-aromatic complex ring group (eg, tetrahydrofuranyl, 1,3-dioxolyl, 1,4) Gio Condensed with kishur, pyrrolidinyl, etc.), and indane, 1,2,3,4-tetrahydronaphthalene, 1,2,3,4-tetrahydroquinoline, 2,3-dihydrobenzo [1,4] dioxin Benzo [1,3] dioxole, 2,3-dihydrobenzofuran, 2,3-dihydro 1H-indole.
  • a C5-C7 cyclohexane ring eg, cyclopentane, cyclohexane, etc.
  • a non-aromatic complex ring group eg, tetra
  • lower alkyl which may be substituted, lower alkenyl, lower alkyloxycarbonyl, phenyl which may be substituted, heteroaryl, NN—O— (acyl) and the like can be mentioned.
  • the nitrogen atom may be substituted with alkyl, oxo, or the like.
  • alkyl or cycloalkyl optionally substituted by one or more substituents selected from Substituent Group B, alkyloxy optionally substituted by one or more substituents selected from Substituent Group B , Alkylthio, halogen, phenyl optionally substituted by one or more substituents selected from substituent group C, and optionally substituted by one or more substituents selected from substituent group C
  • a non-aromatic heterocyclic group which may be substituted by one or more substituents selected from teloaryl or substituent group c (Substituent group B: hydroxy, alkyl, halogen, carboxy)
  • One or more groups selected from lower alkyloxycarbonyl, aryloxycarbonyl, optionally substituted amino, and substituent group C Phenyl which may be substituted by a group, non-aromatic heterocyclic group, and the Teroariru,
  • Substituent group c hydroxy, alkyl, halogen, halo lower alkyl, carboxy, lower alkyloxycarbonyl, alkyloxy, optionally substituted amino, non-aromatic heterocycle, and heteroaryl).
  • R 1 the optionally substituted heteroaryl in R 11 include halogen, optionally substituted alkyl, cycloalkyl, lower alkenyl, lower alkiel, hydroxy, alkyloxy, mercapto, and lower ⁇ .
  • Alkylthio nitro, cyano, carboxy, lower alkyloxycarbonyl, halo lower alkyl, halo lower alkyloxy, optionally substituted amino, substituted Option
  • alkyl or cycloalkyl optionally substituted by one or more substituents selected from Substituent Group B, alkyloxy optionally substituted by one or more substituents selected from Substituent Group B , Alkylthio, halogen, phenyl which may be substituted by one or more substituents selected from substituent group C, may be substituted by one or more substituents selected from substituent group C
  • a heteroaryl group or a non-aromatic heterocyclic group which may be substituted by one or more substituents selected from substituent group C (Substituent group B: hydroxy, alkyloxy, halogen, carboxy, lower)
  • One or more substituents selected from alkyloxycarbonyl, aryloxycarbol, optionally substituted amino, and substituent group C Thus, optionally substituted fuunyl, non-aromatic heterocyclic group, and heteroaryl,
  • Substituent group C hydroxy, alkyl, halogen, halo-lower-alkyl, carboxy, lower-alkyloxycarbonyl, alkyloxy, optionally-substituted amino, non-aromatic heterocycle, and heteroaryl).
  • ( ⁇ ) 0 — ⁇ means that ⁇ exists up to ⁇ /.
  • (CR C R D ). 2 means that there are 0 to 2 (CRCRD), (CH 2 ). - 2 that (CH 2) there are two 0 means that you present five 1 is (CH 2) J _ ⁇ 3 ⁇ 4 (CH 2).
  • platelet production regulator refers to thrombocytopenia (thrombocytopenia after bone marrow transplantation, thrombocytopenia after chemotherapy, aplastic anemia, myelodysplastic syndrome, refractory sudden thrombocytopenia) Drugs for the pathology of blood diseases associated with abnormal platelet count, such as acquired thrombocytopenia such as purpura and congenital thrombocytopenia such as tombopoetin deficiency. For example, if the platelet count decreases due to administration of an anticancer drug, Thus, when a decrease in platelet count due to anticancer drug administration is predicted, it can be used as a prophylactic agent.
  • regulating platelet production refers to 1) increasing the number of platelets decreased by administration of an anticancer agent or the like, 2) maintaining the number of platelets that will decrease due to administration of an anticancer agent or the like, 3) It includes reducing the degree of decrease in platelet count due to administration of an anticancer drug or the like.
  • FIG. 1 is a graph showing the effect of the compound of the present invention on promoting proliferation and differentiation of megakaryocyte precursor cells by measuring the number of megakaryocyte colonies formed from human bone marrow cells.
  • Fig. 2 The concentration of the compound of the present invention is plotted on the horizontal axis, and the absorbance is plotted on the vertical axis as an index of cell proliferation. It is a graph shown. Open circles indicate the response by human TPO, and solid circles indicate the response by compound (B-1).
  • Fig. 3 A graph showing the cell growth of a mouse TPO-dependent cell line expressing the mouse TPO receptor by the compound of the present invention, with the horizontal axis representing the concentration of the compound of the present invention and the vertical axis the absorbance as an indicator of cell proliferation. It is. The triangles indicate the response by mouse TPO, and the closed circles indicate the response by compound (B-1). BEST MODE FOR CARRYING OUT THE INVENTION
  • the compound (I) of the present invention can be synthesized by the following method A, method B, or a method similar thereto. (Law A)
  • This step is a step of protecting the carboxylic acid of the 4-formyl or 4-monosyl-substituted benzoic acid derivative with RE. Since it is necessary to selectively deprotect two carboxylic acid protecting groups in the third step, the combination with RF is important. For example, when RF is a protecting group that can be deprotected under alkaline conditions, such as methyl and ethyl, RE must be a protecting group that can be deprotected under conditions other than alkaline conditions.
  • Aryl group is a protecting group that can be deprotected under alkaline conditions, such as methyl and ethyl
  • a method of reacting with a corresponding halide in the presence of a suitable base can be used.
  • it can also be synthesized by a condensation reaction or the like using an alcohol derivative as a starting material.
  • This step is a step of converting aldehyde or ketone into olefin.
  • Wittig It can be synthesized by performing a reaction using phosphorus ylide such as a Horner-Emmons reaction, or a dehydration condensation reaction such as a Knoevenagel reaction.
  • This step is a step of performing a deprotection reaction of RE.
  • the protective group RE is deprotected under appropriate reaction conditions using the method described in Protective Groups in Organic Synthesis, Theodora W Green (John Wiley & Sons).
  • This step is performed in a solvent such as tetrahydrofuran, dioxane, dichloromethane, toluene and benzene.
  • a solvent such as tetrahydrofuran, dioxane, dichloromethane, toluene and benzene.
  • active ester method 1-hydroxybenzotriazole, hydroxysuccinimide, dimethylaminopyridine and the like, dicyclohexylcarbodiimide, 1-ethyl-3- (3-dimethylaminopropyl) carbopimidide hydrochloride are used.
  • the reaction can be carried out by using thionyl chloride lidoxalyl chloride as a reagent and once converting free carboxylic acid into acid chloride.
  • the mixed acid anhydride method can be carried out by reacting carboxylic acid with ethyl chloroformate, isobutyl chloroformate and the like to obtain a mixed acid anhydride.
  • a base such as triethylamine or pyridine is used as necessary.
  • This step is a step of performing an RF deprotection reaction. Using a method described in Protective Groups in Organic Synthesis, Theodora W Green (John Wiley & Sons), etc., the protecting group RF is deprotected under appropriate reaction conditions.
  • Step 6 the amide derivative (IX) is reacted with the amide derivative (R 3 -NH 2 ) by an active ester method, an acid chloride method, a mixed acid anhydride method, or the like to obtain an amide derivative (IX).
  • This is the process for obtaining I-A).
  • This step is performed in a solvent such as tetrahydrofuran, dioxane, dichloromethane, toluene, and benzene.
  • a solvent such as tetrahydrofuran, dioxane, dichloromethane, toluene, and benzene.
  • the active ester method 1-hydroxybenzotriazole, hydroxysuccinimide, dimethylaminopyridine, etc., and dicyclohexylcarposimid, 1-ethyl-3-
  • the reaction can be carried out by using (3-dimethylaminopropyl) carbodiimide hydrochloride or the like as a condensing agent.
  • the reaction can be carried out by using thionyl-capped lidoxalyl chloride as a reagent and converting free carboxylic acid into monobutyric acid chloride.
  • the reaction can be carried out by reacting carboxylic acid with ethyl chloroformate, isobutyl chloroformate and the like to obtain a mixed acid anhydride.
  • a base such as triethylamine or pyridine is used as necessary.
  • This method is another method for synthesizing the compound (VIII) in Method A.
  • This step is a step of synthesizing a carboxylic acid amide derivative (XI) by using the same method as in Method A, Step 4.
  • This step is a step of converting the aldehyde derivative (XI) to the olefin derivative (XII) by using the same method as in the second step of Method A.
  • Compound (XII) is obtained by performing the same reaction as in Steps 5 and 6 of Method A to give compound (I-A) , And can be converted.
  • the following compounds may be obtained depending on the conditions of the alkylation at the time of synthesizing the compound.
  • the compound when a broken line in the general formulas (I), (II) and (III) indicates the presence of a bond, the compound includes cis-forms, trans-forms and mixtures thereof.
  • W 1 may Mashimashi cis and trans forms, such as: If a compound Ami Dotaipu Son. The same applies when W 1 is a substituent other than the amide type.
  • solvate refers to, for example, a solvate with an organic solvent, Includes hydrates.
  • a pharmaceutically acceptable salt or a hydrate thereof is also conjugated.
  • alkali metals lithium, sodium, potassium, etc.
  • Salts with alkaline earth metals magnesium, calcium, etc.
  • ammonium organic bases and amino acids
  • inorganic acids hydroochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, etc.
  • organic acids acetic acid, quinone
  • Acid maleic acid, fumaric acid, benzenesulfonic acid, p-toluenesulfonic acid, etc.
  • These salts can be formed by a commonly used method. When forming a hydrate, it may be coordinated with any number of water molecules.
  • a prodrug is a derivative of a compound of the present invention that has a chemically or metabolically degradable group and is a compound that becomes a pharmaceutically active compound of the present invention in vivo by solvolysis or under physiological conditions.
  • a method for selecting an appropriate prodrug derivative and a method for producing the same are described in, for example, Design of Prodrugs, Elsevier, and Amsterdam 1985.
  • the conjugate of the present invention has a carboxyl group
  • an ester derivative produced by reacting the base acidic compound with a suitable alcohol, or the base acid compound and a suitable amine are reacted.
  • Prodrugs such as amide derivatives produced by such methods are exemplified.
  • esters as prodrugs include methyl ester, ethyl ester, n-propyl ester, isopropinole ester, II butino ester, isobutyl ester, tert-butyl ester, morpholino ethyl ester, N, N-jetilcoal amide ester and the like are obtained.
  • a prodrug such as an acyloxy derivative produced by reacting a compound having a hydroxyl group with a suitable acyl halide or a suitable acid anhydride is exemplified. .
  • Particularly preferred acyloxy as prodrugs include one OCOC 2 H 5 , one OCO (t-Bu), —O COC 15 H 31 , one O CO (m-COON a-P h), One OC OCH 2 CH 2 COON a, one OC OCH (NH 2 ) CH 3 , —OCOCH 2 N (CH 3 ) 2 and the like.
  • the compound having an amino group may be reacted with a suitable acid halide or a suitable mixed acid anhydride.
  • prodrugs such as amide derivatives produced by the above.
  • a particularly preferred amide for the pro-drug is NHCO (CH 2 ) 2 . CH 3 , 1 N HCO CH (NH 2 ) CH 3 and the like.
  • the compounds of the present invention are not limited to specific isomers, but include all possible isomers and racemates.
  • the compounds of the present invention show excellent tombopoetinagon activity, and thrombocytopenia (after bone marrow transplantation, after chemotherapy, aplastic anemia, bone marrow dysplasia syndrome)
  • Drugs for the pathology of blood diseases associated with abnormal platelet counts such as intractable thrombocytopenic purpura, acquired thrombocytopenia, and thrombopoietin deficiency, etc.
  • the compound of the present invention When the compound of the present invention is administered to humans for the treatment of the above-mentioned diseases, it is administered orally as powders, granules, tablets, capsules, pills, liquids, or the like, or as injections, suppositories. It can be administered parenterally as an agent, transdermal absorber, inhalant and the like.
  • a pharmaceutical formulation can be prepared by mixing an effective amount of the compound with excipients, binders, wetting agents, disintegrating agents, lubricants and other pharmaceutical additives suitable for the dosage form, if necessary. it can.
  • the product In the case of injections, the product should be sterilized with a suitable carrier.
  • Dosages will vary depending on disease state, route of administration, patient age, or body weight, but for oral administration to adults, usually 0.1 to 100 mg / kg / day, preferably 1 to 20 mg / kgZ day.
  • n-Pr n—propyl i — P r: Isopropyl
  • propargyl z ⁇ no noreginole, allyl: arinore, pyrazole: pyrazonole, pyrimidine: hirimycin, pipei'idine: piperidine, methyl: methinolle, cyclohexylmethyl: cyclohexylmethyl:
  • a catalyst amount of DMF was added to a THF (150 ml) solution of the compound (A-2) (690 mg) and oxalyl chloride (420 ⁇ l), and the mixture was stirred at 70 ° C. for 1 hour.
  • the reaction solution was distilled off under reduced pressure, toluene was added to the obtained residue, and toluene was distilled off under reduced pressure.
  • THF 100 ml was added to the obtained carboxylic acid chloride, and the mixture was ice-cooled.
  • ether and sodium hydroxide (5 g) were added to a 28% aqueous ammonia solution (20 ml) under ice cooling, and the mixture was stirred for 10 minutes and allowed to stand.
  • This ether solution was added to a THF solution of the acid chloride, and the mixture was stirred under ice-cooling for 1 hour.
  • the reaction solution was partitioned between ethyl acetate-THF-water.
  • the organic solvent layer was washed with dilute aqueous hydrochloric acid, aqueous sodium bicarbonate, water, and saturated saline, and dried over magnesium sulfate.
  • the compound (B-1) was purified by purifying the residue obtained by evaporating the solvent under reduced pressure by silica gel column column chromatography (ethyl acetate: !! 10-10: 1 to ethyl acetate). Was obtained as colorless crystals (400 mg).
  • Table 19 shows the physical constants of Compound E Group in Table 20
  • Table 21 shows the physical constants of Compound F Group Compounds
  • Table 22 shows the physical constants of Compound G Group Compounds.
  • Table 3 shows the physical constants of the compounds in Group H in Tables 24 to 25, and Table 26 shows the physical constants of the compounds in Compound I group.
  • Table 4
  • Methoxy-methoxycarbonylmethyl-triphenylphosphonium chloride (152 mg) and 2- (4-formylbenzoylamino) -4. (3,4-dichlorophenyl) thiazole (57 mg) ) was suspended in methylene chloride (3 ml), and triethylamine (38 mg) was added. Stirred overnight at room temperature. After concentration, the residue was purified by silica gel column chromatography to obtain 30 rag of the desired compound (A-15).
  • Compound (K-15) was synthesized by performing the same reaction as in the fifth step of Example 1 using aldehyde compound (K-14) as a raw material.
  • the physical constants are shown in Table 29.
  • PhCHaCmO, Br (M.48.0, H, H, F, PliCH 2 CH 20 , CH 3 ), (M-481, H, H, F, CF3O, H), (M-482, H, H , F, CFsO, CI), (M-483, H, H, F, CFsO, F), (M-484, H, H, P, CFsO, CFs), (M-485, H, H, F , CFsO, Br), (M-486, H, H, F, CFsO, CHs), (M-487, H, H, F, Ph, H), (M-488, H, H, F, Ph , CI), (M-489, H, H, F, Ph, F), (M-490, H, H, F, Ph, CFs), (M-491, H, H, F, Ph, Br, ), (M-492, H, H, F, Ph, CH 3 ), (M-493, H, H, F
  • EtOCH 2 CH 2 , CFs (M-641, H, H, F, EtOCH 2 CH 2 , Br), (M-642, H, H, F,-EtOCH 2 CH 2; CH 3 ), (M -643, H, H, F, MeOCH 2 CH 2 OCH 2 CH 2 , H), (M-644, H, H, F, MeOCH 2 CH 2 OCH 2 CH 2 , CI), (M-645, H , H, F, MeOCH 2 CH 2 OCH 2 CH 2) F), (M-646, H, H, F, MeOCHsCH OCHsCHs, CFs), (M-647, H, H, F,
  • EtOCH 2 CH2, CH 3 (M-997, H, H, CI, MeOCH 2 CH 2 OCH 2 CH 2 , H), (M-998, H, H, CI, MeOCHsCHsOCHaCHs, CI), (M- 999, H, H, CI, MeOCHaCHsOCHsCHs, F) ; (M-1000, H, H, CI, MeOCH 2 CH 2 OCH 2 CH 2 , CFs), (M-1001, H, H, Cl,
  • HOCH2CH2OCH2CH2, F (M- 1396, H, F, H, HOCH2CH2OCH2CH2, CPs), (M- 1397, H, F, H, HOCH 2 CH 2 OCH 2 CH 2, Br), (M-1398, H , F, H,
  • MeOCH 2 CH 2 OCH 2 CH 2 , CH 3 (M-2065, H, F, CI, MeOCH 2 CH 2 , H), (M-2066, H, F, CI, MeOCH 2 CH2, CI), (M-2067, H, F, CI, MeOCHaCHa, F), (M-2068, H, F, CI, MeOCH 2 CH 2) CFs), (M-2069, H, F, CI, MeOCH 2 CH 2 , Br), (M-2070, H, F, CI, MeOCH 2 CH 2 , CH 3 ), (M-2071, H, F, CI, HOCH 2; H), (M-2072, H, F, CI, HOCH 2 , CI), (M-2073, H, F ; CI, HOCH 2 , F), (M-2074, H, F, CI, HOCH2, CFs), (M-2075, H, F, CI, HOCHs, Br), (M-2076, H,
  • HOOCCHaCHaCHa, F) (M- 2374, H, CH 3, H, HOOCCH 2 CH 2 CH 2, CFs), (M-2375, H, CHs, H, HOOCCH 2 CH 2 CH 2> Br), (M -2376, H, CHs, H, HOOCCH 2 CH 2 CH 2 , CHs), (M-2377, H, CH 3 , H, HOOCCH 2 CH 2 CH 2 CH 2 , CH), (M-2378, H, CHs, H, HOOCCH2CH 2 CH2CH 2) CI), (M-2379, H, CHs, H, HOOCCH 2 CH 2 CH 2 CH2, F), (M-2380, H, CHs, H, HOOCCH 2 CH 2 CH 2 CH 2 , CFs), (M-2381, H, CHs, H, H,
  • cyclohexylmetliyl, CI) (M-2475, H, CH3, H, cyclohexylmethyl, F), (M-2476, H, CHs, H, cyclohexylmethyl, CFs), (M-2477, H 'CHs, H, cyclohexylmethyl, (Br), (M-2478, H, CHs, H, cyclohexylmethyl, CHs), (M-2479, H, CHs, F, H, H), (M-2480, H, CHs, F, H, CI) , (M-2481, H, CHs, F, H, F), (M-2482, H, CH 3 , F, H, CF 3 ), (M-2483, H, CHa, F, H, Br) , (M-2484, H, CH 3> F, H, CH 3 ), (M-2485, H, CHs, F, F, H), (M-2486, H, CH 3 , F 'F, CI
  • MeOCH 2 CH 2 , H (M-2774, H, CH 8> F, MeOCH 2 CH 2) CI), (M-2775, H, CHs, F, MeOCHaCHs, F), (M-2776, H , CH 3 , F, MeOCH 2 CH 2 , CF 3 ), (M-2777, H, CHs, F, MeOCH 2 CH 2 , Br), (M-2778, H, CHa, F 'MeOCH 2 CH 2 , CHs), (M-2779, H, CHs, F, HOCH 2, H), (M-2780, H, CHs, F, HOCH2, CI), (M-2781, H, CHs, P, HOCH 2) F), (M-2782, H, CH 3, F, HOCH 2, CPs), (M-2783, H, CHs, F, HOCH 2, Br), (M-2784, H, CHs, F, HOCH 2) CHs ), (M-2785, H
  • HOOCCH 2 CH 2 CH2, F (M-3082, H, CH3, CI, HOOCCHaCHaCHs, CFs), (M- 3083, H, CHs, CI, HOO CCH 2 CH 2 CH 2 , Br), (M- 3084, H, CH 3 , CI, HOOCCH 2 CH 2 CH 2 , CHs), (M-3085, H, CH 3 , CI, HOOCCHsCK CHsCHs, H) '(M-3086, H, CHs, CI, HOOCCH2CH2CH2, (CI), (M-3087, H, CH 3 , CI, HOOCCH2CH2CH2CH2, F), (M-3088, H 'CHs, CI, HOO CCHsCHsCHsCHs, CF 3 ), (M-3089, H' CH 3 , CI, HOOC CH2 CH2CH2 CH2, Br), (M-3090, H, CHs, CI, HOOCCH 2 CH 2 CH2, F
  • HOOCCHaCHaCHaCHa, H) (M-3440, F, H, H, HOOCCH2CH2CH2CH2, CI), (M-3441, F, H, H, HOO CCH 2 CH 2 CH 2 CH2, F), (M-3442, F , H, H,
  • MeOCH 2 CH20CH2CH 2) Br (M-3834, F'H, F, MeOCH 2 CH 2 OCH 2 CH2, CH 3 ), (M-3835, F, H, F, MeOCH 2 CH 2 , H), (M-3836, F, H, F, MeOCH 2 CH 2 , CI), (M- 3837, F, H, F, MeOCH 2 CH 2 , F), (M-3838, F 'H, F, MeOCH 2 CH 2 , CF 3 ), (M-3839, F, H, F, MeOCH 2 CH2, Br), (M-3840, F, H, F, MeOCH 2 CH 2) CHs), (M-3841, F, H, F, HOCH 2 , H) '(M-3842, F, H, F, HOCH 2 , CI), (M-3843, F, H, F, HOCH 2 , F), (M-3844 , F, H, F, HOCH2, CF 3
  • HOOCCHaCHsCHsCHs, CI) (M-4503, F, F, H, HOOCCH 2 CH 2 CH 2 CH 2 , F), (M-4504, F, F, H, HOOCCH2CH 2 CH 2 CH 2) CF 3 ), (M-4505, F, P, H,
  • HOCH2CH20CH2CH 2CH 2) H H
  • M-4580 F, F, H, HOCH2CH2OCH2CH2, CI
  • M-4581 F, F, H, HOCH 2 CH 2 OCH 2 CH2, F
  • M-4582 F , F, H, HOCH2CH 2 OCH 2 CH 2; CF 3
  • M-4583 F, F, H, HOCH2CH 2 OCH 2 CH2, Br
  • M-4584 F, F, H,
  • EtOCH 2 CH 2 , CFs (M-4889, F, F, F, EtOCH 2 CH 2) Br), (M-4890, F, F, F, EtOCH 2 CH 2) CH 3 ), (M- 4891, F, F, F, MeOCH 2 CH20CH 2 CH 2 , H), (M-4892, F, F, MeOCH 2 CH20CH2CH 2; CI), (M-4893, F, F, F, MeOCH 2 CH 2 OCH 2 CH2, F), (M-4894, F, F, F, MeOCHaCHsOCHsCHs, CFs), (M-4895, F, F, F,
  • MeOCH 2 CH 2 OCH 2 CH 2 , CF 3 MeOCH 2 CH 2 OCH 2 CH 2 , CF 3 ), (M-5603, F, CH 3 , H, MeOCH 2 CH 2 OCH 2 CH 2 , Br), (M-5604, F, CHs, H, MeOGH2CH 2 OCH 2 CH 2 , CHs), (M-5605, P, CHs, H,
  • MeOCH 2 CH 2 , H (M-5960, F 'CH 3 , F, MeOCH 2 CH 2 , CI), (M-5961, F, CHs, F, MeOCHsCHs, F), (M-5962, F , CHs, F, MeOCH 2 CH 2; CFs), (M-5963, F, CHs, F, MeOCH 2 CH 2 , Br), (M-5964, F, CH 3 , F, MeOCH 2 CH 2 , CHs ), (M-5965, F , CH 3, F, HOCH 2, H), (M-5966, F, CH 3, F, HOCH2, CI), (M-5967, F, CHs, F, HOCH2, F), (M-5'968, F, CH 3) F, HOCH 2 , CFs), (M-5969, F ; CHs, F, HOCH 2 , Br), (M-5970, F, CHs, F , HOCH 2) CH 3 ),
  • EtOCH 2 CH 2 , H (M-7010, CI, H, F, EtOCH 2 CH 2; CI), (M-7011, CI, H, F, EtOCH 2 CH 2) F), (M-7012 , CI, H, F, EtOCH 2 CH 2; CFs), (M-7013, CI, H, F, EtOCH 2 CH 2 , Br), (M-7014, CI, H, F, EtOCH 2 CH 2) CHs), (M-7015, CI, H, F, MeOCH2CH20CH 2 CH 2; H), (M-7016, CI, H, F 'MeOCH 2 CH 2 OCH2CH2 ; CI), (M-7017, Cl ; H , F, MeOCH 2 CH20CH 2 CH 2) F), (M-7018, CI, H, F,
  • MeOCH 2 CH20CH 2 CH 2 , CF 3 MeOCH 2 CH20CH 2 CH 2 , CF 3 ), (M-7019, CI, H, F, MeOCH2CH 2 OCH 2 CH2, Br), (M-7020, CI, H, F, MeOCH2CH 2 OCH 2 CH2 ; CHs) , (M-7021, CI, H, F,
  • PI1CH2CH2O, H (M- 7202, CI, H, CI, PhCH2CH 2 0, CI), (M-7203, CI, H, CI, PliCHsCHsO, F); (M-7204, CI, H, CI, PhCH 2 CH 2 0, CFs), (M-7205, CI, H, CI, PI1CH2CH2O, Br), (M-7206, CI, H, CI, PI1CH2CH2O, CHs), (M-7207, CI, H, (CI, CF 30 , H), (M-7208, CI, H, CI, CFsO, CI), (M-7209, CI, H, CI, CFsO, F), (M-7210, CI, ⁇ , CI, CFsO, CF 3 ), (M-7211, CI, H, CI, CFsO, Br), (M-7212, CI, H, CI, CFsO, CH
  • MeOCH 2 CH 2 OCH2CH 2 , F) (M-7726, CI, F, H, MeOCH 2 CH 2 OCK CH2, CF 3 ), (M-7727, CI, F, H, MeOCH 2 CH 2 OCH2CH2, Br ), (M-7728, CI, F, H,
  • EtOCH 2 , Br (M-8070, CI, F, F, EtOCH 2 , CH 3 ), (M-8071, CI, F, F, EtOCH 2 CH 2 , H), (M-8072, CI, F, F, EtOCH 2 CH 2) CI), (M-8073, CI, F, F, EtOCH 2 CIi 2 'F), (M-8074, CI,, F, EtOCHsCHs, CFs), (M-8075 , CI, P, F, EtOCH 2 CH 2 , Br), (M-8076, CI, F, F, EtOCH 2 CH 2; CH 3 ), (M-8077, CI, F, F, MeOCH 2 CH 2 OCH 2 CH 2) H), (M-8078, CI, F, F, MeOCH 2 CH 2 OCH 2 CH 2 , CI), (M-8079, CI, F, F, F, F, F,
  • MeOCH 2 CH 2 OCH 2 CH 2 , CHs MeOCH 2 CH 2 OCH 2 CH 2 , CHs
  • M-8083 CI, F, F, MeOCH 2 CH 2 , H
  • M-8084 CI, F, F, MeOCH 2 CH 2 , CI
  • M-8085 CI, F, F, MeOCH 2 CH 2) F
  • M-8087, CI, P, F, MeOCH 2 CH 2) Br M-8088, CI, F, F,
  • HOCH2CH2OCH2CH2, F (M- 8122, CI, F, F, HOGH2CH2OCH2CH2, CP 3), (M- 8123, CI, F; F, HOCH2CH20CH 2 CH 2, Br), (M-8124, CI, F, F,
  • HOCH 2 CH 2 CH2CH2, CI) (M-9879, CHs, H, H, HOCH 2 CH 2 CH 2 CH 2 , F), (M-9880, CH 3 , H, H, HOCH 2 CH 2 CH 2 CH 2, CFs), (M -9881, CH 3, H, H, HOCH 2 CH 2 CH2CH 2, Br), (M-9882, CHs, H, H, HOCH 2 CH 2 CH 2 CH 2, CHs) , (M-9883, CH 3 , H, H,
  • M-10239, CHs, H, P, HOCH2CH2CH2CH2, F (M-10240, CH 3; H, F, HOCH 2 CH 2 CH 2 CH 2 CH 2, CFs), (M-10241, CH 3, H, F, HOCH 2 CH 2 CH 2 CH2CH 2, Br), (M-10242, CH 3, H, F, HOCH2CH2CH2CH2CH2, CHs), (M-10243, CHs, H, F, HOCH2CH2OCH2CH2, H), ( M-10244, CH 3; H, F, HOCH 2 CH 2 OCH 2 CH 2, CI), (M-10245, CHs, H, F, HOCH 2 CH 2 OCH 2 CH 2 , F), (M-10246, CHs, H, F ,; HOCH 2 CH 2 OCH2CH 2 , CF 3 ), (M-10247, CH 3 , H, F, HOCH 2
  • HOOCCH2CH2CH2, CF 3 (M -10517, CHs, H, CI, HOOCCH2CH2CH2, Br), (M- 10518, CHs, H, CI, HOOCCH2CH2CH2, CH 3), (M-10519, CH 3, H, CI ,
  • MeOCH 2 CH 2 OCH 2 CH 2 , F MeOCH 2 CH 2 OCH 2 CH 2 , F
  • M-10558, CH 3 , H, CI, MeOCH 2 CH 2 OCH 2 CH 2 , CFs MeOCH 2 CH 2 OCH 2 CH 2 , F
  • M-10564, CHs, H, CI, MeOCH 2 CH 2 , CFs (M-10565, CHs, H, CI, MeOCH 2 CH 2) Br)
  • HOOCCH 2 CH 2 CH 2 CH 2j CFs (M-10877, CH 3 , F, H, HOOCCHsCHsCHsCHa, Br), (M-10878, CHs, F, H, HOOCCHsCHsCH CHb, CH 3 ), (M-10879 , CH 3 , F, H, (Me) 2 NCOCH2CH 2 CH 2 CH2 ; H), (M-10880, CHs, F, H,
  • MeOCH2CH 2 OCH 2 CH 2 'CI (M-10911, CHs, F, H, MeOCH 2 CH 2 OCH2CH 2 , F), (M-10912, CH 3) F, H, MeOCH 2 CH 2 OCH2CH2, CF 3), (M-10913, CH 3, F, H, MeOCH 2 CH20CH 2 CH 2, Br), (M-10914, CHs, F, H, MeOCHsCB OCB CHs, CH 3), (M-10915, CHs , F, H, MeOCH 2 CH 2 , H), (M-10916, CHs, F, H, MeOCHsCHs, CI), (M-10917, CH 3 , F, H, MeOCH 2 CH 2) F), ( M-10918, CHs, F, H, MeOCH 2 CH 2 , CFs), (M-10919, CH 3 , F, H, MeOCH 2 CH 2; Br), (M-10920, CHs, F, H, MeOCH
  • MeOCHsCHsOCHsCHs, CI) (M-11265, CHs, F, F, MeOCH 2 CH 2 OCH2CH 2> F), (M-11266, CHs, F, F, MeOCH 2 CH 2 OCH2CH 2; CF 3 ), (M -11267, CH 3 , F, F, MeOCH 2 CH 2 OCH 2 CH 2 , Br), (M-11268, CHs, F, F, MeOCH 2 CH 2 OCH 2 CH 2) CHs), (M-11269, CHs, F, F, MeOCH 2 CH 2) H), (M-11270, CHs, F, F, MeOCH 2 CH 2 , CI), (M-11271, CHs, F, F, MeOCH 2 CH 2 , F ), (M-11272, CH 3 , F, F, MeOCH 2 CH 2; CF 3 ), (M-11273, CHs, F, F, MeOCH 2 CH 2) Br), (M-11274, CH 3) F, F, MeOCHa
  • HOCH2CH 2 CH2, CI) ( M-11643, CHs, F, CI, HOCHsCHsCH, F), (M-11644, CH 3, F, CI, HOCH2CH2CH2, CP 3), (M-11645, CH 3, F , CI, HOCH 2 CH2CH 2) Br), (M-11646, CH 3 , F, CI, HOCH 2 CH 2 CH 2 , CHs), (M-11647, CH 3 , F, CI,
  • EtOCH 2 CH 2 , F (M-11968, CH 3; CH 3 , H, EtOCH 2 CH 2) CFs), (M-11969, CHa, CH 3 , H, EtOCH2CH 2) Br), (M- 11970, CHs, CHs, H, EtOCH 2 CH 2 , CHa), (M-11971, CH 3) CHs, H, MeOCU 2 CH 2 OCH 2 CH 2 , H), (M-11972, CH 3 , CH 3 ; H, MeOCH 2 CH 2 OCH 2 CH 2 , CI), (M-11973, CH 3 , CH 3) H, MeOCH 2 CH 2 OCH 2 CH 2 , F), (M-11974, CH 3; CHs, H, MeOCH 2 CH20CH 2 CH2, CFa), (M-11975, CH 3 , CH 3 , H, MeOCH 2 CH 2 OCH 2 CH 2 , Br), (M-11976, CHs, CH 3 , H, MeOCH 2 CH 2
  • HOCH 2 CH 2 CH 2 CH 2 , CFs (M-12005, CH 3 , CHs, H, HOCH 2 CH 2 CH 2 CH 2 , Br), (M-12006, CH 3 , CH 3 , H, HOCH 2 CH 2 CH 2 CH2 ; CHs), (M-12007, CHs, CH 3; H, HOCHaCHsCHaCHsCHs, H), (M-12008, CHs, CHs, H, HOCH 2 CH 2 CH 2 CH2CH 2 , CI), (M-12009, CHs, CHs, H, HOCH 2 CH 2 CH 2 CH 2 CH 2 , F), (M-12010, CH 3 , CHs, H, HO CH2CH2CH2CH2, CFs), (M-12011, CHs, CH 3) H,

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Description

明細書 トロンボポェチン受容体ァゴニス ト作用を有する化合物 技術分野
本発明は、 トロンボポェチン受容体ァゴニス ト作用を有する化合物に関する。 背景技術
ト口ンポポェチンは、 3 3 2個のアミノ酸からなるポリぺプチドサイ トカイン であり、 受容体を介して巨核球細胞の分化、 増殖を刺激することにより血小板産 生を亢進することから、 血小板減少症等の血小板数の異常を伴う血液疾患の病態 に対する薬剤と して期待されている。 トロンボポェチン受容体をコードする遺伝 子の塩基配列は、 Proc. Natl. Acad, Sci.89:5640-5644 (1992)に記載されている。 トロンボポェチン受容体に親和性を有する低分子ぺプチドも知られているが （特 開平 1 0— 7 2 4 9 2 , WO 9 6 /4 0 7 5 0) 、 これらのぺプチド誘導体の経 口投与は一般的に実用的でない。
トロンボポェチン受容体に親和性を有する低分子化合物としては、 1 , 4—ベ ンゾチアゼピン誘導体が特開平 1 1一 1 4 7 7およぴ特開平 1 1— 1 5 2 2 7 6 に記載されている。
本発明化合物と類似の構造を有する化合物が、 特開平 1 0— 2 8 7 6 3 4等に 記載されているが、 ト口ンボポェチン受容体親和性に関する記載はない。 発明の開示
ト口ンポポェチン受容体ァゴニス ト作用を有する医薬組成物を創製し、 経口投 与可能な血小板産生調節剤を提供する。
本発明者らは以上の点に鑑み、 鋭意検討を重ねた結果、 以下に示す化合物が強 い ト ロンボポェチン受容体ァゴニス ト活性を示すことを見出した。
すなわち、 本発明は、 1 ) 一般式 （ I ) ：
X1— γ1— z1— w1 (Γ)
[式中、 X 1は置換されていてもよいァリール、 置換されていてもよいァラルキ ル、 置換されていてもよいへテロアリール、 または置換されていてもよいへテロ ァリールアルキル ；
Y 1は— NRACO— （C RCRD) 0一 2—、 一 NRACO— (CH2) 0— 2— V―、 — N R A C O— C R c= C RD—、 - V- (CH2) 1_5-NRACO- (CH2) o一 2—、 - V- (CH2) 5— CONRA— (CH2) 0— 2—、 — CONRA— (CH2) 。― 2—、 - (CH2) 。― 2— NRA— S 02— (CH2) 0— 2—、 - (C H2) 。― 2— S 02 - NRA— (CH2) 。 一、 — NRA— (CH2) 。― 2 -、 一 NRA— CO— NRA—、 一 N RA— C S— N RA—、 一 N= C (- S R A) - N R A—、 一 NRAC S NRACO—、 — N= C (- S RA) — NRACO—、 一 NRA 一 (CH2) 1_2-NRA- CO-N — NRACONRANRBCO—、 または一 N = C (— NRARA) - N RAC O- (式中、 R Aはそれぞれ独立して水素原子ま たは低級アルキル； RBは水素原子またはフエニル； Rcおよび RDはそれぞれ独 立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されて いてもよい低級アルキルォキシ、 置換されていてもよい低級アルキルチオ、 置換 されていてもよい低級アルケニル、 置換されていてもよい低級アルキニル、 置換 されていてもよいァリール、 置換されていてもよいへテロアリール、 置換されて いてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていて もよいへテロァリールアルキル、 置換されていてもよい非芳香族複素環基、 また は置換されていてもよいアミノ ； Vは酸素原子または硫黄原子） ；
Z 1は置換されていてもよいフエ二レン、 置換されていてもよい単環へテロアリ レン、 置換されていてもよい単環非芳香族複素環ジィル、 または置換されていて もよい単環シクロアルカンジィル； w 1は式 b
Figure imgf000005_0001
(式中、 R 、 R 2、 R 3、 R 4、 R 7、 および R 8はそれぞれ独立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されていてもよい低級アル キルォキシ、 置換されていてもよい低級アルキルチオ、 置換されていてもよい低 級ァルケニル、 置換されていてもよ.い低級アルキニル、 置換されていてもよいァ リール、 置換されていてもよいへテロアリール、 置換されていてもよいシクロア ルキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロアリー ルアルキル、 置換されていてもよい非芳香族複素環基、 または置換されていても よいァミノ ； R 5、 R 6、 および R 9はそれぞれ独立して、 水素原子、 置換されていてもよい低 級アルキル、 置換されていてもよい低級アルケニル、 置換されていてもよい低級 アルキニル、 置換されていてもよいァリール、 置換されていてもよいへテロァリ ール、 置換されていてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロアリールアルキル、 または置換されていてもよい非 芳香族複素環基 ；
A 1は置換されていてもよいァリールまたは置換されていてもよいへテロアリー ル；
破線 （ ） は結合の存在または不存在を表わす） で表わされる基] で示され る化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそ れらの溶媒和物を有効成分として含有する トロンボポェチン受容体ァゴニス ト作 用を有する医薬組成物、 に関する。
さらに詳しくは、 以下に示す 2 ) 〜 2 9 ) に関する。
2 ) X 1が置換されていてもよいへテロアリールである 1 ) 記載のトロンボポェ チン受容体ァゴニス ト作用を有する医薬組成物。
3 ) X 1が式 ：
Figure imgf000006_0001
(式中、 R 1。および R 1 1はそれぞれ独立して水素原子、 置換されていてもよい 低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 ハロゲン、 置換さ れていてもよいアミノカルボニル、 置換されていてもよいへテロアリール、 また は置換されていてもよいァリール； R 1 2は水素原子または低級アルキル） で示さ れる基である 1 ) 記載のト口ンボポェチン受容体ァゴニス ト作用を有する医薬組 成物。
4) X 1が式 ：
R1 NV
R" [I S -$
(式中、 R 1。および R 1 1は 3) と同意義） で示される基である 1 ) 記載のトロ ンボポェチン受容体ァゴニス ト作用を有する医薬組成物。
5 ) Y 1がー NH CO—、 一 CONH—、 — NHCH2—、 -NHCO- CH = C H―、 または一 NH S O 2—である 1 ) 〜4) のいずれかに記載のトロンボポェ チン受容体ァゴニス ト作用を有する医薬組成物。
6) Y 1がー NH CO—である 1 ) 〜4) のいずれかに記載のトロンボポェチン 受容体ァゴニス ト作用を有する医薬組成物。
7) Z 1がハロゲンまたは低級アルキルで置換されていてもよい 1 , 4—フエ二 レンである 1 ) 〜 6) のいずれかに記載の トロンボポェチン受容体ァゴニス ト作 用を有する医薬組成物。
8 ) R 1が水素原子または低級アルキルである 1 ) 〜 7) のいずれかに記載のト 口ンボポェチン受容体ァゴニス ト作用を有する医薬組成物。'
9) R 2が水素原子、 低級アルキル、 ハロゲン、 低級アルキルォキシ、 低級アル キルチオ、 または置換されていてもよいァミノである 1 ) 〜8 ) のいずれかに記 载のトロンボポェチン受容体ァゴニス ト作用を有する医薬組成物。
1 0 ) W1が式 ： ，，. .
Figure imgf000007_0001
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン ； R1 4および R1 5はそれぞれ独立して水素原子、 またはそ れぞれ以下の置換基群 Aから選択される 1以上の置換基によって置換されていて もよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリ ール、 ァラルキル、 ヘテロァリール、 もしく はヘテロァリールアルキル ；破線は
I ) と同意義 ；
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ） で表わされる基である、 1 ) 〜 9) のいずれかに記載のトロンボポェチン受容体 ァゴニス ト作用を有する医薬組成物。
I I ) W1が式 ：
Figure imgf000008_0001
(式中、 R1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン； R 2 6は水素原子または低級アルキル；破線は 1 ) と同意義） で表わされる基である、 1 ) 〜 9) のいずれかに記載のトロンボポェチン受容体 ァゴニス ト作用を有する医薬組成物。
1 2) 血小板産生調節剤である 1 ) 〜 1 1 ) のいずれかに記載のトロンボポェチ ン受容体ァゴニス ト作用を有する医薬組成物。
1 3) 血小板産生を調節するための医薬を製造するための 1 ) 〜 1 1 ) のいずれ かに記載の化合物の使用。
1 4) 1 ) 〜 1 1 ) のいずれかに記載の化合物の治療上効果を示す量を人を含む 哺乳動物に投与することからなる、 哺乳動物の血小板産生を調節する方法。
1 5 ) 一般式 （ I I ) ：
X2—丫 2— Z2 - W2 (Π)
[式中、 X 2は置換されていてもよい 5員へテロァリールまたは置換されていて もよいピリジル；
Y2は— NRACO— （C R C RD) 0— 2—、 一 NRAC O— (CH2) 0— 2— V—、 一 N R A C O— C R c= C RD—、 —V— (CH 2) 1_5-NRACO- (CH2) o一 2—、 - V- (CH2) !_5- CONRA- (CH2) 0-2—、 一 CONRA— (CH2) o一 2 -、 一 (CH2) 。一 2 - NRA - S 02— (CH2) 0一 2—、 一 （C H2) 0— 2— S 02— NRA - （CH2) o一 2—、 — NRA - (CH2) 0_2 -、 一 NRA- CO-NRA-s — N R A— C S— N RA—、 - N = C (一 S RA) - N R A―、 一 NRAC S NRACO―、 - N = C (一 S RA) — NRACO—、 - N R A - ( C H z) 1_2-NRA- CO-s 一 NRACONRANRB CO—、 または一 N = C (― NRARA) — NRACO— （式中、 R Aはそれぞれ独立して水素原子ま たは低級アルキル ； RBは水素原子またはフエ-ル； Rcおよび RDはそれぞれ独 立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されて いてもよい低級アルキルォキシ、 置換されていてもよい低級アルキルチオ、 置換 されていてもよい低級アルケニル、 置換されていてもよい低級アルキニル、 置換 されていてもよいァリール、 置換されていてもよいへテロアリール、 置換されて いてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていて もよいへテロァリールアルキル、 置換されていてもよい非芳香族複素環基、 また' は置換されていてもよいアミノ ； Vは酸素原子または硫黄原子） ；
Z 2は置換されていてもよいフエ二レン、 置換されていてもよい 2 , 5—ピリジ ンジィル、 置換されていてもよい 2 , 5—チォフェンジィル、 または置換されて いてもよい 2 , 5—フランジィル；
W2は式： ， . .
Figure imgf000010_0001
(式中、 R1 R2、 R3、 R4、 R7、 および R8はそれぞれ独立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されていてもよい低級アル キルォキシ、 置換されていてもよい低級アルキルチオ、 置換されていてもよい低 級ァルケニル、 置換されていてもよい低級アルキニル、 置換されていてもよいァ リール、 置換されていてもよいへテロアリール、 置換されていてもよいシクロア ルキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロアリー ルアルキル、 置換されていてもよい非芳香族複素環墓、 または置換されていても よいァミノ ；
R5、 R6、 および R 9はそれぞれ独立して、 水素原子、 置換されていてもよい低 級アルキル、 置換されていてもよい低級アルケニル、 置換されていてもよい低級 アルキニル、 置換されていてもよいァリール、 置換されていてもよいへテロァリ ール、 置換されていてもよいシクロアルキル、 置換されていてもよいァラノレキル、 置換されていてもよいへテロアリールアルキル、 または置換されていてもよい非 芳香族複素環基 ；
A 2は置換されていてもよいァリールまたは置換されていてもよいへテロアリー ル ；
破線 （ ） は結合の存在または不存在を表わす） で表わされる基 ； ただし、 R 2はイミダゾリル、 トリァゾリル、 またはテ トラゾリルではない] で 示される化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 ま たはそれらの溶媒和物。
1 6 ) X 2が式 ： .
Figure imgf000011_0001
(式中、 R 1 °および R 1 1はそれぞれ独立して水素原子、 置換されていてもよい 低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、ソ、ロゲン、 置換さ れていてもよいアミノカルボニル、 置換されていてもよいへテロアリール、 また は置換されていてもよいァリール） で示される基である 1 5 ) 記載の化合物、 そ のプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和 物。
1 7 ) X 2が式 ：
Figure imgf000011_0002
または (式中、 R 1 6は水素原子、 置換されていてもよい低級アルキル、 カルボキシ、 低 級アルキルォキシカルボニル、 ハロゲン、 または置換されていてもよいアミノカ ルボニル；
R1 7、 R1 8、 R1 9、 R2 0、 R2 1、 R2 2、 および R 2 3はそれぞれ独立して水 素原子、 置換基群 Bから選択される 1以上の置換基によって置換されていてもよ いアルキル、 シクロアルキル、 置換基群 Bから選択される 1以上の置換基によつ て置換されていてもよいアルキルォキシ、 アルキルチオ、 ハロゲン、 置換基群 C から選択される 1以上の置換基によって置換されていてもよいフユニル、 置換基 群 Cから選択される 1以上の置換基によって置換されていてもよいへテロアリー ル、 または置換基群 Cから選択される 1以上の置換基によって置換されていても よい非芳香族複素環基、
置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカノレボニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエ二 ル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロァリール；
R 1 6および R 1 7は一緒になって— C H 2—、 一 CH2 CH2—、 - C H 2 C H 2 C H2—、 一 O CH2—、 または一 S CH2—を形成してもよい） で示される基であ る 1 5) または 1 6) 記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬 上許容される塩、 またはそれらの溶媒和物。
1 8 ) Y2が— NHCO—である 1 5) 〜 1 7) のいずれかに記載の化合物、 そ のプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和 物。
1 9) Z 2がハロゲンまたは低級アルキルで置換されていてもよい 1 , 4一フエ 二レンである 1 5) 〜 1 8 ) のいずれかに記載の化合物、 そのプロ ドラッグ、 も しくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 0) R1が水素原子または低級アルキルである 1 5) 〜 1 9) のいずれかに記 載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 または それらの溶媒和物。
2 1 ) R 2が水素原子、 低級アルキル、 ハロゲン、 低級アルキルォキシ、 低級ァ ルキルチオ、 または置換されていてもよいァミノである 1 5) 〜 2 0) のいずれ かに記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 2 ) W2が式 ：
Figure imgf000013_0001
,また
(式中、 R 1 R2、 R3、 R4、 R5、 R6、 R7、 R8、 および A 2は 1 5) と同 意義、 ただし、 R 2はイミダゾリル、 トリァゾリル、 またはテ トラゾリルではな い） である 1 5) 〜2 1 ) のいずれかに記載の化合物、 そのプロ ドラッグ、 もし くはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 3 ) W2が式 ：
Figure imgf000013_0002
(式中、 R1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン、 R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそ れぞれ以下の置換基群 Aから選択される 1以上の置換基によって置換されていて もよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリ ール、 ァラルキル、 ヘテロァリール、 ヘテロァリールアルキル、 もしくは非芳香 族複素環基 ；
置換基群 A ： ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ） である 1 5) 〜2 2) のいずれかに記載の化合物、 そのプロ ドラッグ、 もしくは それらの製薬上許容される塩、 またはそれらの溶媒和物。
2 4) W2が式 ：
Figure imgf000014_0001
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン ； R2 6は水素原子または低級アルキル；破線は 1 5) と同意 義） で表わされる基である、 1 5) 〜2 2) のいずれかに記載の化合物、 そのプ ロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 5 ) 一般式 （ I I I ) : -
Figure imgf000014_0002
[式中、 R 1 6は水素原子、 置換されていてもよい低級アルキル、 カルボキシ、 低 級アルキルォキシカルボニル、 ハロゲン、 または置換されていてもよいアミノカ ルホニノレ ；
R1 7、 R 1 S、 R1 9、 R2 °、 および R 2 1はそれぞれ独立して水素原子、 置換基 群 Bから選択される 1以上の置換基によって置換されていてもよいアルキル、 シ ク口アルキル、 置換基群 Bから選択される 1以上の置換基によって置換されてい てもよいアルキルォキシ、 アルキルチオ、 ハロゲン、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエニル、 置換基群 Cから選択さ れる 1以上の置換基によって置換されていてもよいへテロアリール、 または置換 基群 Cから選択される 1以上の置換基によって置換されていてもよい非芳香族複 素環基、
置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカルボニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエ二 ル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 力ルポキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール；
R 1 6およぴ R 1 7は一緒になつて— C H 2—、 — C H 2 C H 2—、 - C H 2 C H 2 C
H 2—、 一 O C H 2—、 または一 S C H 2—を形成してもよい ；
R 3 1および R 3 2はそれぞれ独立して、 水素原子、 低級アルキル、 ハロゲン、 ノヽ 口低級アルキル、 低級アルキルォキシ、 ハロ低級アルキルォキシ、 またはヒ ドロ キシ；
W 3は式 ：
Figure imgf000015_0001
または (式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはノヽロゲン ； R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそれぞれ以下の置換基群 Aにより置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアノレキノレ、 ァ リ ーノレ、 ァラノレキノレ、 ヘテロァ リ ーノレ、 ヘテロァ リ ーノレァノレ キル、 もしくは非芳香族複素環基；
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ； R 2 4は水素原子または低級アルキル；
R 2 5は低級アルキル、 置換されていてもよいァリール、 または置換されていても よい非芳香族複素環 ；
A 3はへテロァリール） で表わされる基] で示される化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 6 ) 一般式 （ I V— A ) ：
Figure imgf000016_0001
[式中、 R 2 7は水素原子、 C 1— 3アルキル、 トリフルォロメチル、 またはハロ ゲン ；
R 2 8、 R 2 9、 および R 3 °はそれぞれ独立して水素原子、 置換基群 Bから選択さ れる 1以上の置換基によって置換されていてもよいアルキル、 シク口アルキル、 置換基群 Bから選択される 1以上の置換基によって置換されていてもよいアルキ ノレォキシ、 アルキルチオ、 ハロゲン、 置換基群 Cから選択される 1以上の置換基 によって置換されていてもよいフユニル、 置換基群 Cから選択される 1以上の置 換基によって置換されていてもよいへテロアリール、 または置換基群 Cから選択 される 1以上の置換基によって置換されていてもよい非芳香族複素環基、 置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカノレポニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエ二 ル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール；
R 3 1および R 3 2はそれぞれ独立して、 水素原子、 低級アルキル、 ハロゲン、 ハ 口低級アルキル、 低級アルキルォキシ、 ハロ低級アルキルォキシ、 またはヒ ドロ キシ ；
W 4は式：
Figure imgf000017_0001
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン ；
R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそれぞれ以下の置換基群 Aにより置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリール、 ァラルキル、 ヘテロァリール、 ヘテロァリールアル キル、 もしくは非芳香族複素環基 ；
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ； R 2 4は水素原子または低級アルキル） で表わされる基] で示される化合物、 その プロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 7 ) 一般式 （ I V— B ) ：
Figure imgf000018_0001
[式中、 R 2 8、 R 2 9、 および R 3 °はそれぞれ独立して水素原子、 置換基群 Bか ら選択される 1以上の置換基によって置換されていてもよいアルキル、 シクロア ルキル、 置換基群 Bから選択される 1以上の置換基によって置換されていてもよ いアルキルォキシ、 アルキルチオ、 ハロゲン、 置換基群 Cから選択される 1以上 の置換基によって置換されていてもよいフユニル、 置換基群 Cから選択される 1 以上の置換基によって置換されていてもよいへテロアリール、 または置換基群 C から選択される 1以上の置換基によって置換されていてもよい非芳香族複素環基- 置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカルボニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエ二 ル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキノレ、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール；
R 3 1および R 3 2はそれぞれ独立して、 水素原子、 低級アルキル、 ハロゲン、 ハ 口低級アルキル、 低級アルキルォキシ、 ハロ低級アルキルォキシ、 またはヒ ドロ キシ；
W 4は式 ：
Figure imgf000018_0002
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハ口ゲン ；
R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそれぞれ以下の置換基群 Aにより置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリール、 ァラルキル、 ヘテロァリール、 ヘテロァリールアル キル、 もしくは非芳香族複素環基 ；
置換基群 A ： ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ ； R 24は水素原子または低級アルキル） で表わされる基；
Tは一 CH2—、 一 CH2 CH2—、 一 CH2 CH2 CH2—、 一 OCH2—、 また は一 S CH2— ] で示される化合物、 そのプロ ドラッグ、 もしくはそれらの製薬 上許容される塩、 またはそれらの溶媒和物。
2 8) 1 5) 〜 2 7) のいずれかに記載の化合物を有効成分と して含有する医薬 組成物。
2 9) 1 5 ) 〜 2 7) のいずれかに記載の化合物を有効成分と して含有する トロ ンボポェチン受容体ァゴニス ト作用を有する医薬組成物。
3 0) 1 5) 〜2 7) のいずれかに記載の化合物を有効成分と して含有する血小 板産生調節剤。
3 1 ) 血小板産生を調節するための医薬を製造するための 1 5) 〜 2 7) のいず れかに記載の化合物の使用。
3 2) 1 5) 〜 2 7) のいずれかに記載の化合物の治療上効果を示す量を人を含 …む哺乳動物に投与することからなる、 哺乳動物の血小板産生を調節する方法。 本明細書中、 「ハロゲン」 とは、 フッ素、 塩素、 臭素、 ヨウ素を意味する。 フ ッ素、 塩素、 および臭素が好ましい。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「アルキル」 とは、 炭素原子数 1〜 1 5の直鎖または分枝鎖の 1価の炭化水素基を包含する。 例えば、 メチル、 ェチル、 n—プロピル、 イソプロピル、 n—プチル、 イソプチ ル、 s e c -プチノレ、 t e r t —ブチノレ、 n—ペンチノレ、 ィソペンチノレ、 n e o —ペンチノレ、 n—へキシ.ル、 イソへキシノレ、 n一へプチル、 n—ォクチノレ、 n 一 ノナニル、 n—デカニル、 n—ゥンデ力ニル、 n— ドデカニル、 n— トリデカニ ル、 IIーテ トラデカニル、 n—ペンタデ力-ル等が挙げられる。 好ましくは、 C
；!〜 C 1 0アルキルが挙げられる。 さらに好ましくは、 C 1〜C 6アルキルが挙 げられる。
本明細書中、 単独でも Lくは他の用語と組み合わせて用いられる 「低級アルキ ル」 とは、 炭素原子数 1 ~ 8の直鎖または分枝鎖の 1価の炭化水素基を包含する。 例えば、 メチル、 ェチル、 n—プロピル、 イソプロピル、 n—プチル、 イソプチ ノレ、 s e c—プチノレ、 t e r t 一プチノレ、 n—ペンチノレ、 イソペンチノレ、 n e o 一ペンチル、 n—へキシル、 イソへキシル、 n一へプチル、 n—ォクチル等が挙 げられる。 好ましくは、 C 1〜C 6アルキルが举げられる。 さらに好ましくは、 C 1〜 C 3アルキルが挙げられる。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「C 1 — 3ァ ノレキレン」 と しては、 メチレン、 エチレン、 およびプロピレンが挙げられる。 本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「シクロアル カン」 とは、 炭素原子数が 3〜 8個である単環のシクロアルカンを包含する。 例 えば、 シク口プロパン、 シクロブタン、 シクロペンタン、 シクロへキサン、 シク 口ヘプタン、 シクロオクタンが挙げられる。 好ましくは C 3〜C 6シクロアルカ ンが挙げられる。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「シクロアル キル」 とは、 炭素原子数が 3〜 8個である単環のシクロアルキルを包含する。 例 えば、 シク口プロピノレ、 シクロプチノレ、 シクロペンチノレ、 シクロへキシノレ、 シク 口へプチル、 シクロォクチルが挙げられる。 好ましくは C 3〜 C 6シクロアルキ ルが挙げられる。
本明細書中、 「低級アルケニル」 とは、 炭素原子数が 2 〜 8個であり、 1個も しくは 2個以上の二重結合を有する、 直鎖または分枝鎖の 1価の炭化水素基を包 含する。 例えば、 ビュル、 ァリル、 1 一プロぺニル、 2—プロぺニル、 種々のブ チニル異性体等が挙げられる。 好ましくは、 C 2 〜 C 6アルキニルが挙げられる。 さらに好ましくは、 C 2 〜 C 4アルキニルが挙げられる。
本明細書中、 「低級アルキニル j とは、 炭素原子数が 2 〜 8個であり、 1個も しくは 2個以上の三重結合を有する、 直鎖または分枝鎖の 1価の炭化水素基を包 含する。 例えば、 ェチニノレ、 1 —プロビュル、 2—プロピニル、 1 一プロぺニル、 2—プロぺニル、 クロ トニル、 イソペンテニル、 種々のブテュル異性体等が挙げ られる。 好ましくは、 C 2 〜 C 6アルケニルが挙げられる。 さらに好ましくは、 C 2 〜 C 4アルケニルが挙げられる。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「ァリール」 とは、 単環状もしくは縮合環状芳香族炭化水素を包含する。 例えば、 フエ-ル、 1 一ナフチル、 2—ナフチル、 アント リル等が挙げられる。
本明細書中、 「ァラルキル」 とは、 前記 「低級アルキル」 に前記 「ァリール」 が 1または 2以上置換したものを包含し、 これらは可能な全ての位置で置換しう る。 例えば、 ベンジル、 フェニルェチル (例えば、 2—フエニルェチル等) 、 フ ェニルプロピル （例えば、 3—フエニルプロピル等） 、 ナフチルメチル （例えば、 1一ナフチルメチル、 2—ナフチルメチル等) 、 アン ト リルメチル (例えば、 9 一アントリルメチル等） 等が挙げられる。 好ましくは、 ベンジル、 フエ二ルェチ ルが挙げられる。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「非芳香族複 素環基」 なる用語は、 任意に選ばれる、 酸素原子、 硫黄原子又は窒素原子を環內 に 1個以上含む非芳香族の 5〜 7員環またはそれらが 2個以上縮合した環を包含 する。 例えば、 ピロ リジニル （例えば、 1一ピロ リジニル、 2—ピロ リジニル） 、 ピロリニル' （例えば、 3 —ピロリニル） 、 イミダゾリジニル （例えば、 2 —イミ ダゾリジニル） 、 ィミダゾリニル （例えば、 ィミダゾリニル） 、 ピラゾリジニル (例えば、 1 一ピラゾリジニル、 2一ピラゾリジニル） 、 ピラゾリニル （例えば、 ビラゾリニル） 、 ピペリジル （例えば、 ピペリジノ、 2—ピペリジル） 、 ピペラ ジニル （例えば、 1 一ピペラジニル) 、 インドリニル （例えば、 1 一インドリニ ル） 、 イソインドリニル （例えば、 イソインドリニル) 、 モルホリニル (例えば、 モルホリノ、 3—モルホリニル） 、 テ トラヒ ドロフラニル、 テ トラヒ ドロビラ二 ル等が挙げられる。
R 1 7、 R 1 8、 R 1 9、 R 2 0、 R 2 1、 R 2 2、 R 2 3、 R 2 8、 R 2 9、 および R 3 。における 「非芳香族複素環基」 としては、 モルホリノ、 ピペラジノ、 ピロリジ ノ、 テ トラヒ ドロフラエル、 テ トラヒ ドロビラニル等が好ましい。
置換基群 Bにおける 「非芳香族複素環基」 と しては、 モルホリノ、 ピペラジノ、 ピぺリジノ、 テ トラヒ ドロフラニル、 テトラヒ ドロビラニル等が好ましい。
置換基群 Cにおける 「非芳香族複素環基」 と しては、 モルホリノ、 ピペラジノ、 ピぺリジノ、 ピロリジノ、 テ トラヒ ドロフラニル、 テ トラヒ ドロビラニル等が好 ましい。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「ヘテロァリ ール」 とは、 任意に選ばれる、 酸素原子、 硫黄原子又は窒素原子を環内に 1個以 上含む 5〜 6員の芳香環を包含する。 これは前記 「シク口アルキル j 、 前記 「ァ リール」 、 前記 「非芳香族複素環基」 、 もしくは他のへテロアリールと可能な全 ての位置で縮合していてもよい。 へテロアリ一ルが単環および縮合環のいずれで ある場合も、 すべての可能な位置で結合しうる。 例えば、 ピロリル （例えば、 1 — ピロ リノレ、 2—ピロ リノレ、 3—ピロ リル） 、 フ リノレ （例えば、 2—フ リノレ、 3 一フ リル） 、 チェニル （例えば、 2—チェニル、 3—チェ二ノレ） 、 イミダゾリル (例えば、 2—イミダゾリル、 4—イミダゾリル） 、 ピラゾリル （例えば、 1― ピラゾリル、 3—ピラゾリル） 、 イソチアゾリル （例えば、 3—イソチアゾリル） 、 イソキサゾリノレ (例えば、 3—イソキサゾリル) 、 ォキサゾリル （例えば、 2 一 ォキサゾリル） 、 チアゾリル （例えば、 2—チアゾリル） 、 ピリジル （例えば、 2 —ピリジル、 3 —ピリジル、 4—ピリジル） 、 ピラジニル （例えば、 2—ビラ ジニル） 、 ピリ ミジニル （例えば、 2 —ピリ ミジニル、 4一ピリ ミジニル） 、 ピ リダジニル （例えば、 3 —ピリダジニル） 、 テ トラゾリル （例えば、 1 H—テ ト ラゾリル） 、 ォキサジァゾリル （例えば、 1 , 3 ， 4—ォキサジァゾリル) 、 チ アジアゾリル (例えば、 1 , 3 , 4ーチアジアゾリル) 、 インドリジニル (例え ば、 2 —イン ドリジニル、 6 —インドリジニル） 、 イソインドリル （例えば、 2 一イソイン ドリル） 、 イン ドリル （例えば、 1—イン ドリル、 2—イン ドリル、 3 —イン ドリル） 、 インダゾリル （例えば、 3 一インダゾリル) 、 プリニル （例 えば、 8—プリニル） 、 キノ リジニル （例えば、 2 —キノ リジニル） 、 イソキノ リル （例えば、 3 —イソキノ リル） 、 キノ リル （例えば、 2 —キノ リル、 5 —キ ノ リル） 、 フタラジュル (例えば、 1—フタラジニル) 、 ナフチリジニル （例え ば、 2 --ナフチリジニル) 、 キノラニル (例えば、 2—キノラニル） 、 キナゾリ ニル (例えば、 2 一キナゾリニル) 、 シンノ リニル （例えば、 3—シンノ リニル） 、 プテリジニル （例えば、 2—プテリジニル) 、 カルパゾリル (例えば、 2—カル バゾリル、 4一力ルパゾリル） 、 フエナントリジニル （例えば、 2—フエナント リジニル、 3 —フエナントリジニル） 、 アタ リジニル （例えば、 1—アタリニジ ル、 2—ァク リニジル） 、 ジベンゾフラニル （例えば、 1ージベンゾフラニル、 2—ジベンゾフラニル） 、 ベンゾイミダゾリル （例えば、 2—ベンゾイミダゾリ ル） 、 ベンゾイソキサゾリル （例えば、 3 —べンゾイソキサゾリル） 、 ベンゾォ キサゾリル （例えば、 2 —べンゾォキサゾリル） 、 ベンゾォキサジァゾリル （例 えば、 4—ベンゾォキサジァゾリル） 、 ベンゾイソチアゾリル （例えば、 3 —べ ンゾイソチアゾリル） 、 ベンゾチアゾリル （例えば、 2—ベンゾチアゾリル） 、 ベンゾフリル （例えば、 3 —べンゾフリル） 、 ベンゾチェニル （例えば、 2 —べ ンゾチェニル） 、 4 , 5 —ジヒ ドロナフ ト [ 1 , 2— d ] チアゾリル、 4 H—ク ロメノ [4, 3 - d ] チアゾリル、 4 H—チォクロメノ [4, 3 - d ] チアゾリ ル、 4, 5—ジヒ ドロチアゾロ [ 5 , 4 - c ] キノ リル、 8 H—インデノ [ 1， 2— d]チアゾリノレ、 5, 6—ジヒ ドロー 4 H— 3—チア一 1—ァザ一ベンゾ [ e ] ァズレニル等が挙げられる。
X 1における 「ヘテロァリール」 と しては、 チアゾリル、 イソキサゾリル、 チ ェニル、 カルパゾリル、 ベンゾチアゾリル、 ピリジル、 ピラゾリル等が好ましい さらに好ましくは、 チアゾリル、 ピリジル等が挙げられる。
R 1 , R2、 R3、 R4、 R7、 および Rsにおける 「ヘテロァリール」 と しては ピリジル、 チアゾリル、 ベンゾチアゾリル等が好ましい。
R 1 0および R 1 1における 「ヘテロァリール」 と しては、 ピリジル、 チェニル、 フリル、 ピリ ミジニル、 ィミダゾリル、 チアゾリル、 ォキサゾリル、 ト リアゾリ ル等が好ましい。
A 1 , A2、 および A 3における 「ヘテロァリール」 としては、 イミダゾリル、 トリァゾリル、 テ トラゾリル、 ピリジル、 ピリ ミジニル等が好ましい。
R 1 7、 R 1 8、 R1 9、 R2 0、 R2 1、 R2 2、 R2 3、 R2 8、 R2 9、 および R3 0における 「ヘテロァリール」 と しては、 ピリジル、 チェニル、 フリル、 ピリ ミ ジニル、 イ ミダゾリル、 チアゾリル、 ォキサゾリル、 ト リァゾリル等が好ましい, 置換基群 Bにおける Γヘテロァリール」 と しては、 ピリジル、 ピラゾリル、 ピ リミジル、 イミダゾリル、 ォキサゾリル、 チアゾリル、 フリル、 チェニル等が好 ましい。
置換基群 Cにおける 「ヘテロァリール」 と しては、 ピリジル、 ピラゾリル、 ィ ミダゾリル等が好ましい。
本明細書中、 「 5員へテロァリール」 とは、 任意に選ばれる、 酸素原子、 硫黄 原子又は窒素原子を環内に 1個以上含む 5員の芳香環を包含する。 例えば、 チェ ニル、 フリル、 ピロリル、 イミダゾリル、 ピラゾリル、 イソチアゾリル、 イソキ サゾリル、 チアゾリル、 ォキサゾリル、 1 , 2 , 3— トリァゾリル、 1， 2 , 4 一 トリァゾリル、 1， 2， 4—チアジアゾリル、 1 , 3 , 4—チアジアゾリル、 1 , 2， 4—ォキサジァゾリル、 1 , 3 , 4 —ォキサジァゾリル等が挙げられる。 チアゾリルが好ましい。
本明細書中、 「ヘテロァリールアルキル」 とは、 前記 「低級アルキル」 の任意 の位置に前記 「ヘテロァリール」 が 1または 2以上置換したものを包含し、 これ らは可能な全ての位置で置換しうる。 例えば、 チェニルメチル （例えば、 2—チ ェニルメチノレ） 、 チェニルェチル (例えば、 2 - (チオフヱン一 2—ィノレ) ェチ ル） 、 フリルメチル （例えば、 2—フリルメチル) 、 フリルェチル （例えば 2— (フラン一 2—ィル） ェチル) 、 ピロリルメチル (例えば、 2—ピロリノレメチル） 、 ピロリルェチル （例えば、 2— (ピロール— 2—ィル） ェチル） 、 イミダゾリル メチル （例えば、 2—イミダゾリルメチル、 4—イミダゾリルメチル） 、 イミダ ゾリルェチル （例えば、 2— （イミダゾールー 2—ィル） ェチル） 、 ピラゾリル メチル （例えば、 3 —ビラゾリルメチル） 、 ピラゾリルェチル （例えば、 2 — (ピ ラゾールー 3—ィル) ェチル） 、 チアゾリルメチル (例えば、 2—チアゾリルメ チル） 、 チアゾリルェチル (例えば、 2 - (チアゾールー 2—ィル) ェチル) 、 イソチアゾリルメチル (例えば、 3—イソチアゾリルメチル） 、 イソキサゾリル メチル （例えば、 3—イソキサゾリルメチル) 、 ォキサゾリルメチル (例えば、 2—ォキサゾリルメチル） 、 ォキサゾリルェチル （例えば、 2— （ォキサゾール 一 2 —ィル） ェチル） 、 ピリジルメチル (例えば、 2 —ピリジルメチル、 3 —ピ リジルメチル、 4 一ピリジルメチル） 、 ピリジルェチル (例えば、 2—ピリジル ェチル） 等が挙げられる。
R 1 N R 2、 R 3、 R 4、 R 7、 および R 8における 「ヘテロァリールアル,キル J と しては、 2—チェニルメチル、 2—フリルメチル等が挙げられる。
本明細書中、 「フエ二レン」 とは、 フエニルめ 2価基を意味する。 例えば、 1， 2 —フエニレ.ン、 1， 3 —フエ二レン、 1， 4—フエ二レンが挙げられる。 好ま しくは 1 , 4一フエ二レンが挙げられる。 本明細書中、 「単環へテロァリ レン」 とは、 前記 「ヘテロァリール」 のうち単 環のへテロアリールの 2価基を意味する。 例えば、 チォフェンジィル、 フランジ ィル、 ピリジンジィル等が挙げられる。 さらに詳しくは、 2， 5—チォフェンジ ィル、 2， 5 _フランジィル、 2 , 5 —ピリジンジィル、 2 , 5 —チアゾールジ ィル、 2 , 5 — （ 1， 3， 4ーチアジアゾール） ジィル、 2， 5 —ピリジンジィ ル、 2 , 5 —ピラジンジィル、 3 , 6 —ピリダジンジィル、 2 , 5 — （ 4 H—ピ ラン） ジィル等が挙げられる。 2 , 5 —チォフェンジィル、 2 , 5 —フランジィ ル、 2， 5 —ピリジンジィルが好ましい。
本明細書中、 「単環非芳香族複秦環ジィル」 とは、 前記 「非芳香族複素環基」 のうち単環の非芳香族複素環基の 2価基を意味する。 例えば、 ピロリジンジィル、 ピペリジンジィル、 ピラジンジィル等が挙げられる。
本明細書中、 「単環シクロアルカンジィル」 とは、 前記 「シクロアルカン」 の うち単環のシクロアルカンの 2価基を意味する。 例えば、 1， 4ーシクロペンタ ンジィル、 1 , 4 一シク口へキサンジィル等が挙げられる。
本明細書中、 「アルキルォキシ」 と しては、 メチルォキシ、 ェチルォキシ、 n 一プロピル才キシ、 イソプロピルォキシ、 n 一プチルォキシ、 イソプチルォキシ、 s e cーブチノレオキシ、 t e r tープチノレオキシ、 一ペンチノレォキシ、 n -へ キシノレオキシ、 n 一ヘプチノレオキシ、 n —才クチノレオキシ、 n —ノナニノレオキシ、 n—デカニルォキシ等が挙げられる。 好ましくは、 メチルォキシ、 ェチルォキシ、 n —プロピルォキシ、 イソプロピルォキシ、 n -プチルォキシが举げられる。 本明細書中、 「低級アルキルォキシ J と しては、 メチルォキシ、 ェチルォキシ、 n —プロピルォキシ、 イソプロピルォキシ、 n 一プチルォキシ、 イソプチルォキ シ、 s e c—プチルォキシ、 t e r t —ブチルォキシ等が挙げられる。 好ましく は、 メチルォキシ、 ェチルォキシ、 n—プロピルォキシ、 イソプロピルォキシ、 n —ブチルォキシが挙げられる。
本明細書中、 「低級アルキルチオ」 と しては、 メチルチオ、 ェチルチオ等が拳 げられる。 ·
本明細書中、 「低級アルキルォキシカルボニル」 としては、 メチルォキシカル ボニル、 ェチルォキシカルボニル、 n —プロピルォキシカルボニル、 イソプロピ ノレォキシカルボニル、 n —ブチルォキシカルボニル、 t—プチルォキシカルボ二 ル、 n—ペンチルォキシカルボニル等が挙げられる。
本明細書中、 「ァリールォキシカルボニル」 としては、 フエニルォキシカルボ ニル、 1 一ナフチルォキシカルボニル、 2—ナフチルォキシカルボニル等が挙げ られる。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「ァシル」 な る用語は、 アルキル部分が前記 「低級アルキル」 であるアルキルカルボニルまた はァリール部分が前記 「ァリ一ル」 であるァリールカルボニルを包含する。 例え ば、 ァセチル、 プロピオニル、 プチロイル、 ベンゾィル等が挙げられる。 「低級 アルキル」 および 「ァリール」 は後述のそれぞれの置換基によって置換されてい てもよい。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「ハロ低級ァ ルキル」 なる用語は、 前記ハロゲンによって 1〜 8個所、 好ましくは 1〜 5個所 置換された前記 「低級アルキル」 を包含する。 例えば、 トリフルォロメチル、 ト リクロロメチノレ、 ジフノレオロェチノレ、 トリフノレオロェチノレ、 ジクロロェチノレ、 ト リクロロェチル等が挙げられる。 好ましくは、 トリフルォロメチルが挙げられる。 本明細書中、 「ハロ低級アルキルォキシ」 としては、 トリフルォロメチルォキ シ、 トリクロロメチノレオキシ、 ジフノレォロェチノレオキシ、 トリフノレォロェチノレオ キシ、 ジクロロェチルォキシ、 トリクロ口ェチルォキシ等が挙げられる。 好まし くは、 トリフ.ルォロメチルォキシが挙げられる。
本明細書中、 「ァシルォキシ」 と しては、 ァセチルォキシ、 プロピオ二ルォキ シ、 ベンゾィルォキシ等が挙げられる。
本明細書中、 「低級アルキルシリル」 と しては、 トリェチルシリル、 t—プチ ルジメチルシリル等が挙げられる。
本明細書中、 単独でもしくは他の用語と組み合わせて用いられる 「置換されて いてもよいァミノ」 なる用語は、 前記 「低級アルキル」 、 前記 「ァリール」 、 前 記 「ァラルキル」 、 前記 「ヘテロァリール」 、 前記 「ヘテロァリールアルキル」 、 または前記 「ァシル」 で 1または 2個所置換されいてもよいアミノを包含する。 例えば、 ァミノ、 メチルァミノ、 ジメチルァミノ、 ェチルメチルァミノ、 ジェチ ルァミノ、 ェチルメチルァミノ、 ベンジルァミノ、 ァセチルァミノ、 ベンゾィル ァミノ等が挙げられる。 好ましくはァミノ、 メチルァミノ、 ジメチルァミノ、 ェ チルメチルァミノ、 ジェチルァミノ、 ァセチルァミノが挙げられる。
本明細書中、 「置換されていてもよいアミノカルポニル」 と しては、 アミノカ ルボニル、 メチルァミノカルボニル、 ジメチルァミノ力ルポ二ル、 ェチルメチル ァミノカルボニル、 ジェチルァミノカルボニル等が挙げられる。 好ましくは、 ァ ミノカルボニル、 メチルァミノカルボニル、 ジメチルァミノカルボニルが挙げら れる。
本明細書中、 「置換されていてもよいウレイ ド」 なる用語は、 前記 「低級アル キル」 、 前記 「ァリール」 、 前記 「ァラルキル」 、 前記 「ヘテロァリール」 、 前 記 「ヘテロァリールアルキル」 、 または前記 「ァシル J で 1または 2個所以上置 換されいてもよいウレィ ドを包含する。
本明細書中、 「置換されていてもよい低級アルキル」 における置換基としては、 シク口アルキル、 低級アルケニル、 低級アルキリデン、 ヒ ドロキシ、 低級アルキ ノレォキシ、 メノレカプト、 低級アルキルチオ、 ハロゲン、 ニトロ、 シァノ、 力ルポ キシ、 低級ァノレキノレオキシカノレボニノレ、 ハロ低級アルキノレ、 ハロ低級アルキルォ キシ、 置換されていてもよいァミノ、 置換されていてもよいアミノカルボニル、 ァシル、 ァシルォキシ、 置換されていてもよい非芳香族複素環基、 ァリールォキ シ (例えば、 フエニルォキシ） 、 ァラルキルォキシ (例えば、 ベンジルォキシ) 、 低級アルキルスルホニル、 グァニジノ、 ァゾ基、 置換されていてもよいウレイ ド、 = N - 0 - (ァシル） 等が挙げられる。 これらは、 全ての可能な位置で 1個以上 置換しうる。
R cおよび R Dにおける 「置換されていてもよい低級アルキル」 の置換基と して は、 ハロゲン、 ハロ低級アルキル等が好ましい。
R 1 , R 2、 R 3、 R 4、 R 5、 R 6、 R 7、 R 8、 および R 9における 「置換され ていてもよい低級アルキル」 の置換基と しては、 ヒ ドロキシ、 カルボキシ、 ハロ ゲン、 アルキルォキシ、 アルキルチオ、 アルキルシリル、 置換されていてもよい ァミノ、 シァノ、 ァシル等が好ましい。
R 1 0、 R 1 1 , および R 1 6における 「置換されていてもよい低級アルキル」 の 置換基と しては、 低級アルキルォキシカルボニル、 ハロゲンが好ましい。
R 1 2における 「置換されていてもよい低級アルキル」 の置換基としては、 シク 口アルキル、 低級アルケニル、 低級アルキリデン等が好ましい。
本明細書中、 「置換されていてもよい低級アルキルォキシ」 および 「置換され ていてもよい低級アルキルチオ」 における置換基としては、 シクロアルキル、 低 級ァルケニル、 低級アルキリデン、 ヒ ドロキシ、 低級アルキルォキシ、 メルカプ ト、 低級アルキルチオ、 ハロゲン、 ニ トロ、 シァノ、 カルボキシ、 低級アルキル ォキシカルボニル、 ハロ低級アルキル、 ハロ低級アルキルォキシ、 置換されてい てもよぃァミノ、 置換されていてもよいアミノカルボニル、 ァシル、 ァシルォキ シ、 置換されていてもよい非芳香族複素環基、 ァリールォキシ （例えば、 フエ二 ルォキシ） 、 ァラノレキルォキシ （例えば、 ベンジルォキシ） 、 低級アルキルスル ホニル、 グァニジノ、 ァゾ基、 置換されていてもよいウレィ ド、 = N— O— （ァ シル） 等が挙げられる。 これらは、 全ての可能な位置で 1個以上置換しうる。 好 ましくは、 ハロゲン等が挙げられる。
本明細書中、 「置換されていてもよい低級アルケニル」 および 「置換されてい てもよい低級アルキニル」 における置換基と しては、 シクロアルキル、 低級アル キリデン、 ヒ ドロキシ、 低級アルキルォキシ、 メルカプト、 低級アルキルチオ、 ハロゲン、 ニ トロ、 シァノ、 カルボキシ、 低級アルキルォキシカルボ二ノレ、 ハロ 低級アルキル、 ハロ低級アルキルォキシ、 置換されていてもよいァミノ、 置換さ れていてもよいアミノカルボニル、 ァシル、 ァシルォキシ、 置換されていてもよ い非芳香族複素環基、 ァリール、 ァリールォキシ （例えば、 フ-ニルォキシ） 、 ァラルキル、 ァラルキルォキシ (例えば、 ベンジルォキシ） 、 低級アルキルスル ホニル、 グァニジノ、 ァゾ基、 置換されていてもよいウレイ ド等が挙げられる。 これらは、 全ての可能な位置で 1個以上置換しうる。
本明細書中、 「置換されていてもよいフエ二レン」 、 「置換されていてもよい 単環へテロァリ レン」 、 「置換されていてもよい 2 , 5 —ピリジンジィル」 、 「置 換されていてもよい 2 , 5—チォフェンジィル」 、 「置換されていてもよい 2 , 5—フランジィル」 、 「置換されていてもよい単環非芳香族複素環ジィル」 、 「置 換されていてもよい単環シクロアルカンジィル」 、 「置換されていてもよいァリ ール」 、 「置換されていてもよいフエニル」 、 「置換されていてもよいへテロア リール」 、 「置換されていてもよい 5員へテロァリール」 、 「置換されていても よいピリジル」 「置換されていてもよい非芳香族複素環基」 、 「置換されていて もよぃシクロアルキル」 、 「置換されていてもよいァラルキル」 、 および 「置換 されていてもよいへテロアリールアルキル」 における置換基と しては、 置換され ていてもよいアルキル、 シクロアルキル、 低級アルケニル、 低級アルキニル、 ヒ ドロキシ、 アルキルォキシ、 ァラルキルォキシ、 メルカプト、 低級アルキルチオ、 ハロゲン、 ニ トロ、 シァノ、 カルボキシ、 低級アルキルォキシ力ルポ-ル、 ァリ ールォキシカルボニル、 ハロ低級アルキル、 ハロ低級アルキルォキシ、 置換され ていてもよいァミノ、 置換されていてもよいアミノカルボニル、 ァシル、 ァシル ォキシ、 置換されていてもよいァリール （置換基と しては、 ハロゲン、 カルボキ シ、 アルキル、 アルキルォキシ等） 、 置換されていてもよいへテロアリール （置 換基と しては、 ハロゲン、 カルボキシ、 アルキル、 アルキルォキシ等） 、 置換さ れていてもよい非芳香族複素環基、 置換されていてもよいァラルキル、 低級アル キルスルホニル、 グァニジノ、 ァゾ基、 一 N = N— （置換されていてもよいフエ ニル） 、 または置換されていてもよいウレイ ド等が挙げられる。 これらは、 全て の可能な位置で 1個以上置換しうる。
「置換されていてもよいフエ二レン」 、 「置換されていてもよい単環へテロァ リ レン」 、 「置換されていてもよい 2 , 5—ピリジンジィル」 、 Γ置換されてい てもよい 2 , 5—チォフェンジィル」 、 「置換されていてもよい 2 , 5—フラン ジィル」 、 「置換されていてもよい単環非芳香族複素環ジィル」 、 および 「置換 されていてもよい単環シクロアルカンジィル」 の置換基と しては、 ハロゲン、 二 トロ、 シァノ、 低級アルキル、 低級アルキルォキシ等が好ましい。 非置換のもの が好ましい。
X 1における 「置換されていてもよいァリール」 および 「置換されていてもよ ぃァラルキル」 の置換基と しては、 低級アルキル、 ヒ ドロキシ低級アルキル、 ヒ ドロキシ、 低級アルキルォキシ、 低級アルキルチオ、 ハロゲン、 ニトロ、 シァノ、 カルボキシ、 ノ、口低級アルキル、 ハロ低級アルキルォキシ、 ァラルキルォキシ、 置換されていてもよいァミノ、 置換されていてもよいアミノカルボニル、 ァリー ル、 ヘテロァリール、 非芳香族複素環基、 一 N = N— (フ-ニル） 等が挙げられ る。 好ましい置換基と しては、 低級アルキル、 ヒ ドロキシ、 低級アルキルォキシ、 低級アルキルチオ、 ハロゲン、 ハロ低級アルキル、 ァラルキルォキシ、 一 N - N - (フエニル） 、 アルキレンジォキシ等が挙げられる。
X 1における 「置換されていてもよいァリール」 と しては、 フエ-ル、 3—メ チルフエニル、 4—メチルフエニル、 3 , 4—ジメチルフエニル、 4ーェチノレフ ェニノレ、 4 — t—プチノレフエ二ノレ、 4— n—プチルフエ二ノレ、 4一 II一へキシノレ フエニノレ、 4一 n—ォクチノレフエ二ノレ、 3 , 5—ジー tーブチノレ一 4ーヒ ドロキ シフエ二ノレ、 4ーェチノレオキシフエ二ノレ、 4—フノレオロフ工ニノレ、 3 , 5—ジク ロロフエ二ノレ、 4一ョードフエニル、 4— トリフルォロメチルフエュル、 4—メ チノレチォフエニル、 4一フエニノレオキシメチルフエニル、 ァゾベンゼン一 4ーィ ル、 ベンゾジォキソリル （例えば、 1 , 3 —べンゾジォキソリル） 等が挙げられ る。
R 1 0および R 1 1における 「置換されていてもよいァリール」 の置換基と して は、 ハロゲン、 置換されていてもよいアルキル、 シクロアルキル、 低級アルケニ ル、 低級アルキニル、 ヒ ドロキシ、 アルキルォキシ、 メルカプト、 低級アルキル チォ、 ニ トロ、 シァノ、 カルボキシ、 低級アルキルォキシ力ルポニル、 ハロ低級 アルキル、 ハロ低級アルキルォキシ、 置換されていてもよいァミノ、 置換されて いてもよいアミ ノカルボニル、 ァシル、 ホルミル、 ァシルォキシ、 置換されてい てもよぃァリール、 置換されていてもよいへテロアリール （例えば、 ピリジル、 イミダゾリル） 、 非芳香族複素環基 （例えば、 モルホリノ、 ピペラジニル） 、 ァ ラルキル等が挙げられる。 好ましくは、，置換基群 Bから選択される 1以上の置換 基によって置換されていてもよいアルキル、 シクロアルキル、 置換基群 Bから選 択される 1以上の置換基によって置換されていてもよいアルキルォキシ、 アルキ ルチオ、 ハロゲン、 置換基群 Cから選択される 1以上の置換基によって置換され ていてもよいフヱニル、 置換基群 Cから選択される 1以上の置換基によって置換 されていてもよいへテロアリール、 または置換基群 Cから選択される 1以上の置 換基によって置換されていてもよい非芳香族複素環基等が挙げられる （置換基群
B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキルォキシ カルボニル、 ァリールォキシカルボニル、 置換されていてもよいァミ ノ、 置換基 群 Cから選択される 1以上の置換基によって置換されていてもよいフエニル、 非 芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール） 。 また、 該ァリールは C 5— C 7シク 口へキサン環 （例えば、 シクロペンタン、 シクロへキサン等） または非芳香族複 素環基 （例えば、 テ トラヒ ドロフラニル、 1 , 3 —ジォキソリル、 1 ， 4ージォ キシュル、 ピロリジニル等） と縮合し、 インダン、 1 , 2, 3 , 4—テトラヒ ド ロナフタレン、 1 , 2 , 3 , 4—テ トラヒ ドロキノ リン、 2 , 3—ジヒ ドロベン ゾ [ 1 , 4] ジォキシン、 ベンゾ [ 1， 3] ジォキソール、 2， 3—ジヒ ドロべ ンゾフラン、 2， 3—ジヒ ドロー 1 H—インドールを形成してもよい。
X 1における 「置換されていてもよいへテロアリール」 および 「置換されてい てもよいへテロァリールアルキル」 の置換基と しては、 置換されていてもよい低 級アルキル、 低級アルケニル （例えば、 = CH— CH3) 、 低級アルキニル、 ヒ ドロキシ、 低級アルキルォキシ、 メルカプト、 低級アルキルチオ、 ハロゲン、 二 トロ、 シァノ、 カノレポキシ、 低級アルキルォキシカルボ二ノレ、 ハロ低級アルキノレ、 ハロ低級アルキルォキシ、 置換されていてもよいァミノ、 置換されていてもよい ァミノカルボニル、 ァシル （例えば、 ハロゲン、 ニ トロ、 シァノ等で置換されて いてもよいァリールォキシカルボニル等） 、 ァシルォキシ、 置換されていてもよ ぃァリール、 置換されていてもよいへテロアリール （例えば、 2—ピリジル、 3 一ピリジル、 4一ピリジノレ、 3—チェ二ノレ、 5—メチノレピリジン一 2—ィノレ、 3 一キノ リノレ、 5—クロロチォフェン一 2—ィノレ、 5—ブロモチォフェン一 2—ィ ル） 、 非芳香族複素環基、 ァラルキル、 =N— O— （ァシル） 等が挙げられる。 好ましくは、 置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキ ルォキシカルポニル、 置換されていてもよいフエニル、 ヘテロァリール、 =N— O— （ァシル） 等が挙げられる。
ヘテロ原子が窒素原子である場合は、 該窒素原子がアルキル、 ォキソ等で置換 されていてもよい。
X 2における 「置換されていてもよい 5員へテロァリール」 の置換基と しては、 置換されていてもよい低級アルキル、 低級アルケニル （例えば、 = CH— CH 3) 、 低級アルキニル、 ヒ ドロキシ、 低級アルキルォキシ、 メルカプト、 低級アルキル チォ、 ハロゲン、 ニトロ、 シァノ、 カルボキシ、 低級アルキルォキシカルボニル、 ハロ低級アルキル、 ハロ低級アルキルォキシ、 置換されていてもよいァミノ、 置 換されていてもよいアミノカルボニル、 ァシル （例えば、 ハロゲン、 ニトロ、 シ ァノ等で置換されていてもよいァリールォキシカルボニル等） 、 ァシルォキシ、 置換されていてもよいァリール、 置換されていてもよいへテロアリール （例えば、 2 —ピリ ジル、 3 —ピリジル、 4 一ピリジル、 2 —フリル、 3 —フリル、 2—チ ェニル、 3—チェニル、 5 _メチルピリジン一 2—ィル、 インドールー 3 —ィル、 3 —キノ リル、 5 —クロロチォフェン一 2—ィノレ、 5 —プロモチォフェン一 2— ィル） 、 非芳香族複素環基、 ァラルキル、 — (ァシル） 等が挙げられる。 好ましくは、 置換基群 Bから選択される 1以上の置換基によって置換されていて もよいアルキル、 シクロアルキル、 置換基群 Bから選択される 1以上の置換基に よって置換されていてもよいアルキルォキシ、 アルキルチオ、 ハロゲン、，置換基 群 Cから選択される 1以上の置換基によって置換されていてもよいフエニル、 置 換基群 Cから選択される 1以上の置換基によって置換されていてもよいへテロア リール、 または置換基群 cから選択される 1以上の置換基によって置換されてい てもよい非芳香族複素環基等が挙げられる （置換基群 B ： ヒ ドロキシ、 アルキル 才キシ、 ハロゲン、 カルボキシ、 低級アルキルォキシカルボ二ノレ、 ァリールォキ シカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上 の置換基によって置換されていてもよいフエニル、 非芳香族複素環基、 およびへ テロァリール、
置換基群 c ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール） 。
R 1。および R 1 1における Γ置換されていてもよいへテロアリール」 の置換基 としては、 ハロゲン、 置換されていてもよいアルキル、 シクロアルキル、 低級ァ ルケニル、 低級アルキエル、 ヒ ドロキシ、 アルキルォキシ、 メルカプト、 低級ァ ルキルチオ、 二卜口、 シァノ、 カルボキシ、 低級アルキルォキシカルボニル、 ハ 口低級アルキル、 ハロ低級アルキルォキシ、 置換されていてもよいァミノ、 置換 されていてもよいアミノカルボニル、 ァシル、 ホルミル、 ァシルォキシ、 置換さ れていてもよいァリール、 置換されていてもよいへテロアリール （例えば、 ピリ ジル、 ィミダゾリル） 、 非芳香族複素環基 （例えば、 モルホリノ、 ピペラジニル） 、 ァラルキル等が挙げられる。 好ましくは、 置換基群 Bから選択される 1以上の置 換基によって置換されていてもよいアルキル、 シクロアルキル、 置換基群 Bから 選択される 1以上の置換基によって置換されていてもよいアルキルォキシ、 アル キルチオ、 ハロゲン、 置換基群 Cから選択される 1以上の置換基によって置換さ れていてもよいフエニル、 置換基群 Cから選択される 1以上の置換基によって置 換されていてもよいへテロァリール、 または置換基群 Cから選択される 1以上の 置換基によって置換されていてもよい非芳香族複素環基等が挙げられる （置換基 群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキルォキ シカルボニル、 ァリールォキシカルボ-ル、 置換されていてもよいァミノ、 置換 基群 Cから選択される 1以上の置換基によって置換されていてもよいフユニル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール） 。
本明細書中、 （ α ) 0— γは αが 〜 τ /個存在することを意味する。 例えば、 （C R C R D ) 。 2は （C R C R D ) が 0〜 2個存在することを、 （C H 2 ) 。― 2は （C H 2 ) が 0〜 2個存在することを、 （C H 2 ) J _ ε ¾ ( C H 2 ) が 1〜 5個存在す ることを意味する。
本明細書中、 「血小板産生調節剤」 とは、 血小板減少症 （骨髄移植後の血小板 減少、 化学療法後の血小板減少、 再生不良性貧血、 骨髄異形成症候群、 難治性突 発性血小板減少性紫斑病等の後天性血小板減少症、 ト口ンボポェチン欠損症等の 先天性血小板減少症） 等の血小板数の異常を伴う血液疾患の病態に対する薬剤を 包含する。 例えば、 抗癌剤の投与により血小板数が減少した場合には治療剤と し て、 抗癌剤投与による血小板数の減少が予測される場合には予防剤として使用す ることができる。
本明細鲁中、 「血小板産生を調節する」 とは、 1 ) 抗癌剤の投与等により減少 した血小板数を増加させる、 2 ) 抗癌剤の投与等により減少するであろう血小板 数を維持させる、 3 ) 抗癌剤の投与等による血小板数の減少度を低下させること を包含する。 図面の簡単な説明
図 1 ：本発明化合物により ヒ ト骨髄細胞より形成される巨核球コロニー数を測定 し、 本発明化合物の巨核球前駆細胞の増殖 ·分化促進作用を示したグラフである。 図 2 ：横軸に本発明化合物の濃度、 縦軸に細胞増殖の指標とした吸光度をと り、 本発明化合物によるヒ ト TPO受容体を発現したヒ ト TPO依存性細胞株の細胞増 殖を示したグラフである。 白丸はヒ ト TPOによる応答を、 黒丸は化合物 (B-1)に よる応答を示している。
図 3 ：横軸に本発明化合物の濃度、 縦軸に細胞増殖の指標と した吸光度をとり、 本発明化合物によるマウス TPO受容体を発現したマウス TPO依存性細胞株の細 胞増殖を示したグラフである。 三角はマウス TPOによる応答を、 黒丸は化合物 (B-1)による応答を示している。 発明を実施するための最良の形態
本発明化合物 （ I ) は、 以下の A法ならぴに B法、 およびぞれらに類似の方法 で合成することができる。 . ( A法）
Figure imgf000037_0001
(式中、 R R 2、 R 3、 および X 1は前記と同意義）
(第 1工程）
本工程は、 4 _ホルミルまたは 4一ァシル置換安息香酸誘導体のカルボン酸を REで保護する工程である。第 3工程において 2つのカルボン酸保護基を選択的に 脱保護する必要があることから、 RFとの組み合わせが重要となる。 例えば RFが メチル、 ェチル等のアル力リ条件で脱保護が可能な保護基である場合、 REはアル 力リ条件以外での脱保護が可能な保護基である必要があり、 具体的にはァリル基
(Pd(0)錯体にて脱保護） 、 tert-プチル基、 p-メ トキシベンジル基、 トリフエニル メチル基、 ジフエニルメチル基 （酸性条件で脱保護） 、 トリメチルシリルェチル 基、 トリメチルシリルエ トキシメチル基、 tert-プチルジメチルシリル基 （フッ素 イオンで脱保護） 等が挙げられる。
エステル化の条件と しては適当な塩基の存在下、 相当するハロゲン化物と反応 させる方法を用いることができる。 またはアルコール誘導体を出発原料と して用 いた縮合反応等によっても合成することができる。
(第 2工程）
本工程は、アルデヒ ドまたはケ トンをォレフィンに変換する工程である。 Wittig 反応、 Horner-Emmons反応等のリンイリ ドを用いる反応、 またはクネフエネ一 ゲル （Knoevenagel) 反応等の脱水縮合反応を行うことにより合成することがで きる。
(第 3工程）
本工程は、 REの脱保護反応を行う工程である。 Protective Groups in Organic Synthesis, Theodora W Green (John Wiley & Sons)等に記載の方法を用いて、 保 護基である REを適当な反応条件で脱保護する。
(第 4工程）
本工程は、 カルボン酸誘導体 （V I I ) とァミン誘導体 （Χΐ-ΝΗ2) を、 活性ェ ステル法、 酸クロリ ド法、 混合酸無水物法等により反応させることにより、 アミ ド誘導体 （V I I I ) を得る工程である。 本工程は、 テ トラヒ ドロフラン、 ジォ キサン、 ジクロロメタン、 トルエン、 ベンゼン等の溶媒中で行われる。 活性エス テ レ法では、 1 ーヒ ドロキシペンゾ ト リァゾール、 ヒ ドロキシスクシンイミ ド、 ジメチルァミ ノ ピリジン等と、 ジシクロへキシルカルボジイ ミ ド、 1ーェチル一 3— ( 3—ジメチルァミノプロピル) カルポジイミ ド塩酸塩等を縮合剤と して用 いることにより行うことができる。 酸ク口リ ド法ではチォニルク口リ ドゃォキザ リルクロリ ドを試薬と して遊離のカルボン酸を一旦酸クロ リ ドとすることにより 行うことができる。 混合酸無水物法では、 カルボン酸にェチルクロ口ホルメート、 ィソブチルクロロホルメート等を反応させ、 混合酸無水物とすることにより行う ことができる。 反応には必要に応じて トリェチルァミン、 ピリジン等の塩基が用 いられる。
(第 5工程）
本工程は、 RFの脱保護反応を行う工程である。 Protective Groups in Organic Synthesis, Theodora W Green (John Wiley & Sons)等に記載の方法を用いて、 保 護基である RFを適当な反応条件で脱保護する。
(第 6工程） 本工程は、 カルボン酸誘導体 （ I X) とァミ ン誘導体 （R3-NH2) を、 活性エス テル法、 酸クロリ ド法、 混合酸無水物法等により反応させることにより、 アミ ド 誘導体 （ I 一 A) を得る工程である。 本工程は、 テ トラヒ ドロフラン、 ジォキサ ン、 ジクロロメタン、 トルエン、 ベンゼン等の溶媒中で行われる。 活性エステル 法では、 1ーヒ ドロキシベンゾ トリァゾール、 ヒ ドロキシスクシンイミ ド、 ジメ チルァミノピリジン等と、 ジシクロへキシルカルポジイミ ド、 1一ェチル _ 3—
( 3—ジメチルァミノプロピル） カルポジイミ ド塩酸塩等を縮合剤と して用いる ことにより行う ことができる。 酸クロリ ド法ではチォニルク口リ ドゃォキザリル クロリ ドを試薬と して遊離のカルボン酸を一且酸クロリ ドとすることにより行う ことができる。 混合酸無水物法では、 カルボン酸にェチルクロ口ホルメート、 ィ ソブチルクロロホルメート等を反応させ、 混合酸無水物とすることにより行う こ とができる。 反応には必要に応じて トリェチルァミン、 ピリジン等の塩基が用い られる。
(B法）
本法は、 A法における化合物 （V I I I ) を合成するための別法である。
Figure imgf000039_0001
(式中、 R1 R2、 および X 1は前記と同意義）
(第 1工程）
本工程は、 A法第 4工程と同様の方法を用いることにより、 カルボン酸アミ ド 誘導体 （X I ) を合成する工程である。
(第 2工程）
本工程は、 A法第 2工程と同様の方法を用いることにより、 アルデヒ ド誘導体 (X I ) をォレフィン誘導体 （X I I ) に変換する工程である。 化合物 （X I I ) は、 A法第 5工程および第 6工程と同様の反応を行うことにより化合物（ I 一 A) 、と変換することができる。
Y1がー N (—アルキル） 一 CO—であり、 Z 1が置換されていてもよいチアゾ -ル等である化合物 ：
Figure imgf000040_0001
(W1および Z 1は前記と同意義、 A l kは低級アルキル）
を合成する際のアルキル化の条件によっては、 以下に示す化合物を得る場合があ る。
Figure imgf000040_0002
(W Z 1 , および A 1 kは前記と同意義）
一般式 （ I ) 、 （ I I ) 、 および （ I I I ) において破線が結合の存在を示す 場合は、 シス体、 トランス体、 およびそれらの混合物を包含する。 例えば、 W1 がアミ ドタイプの化合物である場合は以下のようなシス体およびトランス体が存 在しうる。 W1がアミ ドタイプ以外の置換基である場合も同様である。
Figure imgf000040_0003
(式中、 R 1 R2、 R3、 R4、 X 1、 Y および Ζ 1は前記と同意義） 本明細書中、 「溶媒和物」 とは、 例えば有機溶媒との溶媒和物、 水和物等を包 含する。
「本発明化合物」 という場合には、 製薬上許容される塩、 またはその水和物も 抱合される。 例えば、 アルカリ金属 （リチウム、 ナトリ ウム、 カリウム等） 、 ァ ルカリ土類金属 （マグネシウム、 カルシウム等） 、 アンモニゥム、 有機塩基およ びアミノ酸との塩、 または無機酸 （塩酸、 臭化水素酸、 リン酸、 硫酸等） 、 およ ぴ有機酸 （酢酸、 クェン酸、 マレイン酸、 フマル酸、 ベンゼンスルホン酸、 p — トルエンスルホン酸等） との塩が挙げられる。 これらの塩は、 通常行われる方法 によって形成させることができる。 水和物を形成する時は、 任意の数の水分子と 配位していてもよい。
プロ ドラッグは、 化学的または代謝的に分解できる基を有する本発明化合物の 誘導体であり、 加溶媒分解によりまたは生理学的条件下でインビボにおいて薬学 的に活性な本発明化合物となる化合物である。 適当なプロ ドラッグ誘導体を選択 する方法おょぴ製造する方法は、 例えば D e s i g n o f P r o d r u g s , E l s e v i e r , Am s t e r d a m 1 9 8 5に記載されている。 本発明ィ匕 合物がカルボキシル基を有する場合は、 もとになる酸性化合物と適当なアルコー ルを反応させることによって製造されるエステル誘導体、 またはもとになる酸性 化合物と適当なアミンを反応させることによって製造されるアミ ド誘導体のよう なプロ ドラッグが例示される。 プロ ドラッグと して特に好ましいエステルと して は、 メチルエステノレ、 ェチノレエステル、 n—プロピルエステル、 イソプロピノレエ ステノレ、 IIーブチノレエステノレ、 イソブチルエステル、 t e r t ーブチルエステル、 モルホリ ノエチノレエステル、 N, N—ジェチルダリ コールアミ ドエステル等が举 げられる。 本発明化合物がヒ ドロキシル基を有する場合は、 例えばヒ ドロキシル 基を有する化合物と適当なァシルハライ ドまたは適当な酸無水物とを反応させる ことに製造されるァシルォキシ誘導体のようなプロ ドラッグが例示される。 プロ ドラッグと して特に好ましいァシルォキシと しては、 一 OCOC2H5、 一 OCO ( t - B u ) 、 — O COC 1 5H3 1、 一 O CO (m- COON a - P h) 、 一 O C OCH2 CH2 COON a、 一 OC OCH (NH 2) CH3、 - O C O C H 2 N ( C H3) 2等が挙げられる。 本発明化合物がアミノ基を有する場合は、 アミノ基を有 する化合物と適当な酸ハロゲン化物または適当な混合酸無水物とを反応させるこ とにより製造されるアミ ド誘導体のようなプロ ドラッグが例示される。 プロ ドラ ッグと して特に好ましいアミ ドとしては、 一 NHCO (CH2) 2。 CH3、 一 N HCO CH (NH2) CH 3等が挙げられる。
また、 本発明化合物は特定の異性体に限定するものではなく、 全ての可能な異 性体やラセミ体を含むものである。
本発明化合物は後述する実験例の記載の通り、 優れた ト口ンボポェチンァゴニ ス ト活性を示し、 血小板減少症 （骨髄移植後、 化学療法後、 再生不良性貧血、 骨 髄異形成症候群、 難治性突発性血小板減少性紫斑病等の後天性血小板減少症、 ト ロンボポェチン欠損症等の先天性血小板減少症） 等の血小板数の異常を伴う血液 疾患の病態に対する薬剤 （血小板産生調節剤） として使用しうる。 抗癌剤投与に よる血小板数の異常の治療および/または予防に対して使用することができる。 本発明化合物を、 上記の疾患の治療を目的と してヒ トに投与する場合は、 散剤、 顆粒剤、 錠剤、 カプセル剤、 丸剤、 液剤等と して経口的に、 または注射剤、 坐剤、 経皮吸収剤、 吸入剤等と して非経口的に投与することができる。 また、 本化合物 の有効量にその剤型に適した賦形剤、 結合剤、 湿潤剤、 崩壊剤、 滑沢剤等の医薬 用添加剤を必要に応じて混合し、 医薬製剤とすることができる。 注射剤の場合に は、 適当な担体と共に滅菌処理を行つて製剤とする。
投与量は疾患の状態、 投与ルート、 患者の年齢、 または体重によっても異なる が、 成人に経口で投与する場合、 通常 0. 1〜 1 0 0 mg/kg/日であり、 好まし くは 1〜 2 0 mg/kgZ日である。
以下に実施例おょぴ試験例を挙げて本発明をさらに詳しく説明するが、 本発明 はこれらにより限定されるものではない。
実施例中、 以下の略号を使用する。
M e ： メチノレ
E t ： ェチル
n - P r ： n—プロピル i — P r ： イ ソプロピル
c一 P r ： シクロプロピノレ
n— B u ： n—プチノレ
i - B u ： イソブチル
s e c — B u : s e c—プチノレ
t - B u ： t e r t —プチノレ
i - B u ： イ ソブチル
n— P e n ： n一ペンチノレ
c一 P e n ： 、ンクロペンチノレ
n— H e x : 11—へキシル
c 一 H e X ： シクロへキシル
i 一 H e X ： ィソへキシノレ
P h ： フエニル
B n ： ベンジル
B z ： ベンゾィノレ
P y ： ピリジル
T h ： チェニル
A c ： ァセチル
Z ： ベンジルォキシカルボニル
DMF ： N, N—ジメチノレホルムアミ ド
TH F ： テ トラヒ ドロフラン
propargyl：ズ ρノ ノレギノレ、 allyl： ァリノレ、 pyrazole ： ピラゾーノレ、 pyrimidine ： ヒ リ ミ シン、 pipei'idine ： ピぺリジン、 methyl： メチノレ、 cyclohexylmethyl： シ ク口へキシノレメチノレ
実施例
実施例 1 化合物 (A-l、 A-2、 および B-l)の調製
Figure imgf000044_0001
B-1
(第 1工程）
テレフタルアルデヒ ド酸（7.5g)、臭化ァリル（4.41nil)、および炭酸力リ ゥム（7.0 g)の DMF(lOOml)溶液を 60°Cにて 1 6時間攒拌した。 反応溶媒を減圧下留去し、 残留物を酢酸ェチルー水に分配した。 酢酸ェチル層を重曹水、 水、 飽和食塩水に て洗浄し、 硫酸マグネシウムにて乾燥した。 溶媒を減圧留去することによって化 合物（2)を無色透明油状化合物と して（9.2 g)得た。
iH NMR(CDC13) δ ppm): 4.87 (2H， dt, J = 1.2, 5.7 Hz), 5.30 - 5.47 (2H; m); 5.99 - 6.12 (1H, ), 7.94 - 7.98 (2H, m), 8.20 - 8.25 (2H, m), 10.11 (1H, s).
(第 2工程）
化合物（2) (4.37g)、 2— （トリフエニルホスホルァニリデン） プロピオン酸ェ チル（10.63 g)の トルエン（100 ml)溶液を 70°Cにて 1時間加熱攪拌した。 反応溶媒 をおよそ 30〜40mlまで減圧留去し、 析出する トリフエニルホスフィンォキシド を濾去した。 濾液を濃縮後、 残留物をシリカゲルカラムクロマ トグラフィー （酢 酸ェチル： n—へキサン = 1 : 1 0 ) にて精製することによって化合物（3)を無色 透明油状化合物と して（6.9 g)得た。
iH NMR (CDCls, δ ppm): 1.36 (3H; t, J = 7.2 Hz), 2.11 (3H, d, J = 1.5 Hz), 4.29 (2H, q, J= 7.2 Hz), 4.84 (2H; dt, J = 1.2, 5.7 Hz), 5.28 - 5.46 (2H, m), 5.98 - 6.11 (1H, m), 7.43 - 7.47 (2H; m), 7.69 (1H, d, J = 1.5 Hz), 8.06 - 8.10 (2H， m).
(第 3工程）
化合物（3) (6 g)、 テ トラキス ト リフエニルホスフィンパラジウム（1.27 g；)、 お よびモルホリン（2.68g)の THF(lOOml)溶液を 60°Cにて 30分攪拌した。 反応溶媒 をおよそ 30〜40mlまで減圧留去し、 残留物に酢酸ェチルを加え、 重曹水にて 3 回抽出操作を行った。 全ての重曹抽出溶液を 3 M—塩酸水溶液によって酸性と し、 析出する結晶を酢酸ェチルにて抽出した。 酢酸ェチル層を飽和食塩水にて洗浄し、 硫酸マグネシウムにて乾燥した。 溶媒を減圧留去することによって化合物（4)を 白色結晶として（4.5 g)得た。
iH NMR (CDCls, δ ppm): 1.37 (3H, t, J = 7.2 Hz), 2.13 (3H, d, J = 1.2 Hz), 4.30 (2H, q, J= 7.2 Hz), 7.49 (2H, d, J = 8.4 Hz), 7.71 (IH, s), 8.14 (2H, d, J = 8.4 Hz). (第 4工程）
ィ匕合物（4) (1.05 g)およびォキサリルク口リ ド（1.3 ml)の THF(100 ml)溶液に触 媒量の DMFを加え、 2時間室温にて攪拌した。 反応溶液を減圧溜去し、 得られ た残渣にトルエンを加えて、 トルエンを減圧溜去した。 得られたカルボン酸塩化 物をジォキサン（70 ml)に溶解し、 2 —アミ ノー 4— ( 3 , 4—ジクロロフエニル） チアゾール（1 g)およぴピリジン（970 μ 1)を加えた。 反応溶液を 100°Cにて 1 6時 間加熱攪拌後、 反応溶液を酢酸ェチルー水に分配した。 酢酸ェチル層を希塩酸水、 重曹水、 水、 飽和食塩水にて洗浄し、 硫酸マグネシウムにて乾燥した。 溶媒を減 圧留去することによって化合物（A-1)を白色結晶と して（1.5 g)得た。
iH NMR (DMSO-de, δ ppm): 1.29 (3H, t, J = 7.2 Hz), 2.10 (3H， d, J = 1.2 Hz), 4.23 (2H, q, J = 7.2 Hz), 7.62 - 7.68 (3H, m), 7.72 (IH, d, J = 8.4 Hz), 7.91 (1H， s), 7.94 (IH, dd; J = 1.8, 8.4 Hz), 8,15 - 8.20 (2H, m), 8.21 (1H， d, J = 1.8 Hz), 12.84 (IH, br).
(第 5工程）
化合物 (A-l) (1.7 g；)、 4M—水酸化ナトリ ゥム水溶液（5.5 ml)、 THF(150ml)の溶 液を 1 8時間 8 5°Cにて加熱攪拌した。 反応溶液を希塩酸水溶液にて酸性と し、 析出する結晶を濾取する。 得られた粉末をメタノール、 酢酸ェチルにて洗浄する ことによって化合物 (A-2)を白色粉末と して（1.5 g)得た。
iH NMR (DMSO-de, δ ppm): 2.08 (3H, d, J = 0.9 Hz), 7.62 - 7.68 (3H, m), 7.72 (IH, d, J = 8.7 Hz), 7.92 (IH, s), 7.95 (IH, dd, J = 2.1, 8.7 Hz), 8.16 - 8.20 (2H, m), 8.22 (IH, d, J = 1.8 Hz), 12.84 (IH, br).
(第 6工程）
ィ匕合物（A-2) (690 mg), ォキサリルクロリ ド（420 μ 1)の THF(150 ml)溶液に触 媒量の DMFを加え、 7 0°Cにて 1時間攪拌した。 反応溶液を減圧溜去し、 得ら れた残渣にトルエンを加えて トルエンを減圧溜去した。 得られたカルボン酸塩化 物に THF(100 ml)を加え、 氷冷した。 別途に 28%アンモニア水溶液（20 ml)に、 氷冷下エーテル及び水酸化ナトリウム（5 g)を加えて 10分間攪拌し静置した。 こ のエーテル溶液を酸塩化物の THF溶液に加えて氷冷下 1時間攪拌した。反応溶液 を酢酸ェチルー THF—水に分配した。 有機溶媒層を希塩酸水、 重曹水、 水、 飽和 食塩水にて洗浄し、 硫酸マグネシウムにて乾燥した。 溶媒を減圧留去して得られ る残留物をシリ力ゲルカラムコロマ トグラフィー （酢酸ェチル ：！!一へキサン- 1 0 : 1〜酢酸ェチル） にて精製することによって化合物（B-1)を無色結晶として (400 mg)得た。
NMR (DMSO-ds, δ ppm): 2.04 (3Η, d, J = 1,5 Hz), 7.18 (IH, br), 7.32 (IH, s), 7.52 - 7.58 (2H, m), 7.60 (IH, br), 7.72 (IH, d, J= 8.1 Hz), 7.91 (IH, s), 7.94 (1H， dd, 3 = 2.1, 8.4 Hz), 8.14 - 8.19 (2H, m), 8.22 (IH, d, J = 2.4 Hz), 12.81 (1H， br). 実施例 2 化合物 (A- 7)の調製
Figure imgf000047_0001
(第 1工程）
4ーァセチル安息香酸ひ. ォキサリルクロリ ドひ .31 ml)の THF(30 ml)溶 液に触媒量の DMFを加え、 2時間室温にて攪拌した。 反応溶液を減圧溜去し、 得られた残渣にトルエンを加えて、 トルエンを減圧溜去する。 こう して得られた カルボン酸塩ィ匕物に THF(50 ml)、tert-プチルアルコール（1. 15 ml)、ピリジン（1.21 ml)を加え、 40時間加熱還流した。 反応溶液を塩酸酸性氷水一酢酸ェチルに分配 した後、 酢酸ェチル層を重曹水、 水、 飽和食塩水にて洗浄し、 硫酸マグネシウム にて乾燥した。溶媒を濃縮後、残留物をシリカゲルカラムク口マ トグラフィー（酢 酸ェチル ： n キサン = 1 ： 5 ) にて精製し、 化合物（7 )を白色結晶と して（2.0 g)得た。
NMR(CD C13, δ ppm) : 1.61 (9H, s), 2.64 (3H, s), 7.96 - 7.00 (2H, m), 8.04 - 8.09 (2H, m) .
(第 2工程）
水素化ナト リ ゥム（60% 360 mg)の THF(10 ml)懸濁溶液に 2—ホスホノプロピ オン酸トリェチル（2. 14 g)を氷冷下加える。 30分攪拌後、 ィヒ合物（7 ) (1.9 の THF(15 ml)溶液を氷冷下、 滴下した。 反応溶液を 50°Cにて 3時間攪拌後、 塩酸 . 酸性氷水一酢酸ェチルに分配した。 酢酸ェチル層を重曹水、 水、 飽和食塩水にて 洗浄し、 硫酸マグネシウムにて乾燥した。 溶媒を濃縮後、 残留物をシリカゲル力 ラムクロマ トグラフィー (酢酸ェチル： 11—へキサン = 1 ： 1 5 ) にて精製し、 化合物（8 )を無色油状物質と して（1.0 g)得た。 iH NMR(CDC13, 5 ppm): 1.35 (3H, t, J = 7.2 Hz), 1.60 (9H, s), 1.74 (3H, q, J = 1.5 Hz), 2.24 (3H, q, J = 1.5 Hz), 4.27 (2H, q, J = 6.9 Hz), 7.18 - 7.22 (2H, m), 7.97 - 8.10 (2H, m).
(第 3工程）
化合物（8 ) (900 mg)のぎ酸（98〜100%, 10 ml)溶液を室温にて 3時間攪拌した。 反応溶液を濃縮後、 残渣にトルエンを加え再ぴ濃縮した。 得られた残渣を n—へ キサンにて濾取することによって化合物（9 )を白色結晶と して（680 mg)得た。
NMR(CDC13, δ ppm): 1.36 (3H, t, J = 7.2 Hz), 1.74 (3H, q， J = 1.5 Hz), 2.26 (3H, q, J = 1.5 Hz), 4.28 (2H, q, J = 7.2 Hz), 7.25 - 7.29 (2H, m), 8.10 - 8.14 (2H; m).
(第 4工程）
化合物（9 )を原料として、 実施例 1—第 4工程と同様の反応を行うことにより ィ匕合物（A-7)を合成した。
iH NMR(CDC13) δ ppm): 1.36 (3H, t, J = 7.2 Hz), 1.74 (3H, q, J = 1.5 Hz), 2.25 (3H, q, J = 1.5 Hz), 4,28 (2H, q, J = 7.2 Hz), 7.26 - 7.29 (2H, m), 7.44 (IH, d, J = 8.4 Hz), 7.61 (IH, dd, J = 2.1, 8.4 Hz), 7.91 (IH, d, J = 2.1 Hz), 7.91 - 7.95 (2H, m), 10.09 (IH, br).
化合物 (A-3；)〜 (A-6)、 (A-8)〜(A-107)、（B-2)〜（B-46)、（C-l)〜（C-5)、（D-l)、 (E-l) 〜（E-2)、 （F-l)〜（F-3)、 （F-l)〜（F-3)、 （G-:！)〜（G-8)、 （H-:！)〜（H-8)、 および (1-1) 〜(I-6)を実施例 1および 2に記載の方法と同様の方法で合成した。 化合物群 Aの 物理恒数を表 1 〜 1 0に、 化合物群 Bの物理恒数を表 1 1 〜 1 7に、 化合物 C群 の物理恒数を表 1 8に、 化合物 D群の物理恒数を表 1 9に、 化合物 E群の物理恒 数を表 2 0に、 化合物 F群の化合物の物理恒数を表 2 1に、 化合物 G群の化合物 の物理恒数を表 2 2 〜 2 3に、 化合物 H群の化合物の物理恒数を表 2 4〜 2 5に、 化合物 I群の化合物の物理恒数を表 2 6に示した。
Figure imgf000049_0001
Figure imgf000050_0001
Figure imgf000051_0001
表 4
Figure imgf000052_0001
Figure imgf000053_0001
Figure imgf000054_0001
Figure imgf000055_0001
Figure imgf000056_0001
Figure imgf000057_0001
0
Figure imgf000058_0001
Figure imgf000059_0001
1 2
Figure imgf000060_0001
1 3
Figure imgf000061_0001
1 4
Figure imgf000062_0001
1 5
Figure imgf000063_0001
1 6
Figure imgf000064_0001
1 7
Figure imgf000065_0001
1 8
Figure imgf000066_0001
9
Figure imgf000067_0001
化合物
R10 R2 Het iH-NMR (DMSO d-6)
No.
2.35 (3H, d, J = 0.9 Hz), 7.12 (2H, bs), 7.32 (IH, s), 7.58 (2H, d, J = 8.1 Hz), 7.72 (IH, d, J = 7.8 Hz), 7.92 (IH, s), 7.95 (IH, dd, J =
D-l H Me
Cl 8.4 Hz, 2.1 Hz), 8.17 (2H, d, J = 8.4 Hz),
8.22 (IH, d, J = 1.8 Hz), 12.31 (IH, s)， 12.79 ひ H, s)
0
Figure imgf000068_0001
Figure imgf000069_0001
Figure imgf000070_0001
Figure imgf000071_0001
2 4
Figure imgf000072_0001
2 5
Figure imgf000073_0001
表 2 6
Figure imgf000074_0001
実施例 3 化合物 (A-15)の調製
Figure imgf000075_0001
メ トキシ-メ トキシカルボニルメチル-ト リフエニルホスホニゥム クロ リ ド (152 mg)と 2-(4-ホルミルベンゾィルァミノ） -4.(3, 4-ジクロロフエニル）チアゾー ル （57 mg) を塩化メチレン（3 ml)に懸濁させトリェチルァミ ン （38 mg)を加えた。 室温で一夜攪拌した。 濃縮後、 シリカゲルカラムクロマ トグラフィーにより精製 し目的とする化合物 （A- 15) を 30 rag得た。
融点 203〜205。C
iH-NMR (CDCh) δ ppm: 3.85 (s, 3H), 3.89 (s， 3H), 6.96 (s, 1H), 7.22 (s， 1H), 7.46 (dd, 1H， J = 8.2, 1.9 Hz), 7.63 (d, 1H, J = 8.2 Hz) 7.86 (d, 2H, J = 8.6 Hz), 7.92 (d, 1H, J = 1.9 Hz), 7,94 (d, 2H, J = 8.6 Hz), 9.82 (brs, 1H). 実施例 4 化合物（J-3)の調製 '
(E)-3-(4-ョー ドフエニル） -2-メチルァク リル酸ェチルエステル（200mg)、 ジク口 口ビス（ト リフエニルホスフィン）パラジウム（n)(22mg；)、 2-ァミ ノ -4-(4'-クロロフ ヱニル） - 1H-ィ ミダゾール（277mg)、 ト リエチルアミ ン（0.27ml)の DMF(7ml)溶液 を一酸化炭素ガス雰囲気下 90°Cにて 15分間攪拌した。反応液を放冷後氷にあけ、 析出する結晶を濾取し DMFで再結晶して化合物（J- 3)を淡黄色結晶として 117mg 得た。 実施例 5 化合物（J- 16)の調製
ィ匕合物（A-53)のェチルエステル体（300mg)のァセ トニ ト リル-テ トラヒ ドロフ ラン（1: 1)溶液（80ml)に 1-フルォ口- 4-ヒ ドロキシ - 1,4-ジァゾ二アビシク口 [2.2.2] ォクタン ビステ トラフルォロボレート（50% o アルミナ 1.24 g)を加えて 80°Cに て 30分間攪拌した。 アルミナを濾別後、 濾液を減圧濃縮し、 クロ口ホルムを加 えて懸濁させ、再度不溶物を濾別し減圧濃縮した。分取用 TLCプレートで精製後、 フッ素化体を黄色結晶と して 20mg得た。得られたエステル体を化合物（A-2)の調 製と同様の方法にて加水分解し、 化合物（J-16)を得た。
実施例 4および 5 と同様の方法で化合物（J-1)〜(； J-2)、 （J-4)〜（J-15)、 および (J-17)を合成した。 物理恒数を表 2 7および 2 8に示した。
7
Figure imgf000077_0001
8
Figure imgf000078_0001
実施例 6
化合物 (K-14, 15, 18)の調製
Figure imgf000079_0001
(第 1工程）
化合物（11)(1.1 g)、 (12)(760 mg), 炭酸カリ ウム（1.44 g)、 テ トラキス トリフエ ニルホスフィンパラジウム（250 mg)の DMF溶液を 110°Cにて 2時間攪拌した。 反応溶液を酢酸ェチルに注ぎ、 水にて 4回、 飽和食塩水にて洗浄し、 硫酸マグネ シゥムにて乾燥した。 溶媒を濃縮後、 残留物をシリカゲルカラムクロマ トグラフ ィー （酢酸ェチル： n—へキサン = 2 ： 3 ) にて精製し、 化合物（13)をァモルファ スと して （870 mg) 得た。
iH NMR(CDC13) δ ppm): 4.06 (3H, s), 7.16 (1H， s), 7.28 - 7.50 (雇, m); 7.72 (1H, dd, J = 4.8 Hz, 1.8 Hz), 7.75 - 7.80 (2H, m), 8.25 - 8.30 (2H, m), 8.40 (IH, d, J = 2.1 Hz).
(第 2工程）
化合物（13) (870
Figure imgf000079_0002
50°Cにて 3時間攪拌した。 反応溶液を濃縮後、 残渣にトルエンを加え再び濃縮した。 得られた残渣をイソプ 口ピルエーテルにて濾取することによって化合物（4)を白色結晶として（473 mg) 得た。
iH NMR(CDC13) δ ppm): 3.93 (3H, s), 7.97 - 8.02 (2H, m), 8.04 (IH, dd, J = 7.8 Hz, 1.8 Hz), 8.07 - 8.12 (2H, m), 8.35 (IH, d, J = 1.5 Hz), 8.82 (IH, d, J = 4,8 Hz). (第 3工程）
化合物 (K-14)は、 化合物（4)を原料と し実施例 1の第 4工程と同様の反応を行う ことによって合成した。 物理恒数は表 2 9に示した。
(第 4工程）
化合物（K-15)は、 ィヒ合物（K-14)を原料と し実施例 1の第 5工程と同様の反応を 行うことによって合成した。 物理恒数は表 2 9に示した。
(第 5工程）
ィ匕合物（K-15) (100 mg)、 ジフエ二ルリン酸アジド （55 μ1)、 トリェチルァミン (351 μ1)、 tert-プタノール (1 nil)のジメチルホルムァミ ド (15 ml)溶液を 100°Cに て 1時間攪拌した。 反応溶液を酢酸ェチルに注ぎ （析出した場合は必要に応じて THFを加えた） 、 水にて 2回、 炭酸水素ナトリウム水溶液、 飽和食塩水にて洗浄 し、 硫酸マグネシウムにて乾燥した。 溶媒を濃縮後、 残留物をシリカゲルカラム クロマ トグラフィー（酢酸ェチル：n キサン = 1 ： 1 )にて精製し、化合物（K-18) を白色結晶と して （60 mg) 得た。 物理恒数は表 2 9に示した。
実施例 6 と同様の方法を用いて（K-16)〜（K-17)および (K-19)を合成した。 実施 例 1 と同様の方法を用いて化合物（K-1)〜(； K-13)を合成した。物理恒数を表 2 9 3 1に示した。 9
Figure imgf000081_0001
0
Figure imgf000082_0001
Figure imgf000083_0001
実施例 7 化合物（L-l、 L- 2 )の調製
Figure imgf000084_0001
(第 1工程）
化合物（15)(6·3 g；)、 （16)(2.0 ml)、 ト リヱチルァミ ン（6.3 ml)、 テ トラキス ト リ フエ二ノレホスフィンパラジウム（870 mg)、 よ う化銅（I) (290 mg〉の DMF(70 ml) 溶液を 90°Cにて 4時間攪拌した。 反応溶液を酢酸ェチルに注ぎ、 水にて 4回、 飽 和食塩水にて洗浄し、 硫酸マグネシウムにて乾燥した。 '溶媒を濃縮後、 残留物を シリ力ゲル力ラムクロマ トグラフィー （酢酸ェチル ： n—へキサン = 1 ： 4 ) に て精製し、 化合物（17)をアモルファスとして （2.25 g) 得た。
iH NMR(CDC13) δ ppm): 3.81 (3H, s), 7.06 (IH, s), 7.28 - 7.42 (6H, m), 7.51 - 7.55 (4H, m), 7.85 (2H, d, J = 8.7 Hz), 8.17 (2H, d, J = 8.7 Hz).
(第 2工程）
化合物（17) (180 mg)のぎ酸（98〜100%, 4 ml), THF(4 ml)の溶液を室温にて 18 時間攪拌した。 反応溶液を濃縮後、 残渣にトルエンを加え再び濃縮した。 得られ た残渣をィソプロピルエーテルにて濾取することによって化合物（18)を白色針状 晶と して（95 mg)得た。 iH NMR(CDC13, δ ppm): 3.80 (3H, s), 7.79 (2H, d, J = 8.1 Hz), 8.00 (2H, d, J = 8,1 Hz), 13.33 (IH, bs).
(第 3工程）
化合物 (L-1)は、 化合物（4)を原料と し実施例 1の第 4工程と同様の反応を行う ことによって合成した。 物理恒数は表 3 2に示した。
(第 4工程）
化合物（L-2)は、 化合物（L-1)を原料とし実施例 1の第 5工程と同様の反応を行 うことによって合成した。 物理恒数は表 3 2に示した。
実施例 7 と同様の方法で化合物（L-3：)〜（L-4)を合成した。 物理恒数を表 3 2に 示した。
2
Figure imgf000086_0001
上記の方法と同様の反応を行うことにより、 以下に示す化合物を合成すること ができる。
Figure imgf000087_0001
(化合物 No., Ra, R ; RC; Rd, Re) = (M-l, H, H, H, H, H), (M-2, H， H, H, H, CI), (M-3, H， H, H, H, F), (M-4, H, H, H, H, CFs), (M-5, H, H, H, H, Br), (M-6, H, H, H, H, CHs), (M-7, H, H, H, F, H), (M-8, H, H， H, F, CI), (M-9, H, H, H, F, F), (M-10, H, H, H, F, CFs), (M-11, H, H, H, F, Br), (M-12, H, H, H, F, CHs), (M- 13, H, H, H, CI, H), (M-14, MeO, H, H, CI, CI), (M-15, H, H, H, CI, F), (M-16, H, H, H, CI, CFs), (M-17, H, H, H, CI, Br), (M-18, H, H, H, CI, CHs), (M-19, H, H, H, CH3, H), (M-20, H， H, H， CHs, Cl)， (M-21, H, H, H, CH3, P); (M-22, H, H， H, CHs, CFs), (M-23, H, H, H, CHs, Br), (M-24, H, H, H, CHs, CHs), (M-25, H, H, H， Et, H), (M-26, H, H, H, Et, CI), (M-27, H, H, H, Et, F), (M-28, H， H, H, Et, CFs), (M-29, H, H, H, Et, Br), (M-30, H, H, H, Et, CH3), (M-31, H, H, H, n-Pr, H), (M-32, H, H, H, n-Pr, CI), (M-33, H, H, H, n-Pr, F), (M-34, H, H, H， n-Pr, CFs), (M-35, H, H, H, n-Pr, Br), (M-36, H, H， H, n-Pr, CHs), (M-37, H' H, H, c-Pr, H)， (M-38, H, H, H, c-Pr, CI), (M-39, H, H， H, c-Pr, F), (M-40, H, H, H, c-Pr, CFs), (M-41, H, H, H, c-Pr, Br), (M-42, H, H, H, c-Pr, CHs), (M-43, H, H, H， i-Pr, H), (M-44, H, H, H, i-Pr, CI), (M-45, H, H, H, i-Pr, F), (M-46, H, H, H, i-Pr, CF3), (M-47, H, H, H, i-Pr, Br), (M-48, H, H, H, i-Pr, CH3), (M-49, H, H, H， n-Bu, H), (M-50, H, H， H, n-Bu, CI), (M-51, H, H, H, n-Bu, F)， (M-52, H， H, H, n-Bu, CF3), (M-53, H, H, H, n-Bu, Br), (M-54, H， H, H, n-Bu, CHs), (M-55, H, H, H, i-Bu, H), (M-56, H, H, H， i-Bu, CI), (M-57, H, H, H, i-Bu, F), (M-58, H, H, H, i-Bu, CFs), (M-59, H， H, H, i-Bu, Br), (M-60, H, H, H, i-Bu, CHs), (M-61, H, H, H, sec-Bu, H), (M-62, H' H, H, sec-Bu, CI), (M-63, H, H, H, sec-B , F), (M-64, H, H, H, sec-Bu, CFs), (M-65, H, H, H, sec-Bu, Br), (M-66, H, H, H, sec-Bu, CHs), (M-67, H, H, H， n-Pen, H), (M-68, H, H, H, n-Pen, CI), (M-69, H, H, H， n-Pen, F), (M-70, H, H, H, n-Pen, CFs), (M-71, H, H, H, n-Pen, Br), (M-72, H, H, H, n-Pen, CH3), (M-73, H, H, H, c-Pen, H), (M-74, H, H, H, c-Pen, CI), (M-75, H, H， H, c-Pen, F), (M-76, H, H, H, c-Pen, CFs), (M-77, H, H, H, c-Pen, Br), (M-78, H, H, H, c-Pen, CH3), (M-79, H， H, H, n-Hex, H)' (M-80, H, H, H, n-Hex, CI), (M-81, H, H， H, n-Hex, F), (M-82, H, H, H, n-Hex, CFs), (M-83, H， H, H, n-Hex, Br), (M-84, H, H, H, n-Hex, CHs), (M-85, H， H, H, c-Hex, H), (M-86, H, H, H, c-Hex, CI), (M-87, H, H, H, c-Hex, F), (M-88, H' H， H, c-Hex, CFs), (M-89, H, H, H, c-Hex, Br), (M- 90' H, H' H, c-Hex, CHs), (M-91, H, H, H' OH, H), (M-92, H, H, H, OH, CI), (M-93, H, H, H， OH, F), (M-94, H， H, H, OH, CFs), (M-95, H， H， H, OH, Br), (M-96, H， H, H, OH, CHs), (M-97, H, H, H, EtO, H), (M-98， H， H, H, EtO, CI), (M-99, H， H, H， EtO, F), (M-100, H, H, H, EtO, CF3), (M-101, H, H, H, EtO, Br), (M-102, H, H, H, EtO, CHs), (M-103, H, H, H, n-PrO, H)， (M-104, H, H, H, n- PrO, CI), (M-105, H, H, H, n-PrO, F), (M-106, H, H, H, n-PrO, CFs), (M-107, H, H, H, n-PrO, Br), (M-108, H, H, H, n-PrO, CHs), (M-109, H, H, H, PhO, H), (M-110, H, H, H, PhO, CI), (M-lll, H, H， H, PhO, F), (M-112, H, H, H, PhO, CF3), (M-113, H, H, H, PhO, Br), (M-114, H, H, H, PhO, CHs), (M-115, H, H, H, BnO, H), (M-116, H, H, H, BnO, CI), (M-117, H， H, H, BnO, F), (M-118, H, H， H, BnO, CFs), (M-119, H, H， H, BnO, Br), (M-120, H, H, H, BnO, CHs), (M-121, H, H' H, P1LCH2CH20 , H), (M- 122, H， H， H, PI1CH2GH2O, CI), (M- 123, H, H, H, PhCH2CH20, P), (M-124, H, H, H, PhCH2CH20, CF3), (M-125, H， H, H, PhCH2CH20, Br), (M-126, H， H, H, PhCH2CH20, CHs), (M-127, H, H, H, CPsO, H), (M-128, H, H, H, CFsO, CI), (M-129, H, H, H, CFsO, P), (M-130, H， H， H, CFsO, CFs), (M-131, H, H, H, CFsO, Br), (M-132, H, H, H, CFsO, CHs), (M-133, H, H， H, Ph, H), (M- 134, H, H' H, Ph, CI), (M-135, H, H, H, Ph, F), (M-136, H, H, H, Ph, CFs), (M-137, H, H, H, Ph, Br), (M-138, H, H, H, Ph, CHs), (M-139, H, H, H, 4-F-P H), (M-140, H, H, H, 4-F-Ph, CI), (M-141, H, H, H, 4-F-Ph, F), (M-142, H, H, H, 4-F-Ph, CFs), (M-143, H， H, H, 4-F-P , Br), (M-144, H, H, H, 4-F-Ph, CHs), (M- 145, H, H， H, 4-CFs-Ph, H), (M-146, H, H, H, 4-CFs-Ph, CI), (M-147, H, H, H, 4-CFs-Pli, F)， (M-148, H, H, H, 4-CFs-Ph, GFs), (M-149, H， H, H, 4-CFs-Pli, Br), (M-150, H, H, H, 4-CF3-Ph, CH3), (M-151, H, H' H, 4- (Me)2N-Pli, H), (M-152, H, H, H, 4-(Me)2N-Pli; CI), (M-153, H, H, H, 4- (Me)2N-Pli; F), (M- 154, H, H, H, 4-(Me)2N-Ph> CP3), (M-155, H, H, H, 4- (Me)2N-Ph, Br), (M- 156, H, H, H, 4-(Me)2N-Pli) CHs), (M- 157, H， H, H, 4-OH- Ph, H), (M- 158, H' H, H, 4-OH-Ph, CI), (M-159, H, H， H, 4-OH-Ph, F), (M-160, H, H, H, 4-OH-Ph, CF3), (M- 161, H, H, H, 4-OH-Ph, Br), (M-162, H, H， H, 4- OH-Ph, CHs), (M-163, H， H, H, 3,4-di-F-Ph, H), (M- 164, H, H, H, 3, 4-di-F-Ph, CI), (M-165, H, H, H, 3,4-di-F-Ph, F), (M- 166, H, H, H， 3, 4-di-F-Ph, CF3), CM- 167, H， H， H, 3,4-di-F-Ph, Br), (M- 168, H， H, H, 3,4-di-F-Ph, CHs), (M-169, H, H, H, 4-COOH-Ph, H), (M-170, H, H, H, 4-COOH-Ph, CI), (M-171, H, H， H, 4- COOH-Ph, F), (M-172, H, H, H， 4-COOH-Ph, CFs), (M-173, H, H, H, 4-COOH- Ph, Br), (M-174, H, H, H, 4-COOH-Ph, CHs), (M-175, H, H, H, Bn, H), (M-176, H, H, H, Bn, CI), (M- 177, H, H, H, Bn, F), (M-178, H, H, H, Bn, CFs), (M-179, H, H, H, Bn, Br), (M-180, H， H, H, Bn, CHs), (M-181, H, H, H, 4-F-Bn, H)， (M-182, H, H, H, 4-F-Bn, CI), (M- 183, H, H, H, 4-F-Bn, F), (M-184, H， H, H， 4-F-Bn, CFs), (M-185, H, H, H, 4-F-Bn, Br), (M-186, H' H, H, 4-F-Bn, CH3), (M-187, H, H, H, 2-Py, H)， (M- 188, H, H, H, 2-Py, CI), (M-189, H, H, H， 2-Py, F); (M-190, H， H, H, 2-Py, CFs), (M-191, H, H, H, 2-Py, Br), (M-192, H, H, H, 2-Py, CHs), (M-193, H, H, H, 3-Py, H), (M-194, H， H， H, 3-Py, CI), (M-195, H, H, H， 3-Py, F), (M-196, H, H, H, 3-Py, CF3), (M-197, H, H, H, 3-Py, Br), (M-198, H, H, H， 3-Py, b
ο
Figure imgf000090_0001
HOOCCH2CH2CH2CH2, F), (M-256, H, H, H, HOOCCH2CH2CH2CH2, CF3), (M-257, H, H， H， HOOCCH2CH2CH2CH2, Br), (M-258, H， H, H,
HOOCCH2CH2CH2CH2, CHs), (M-259, H, H, H，（Me)2NCOCH2CH2CH2GH2, H), (M-260, H' H, H, (Me)2NCOCH2CH2CH2CH2, CI), (M-261, H, H, H，
(Me)2NCOCH2CH2CH2CH2, F), (M-262, H, H, H, (Me)2NCOCH2CH2CH2CH2, CPs), (M-263, H, H, H, (Me)2NCOCH2CH2CH2CH2, Br), (M-264, H, H， H, (Me)2NCOCH2CH2CH2CH2, CHs), (M-265, H, H， H,
(Me)2NCOCH2CH2CH2CH2CH2! H), (M-266, H, H, H,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-267, H, H， H,
(Me)2NC0CH2CH2CH2CH2CH2; F), (M-268, H, H, H,
(Me)2NC0CH2CH2CH2CH2CH2> CF3), (M-269, H, H， H,
(Me)2NCOCH2CH2CH2CH2CH2; Br), (M-270, H, H, H，
(Me)2NCOCH2CH2CH2CH2CH2， CHs), (M-271, H, H, H, MeOCH2) H), (M-272, H, H, H, MeOCHa, CI), (M-273, H, H， H, MeOCH2) F), (M-274, H, H， H, MeOCHa, CF3), (M-275, H, H, H, MeOCHa, Br), (M-276, H, H, H, MeOCH2, CH3), (M-277, H, H, H' EtOCH2) H), (M-278, H, H, H, EtOCHs, CI), (M-279, H, H, H, EtOCH2; F), (M-280, H, H， H， EtOCH , CF3), (M-281, H, H, H, EtOCH2; Br), (M-282, H, H, H, EtOCHa, CH3), (M-283, H, H, H, EtOCH2CH2> H), (M-284, H, H, H, EtOCH2CH2, CI), (M-285, H, H, H, EtOCH2CH2, F), (M-286, H， H, H,
EtOCHaCHa, CFs), (M-287, H, H, H, EtOCH2C¾ Br), (M-288, H, H, H,
EtOCH2CH2; CHs), (M-289, H, H, H， MeOCH2CH2OCH2CH2, H), (M-290, H, H, H, MeOCH2CH2OCH2CH2; CI), (M-291, H, H, H, MeOCH2.CH2OCH2CH2, F), (M-292, H, H, H, MeOCH2CH2OCH2CH2, CF3), (M-293, H, H, H,
MeOCH2CH2OCH2CH2, Br), (M-294, H, H, H, MeOCH2CH2OCH2CH2, CH3)， (M-295, H, H, H, MeOCH2CH2, H), (M-296, H' H, H, MeOCH2CH2, CI), (M-297, H, H, H, MeOCH2CH2) F), (M-298, H, H, H, MeOCH2CH2) GF3), (M-299, H, H, H, MeOCH2CH2, Br), (M-300, H, H, H, MeOCH2CH2, CH3)， (M-301, H, H, H, HOCHa, H), (M-302, H, H' H， HOCH2, CI), (M-303, H, H, H, HOCH2; F), (M-304, H, H, H， H0CH2, CFs), (M-305, H， H, H, HOCHa, Br), (M-306, H, H, H, HOCH2, CH3), (M-307, H, H, H, HOCH2CH2， H), (M-308, H, H, H, HOCH2CH2, CI), (M-309, H, H, H, HOCH2CH2, F), (M-310, H, H, H, HOCH2CH2, CFs), (M-311, H, H， H， HOCH2CH2, Br), (M-312, H, H, H, HOCH2CH2, CHs), (M-313, H, H， H, HOC CH2CH2， H), (M-314, H, H, H， HOCH2CH2CH2j CI), (M-315, H， H, H, HOCHaCHaCHa, F), (M-316, H, H, H， HOCH2CH2CH2, CF3), (M-317, H, H, H, HOCH2CH2CH2; Br), (M-318, H， H, H, HOCH2CH2CH2, CHs), (M-319, H, H, H, HOCH2CH2CH2CH2> H), (M-320, H, H, H, HOCH2CH2CH2CH2, CI), (M-321, H, H, H, HOCH2CH2CH2CH2, F), (M-322, H, H, H, HOCH2CH2CH2CH2, CF3), (M-323, H, H, H, HOCH2CH2CH2CH2, Br), (M-324, H， H, H,
HOCH2CH2CH2CH2, GH3); (M-325, H' H， H, HOCH2CH2CH2CH2CH2， H), (M- 326, H, H, H, HOCH2CH2CH2CH2CH2, CI), (M-327, H, H, H,
HOCH2CH2CH2CH2CH2, F), (M-328, H, H， H， HOCH2CH2CH2CH2CH2, CFs), (M-329, H, H, H, HOCH2CH2CH2CH2CH2, Br), (M-330, H, H, H,
HOCH2CH2CH2CH2CH2) CHs), (M-331, H, H， H, HOCH2CH2OCH2CH2, H)， (M-332, H, H， H, HOCH2CH2OCH2CH2, CI), (M-333, H, H, H，
HOCH2CH2OCH2CH2, F), (M-334, H, H, H, HOCH2CH2OCH2CH2, CF3), (M-335, H, H, H, HOCH2CH2OCH2CH2, Br), (M-336, H, H, H, HOCH2CH2OCH2CH2, CHs), (M-337, H, H， H, (Me)2N, H), (M-338, H, H, H, (Me)2N, CI), (M-339, H, H, H, (Me)2N, F), (M-340, H, Η,,,Η, (Me)2N, CF3), (M-341, H, H， H, (Me)2N, Br), (M-342, H, H, H' (Me N, CHs), (M-343, H, H, H, piperidm-4-yl-methyl, H), (M-344, H, H, H, piperidin-4-yl-methyl; CI), (M-345, H, H, H, piperidin-4-yl- methyl, F), (M-346, H, H, H, piperidin-4-yl-metliyl, CFs), (M-347, H, H' H, piperidin-4-yレ methyl, Br), (M-348, H, H, H, piperidin-4-yl-metliyl, CHs), (M- 349, H, H, H, cyclohexylmetliyl, H), (M-350, H， H, H, cyclohexylmethyl, CI), (M-351, H, H, H， cyclohexylmethyl, F), (M-352, H, H, H, cyclohexylmetliyl, CFs), (M-353, H, H, H' cyclohexylmet yl, Br), (M-354, H, H， H,
cyclohexylmethyl, CH3), (M-355, H, H, F, H, H), (M-356, H, H' F, H， CI), (M-357, H， H, F, H， F), (M- 358, H, H, F, H， CFs), (M-359, H， H, F, H, Br), (M-360, H， H, F, H, CHs), (M-361, H, H， F, F, H), (M-362, H, H, F, F, CI), (M- 363, H， H, F， F, F), (M-364, H, H, F， F, CF3)， (M-365, H, H, F, F, Br), (M-366, H, H, F, F, CH3), (M-367, H, H, F, CI, H), (M-368, H, H, F, CI, CI), (M-369, H, H, F, CI, F), (M- 370, H, H, F, CI, CFs), (M-371, H, H, F, CI, Br), (M-372, H; H, F, CI, CHs), (M-373, H, H， F, CHs, H), (M-374, H, H, F, CHs, CI), (M-375, H, H, F, CH3, F), (M-376, H, H, F; CH3, CF3); (M-377, H, H, F, CHs, Br), (M-378, H, H, F, CH3, CHs), (M-379, H, H, F， Et, H), (M-380, H， H, F; Et, CI), (M-381, H, H, F， Et, F)， (M-382, H， H， F, Et, CFs), (M-383, H， H, F, Et, Br), (M-384, H, H, F, Et, CH3), (M-385, H, H， F, n-Pr, H), (M-386, H, H， F, n-Pr, CI), (M-387, H, H, F, n-Pr, F), (M-388, H, H， F' n-Pr, CFs), (M-389, H, H, F, n-Pr, Br), (M-390, H, H， F, n-Pr, CHs), (M-391, H, H, F, c-Pr, H), (M-392, H, H, F, c-Pr, CI), (M-393, H, H， F, c-Pr, F), (M-394, H, H, F, c-Pr, CF3), (M-395, H, H, F, c-Pr, Br), (M-396, H， H, F， c- Pr, CHs), (M- 397, H, H, F, i-Pr, H), (M-398, H, H, F, i-Pr, CI), (M-399, H， H, F, i-Pr, F), (M-400, H, H, F, i-Pr, CFa), (M-401, H, H, P, i-Pr, Br), (M-402, H, H， F, i-Pr, CHs), (M-403, H, H, F, n-Bu, H), (M-404, H, H, F, n-Bu, CI), (M-405, H, H, F, n-Bu, F), (M-406, H, H, F， n-Bu, CFs), (M-407, H, H, F, n-Bu, Br), (M-408, H, ·. ~. H, F, n-Bu, CHs), (M-409, H' H， F, i-Bu, H), (M-410, .H,,H; F, i-Bu, CI), (M-411, H, H, F, i-Bu, F), (M-412, H, H， F, i-Bu, CF3), (M-413, H, H, F, i-Bu, Br), (M- 414， H, H, F, i-Bu, CHs), (M-415, H, H, F, sec-Bu, H), (M-416, H, H, F, sec-Bu, CI), (M-417, H, H, F, sec-Bu, F), (M-418, H, H, F, sec-Bu, CFs), (M-419, H, H, F, sec-Bu, Br), (M-420, H' H, F, sec-Bu, CHs), (M-421, H, H, F, n-Pen, H), (M-422, H, H, F, n-Pen, CI), (M-423, H, H, F, n-Pen, F), (M-424, H, H, F, n-Pen, CF3), (M-425, H, H, F, n-Pen, Br), (M-426, H' H， F, n-Pen, CHs), (M-427, H, H, F, c-Pen, H), (M-428, H, H, F, c-Pen, CI), (M-429, H, H, F, c-Pen, F)， (M-430, H, H, F, c-Pen, CFs), (M-431, H, H, F， c-Pen, Br), (M-432, H, H， F, c-Pen, CH3), (M- 433, H, H, F, n-Hex, H), (M-434, H, H, F, n-Hex, CI), (M-435, H, H, F, n-Hex, F), (M-436, H, H, F, n-Hex, CFs), (M-437, H， H, F, n-Hex, Br), (M-438, H, H, F, n-Hex, CH3), (M-439, H, H, F, c-Hex, H), (M-440, H, H, F, c-Hex, CI), (M-441, H, H, F， c-Hex, F)，（M-442, H' H, F, c-Hex, CFs), (M-443, H， H, F' c-Hex, Br), (M-444, H， H, F, c-Hex, CH3)， (M-445, H, H, F， OH, H), (M-446, H, H, F, OH, CI), (M-447, H， H， F, OH, F), (M-448, H, H, F， OH, CFs), (M-449, H, H, F, OH, Br), (M-450, H， H, F, OH, CHs), (M-451, H, H, F, EtO, H), (M-452, H, H, F, EtO, CI), (M-453, H' H, F， EtO, F)， (M-454, H, H， F, EtO, CFs), (M-455, H, H, F, EtO, Br), (M-456, H, H， F, EtO, CH3), (M-457, H, H, F, n-PrO, H), (M-458, H, H, F， n-PrO, CI), (M-459, H， H, F, n-PrO, F), (M-460, H, H, F, n-PrO; CF3), (M-461, H, H, F， n-PrO, Br), (M-462, H， H, F, n-PrO, CHs), (M-463, H, H, F, PhO, H), (M-464, H, H, F, PhO, CI), (M-465, H, H, F， PhO, F), (M-466, H, H, F, PhO, CFs), (M-467, H, H, F, PhO, Br), (M-468, H， H, F, PhO, CHs), (M-469, H， H, F, BnO, H), (M-470, H, H, F, BnO, CI), (M-471, H, H, F, BnO, F), (M-472, H, H, F, BnO, CF3), (M- 473, H, H, F， BnO, Br), (M-474, H， H, F, BnO, CHs), (M-475, H, H, F,
PhCH2CH20; H), (M-476, H, H, F, PhCH2CH20, CI), (M-477, H, H, F,
PhCH2CH20, F), (M-478, H， H, F， PI1CH2CH2O, CF3), (M-479, H, H， F，
PhCHaCmO, Br), (M.48.0, H, H, F, PliCH2CH20， CH3), (M-481, H, H, F, CF3O, H), (M-482, H, H, F, CFsO, CI), (M-483, H, H, F, CFsO, F), (M-484, H, H, P, CFsO, CFs), (M-485, H, H, F, CFsO, Br), (M-486, H, H, F, CFsO, CHs), (M-487, H, H, F， Ph, H), (M-488, H， H, F, Ph, CI), (M-489, H, H， F, Ph, F), (M-490, H, H, F, Ph, CFs), (M-491, H, H, F, Ph, Br), (M-492, H, H, F, Ph, CH3), (M-493, H, H, F, 4-F-Ph, H), (M-494, H， H, F, 4-F-Ph, CI), (M-495, H, H, F, 4-F-Ph, F)， (M-496, H, H， F， 4-F-Ph, CFs), (M-497, H, H, F, 4-F-Ph, Br), (M-498, H, H, F, 4-F-Ph, CHs), (M-499, H, H, F, 4-CF3-Ph, H)， (M-500, H, H, F， 4-CFs-Ph, CI), (M-501, H， H, F, 4-CFs-Ph, F), (M-502, H， H, F, 4-CF3-Ph, CFa), (M-503, H, H, F, 4-CF3-Ph, Br), (M-504, H, H, F, 4-CFs-Ph, CHs), (M-505, H, H, F, 4-(Me)2N-Pli, H), (M-506, H, H, F, 4-(Me)2N-Ph, CI), (M-507, H, H, F, 4-(Me)2N-Ph, F), (M-508, H, H, F, 4-(Me)2N-Ph) CF3), (M-509, H, H， F, 4-(Me)2N-Ph; Br), (M-510, H, H, F, 4- (Me)2N-Ph， CHs), (M-5H, H, H, F, 4-OH-Ph, H), (M-512, H, H, F, 4-OH-Ph, CI), (M-513, H， H, F, 4-OH-Ph, F), (M-514, H, H， F, 4-OH-Ph, CFs), (M-515, H, H, F， 4-OH-Ph, Br), (M-516, H, H, F, 4-OH-Ph, CH3), (M-517, H, H, F， 3,4-di-F-Ph, H)， (M-518, H， H, F, 3,4-di-F-Ph, CI), (M-519, H, H, F, 3,4-di-F-Ph, F), (M-520, H, H, F， 3,4-di-F-Ph, CFs), (M-521, H, H, F, 3,4-di-F-Ph, Br), (M-522, H, H, F， 3,4- di-F-Ph, CHa), (M-523, H, H， F, 4-COOH-Ph, H), (M-524, H, H, F, 4-COOH-Ph, CI), (M-525, H, H, F, 4-COOH-Ph, F), (M-526, H， H, F， 4-COOH-Ph, CF3), (M- 527, H, H, F, 4-COOH-Ph, Br), (M-528, H, H, F, 4-COOH-Ph, CH3)， (M-529, H, H， F, Bn, H), (M-530, H, H, F, Bn, CI), (M-531, H, H， F, Bn, F), (M-532, H, H, F, Bn, CFs), (M-533, H, H, P, Bn, Br), (M-534, H, H, F, Bn, CH3), (M-535, H, H, F, 4-F-Bn, H)， (M-536, H, H, F, 4-F-Bn, CI), (M-537, H， H， F, 4-F-Bn, F), (M-538, H, H, F， 4-F-Bn, CF3), (M-539, H, H, F, 4-F-Bn, Br), (M-540, H， H, F, 4-F-Bn, CHs), (M-541, H, H, F, 2-Py, H), (M-542, H, H, F, 2-Py, CI), (M-543, H, H, F, 2-Py, F), (M-544, H， H， F, 2-Py, CFs), (M-545, H, H, F, 2-Py, Br), (M-546, H, H, F, 2-Py, CHs), (M-547, H, H, F, 3-Py, H), (M-548,. H, H, P, 3-Py, CI), (M-549, H, H, F, 3-Py, E), (M-550, H, H, F, 3-Py, CPs), (M-551, H, H, F, 3-Py, Br), (M-552, H, H， F, 3-Py, CHs), (M-553, H, H, F, 4-Py, H), (M-554, H, H, F, 4-Py, CI), (M-555, H, H, F, 4-Py, F), (M-556, H, H, F, 4-Py, CFs), (M-557, H, H, F, 4-Py, Br), (M-558, H, H， F, 4-Py, CHs), (M-559, H, H, F, 2-Th, H), (M-560, H, H, F, 2- Th, CI), (M-561, H, H, F， 2-Th, F), (M-562, H, H, F, 2-Th, CF3), (M-563, H， H, F, 2-Th, Br), (M-564, H， H， F, 2-Th, CHs), (M-565, H, H, F, 3-Th, H), (M-566, H, H， F， 3-Th, CI), (M-567, H, H， F, 3-Th, F), (M-568, H, H, F, 3-Th, CF3), (M-569, H, H, F， 3-Th, Br), (M-570, H, H， F, 3-Th, CHs), (M-571, H, H, F, pyrazol-2-yl, H), (M-572, H， H, F, pyrazol-2-yl, CI), (M-573, H, H, F, pyrazol-2-yl, F), (M-574, H, H, F, pyrazol-2-yl, CFs), (M-575, H， H, F, pyrazol-2-yl, Br), (M-576, H, H， F, pyrazol-2-yl, CHs), (M-577, H, H, F, pyrazol-3-yl, H), (M-578, H, H, F, pyrazol-3-yl, CI), (M-579, H' H， F, pyrazol-3-yl, F), (M-580, H, H, F, pyrazol-
3- yl, CF3), (M-581, H， H, F, pyrazol-3-yl, Br), (M-582, H， H, F, pyrazol-3-yl, CHs), (M-583, H, H, F, pyrimidin-2-yl, H), (M-584, H, H, F, pyrimidin-2-yl, CI),
(M-585, H, H, F, pyrimidin-2-yl, F), (M-586, H, H, F, pyrimidin-2-yl; CF3); (M-587, H, H, F, pyrimidin-2-yl, Br), (M-588, H, H, F, pyrimidin-2-yl, CHs), (M-589, H, H, F, pyrimidin-4-yl; H), (M-590, H, H, F, pyrimidin-4-yl, CI), (M- 591, H, H, F, pyrimidin-4-yl, F)， (M-592, H, H, F, pyrimidm-4-yl, CFs), (M-593, H, H, F, pyrimidin-4-yl, Br), (M-594, H, H, F, pyrimidin-4-yl, CHs), (M-595, H, H, F, pyrimidin-5-yl, H), (M-596, H, H， F, pyrimidin-5-yl, CI), (M-597, H, H, F, pyrimidin-5-yl, F); (M-598, H, H, F, pyrimidin-5-yl, CF3), (M-599, H, H, F， pyrimidin-5-yl, Br), (M-600, H, H, F, pyrimidin-5-yl, CHs), (M-601, H, H, F, HOOCCH2CH2CH2, H), (M-602, H, H, F, HOOCCH2CH2CH2, CI), (M-603, H， H, F, HOOCCHaCHsCHa, F), (M-604, H, H, F, HOOCCE CH2CH2, CFs), (M-605, H, H, F， HOOCCH2CH2CH2; Br), (M-606, H, H, F, HOOCCH2CH2CH2, CHs), (M- 607, H, H, F, HOO.C CH2CH2CH2CH2, H), (M-608, H， H, F, ,„一
HOOCCH2CH2CH2CH2; CI), (M-609, H; H, F, HOOCCHsCHaCHaCHa, F), (M- 610, H' H, F, HOOCCH2CH2CH2CH2, CFs), (M-611, H, H, F,
HOOCCH2CH2CH2CH2, Br), (M-612, H, H, F, HOOCCH2CH2CH2CH2, CHs), (M-613, H， H, F, (Me)2NCOCH2CH2CH2CH2, H), (M-614, H， H, F, (Me)2NCOCH2CH2CH2CH2, CI), (M-615, H, H, F, (Me)2NCOCH2CH2CH2CH2, F), (M-616, H, H, F, (Me)2NCOCH2CH2CH2CH2, CF3)， (M-617, H, H, F,
(Me)2NCOCH2CH2CH2CH2, Br), (M-618, H, H, F, (Me)2NCOCH2CH2CH2CH2; CH3), (M-619, H, H, F, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-620, H, H, F, (Me)2NCOCH2CH2CH2CH2CH2' CI), (M-621, H, H, F,
(Me)2NCOCH2CH2CH2CH2CH2! P), (M-622, H, H' F,
(Me)2NCOCH2CH2CH2CH2CH2, CF3), (M-623, H, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-624, H, H， F,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-625, H， H, F, MeOCHa, H)， (M-626, H, H, F, MeOCH2, CI), (M-627, H, H, F, MeOCH2; P), (M-628, H, H, F, MeOCH2) CFs), (M-629, H， H, F, MeOCH2, Br), (M-630, H, H, F， MeOCHs, CHs), (M-631, H, H, F, EtOCHz, H), (M-632, H, H, F, EtOCH2) CI), (M-633, H, H, F, EtOCH2, F), (M-634, H, H, F, EtOCH2, CFs), (M-635, H, H, F, EtOCHa, Br), (M-636, H, H, F, EtOCHa, CHs), (M-637, H, H, F, EtOCHaCHa, H)， (M-638, H, H, F,
EtOCHsCHa, CI), (M-639, H, H, F, EtOCH2CH2) F)， (M-640, H, H, F，
EtOCH2CH2, CFs), (M-641, H, H, F, EtOCH2CH2, Br), (M-642, H, H, F, - EtOCH2CH2; CH3), (M-643, H, H, F, MeOCH2CH2OCH2CH2， H), (M-644, H, H, F, MeOCH2CH2OCH2CH2, CI), (M-645, H, H, F, MeOCH2CH2OCH2CH2) F), (M-646, H, H, F, MeOCHsCH OCHsCHs, CFs), (M-647, H, H, F,
MeOCH2CH2OCH2CH2, Br), (M-648, H' H, F, MeOCH2CH2OCH2CH2, CHs),
(M-649, H, H, F, MeOCH2CH2, H), (M-650, H, H, F, MeOCHaCHa, CI), (M-651, H, H, F, MeOCH2CH2, F), (M-652, H, H, F, MeOCH2CH2, CFs), (M-653, H, H' F, MeOCH2CH2， Br), (M-654, H, H， F, MeOCH2CH2) CHs), (M-655, H, H, F, HOCHa, H), (M-656, H, H, F, HOCH2, CI), (M-657, H, H, F, HOCH2, F), (M-658, H, H, F, HOCH2, CFs), (M-659, H, H, F, HOCH2, Br), (M-660, H, H, F, HOCH2, CHs), (M-661, H, H, F, HOCH2CH2, H), (M-662, H, H, F' HOCH2CH2; CI), (M- t
o
Figure imgf000098_0001
,),,,,,,,),,,, H22 663 H HO2 664OCHC2 C3 665 H FCHCH H H F HHF H F H， CI, H, Br), (M-714, H, H, CI, H, CHs), (M-715, H, H, CI, F, H), (M-716, H, H, CI, F, CI), (M-717, H, H, CI, F， F)，（M-718, H, H, CI, F, CFs), (M-719, H， H, CI, F, Br), (M-720, H, H, CI, F, CH3)， (M-721, H, H, CI, CI, H), (M-722, H, H, CI, CI, CI), (M-723, H, H, CI, CI, F), (M-724, H， H, CI, CI, CF3), (M-725, H， H， CI, CI, Br), (M-726, H, H, CI, CI, CHs), (M-727, H, H， CI, CHs, H), (M-728, H, H, CI, CH3; CI), (M-729, H, H, CI, CH3, F), (M-730, H, H, CI, CHs, CFs), (M-731, H, H, CI, CH3, Br), (M-732, H， H, CI, CH3, CHs), (M-733, H' H, CI, Et, H), (M-734, H, H, CI, Et, CI), (M-735, H, H, CI, Et, F)， (M-736, H, H, CI, Et, CFs), (M-737, H， H, CI, Et, Br), (M-738, H， H, CI, Et, CHs), (M-739, H, H, CI, n-Pr, H), (M-740, H, H， CI, n-Pr, CI), (M-741, H, H, CI, n-Pr, F), (M-742, H, H, CI, n-Pr, CFs), (M-743, H, H, CI, n-Pr, Br), (M-744, H, H, CI, n-Pr, CHs), (M-745, H, H， CI, c-Pr, H), (M- 746, H, H, CI, c-Pr, CI), (M-747, H, H, CI, c-Pr, F), (M-748, H, H, CI, c-Pr, CFs), (M-749, H, H， CI, c-Pr, Br), (M-750, H, H, CI, c-Pr, CHs), (M-751, H， H, CI, i- Pr, H), (M-752, H, H, CI, i-Pr, CI), (M-753, H, H, CI, i-Pr, P), (M-754, H, H, CI, i-Pr, CF3), (M-755, H, H' CI, i-Pr, Br), (M-756, H, H, CI, i-Pr, CHs), (M-757, H, H, CI, n-Bu, H)， (M-758, H, H， Cl， n-Bu, CI), (M-759, H, H， CI, n-Bu, F), (M-760, H, H， CI, n-Bu, CF3), (M-761, H, H， CI; n-Bu, Br), (M-762, H, H， CI, n-Bu, CHs), (M-763, H, H, CI, i-Bu, H), (M-764, H, H， CI, i-Bu, CI), (M-765, H, H， CI, i-Bu, F), (M-766, H， H, CI, i-Bu, CF3), (M-767, H, H, CI, i-Bu, Br), (M-768, H, H， CI, i-Bn, CHs), (M-769, H, H, CI, sec-Bu, H), (M-770, H, H, CI, sec-Bu, CI), (M-771, H, H, CI, sec-Bu, F), (M-772, H， H, CI, sec-Bu, CPs), (M-773, H, H, CI, sec-Bu, Br), (M-774, H, H, CI, sec-Bu, CHs), (M-775, H, H, CI, n-Pen, H), (M-776, H, H, CI, n-Pen, CI), (M-777, H, H, CI, n-Pen, F), (M-778, H, H, CI, n-Pen, CFs), (M- 779, H, H, CI, n-Pen, Br), (M-780, H, H, CI, n-Pen, CHs), (M-781, H, H, CI, c- Pen, H)， (M-782, H, H, CI, c-Pen, CI), (M-783, H, H, CI, c-Pen, F), (M-784, H, H, CI, c-Pen, CFs), (M-785, H, H, CI, c-Pen; Br), (M-786, H, H, CI, c-Pen, CH3), (M-787, H, H, CI, n-Hex, H), (M-788, H, H, CI, n-Hex, CI), (M-789, H, H, CI, n-Hex, F), (M-790, H, H, CI, n-Hex, CFs), (M-791, H, H' CI, n-Hex, Br), (M-792, H, H, CI, n-Hex, CHs), (M-793, H, H, CI, c-Hex, H)， (M-794, H, H, CI, c-Hex, CI), (M-795, H, H, CI, c-Hex, F), (M-796, H, H, CI, c-Hex, CF3), (M-797, H, H, CI, c-Hex, Br), (M-798, H, H, CI, c-Hex, CHs), (M-799, H, H, CI, OH, H)， (M-800, H， H, CI, OH, CI), (M-801, H, H, CI, OH, F), (M-802, H, H, CI, OH, CFs), (M-803, H, H, CI, OH, Br), (M-804, H, H, CI, OH, CH3)， (M-805, H, H, CI, EtO, H)， (M-806, H, H, CI, EtO, CI), (M-807, H, H, CI, EtO, F), (M-808, H, H, CI, EtO, CFs), (M-809, H， H， CI, EtO, Br), (M-810, H, H, CI, EtO, CHs), (M-811, H, H, CI, n- PrO, H)， (M-812, H, H, CI, n-PrO, CI), (M-813, H， H， CI, n-PrO, F)， (M-814, H, H, CI, n-PrO, CFs), (M-815, H, H, CI, n-PrO, Br), (M-816, H, H, CI, n-PrO, CH3), (M-817, H' H, CI, PhO, H)' (M-818, H, H， CI, PhO, CI), (M-819, H, H, CI, PhO, F), (M-820, H, H, CI, PhO, CFs), (M-821, H, H, CI, PhO, Br), (M-822, H, H, CI, PhO, CHs), (M-823, H, H, CI, BnO, H), (M-824, H, H, CI, BnO, CI), (M-825, H, H, CI, BnO, F), (M-826, H, H, CI, BnO, CFa), (M-827, H, H, CI, BnO, Br), (M-828, H, H, CI, BnO, CHs), (M-829, H, H, CI, PI1CH2CH2O, H), (M-830, H, H, CI, PhCffiCHzO, CI), (M-831, H， H, CI, PhCH2CH20; F), (Μ-832,Ή, H, CI,
PhCHaCHsO, CF3); (M-833, H， H, CI, PhCH2CH20; Br), (M-834, H, H, CI, PhCH2CH20, CHs), (M-835, H, H， CI, CFsO, H), (M-836, H, H, CI, CF30， CI), (M-837, H, H， CI, CFsO, F), (M-838, H, H, CI, CF30, CF3), (M-839, H, H, CI, CFsO, Br), (M-840, H, H, CI, CP30; CHs), (M-841, H, H, CI, Ph, H), (M-842, H, H, Cl;,.Ph; CI), (M-843, H, H, CI, Ph, F), (M-844, H, H, CI, Ph., CFs), (M-845, H, H, CI, Ph, Br), (M-846, H， H, CI, Ph, CHs), (M-847, H, H， CI, 4-F-Ph, H), (M-848, H, H, CI, 4-F-Ph, CI), (M-849, H, H, CI, 4-F-Ph, F), (M-850, H, H, CI, 4-F-Ph, CFs), (M-851, H, H, CI, 4-F-Ph, Br), (M-852, H, H, CI, 4-F-Ph, CHs), (M-853, H, H, CI, 4-CF3-Ph, H), (M-854, H, H, CI, 4-CF3-Pli; Cl)， (M-855, H, H, CI, 4-CFs- Ph, F), (M-856, H, H, CI, 4-CF3-Ph, CF3), (M-857, H， H, CI, 4-CFs-Ph, Br), (M-858, H, H, CI, 4-CFa-Pli, CH3), (M-859, H, H, CI, 4-(Me)2N-Ph, H), (M-860, H, H, CI, 4-(Me)2N-Ph, CI), (M-861, H， H, CI, 4-(Me)2N-Ph, P), (M-862, H, H, CI, 4-(Me)2N-Ph, CFs), (M-863, H, H; CI, 4-(Me)2N-Pli, Br), (M-864, H, H, CI, 4- (Me)2N-Ph， CH3)， (M-865, H, H, CI, 4-OH-Ph, H), (M-866, H， H, CI, 4-OH-Ph, CI), (M-867, H, H, CI, 4-OH-Ph, F), (M-868, H, H, CI, 4-OH-Ph, CFs), (M-869, H, H' CI, 4-OH-Ph, Br), (M-870, H, H, CI, 4-OH-Ph, CH3), (M-871, H, H, CI, 3,4- di-F-Ph, H), (M-872, H， H, CI, 3,4-di-F-Ph, CI), (M-873, H, H, Cl， 3,4-di-F-Ph; F), (M-874, H, H, CI, 3,4-di-F-Ph, CFs), (M-875, H, H, CI, 3,4-di-F-Ph, Br), (M-876, H， H, CI, 3,4-di-F-Ph, CHs), (M-877, H， H, CI, 4-COOH-Ph, H), (M-878, H, H, CI, 4-COOH-Ph, CI), (M-879, H, H, CI, 4-COOH-Ph, F), (M-880, H, H， CI, 4-COOH-Ph, CPs), (M-881, H, H, CI, 4-COOH-Ph, Br), (M-882, H, H, CI, 4- COOH-Ph, CHs), (M-883, H, H, CI, Bn, H), (M-884, H, H, CI, Bn, CI), (M-885, H, H, CI, Bn, P), (M-886, H' H, CI, Bn, CFs), (M-887, H, H, CI, Bn, Br), (M-888, H, H, CI, Bn, CHs), (M-889, H, H, CI, 4-F-Bn, H), (M-890, H, H, CI, 4-F-Bn, CI), (M-891, H, H, CI, 4-F-Bn, F), (M-892, H, H, CI, 4-F-Bn, CFs), (M-893, H, H, CI, 4-F-Bn, Br), (M-894, H， H, CI, 4-F-Bn, CH3), (M-895, H, H, CI, 2-Py, H), (M-896, H, H, CI, 2-Py, CI), (M-897, H, H， CI, 2-Py, F), (M-898, H, H, CI, 2-Py, CF3), (M-899, H, H， CI, 2-Py, Br), (M-900, H, H, CI, 2-Py, CH3), (M-901, H, H, CI, 3-Py, H), (M-9.02, H, H, CI, 3-Py, Gl), (M-903, H, H， CI, 3-Py, F), (M-904, H, H, CI, 3-Py, CFs), (M-905, H, H， CI, 3-Py, Br), (M-906, H, H, CI, 3-Py, CH3), (M-907, H, H, CI, 4-Py, H), (M-908, H, H, CI, 4-Py, CI), (M-909, H, H, CI, 4-Py, F), (M-910, H, H, CI, 4-Py, CF3), (M-911, H, H, CI, 4-Py, Br), (M-912, H, H, CI, 4-Py, CH3)， (M-913, H, H, CI, 2-Th, H), (M-914, H, H, CI, 2-Th, CI), (M-915, H, H, CI, 2-Th, F), (M-916, H, H, Cl; 2-Th, CFs), (M-917, H, H, CI, 2-Th, Br), (M-918, H, H, CI, 2-Th, CHa), (M-919, H, H, CI, 3-Th, H), (M-920, H, H, CI, 3-Th, CI), (M-921, H， H, CI, 3-Th, F), (M-922, H, H, CI, 3-Th, CFs), (M-923, H, H, CI, 3-Th, Br), (M- 924, H, H, CI, 3-Th, CHs), (M-925, H, H, CI, pyrazol-2-yl, H), (M-926, H, H, CI, pyrazol-2-yl, CI), (M-927, H， H, CI, pyrazol-2-yl, F)， (M-928, H, H, CI, pyrazoレ 2-yl' CPs), (M-929, H, H' CI, pyrazoレ 2-yl, Br), (M-930, H, H, CI, pyrazol-2-yl, CHs), (M-931, H, H, CI, pyrazol-3-yl, H), (M-932, H, H, CI, pyrazol-3-yl, CI), (M-933, H, H, CI, pyrazol-3-yl, F), (M-934, H' H， CI, pyrazol-3-yl, CFs), (M-935, H， H, CI, pyrazol-3-yl, Br), (M-936, H, H, CI, pyrazol-3-yl, CHs), (M-937, H, H, CI, pyrimidin-2-yl, H), (M-938, H' H, CI, pyrimidin-2-yl, CI), (M-939, H, H， CI, pyrimidin-2-yl, F), (M-940, H, H, CI, pyrimidin-2-yl; CFs), (M-941, H' H, CI, pyrimidin-2-yl, Br), (M-942, H, H, CI, pyrimidin-2-yl, CHs), (M-943, H, H, CI, pyrimidin-4-yl, H), (M-944, H, H， CI, pyrimidin-4-yl, CI), (M-945, H, H, CI, pyrimidin-4-yl, F), (M-946, H, H, CI, pyrimidin-4-yl, CF3), (M-947, H, H, CI, pyrimidin-4-yl, Br), (M-948, H, H, CI, pyrimidin-4-yl, CHs), (M-949, H, H, CI, pyrimidin-5-yl, H), (M-950, H, H, CI, pyrimidin-5-yl, CI), (M-951, H, H, CI, pyrimidin-5-yl, P), (M-952, H， H， CI, pyrimidin-5-yl, CFs), (M-953, H; H, CI, pyrimidin-5-yl, Br), (M-954, H, H， CI, pyrimidin-5-yl; CHs), (M-955, H, H, CI, HOOCCH2CH2CH2) H), (M-956, H, H, CI, HOOCCH2CH2CH2, CI), (M-957, H, H, CI, ΗΟΟΟΟΗ2ΟΗ2ΟΗ2) F), (M-958, H, H, CI, HOOCCH2CH2CH2; CF3), (M-959, H， H, CI, HOOCCH2CH2CH2, Br), (M-960, H, H， CI, HOOCCH2CH2CH2, CH3), (M-961, H, H, CI,
HOOCCH2CH2CH2CH2, H)， （M-962, H, H, CI, HOOCCH2CH2CH2CH2, CI), (M- 963, H, I-I, CI, HOOCCH2CH2CH2CH2, F), (M-964, H, H, CI,
HOOCCH2CH2CH2CH2, CFs), (M-965, H, H, CI, HOOCCH2CH2CH2CH2, Br), (M-966, H, H, CI, HOOCCH2CH2CH2CH2， CHs), (M-967, H, H, CI,
(Me)2NCOCH2CH2CH2CH2! H), (M-968, H, H, CI, (Me)2NCOCH2CH2CH2CH2, CI), (M-969, H, H, CI, (Me)2NCOCH2CH2CH2CH2, F), (M-970, H, H' CI, (Me)2NCOCH2CH2CH2CH2) CFs), (M-971, H, H, CI, (Me)2NCOCH2CH2CH2CH2, Br), (M-972, H, H, CI, (Me)2NCOCH2CH2CH2CH2， CHs), (M-973, H, H, CI, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-974, H, H， CI,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-975, H， H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-976, H, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-977, H, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-978, H, H' CI,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-979, H, H, CI, MeOCH2; H), (M-980, H, H, CI, MeOCH2, CI), (M-981, H, H, CI, MeOCH2) F), (M-982, H, H, CI, MeOCH2, CFs), (M-983, H, H, CI, MeOCHs, Br), (M-984, H, H, CI, MeOCHs, CHs), (M-985, H, H， CI, EtOCH2, H), (M-986, H, H， CI, EtOCH2; CI), (M-987, H, H, CI, EtOCE ' F), (M-988, H, H, CI, EtOCH2) CF3), (M-989, H, H, CI, EtOCH2, Br), (M-990, H， H, CI, EtOCH2) CHs), (M-991, H, H， CI, EtOCH2CH2) H), (M-992, H, H, CI, EtOCH2CH2; CI), (M-993, H, H, CI, EtOCH2CH2, F), (M-994, H, H, CI, EtOCH2CH2, CFs), (M-995, H， H, CI, EtOCH2CH2) Br), (M-996, H, H, CI,
EtOCH2CH2, CH3)， (M-997, H, H, CI, MeOCH2CH2OCH2CH2, H), (M-998, H, H， CI, MeOCHsCHsOCHaCHs, CI), (M-999, H, H, CI, MeOCHaCHsOCHsCHs, F); (M-1000, H, H, CI, MeOCH2CH2OCH2CH2, CFs), (M-1001, H, H, Cl，
MeOCH2CH2OCH2CH2, Br), (M-1002, H, H, CI, MeOCH CHsOCHsCHs, CHs), (M-1003, H, H, CI, MeOCH2CH2, H), (M-1004, H, H, CI, MeOCH2CH2, CI), (M-1005, H, H, CI, MeOCH2CH2, F), (M-1006, H, H, CI, MeOCH2CH2, CPs), (M-1007, H, H, CI, MeOCH2CH2, Br), (M-1008, H, H, CI, MeOCH2CH2, CH3), (M-1009, H, H, CI, HOCH2) H); (M-1010, H, H, CI, HOCH2, CI), (M-1011, H, H, CI, HOCH2, F), (M-1012, H, H, CI, HOCH2, CFs), (M-1013, H, H, CI, HOCH2, Br), (M-1014, H, H, CI, HOCH2; CHs), (M-1015, H, H, CI, HOCH2CH2) H), (M- 1016, H, H, CI, HOCH2CH2; CI), (M-1017, H, H， CI, HOCH2CH2, F), (M-1018, H, H, CI, HOCH2CH2) CF3), (M-1019, H, H, CI, HOCH2CH2) Br), (M-1020, H， H, CI, HOCH2CH2, CH3), (M-1021, H, H, CI, HOCH2CH2CH2, H), (M-1022, H, H, CI, HOCH2CH2CH2, CI), (M-1023, H, H, CI, HOCH2CH2CH2, F), (M-1024, H, H, CI, HOCH2CH2CH2, CF3), (M-1025, H， H, CI, HOCH2CH2CH2; Br), (M-1026, H, H, CI, HOCHaCHzCHs, CHs), (M-1027, H, H, CI, HOCH2CH2CH2CH2, H), (M-1028, H, H, CI, HOCH2CH2CH2CH2; CI), (M-1029, H, H, CI, HOCH2CH2CH2CH2, F)， (M-1030, H， H， CI, IiOCH2CH2CH2CH2， CF3), (M-1031, H, H， CI,
HOCH2CH2CH2CH2, Br), (M-1032, H, H, CI, HOCH2CH2CH2CH2， CHs), (M- 1033, H, H, CI, HOCH2CH2CH2CH2CH2， H), (M-1034, H, H, CI,
HO CHs CH2 CI-I2 CH2 CH2, CI), (M-1035, H, H, CI, HOCH2CH2CH2CH2CH2, F), (M-1036, H, H， CI, HOCH2CH2CH2CH2CH2, CFs), (M-1037, H, H， CI,
HOCH2CH2CH2CH2CH2) Br), (M-1038, H, H, CI, HOCH2CH2CH2CH2CH2, CHs), (M-1039, H, H, CI, HOCHsCHaOCI-hCHs, H), (M-1040, H， H, CI,
HOCH2CH2OCH2CH2, CI), (M-1041, H， H, CI, HOCH2CH2OCH2CH2, F), CM- 1042, H, H， CI, HOCH2CH2OCH2CH2, CPs), (M-1043, H， H, Gl,
HOCH2CH2OCH2CH2, Br), (M-1044, H, H, CI, HOCH2CH2OCH2CH2, CHs), (M-1045, H, H， CI, (Me)2N, H), (M-1046, H, H， CI,— (Me)2N, CI), (M-1047, H, H， CI, (Me)2N, F), (M-1048, H, H, CI, (Me)2N, CFs), (M-1049, H, H, CI, (Me)2N， Br), (M-1050, H， H, CI, (Me)2N, CHs), (M-1051, H, H, CI, piperidin-4-yl-methyl, H), (M-1052, H, H, CI, piperidm-4-yl-metliyl, CI), (M-1053, H， H, Gl, piperidin-4- yl-methyl, F)， (M-1054, H, H, CI, piperidin-4-yレ methyl, CFs), (M-1055, H, H, CI, piperidin-4-yl-methyl, Br), (M-1056, H, H， CL, piperidin-4-yl-methyl, CHs), (M-1057, H, H, CI, cyclohexylmethyl, H), (M-1058, H, H, CI, cyclohexylmethyl, CI), (M-1059, H, H, CI, cyclohexylmethyl, F), (M-1060, H, H' CI,
cyclohexylmethyl, CFs), (M-1061, H, H, CI, cyclohexylmethyl, Br), (M-1062, H, H' CI, cyclohexylmethyl, CH3), (M-1063, H, F, H, H, H), (M-1064, H, F, H, H, CI), (M-1065, H, F， H, H, F)， (M-1066, H, F, H， H， CFs), (M-1067, H, F, H, H, Br), (M-1068, H' F, H, H, CHs), (M-1069, H, F, H, F, H), (M-1070, H, F, H, F, CI), (M-1071, H, F, H, P, F), (M-1072, H, F, H, F, CFs), (M-1073, H， F, H, F, Br), (M-1074, H, F, H, F, CH3), (M-1075, H' F, H, CI, H), (M-1076, H, F, H, CI, CI), (M-1077, H, F, H, CI, F), (M-1078, H, F, H' CI, CF3), (M-1079, H, F, H, CI, Br), (M-1080, H, F, H, CI, CHs), (M-1081, H, F, H, CHs, H), (M-1082, H, F' H, CH3; CI), (M-1083, H， F， H, CH3, F), (M-1084, H, F, H, CHs, CF3), (M-1085, H, F, H, CHs, Br), (M-1086, H, F' H, CHs, CHs), (M-1087, H, F, H, Et, H), (M-1088, H; F, H, Et, CI), (M-1089, H, F, H, Et, F), (M-1090, H, F, H, Et, CFs), (M-1091, H, F, H, Et, Br), (M-1092, H, F, H, Et, CHs), (M-1093, H, F, H, n-Pr, H), (M-1094, H， F, H, n-Pr, CI), (M-1095, H, F, H, n-Pr, F), (M-1096, H, F, H, n-Pr, CFs), (M- 1097, H， F, H, n-Pr, Br), (M-1098, H, F， H, n-Pr, CHs), (M-1099, H, F, H， c-Pr, H), (M-1100, H, F， H, c-Pr, CI), (M-1101, H, F, H, c-Pr, F), (M-1102, H, F, H， c-Pr, CF3), (M-1103, H, F, H, c-Pr, Br), (M-1104, H, F, H, c-Pr, CHs), (M-1105, H, F， H, i-Pr, H), (M-1106, H, F, H, i-Pr, CI), (M-1107, H, P, H, i-Pr, F), (M-1108, H, F, H, i-Pr, CFs), (M-1109, H, F, H, i-Pr, Br), (M-1110, H， P, H, i-Pr, CHs), (M-1111, H， F, H, n-Bu, H), (M-1112, H, F, H, n-Bu, CI), (M-1113, H, F, H, n- Bu, F); (M-1114, H, F, H， n-Bu, CFs), (M-1115, H, F, H, n-Bu, Br), (M-1116, H, F, H, n-Bu, CHs), (M-1117, H, F, H， i-Bu, H), (M-1118, H, F, H, i-Bu, CI), (M- 1119, H, F, H, i-Bu, F), (M-H20, H, F, H, i-Bu, CFs), (M-1121, H, F, H, i-Bu, Br), (M-1122, H， F, H, i-Bu, CHs), (M-1123, H, F, H, sec-Bu, H), (M-1124, H, F， H, sec-Bu, CI), (M-1125, H, F, H, sec-Bu, F), (M-1126, H, F, H, sec-Bu, CPs).,. (M- 1127, H, P, H, sec-Bu, Br), (M-1128, H, F, H, sec-Bu, CHs), (M-1129, H, F, H, n-Pen, H), (M-1130, H, F, H, n-Pen, CI), (M-1131, H, F, H, n-Pen, F), (M-1132, H, F, H, n-Pen, CFs), (M-1133, H, F, H, n-Pen, Br), (M-1134, H, F, H, n-Pen, CHs), (M-1135, H, F, H, c-Pen, H), (M-1136, H, F, H, c-Pen, CI), (M-1137, H, F， H, c-Pen, F), (M-1138, H, F, H, c-Pen, CFs), (M-1139, H, F; H, c-Pen, Br), (M- 1140, H, F, H, c-Pen; CHs), (M-1141, H, F, H, n-Hex, H), (M-1142, H, F, H, n- Hex, CI), (M-1143, H, F， H, n-Hex, P), (M-1144, H, F, H， n-Hex, CPs), (M-1145, H, F, H, n-Hex, Br), (M-1146, H, F, H, n-Hex, CHs), (M-1147, H, F, H, c-Hex, H), (M-1148, H, F, H, c-Hex, CI), (M-1149, H, F, H， c-Hex, F), (M-1150, H, F, H, c-Hex, CFs), (M-1151, H, F, H, c-Hex, Br), (M-1152, H, F, H, c-Hex, CHs), (M- 1153， H， F， H, OH, H)， (M-1154, H， F， H, OH, CI), (M-1155, H, F, H, OH, F)， (M-1156, H， F, H, OH, CFs), (M-1157, H， F, H, OH, Br), (M-1158, H， F, H, OH, CHs), (M-1159, H, F, H, EtO, H), (M-1160, H, F, H, EtO, CI), (M-1161, H， F, H, EtO, F)， (M-1162, H, F, H, EtO, CF3), (M-1163, H, F, H， EtO, Br), (M-1164, H, P, H, EtO, CHs), (M-1165, H, F, H, n-PrO, H), (M-1166, H, F, H, n-PrO, CI), (M-1167, H, F, H, n-PrO, F), (M-1168, H, F, H, n-PrO, CFs), (M-1169, H， F, H, n-PrO, Br), (M-1170, H, F, H, n-PrO, CHs), (M-1171, H, F, H, PhO, H), (M-1172, H， F, H, PhO, CI), (M-1173, H, F, H, PhO, F)， (M-1174, H, F, H, PhO, CFs), (M-1175, H， F, H, PhO, Br), (M-1176, H, F, H， PhO, CH3), (M-1177, H, F, H， BnO, H), (M-1178, H, F, H, BnO, CI), (M-1179, H, F, H, BnO, F), (M-1180, H, F, H, BnO, CF3), (M-1181, H, F, H, BnO, Br), (M-1182, H, F， H, BnO, CH3), (M- 1183, H, F, H, PhCH2CH20, H), (M-1184, H, F, H, PhCH2CH20, CI), (M-1185, H, F, H, PhCH2CH20, F), (M-1186, H, F; H, PhCH2CH20, CFs), (M-1187, H, F, H, PhCHaCHaO, Br), (M-1188, H， F, H, PI1CH2CH2O, CHs), (M-1189, H, F, H, CPsO, H), (M-1190, H, F, H， CF3O' CI), (M-1191, H， F, H, CFsO, F), (M-1192, H， F, H， CFsO, CFs), (M-1193, H, F， H, CFsO, Br), (M-1194, H, F， H' CFsO, CH3), (M- 1195, H, F, H， Ph, H), (M-1196, H, F, H, Ph, CI), (M-1197, H， F, H, Ph, F), (M-1198, H, F, H, Ph, CFs), (M-1199, H, F, H, Ph, Br), (M-1200, H, F, H, Ph, CHs), (M-1201, H, F, H, 4-F-Ph, H), (M-1202, H, F, H, 4-F-Ph, CI), (M-1203, H, F, H, 4-F-Ph, F)， (M-1204, H, P; H, 4-F-Ph, CPs), (M-1205, H, F, H， 4-F-Ph, Br), (M-1206, H, F, H， 4-F-Ph, CHs), (M-1207, H, F, H， 4-CFs-Pli, H)， (M-1208, H, F, H, 4-CFs-Pli, CI), (M-1209, H, F, H, 4-CFs-Pli, F); (M-1210, H, F, H, 4-CFs-Pli, CFs), (M-1211, H， F， H, 4-CF3-Pli; Br), (M-1212, H, F, H, 4-CFs-Ph, CH3), (M- 1213, H, F, H, 4-(Me)2N-Pli) H), (M-1214, H， F, H, 4-(Me)2N-Ph, CI), (M-1215, H, F, H, 4-(Me)2N-Ph, F), (M-1216, H, F, H, 4-(Me)2N-Ph, CF3), (M-1217, H， F, H, 4-(Me)2N-Ph, Br), (M-1218, H, F, H, 4-(Me)2N-P , CHs), (M-1219, H, F; H, 4- OH-Ph, H), (M-1220, H， F, H， 4-OH-Ph, CI), (M-1221, H, F, H， 4-OH-Ph, F), (M-1222, H, F, H， 4-OH-Ph, CF8), (M-1223, H, F, H, 4-OH-Ph, Br), (M-1224, H, F, H, 4-OH-Ph, CHs), (M-1225, H， F， H, 3,4-di-F-Ph, H)， (M-1226, H, P, H, 3,4-di-F-Ph; CI), (M-1227, H, F, H, 3,4-di-F-Ph, F), (M-1228, H, F, H, 3,4-di- F-Ph, CFs), (M-1229, H, F, H, 3,4-di-F-Ph, Br), (M-1230, H, F， H， 3,4-di-F-Pli, CHs), (M-1231, H, F, H; 4-COOH-Pli, H)， (M-1232, H, F' H, 4-COOH-Ph, CI), (M-1233, H, F, H, 4-COOH-Pli, F), (M-1234, H， F, H, 4-COOH-Ph, CFs), (M- 1235， H, F, H, 4-COOH-Ph, Br), (M-1236, H, P, H, 4-COOH-Pli, CHs), (M-1237, H， F, H, Bn, H), (M-1238, H, F， H, Bn, CI), (M-1239, H, F, H, Bn, F)， (M-1240, H, F, H, Bn, CF3), (M-1241, H, F, H, Bn, Br), (M-1242, H, F, H, Bn, CHs), (M- 1243, H, F; H, 4-F-Bn, H)， (M-1244, H, F， H， 4-F-Bn, CI), (M-1245 H, F, H, 4- F-Bn, F), (M-1246, H, F, H, 4-F-Bn, CFs), (M-1247, H, F, H， 4-F-Bn, Br), (M- 1248, H, F, H， 4-F-Bn, CHs), (M-1249, H, F, H, 2-Py, H), (M-1250, H, F, H, 2- Py, CI), (M-1251, H, F, H， 2-Py, F), (M-1252, H, F, H， 2-Py, CFs), (M-1253, H, F, H, 2-Py, Br), (M-1254, H, F， H, 2-Py, CHs), (M-1255, H, F, H, 3-Py, H), (M-1256, H, F, H 3-Ey, CI), (M-1257, H, F, H, 3-Py, F), (M-1258, H, P, H,,3-Py, CFs), (M-1259, H, E, H, 3-Py, Br), (M-1260, H, F, H, 3-Py, CHs), (M-1261' H， F, H, 4-Py, H), (M-1262, H, F, H， 4-Py, CI), (M-1263, H, F, H, 4-Py, F), (M-1264, H， F, H， 4-Py, CFs), (M-1265, H, F， H, 4-Py, Br), (M-1266, H, F, H, 4-Py, CH3), (M- 1267, H, F, H, 2-Th, H), (M-1268, H, F, H, 2-Th, CI), (M-1269, H, F, H, 2-Th, F), (M-1270, H, F, H, 2-Th, CFs), (M-1271, H, F, H, 2-Th, Br), (M-1272, H, F, H, 2-Th, CH3), (M-1273, H, F， H, 3-Th, H), (M-1274, H， F, H, 3-Th, CI), (M-1275, H, F, H, 3-Th, F), (M-1276, H, F' H， 3-Th, CFs), (M-1277, H, F， H, 3-Th, Br), (M- 1278, H, F， H, 3-Th, CHs), (M-1279, H, F, H, pyrazol-2-yl, H), (M-1280, H, F, H, pyrazol-2-yl, CI), (M-1281, H, F, H, pyrazol-2-yl, F), (M-1282, H, F, H, pyrazol-2-yl, CF3), (M-1283, H, F, H, pyrazol-2-yl, Br), (M-1284, H, F, H, pyrazol-2-yl; CHs), (M-1285, H, F, H, pyrazol-3-yl, H), (M-1286, H, F, H, pyrazol-3-yl, CI), (M-1287, H, F, H, pyrazol-3-yl, F)， (M-1288, H, F, H, pyrazol-3-yl, CFs), (M-1289, H, F, H, pyrazol-3-yl, Br), (M-1290, H, F, H， pyrazol-3-yl, CH3), (M-1291, H， F, H, pyrimidin-2-yl, H), (M-1292, H， F, H, pyrimidin-2-yl, CI), (M-1293, H， F' H, pyrimidin-2-yl, F), (M-1294, H, F, H， pyrimidin-2-yl, CFs), (M-1295, H, F; H, pyrimidin-2-yl, Br), (M-1296, H, F, H， pyrimidin-2-yl; CHs), (M-1297, H， F, H, pyrimidin-4-yl, H), (M-1298, H， F, H, pyrimidin-4-yl, CI), (M-1299, H, F, H, pyrimidin-4-yl, F), (M-1300, H, F, H, pyrimidin-4-yl, CFs), (M-1301, H, F， H, pyrimidin-4-yl, Br), (M-1302, H, F, H, pyrimidin-4-yl, CHs), (M-1303, H, P, H, pyrimidin-5-yl, H)， (M-1304, H, F, H， pyrimidin-5-yl, CI), (M-1305, H, F, H, pyrimidin-5-yl, F); (M-1306, H, F, H, pyrimidin-5-yl, CF3), (M-1307, H, F, H' pyrimidin-5-yl, Br), (M-1308, H, F, H, pyrimidin-5-yl, CHs), (M-1309, H, F, H, HOOCCH2CH2CH2) H), (M-1310, H, F, H, HOOCCH2CH2CH2, CI), (M-1311, H, F, H, HOOCCH2CH2CH2, F), (M-1312, H, F, H, HOOCCH2CH2CH2; CPs), (M-1313, H' F, H, HOOCCH2CH2CH2) Br), (M-1314, H, F, H, HOOCCH2CH2CH2, CHs), (M-1315, H, F, H,
HOOCCH2CH2CH2CH2, H), (M-1316, H, F, H' HOOCCH2CH2CH2CH2, CI), (M- 1317, H, F, H, HO〇CCH2CH2CH2C F), (M-1318, H, F, H,
HOOCCHsCH^CHaCHs, CFs), (M-1319, H, F, H, HOOCCH2CH2CH2CH2, Br), (M-1320, H, F, H, HOOCCH2CH2CH2CH2, CH3), (M-1321, H, F, H, (Me)2NCOCH2CH2CH2CH2， H), (M-1322, H, F, H, (Me)2NCOCH2CH2CH2CH2, CI), (M-1323, H, F, H, (Me)2NCOCH2CH2CH2CH2, F), (M-1324, H, F, H, (Me)2NCOCH2CH2CH2CH2, CFs), (M-1325, H, F, H, (Me)2NCOCH2CH2CH2CH2, Br), (M-1326, H, F, H, (Me)2NCOCH2CH2CH2CH2, CHs), (M-1327, H, F, H, (Me)2NCOCH2CH2CH2CH2CH2， H), (M-1328, H, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-1329, H, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, F)， (M-1330, H' F, H,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-1331, H, F, H，
(Me)2NCOCH2CH2CH2CH2CH2) Br), (M-1332, H, F, H,
(Me)2NCOCH2CH2CH2CH2CH2， CH3), (M-1333, H， P, H， MeOCHs, H), (M-1334, H, F, H, MeOCH2, CI), (M-1335, H, F, H, MeOCH2, F), (M-1336, H, F, H, MeOCH2) CFs), (M-1337, H, F, H， MeOCH2, Br), (M-1338, H, F, H, MeOCHa, CHs), (M-1339, H, F, H, EtOCH2, H), (M-1340, H, F， H, EtOCB , CI), (M-1341, H, F, H, EtOCH2) F), (M-1342, H, F, H, EtOCH2) CFs), (M-1343, H, F, H, EtOCHa, Br), (M-1344, H, F, H, EtOCH2) CHa), (M-1345, H, F, H, EtOCH2CH2, H), (M-1346, H, F, H, EtOCH2CH2, CI), (M-1347, H, F, H, EtOCH2CH2, F), (M-1348, H, F, H' EtOCH2CH2, CFs), (M-1349, H, F, H, EtOCH2CH2, Br), (M- 1350, H, F, H, EtOCH2CH2, CHs), (M-1351, H, F; H, MeOCHsCHsOCHsCB , H), (M-1352, H, F， H, MeOCH2CH2OCH2CH2, CI), (M-1353, H, F, H,
MeOCH2CH20CH2CH2, F), (M-1354, H' F, H, MeOCE CHsOCHsCB , CFs), (M-1355, H， F, H, MeOCH2CH2OCH2CH2, Br), (M-1356, H, F, H,
MeO.CH2CH20CH2CH2, CHa), (M-1357, H' F, H, MeOCH2CH2, H), (M-1358, H, F， H, MeOCH2CH2) CI), (M-1359, H, F, H, MeOCH2CH2, F)， (M-1360, H, F, H， MeOCH2CH2, CFs), (M-1361, H， Έ, H, MeOCH2CH2, Br), (M-1362, H, P, H, MeOCHsCHa, CHs), (M-1363, H, F, H, HOCH2, H), (M-1364, H, F, H, HOCH2, CI), (M-1365, H， F， H, HOCH2, F), (M-1366, H， F, H, HOCH2, CFs), (M-1367, H, F, H, HOCHs, Br), (M-1368, H, F, H, HOCH2' CHs), (M-1369, H, F, H,
HOCH2CH2, H), (M-1370, H, F, H， HOCH2CH2, CI), (M- 1371, H, F, H,
HOCH2CH2' F), (M- 1372, H, F, H, HOCH2CH2, CFs), (M-1373, H, F, H,
HOCH2CH2, Br), (M-1374, H, F， H, HOCH2CH2> CHs), (M- 1375, H, F, H, HOCH2CH2CH2> H), (M-1376, H， F, H， HOCHaCHaCHa, CI), (M-1377, H, F, H, HOCH2CH2CH2, F), (M-1378, H, F, H, HOCH2CH2CH2) CFs), (M-1379, H, F， H, HOCH2CH2CH2, Br), (M- 1380, H, F, H, HOCH2CH2CH2， CHs), (M-1381, H, F, H, HOCH2CH2CH2CH2, H)， (M-1382, H, F, H, HOCH2CH2CH2CH2, CI), (M-1383, H' F, H， HOCH2CH2CH2CH2, F), (M-1384, H, F, H, HOCH2CH2CH2CH2, CFs), (M- 1385, H， F, H, HOCH2CH2CH2CH2, Br), (M-1386, H, F, H,
HOCH2CH2CH2CH2, CHs), (M-1387, H, F, H, HOCH2CH2CH2CH2CH2, H), (M- 1388, H， F, H, HOCH2CH2CH2CH2CH2, CI), (M- 1389, H, F; H,
HOCH2CH2CH2CH2CH2, F), (M-1390, H, F, H, HOCH2CH2CH2CH2CH2, CFs), (M-1391, H， F, H, HOCH2CH2CH2CH2CH2, Br), (M-1392, H, F, H,
HOCHsCHsCHsCHzCHa, CH3)， (M-1393, H, F, H, HOCH2CH2OCH2CH2, H)， (M-1394, H' F, H, HOCH2GH2OCH2CH2, CI), (M-1395, H, F, H,
HOCH2CH2OCH2CH2, F)， (M-1396, H, F, H, HOCH2CH2OCH2CH2, CPs), (M- 1397, H, F, H, HOCH2CH2OCH2CH2, Br), (M-1398, H, F, H，
HOCH2CH2OCH2CH2, CHs), (M-1399, H' F, H, (Me)2N, H), (M-1400, H, F' H, (Me)2N, CI), (M- 1401, H, F, H, (Me)2N, F)， (M-1402, H, F， H, (Me)2N, CF3),
(M-1403, H, F, H, (Me)2N, Br), (M-1404, H, F, H, (Me)2N, CHs), (M-1405, H, F, H, piperidin-4-yl-metliyl, H) (M-1406, H， P, H, piperidin-4-yl-methyl, CI), (M-1407, H, F, H, piperidin-4-yl-metliyl, F), (M-1408, H, F, H' piperidin-4-yl- methyl, CFs), (M-1409, H, F, H, piperidin-4-yl-methyl, Br), (M-1410, H, F; H, piperidin-4-yl-metliyl, CHs), (M-1411, H, F, H, cyclohexylmethyl, H), (M- 1412, H, F, H, cyclohexylmethyl, CI), (M- 1413, H, F, H, cyclohexylmethyl, F), (M- 1414, H, P, H, cyclohexylmethyl, CF3), (M-1415, H, F, H, cyclohexylmethyl, Br), (M-1416, H, F, H, cyclohexylmethyl, CHs), (M-1417, H, P, F, H, H), (M-1418, H, F， F, H, CI), (M-1419, H' F, F, H, F), (M-1420, H, F, F, H' CFs), (M-1421, H, F, F' H, Br), (M-1422, H， F; F, H, CHs), (M-1423, H, P, F, F, H)， (M-1424, H, F, F, F, CI), (M-1425, H, F, F， F, F), (M-1426, H, P, F, F, CFs), (M-1427, H, F, F, F, Br), (M-1428, H, F, F, F, CHs), (M-1429, H， F, F, CI, H), (M-1430, H, F, F， CI, CI), (M-1431, H, F, F， CI, F), (M-1432, H, F， F, CI, CF3), (M-1433, H, F, F, CI, Br), (M-1434, H， F, F, CI, CHs), (M-1435, H, F, F, CHs, H), (M-1436, H, F, F, CHs, CI), (M-1437, H, F, F， CHs, F), (M-1438, H, F, F' CH3) CF3), (M-1439, H, F, F, CH3, Br), (M-1440, H, F, F, CH3, CHs), (M-1441, H, F, F, Et, H), (M-1442, H' F, F, Et, CI), (M-1443, H, F, F, Et, F), (M-1444, H, F, F, Et, CFs), (M-1445, H, F, F, Et, Br), (M-1446, H, F, F, Et, CHs), (M-1447, H, F, F, n-Pr, H), (M-1448, H' F, F, n-Pr, CI), (M-1449, H, F, F, n-Pr, F), (M-1450, H, F, F, n-Pr, CF3), (M-1451, H, F; F, n-Pr, Br), (M-1452, H, F， F, n-Pr, CHs), (M-1453, H， F， F, c-Pr, H), (M-1454, H, F, F, c-Pr, CI), (M-1455, H, F, c-Pr, F), (M-1456, H, F, F, c-Pr, CFs), (M-1457, H, F, F, c-Pr, Br), (M-1458, H, F, F' c-Pr, CH3), (M-1459, H' F, F， i-Pr, H), (M-1460, H, F, F， i-Pr, CI), (M-1461, H, F, F, i-Pr, F), (M-1462, H, F, F, i-Pr, CFs), (M-1463, H, F, F, i-Pr, Br), (M-1464, H, F, F, i-Pr, CHs), (M-1465, H, F, F, n-Bu, H), (M-1466, H, F, F, n-Bu, CI), (M-1467, H, P, F, n-Bu, F)， (M-1468, H, F, F, n-Bu, CFs), (M-1469, H, F, F, n-Bu, Br), (M-1470, H， F, F, n-Bu, CHs), (M-1471, H, F， F, i-Bu, H), (M-1472, H, F, F, i-Bu, CI), (M-1473, H, F, F, i-Bu, F), (M-1474, H, F, F， i-Bu, CF3)， (M-1475, H, F, F， i-Bu,, Br), (M-1476, H， F, F, i-Bu, CHs), (M-1477, H, F, F, sec-Bu, H)， (M-1478, H, F, F, sec-Bu, CI), (M-1479, H, F, F, sec-Bu, F), (M-1480, H, F, F, sec-Bu, CFs), (M-1481, H, F, F, sec-Bu, Br), (M-1482, H, F, F, sec-Bu, CH3), (M-1483, H, F, F, n-Pen, H), (M-1484, H, F, F, n-Pen, CI), (M-1485, H, F, F, n-Pen, F), (M-1486, H, F, F， n-Pen, CF3), (M-1487, H, F, F, n-Pen, Br), (M-1488, H, F' F' n-Pen, CHs), (M-1489, H, F, F, c-Pen, H), (M-1490, H, F， F, c-Pen, CI), (M-1491, H, F, P, c-Pen, F), (M-1492, H, F, F, c- Pen, CFs), (M-1493, H, F, F, c-Pen, Br), (M-1494, H, F, F, c-Pen, CHs), (M-1495, H, F, F, n-Hex, H), (M-1496, H, F, F, n-Hex, CI), (M-1497, H' F, F， n-Hex, F), (M-1498, H, F， F, n-Hex, CFs), (M-1499, H' F, F, n-Hex, Br), (M-1500, H, F, F, n-Hex, CHs), (M-1501, H, F, F, c-Hex, H), (M-1502, H, F, F, c-Hex, CI), (M-1503, H, F, F, c-Hex, F), (M-1504, H, F, F' c-Hex, CFs), (M-1505, H, F, F, c-Hex, Br), (M-1506, H， P, F, c-Hex, CHs), (M-1507, H, F, F, OH, H), (M-1508, H， F, F, OH, CI), (M-1509, H, F, F, OH, F), (M-1510, H, F, F, OH, CF3), (M-1511, H, F, F, OH, Br), (M-1512, H, F, F, OH, CHs), (M-1513, H, F, F, EtO, H), (M-1514, H, F, F, EtO, CI), (M-1515, H, F, F, EtO, F), (M-1516, H, F, F, EtO, CF3), (M-1517, H, F， F, EtO, Br), (M-1518, H, F， F, EtO, CH3)， (M-1519, H， F, F, n-PrO, H), (M-1520, H， F， F, n-PrO, CI), (M-1521, H, F， F, n-PrO, P), (M-1522, H， F, F， n-PrO, CFs), (M-1523, H， F, F, n-PrO, Br), (M-1524, H, F, F, n-PrO, CHs), (M-1525, H, F, F, PhO, H), (M-1526, H, F, F, PhO, CI), (M-1527, H, F, F, PhO, F)， (M-1528, H, P, F, PhO, CF3), (M-1529, H' F, F, PhO, Br), (M-1530, H, F, F, PhO, CHs), (M-1531, H, F, F， BnO, H), (M-1532, H, F, F, BnO, CI), (M-1533, H, F, F, BnO, F), (M- 1534, H, F， F, BnO, CPs), (M-1535, H, F, F, BnO, Br), (M-1536, H, F， F, BnO, CHs), (M-1537, H， F, F, PhCH2CH20, H), (M-1538, H, F, F, PliCH2CH20, CI), (M-1539, H, F, F, PI1CH2CH2O, F), (M-1540, H, F, F, PhCH2CH20, CF3), (M- 1541, H, F, F, PhCH2CH20, Br), (M-1542, H, P, F, PI1CH2CH2O, CHa), (M-1543, H, F, F， CFsO, H), (Mrl 544, H, F, F, CFsO, CI), (M-1545, H, F， F, CFsO, F)， . (M-1546, H, F, F, CFsO, CP3), (M-1547, H, F, F, CFsO, Br), (M-1548, H, F, F, CFsO, CHs), (M-1549, H, F, F, Ph, H), (M-1550, H, F， F, Ph, CI), (M-1551, H, F， F, Ph, F), (M-1552, H, F, P, Ph, CFs), (M-1553, H, F, F, Ph, Br), (M-1554, H, F, F, Ph, CHs), (M-1555, H, F; F, 4-F-Ph, H), (M-1556, H， F, F, 4-F-Ph, CI), (M- 1557, H， F， F, 4-F-Ph; F), (M-1558, H, F, F, 4-F-Ph, CFs), (M-1559, H， F, F, 4- F-Ph, Br), (M-1560, H, F, F, 4-F-Ph, CH3), (M-1561, H， F, F, 4-CFs-Pli, H), (M-1562, H, P, F, 4-CFs-Pli, CI), (M-1563, H, F, F, 4-CFs-Pli, F), (M-1564, H, F, F, 4-CF3-P11, CFs), (M-1565, H, F, F, 4-CF3-Ph, Br), (M-1566, H, F, F， 4-CFs-Ph, CHs), (M-1567, H, F, F, 4-(Me)2N-Ph, H), (M-1568, H, F, F， 4-(Me)2N-Ph, CI), (M-1569, H， P, F, 4-(Me)2N-Ph, F), (M-1570, H, F, F, 4-(Me)2N-Pli) CFa), (M- 1571, H, F, F, 4-(Me)2N-Ph; Br), (M-1572, H, F, F, 4-(Me)2N-Ph, CHs), (M-1573, H, F, F， 4-OH-Ph, H), (M-1574, H, F, F, 4-OH-Ph, CI), (M-1575, H， F, F, 4- OH-Pli, F), (M-1576, H, F, F, 4-OH-Ph, CFs), (M-1577, H, F, F, 4-OH-Ph, Br), (M-1578, H, F' F, 4-OH-Ph, CHs), (M-1579, H, F, F, 3,4-di-F-Ph, H), (M-1580, H, F, F, 3,4-di-F-Ph, CI), (M-1581, H, F, F, 3,4-di-F-Ph, F), (M-1582, H, F, F， 3,4-di-F-Ph, CFs), (M-1583, H, F, F, 3,4-di-F-Ph, Br), (M-1584, H, F, F, 3,4-di- F-Ph, CHs), (M-1585, H, F, F, 4-COOH-Ph, H), (M-1586, H, F, F, 4-COOH-Ph, CI), (M-1587, H, F， F, 4-COOH-Ph, F)， (M-1588, H， F, F, 4-COOH-Ph, CFs), (M-1589, H, F, F, 4-COOH-Ph, Br), (M-1590, H, F, F， 4-COOH-Ph, CHs), (M- 1591, H, F, F, Bn, H), (M-1592, H, F, F, Bn, CI), (M-1593, H， F, F, Bn, F)， (M- 1594, H, F, F, Bn, CFs), (M-1595, H, F, F， Bn, Br), (M-1596, H, F, F, Bn, CHs), (M-1597, H, F， F, 4-F-Bn, H)， (M-1598, H, F, F, 4-F-Bn, CI), (M-1599, H, F, F, 4-F-Bn, F), (M-1600, H, F, F, 4-F-Bn, CF3), (M-1601, H, F， F, 4-F-Bn, Br), (M- 1602, H, F, F, 4-F-Bn, CHs), (M-1603, H, F, F, 2-Py, H), (M-1604, H, F, F, 2-Py, CI), (M-1605, H, F, F, 2-Py, F)， (M-1606, H, F, F, 2-Py, CFs), (M-1607, H， F， F, 2-Py, Br), (M-1608, H, F, F, 2-Py, CHs), (M-1609, H, F, F, 3-Py, H), (M-1610, H, F, F， 3-Py, CI), (M-1611, H, F, F, 3-Py, F), (M-1612, H, F, F， 3-Py, CFa), (M-1613, H, F, F, 3-Py, Br), (M-1614, H, F, F, 3-Py, CHs), (M-1615, H, F, F, 4-Py, H), (M-1616, H, F, F， 4-Py, CI), (M-1617, H, F, F, 4-Py, F), (M-1618, H, F, F, 4-Py, CFs), (M-1619, H, F, F, 4-Py, Br), (M-1620, H, F, F, 4-Py, CHs), (M-1621, H， F, 〇 ),,,,C223OOCWCHH2C222C 67 H FOOCHCHCC CHC4 FH
,,,,)O2 672 H F F2 C3 673 JBO2cCHFCCCHffi
Figure imgf000114_0001
(M-1675, H, F, F, (Me)2NCOCH2CH2CH2CH2, H), (M-1676, H, F, F,
(Me)2NCOCH2CH2CH2CH2, CI), (M-1677, H, F; F, (Me)2NCOCH2CH2CH2CH2, F), (M-1678, H, F, F, (Me)2NCOCH2CH2CH2CH2, CFs), (M-1679, H, F, F, (Me)2NCOCH2CH2CH2CH2， Br), (M-1680, H， F， F, (Me)2NCOCH2CH2CH2CH2, CH3), (M-1681, H, F， F, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-1682, H, F, P, (Me)2NCOCH2CH2CH2CH2CH2' CI), (M-1683, H, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, F); (M-1684, H, F， F，
(Me)2NCOCH2CH2CH2CH2CH2) CFs), (M-1685, H, F, F,
(Me)2NCOCH2CH2CH2CH2CH2， Br), (M-1686, H, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-1687, H, F, F, MeOCH2; H), (M-1688, H, F, F, MeOCH2, CI), (M-1689, H, F, F, MeOCH2, F), (M-1690, H, F, F, MeOCHa, CF3), (M-1691, H, F， F, MeOCH2) Br), (M-1692, H, F, F, MeOCH2， CHs), (M-1693, H, F, F, EtOCH2, H), (M-1694, H, F, F, EtOCH2; CI), (M-1695, H, F， F, EtOCHa, F)，（M-1696, H, P, F， EtOCH2) CF3), (M-1697, H， F, F, EtOCH2， Br), (M-1698, H, F, F, EtOCHs, CHs), (M-1699, H, F, F, EtOCHsCHs, H), (M- 1700, H' F, F, EtOCH2CH2; CI), (M-1701, H， F, F, EtOCH2CH2; F), (M-1702, H' F' F, EtOCHaCHa, CFs), (M-1703, H, F, F, EtOCHaCHs, Br), (M-1704, H, F, F, EtOCH2CH2) CHs), (M-1705, H， F, F, MeOCH2CH2OCH2CH2, H), (M-1706, H, F, F, MeOCH2CH2OCH2CH2, CI), (M-1707, H, F, F, MeOCH2CH2OCH2CH2, F), (M-1708, H, F, F, MeOCH CHbOCHsCH , CF3), (M-1709, H, F, F,
MeOCH2CH2OCH2CH2， Br), (M-1710, H, F, P, MeOCH2CH2OCH2CH2， CHs), (M-1711, H， F, F, MeOCH2CH2, H), (M-1712, H' F, F, MeOCH2CH2, CI), (M- 1713, H, F, P, MeOCH2CH2, F), (M-1714, H, F, F, MeOCH2CH2, CF3)， (M-1715, H, F, F, MeOCHaCHs, Br), (M-1716, H, F, F, MeOCH2CH2, CH3), (M-1717, H， F, F, HOCHa, H), (M-1718, H, F, F, HOCH2' CI), (M-1719, H, F, F, HOCH2, F), (M-1720, H， F, F, HOCHa, CFs), (M-1721, H, F, F, HOCH2, Br), (M-1722, H, F, t o
o o
yyy) yy),,y,,,ocllie3 76ee Br Fclo!xltxl:9 H F hl CFlmlll
y,yy,,,yy,y,β,,)68 ccoe 7 H FPllixm F ccloel Jll 0 Ί H Fhxm ;hl F h
pyypyyy),,,),,,d6iin:lm3 F coe 76 ;htH 765 Hclhxlm ;hlll C F H--- -
Figure imgf000116_0001
(,,,,.,SC2H CHM 730HC F2 H F F H 7 ffi ¾ 1770, H， P, F, cyclohexylmethyl, CHs), (M-1771, H, F, CI, H, H), (M-1772, H, F' CI, H, CI), (M-1773, H, F, CI, H, P), (M-1774, H, F, CI, H, CFs), (M-1775, H, F, CI, H, Br), (M-1776, H, F, CI, H, CH3), (M-1777, H, F, CI, F， H), (M-1778, H, F, CI, F, CI), (M-1779, H， F, CI, F, F)， (M-1780, H, F, CI, F, CFs), (M-1781, H' F, CI, F, Br), (M-1782, H, F, CI, F, CHs), (M-1783, H, F, CI, CI, H), (M-1784, H, F， CI, CI, Cl)， (M-1785, H, F, CI, CI, F)， (M-1786, H, F， CI, CI, CF3), (M-1787, H, F, CI, CI, Br), (M-1788, H, F, CI, CI, CHs), (M-1789, H, F, CI, CHs, H)， (M-1790, H, F, CI, CHs, CI), (M-1791, H, F， CI, CHs, F), (M-1792, H, F, CI, CH3) CF3), (M-1793, H， F, CI, CH3) Br), (M-1794, H， F, CI, CHs, CHs), (M-1795, H, F, CI, Et, H), (M-1796, H, F, CI, Et, CI), (M-1797, H, F， CI, Et, F), (M-1798, H, F, CI, Et, CF3), (M-1799, H, F' CI, Et, Br), (M-1800, H, F, CI, Et, CH3)， (M-1801, H， F, CI, n-Pr, H), (M-1802, H, F， CI, n-Pr, CI), (M-1803, H， F, CI, n-Pr, F), (M-1804, H, F, CI, n-Pr, CF3)， (M-1805, H, F， CI, n-Pr, Br), (M-1806, H, F, CI, n-Pr, CHs), (M-1807, H, F, CI, c-Pr, H)， (M-1808, H, F, CI, c-Pr, CI), (M-1809, H, F, CI, c-Pr, F), (M-1810, H, F, CI, c-Pr, CFs), (M-1811, H, F， CI, c-Pr, Br), (M-1812, H' F, CI, c-Pr, CHs), (M-1813, H, F, CI, i-Pr, H), (M-1814, H, F, CI, i-Pr, CI), (M-1815, H, F, CI, i-Pr, F), (M-1816, H, F, CI, i-Pr, CFs), (M-1817, H, F, CI, i-Pr, Br), (M- 1818, H, F, CI, i-Pr, CH3), (M-1819, H, F, CI, n-Bu, H), (M-1820, H, F, CI, n-Bu, CI), (M-1821, H, F， CI, n-Bu, F), (M-1822, H, F, CI, n-Bu, CFs), (M-1823, H， F' CI, n-Bu, Br), (M-1824, H, F, CI, n-Bu, CHs), (M-1825, H, F， CI, i-Bu, H), (M- 1826, H, F, CI, i-Bu, CI), (M-1827, H, F, CI, i-Bu, F), (M-1828, H, F, CI, i-Bu, CFs), (M-1829, H， F, Cl; i-Bu, Br)，,(M 1830, H' F, CI, i-Bu, CH3)，（M-1831, H, F, CI, sec-Bu, H), (M-1832, H, F, CI, sec-Bu, CI), (M-1833, H, F, CI, sec-Bu, F), (M-1834, H, F, CI, sec-Bu, CFs), (M-1835, H, F, CI, sec-Bu, Br), (M-1836, H, F， CI, sec-Bu, CHs), (M-1837, H, F, CI, n-Pen, H), (M-1838, H, F, CI, n-Pen, CI), (M-1839, H, F' CI, n-Pen, F), (M-1840, H, F, CI, n-Pen, CFs), (M-1841, H, F, CI, n-Pen, Br), (M-1842, H, P, CI, n-Pen, CH3), (M-1843, H, F, CI, c-Pen, H), (M- 1844, H, F, CI, c-Pen, CI), (M-1845, H' F, CI, c-Pen, F), (M-1846, H, F, CI, c-Pen, CF3), (M-1847, H, F, CI, c-Pen, Br), (M-1848, H, F, CI, c-Pen, CH3), (M- 1849, H, F, CI, n-Hex, H), (M-1850, H, F, CI, n-Hex, CI), (M-1851, H， F, CI, n-Hex, F), (M-1852, H, F, CI, n-Hex, CFs), (M-1853, H, F, CI, n-Hex, Br), (M-1854, H, F, CI, n-Hex, CHs), (M- 1855, H, F, CI, c-Hex, H), (M-1856, H, F, CI, c-Hex, CI), (M- 1857, H, F, CI, c-Hex, F), (M- 1858, H, F, CI, c-Hex, CFs), (M- 1859, H, F， CI, c- Hex, Br), (M-1860, H, F, CI, c-Hex, CHs), (M-1861, H, F, CI, OH, H), (M-1862, H, F, CI, OH, CI), (M-1863, H, F, CI, OH, F), (M-1864, H, F, CI, OH, CFs), (M-1865, H, F, CI, OH, Br), (M-1866, H， F, CI, OH, CH3)， (M-1867, H， F， CI, EtO, H),
(M-1868, H， F, CI, EtO, CI), (M- 1869, H, F, CI, EtO, F), (M-1870, H, F, CI, EtO, CFs), (M-1871, H， F, CI, EtO, Br), (M-1872, H, F, CI, EtO, CHs), (M-1873, H， F, CI, n-PrO, H), (M- 1874, H， F, CI, n-PrO, CI), (M-1875, H， F, CI, n-PrO, F), (M-1876, H， F' CI, n-PrO, CFs), (M-1877, H, F, CI, n-PrO, Br), (M-1878, H， P, CI, n-PrO, CH3), (M- 1879, H, F， CI, PhO, H), (M- 1880, H, F, CI, PhO, CI), (M-1881, H, F, CI, PhO, F), (M-1882, H, F, CI, PhO, CFs), (M- 1883, H, F， CI, PhO, Br), (M-1884, H， F, CI, PhO, CHs), (M- 1885, H, F, CI, BnO, H), (M- 1886, H, F, CI, BnO, CI), (M- 1887, H, F, CI, BnO, F)， (M-1888, H， F, CI, BnO, CF3), (M-1889, H, F, CI, BnO, Br), (M-1890, H， F, CI, BnO, CH3), (M-1891, H, F， CI, PhCH2CH20, H), (M-1892, H, F, CI, PI1CH2CH2O, CI), (M-1893, H, F; CI, PhCHaCHaO, F), (M- 1894, H, F, CI, PhCH2CH20, CPs), (M-1895, H， F， CI, PhCHsCH O, Br), (M.-1896, H, P, CI, PhCH2CH20, CH3)， (M-1897, H, F, CI, CF.sQ, H), (M-1898, H, F, CI, CF30'. C1), (M- 1899, H, F, CI, CF3O, F)，（M- 1900, H, F, CI, CFsO, CF3), (M- 1901, H, F, CI, CFsO, Br), (M-1902, H, F, CI, CF3O, CH3), (M- 1903, H, F, CI, F , H), (M-1904, H, F, CI, Ph, CI), (M-1905, H, F， CI, Ph, F), (M- 1906, H, F, CI, Ph, CF3), (M-1907, H, F, CI, Ph, Br), (M-1908, H, F, CI, Ph, CHs), (M-1909, H, F, CI, 4-F-Ph, H)， (M-1910, H, F, CI, 4-F-Ph, CI), (M- 1911, H， F， CI, 4-F-Ph, F), (M-1912, H, F, CI, 4-F-Ph, CFs), (M-1913, H, F, CI, 4-F-Ph, Br), (M-1914, H, F, CI, 4-F-Ph, CHa), (M-1915, H, F, CI, 4-CFs-Ph, H), (M-1916, H, F, Cl， 4-CF3-Ph, CI), (M-1917, H' F, CI, 4-CFs-Pli, F)， (M-1918, H, F, CI, 4-CFs-Ph, CFs), (M-1919, H, F， CI, 4-CF3-Ph, Br), (M-1920, H, F, CI, 4-CF3-Ph, CHs), (M-1921, H, F, CI, 4-(Me)2N-Pli, H)， (M- 1922, H, F， CI, 4-(Me)2N-Ph, CI), (M- 1923, H, F; CI, 4- (Me)2N-Ph, F), (M-1924, H, F, CI, 4-(Me)2N-Ph, CF3), (M-1925, H, F, CI, 4- (Me)2N-Ph， Br), (M- 1926, H， F, CI, 4-(Me)2N-Ph, CH3), (M-1927, H, F, CI, 4- OH-Ph, H), (M- 1928, H, F, CI, 4-OH-Ph, CI), (M-1929, H, F, CI, 4-OH-Ph, P), (M-1930, H, F, CI, 4-OH-Ph, CF3), (M-1931, H, F， CI, 4-OH-Ph, Br), (M-1932, H， F, CI, 4-OH-Ph, CHs), (M- 1933, H'. F, CI, 3,4-di-F-Ph, H), (M-1934, H, F, CI, 3,4-di-F-Ph, Cl)， (M-1935, H, F， CI, 3,4-di-F-Ph, F), (M-1936, H, F, CI, 3,4-di- F-Ph, CF3), (M-1937, H, F, CI, 3, 4-di-F-Ph, Br), (M-1938, H, F, CI, 3;4-di-F-Ph, CHs), (M- 1939, H， F， CI, 4-COOH-Ph, H), (M- 1940, H， F, CI, 4-COOH-Ph, CI), (M-1941, H, F, CI, 4-COOH-Ph, F), (M-1942, H, F, CI, 4-COOH-Ph, CFs), (M- 1943, H, F, CI, 4-COOH-Ph, Br), (M-1944, H， F' CI, 4-COOH-Ph, CHs), (M- 1945, H, F' CI, Bn, H), (M-1946, H， F, Cl， Bn, CI), (M-1947, H, F, CI, Bn, F), (M-1948, H, F, CI, Bn, CFs), (M-1949, H, F, CI, Bn, Br), (M-1950, H, F, CI, Bn, CHs), (M-1951, H， F, CI, 4-F-Bn, H), (M-1952, H, F, CI, 4-F-Bn, CI), (M-1953, H, F, CI, 4-F-Bn, F), (M-1954, H, F, CI, 4-F-Bn, CF3), (M-1955, H, F, CI, 4-F-Bn, Br),
(M-1956, H, F, CI, 4-F-Bn, CHs), (M-1957, H' F， CI, 2-Py, H), (M-1958, H, F, CI, 2-Py, CI), (M-1959, H, F, CI, 2-P.y, F), (M-1960, H, F, Cl; 2-Py, CF3), (M- 1961, H, F, CI, 2-Py, Br), (M- 1962, H， F, CI, 2-Py, CHa), (M-1963, H, F' CI, 3-Py, H), (M-1964, H， F, CI, 3-Py, CI), (M-1965, H, F, CI, 3-Py, F), (M- 1966, H, F, CI, 3- Py, CPs), (M-1967, H, F, CI, 3-Py, Br), (M-1968, H, F, CI, 3-Py, CHs), (M-1969, H, F, CI, 4-Py, H)，（M- 1970, H, F, CI, 4-Py, CI), (M-1971, H, F, CI, 4-Py, F), t to
00
Figure imgf000120_0001
HOOCCHaCHsCHsCHs, CFs), (M-2027, H, F, CI, HOOCCH2CH2CH2CH2, Br), (M-2028, H, F, CI, HOOCCHs CHs CHs CH2， CHs), (M-2029, H, F, CI,
(Me)2NCOCH2CH2CH2CH2, H), (M-2030, H, F, CI, (Me)2NCOCH2CH2CH2CH2, CI), (M-2031, H, F, CI, (Me)2NCOCH2CH2CH2CH2, F), (M-2032, H' F, CI, (Me)2NCOCH2CH2CH2CH2; CF3), (M-2033, H, F， CI, (Me)2NCOCH2CH2CH2CH2, Br), (M-2034, H, F, CI, (Me)2NCOCH2CH2CH2CH2; CHs), (M-2035, H, F, CI, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-2036, H, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2; CI), (M-2037, H, F, CI,
(Me)2NCOCH2CH2CH2CH2C F), (M-2038, H, F, Gl,
(Me)2NCOGH2CH2CH2CH2CH2, CFs), (M-2039, H, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2， Br), (M-2040, H, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-2041, H, F, CI, MeOCH2, H), (M-2042, H, F， CI, MeOCH2, CI), (M-2043, H, F, CI, MeOCH2; F), (M-2044, H, F, CI, MeOCH2, CFs), (M-2045, H, F, CI, MeOCH2) Br), (M-2046, H, F, CI, MeOCHs, CH3), (M-2047, H, F, CI, EtOCH2j H), (M-2048, H, P, CI, EtOCH2, CI), (M-2049, H, F， CI, EtOCH2, F), (M-2050, H, F, CI, EtOCH2, CFs), (M-2051, H, F, CI, EtOCH2; Br), (M-2052, H, F, CI, EtOCH , CHs), (M-2053, H, F, CI, EtOCH2CH2, H), (M-2054, H, F， CI, EtOCHsCHs, CI), (M-2055, H， F, CI, EtOCH2CH2, F), (M-2056, H, F， CI, EtOCH2CH2! CFs), (M-2057, H, F, CI, EtOCH2CH2, Br), (M-2058, H, F, CI, EtOCH2CH2, CHs), (M-2059, H, F, CI, MeOCH2CH2OCH2CH2, H), (M-2060, H, F, CI, MeOCH2CH2OCH2CH2, CI), (M-2061, H, F, CI,
MeOCH2CH2OCH2CH2, E), (M-2062, H, F, CI, MeOCH2CH2OCH2CH2, CFs), (M-2063, H, F, CI, MeOCH2CH2OCH2CH2) Br), (M-2064, H, F, CI,
MeOCH2CH2OCH2CH2, CH3), (M-2065, H, F, CI, MeOCH2CH2, H), (M-2066, H, F, CI, MeOCH2CH2, CI), (M-2067, H, F, CI, MeOCHaCHa, F), (M-2068, H, F, CI, MeOCH2CH2) CFs), (M-2069, H, F, CI, MeOCH2CH2, Br), (M-2070, H, F, CI, MeOCH2CH2, CH3), (M-2071, H, F, CI, HOCH2; H), (M-2072, H, F， CI, HOCH2, CI), (M-2073, H, F; CI, HOCH2, F)， (M-2074, H, F, CI, HOCH2, CFs), (M-2075, H, F, CI, HOCHs, Br), (M-2076, H, F, CI, HOCH2, CHs), (M-2077, H, F, CI, HOCH2CH2; H), (M-2078, H, F, CI, HOCH2CH2, CI), (M-2079, H, F, CI, HOCH2CH2, F), (M-2080, H, F, CI, HOCH2CH2, CFs), (M-2081, H, F, CI, HOCH2C Br), (M-2082, H, F, CI, HOCH2CH2; CHs), (M-2083, H, F; CI, HOCH2CH2CH2， H)， (M-2084, H, F， CI, HOCH2CH2CH2) Cl)， (M-2085, H, F, CI, HOCH2CH2CH2, F), (M-2086, H, F, CI, HOCH2CH2CH2, CF3); (M-2087, H, F, CI, HOCH2CH2CH2, Br), (M-2088, H, F, CI, HOCH2CH2CH2, CHs), (M-2089, H, F, CI, HOCH2CH2CH2CH2j H), (M-2090, H, F, CI, HOCH2CH2CH2CH2; CI), (M- 2091, H, F， CI, HOCH2CH2CH2CH2， F), (M-2092, H, F， CI, HOCH2CH2CH2CH2, CFs), (M-2093, H, F， CI, HOCHsCH CHsCH , Br), (M-2094, H, F, CI,
HOCH2GH2CH2CH2, CH3), (M-2095, H， F, CI, HOCH2CH2CH2CH2CH2, H), (M-2096, H, F, CI, HOCH2CH2CH2CH2CH2, CI), (M-2097, H, F, CI,
HOCH2CH2CH2CH2CH2, F), (M-2098, H, F, CI, HOCH2CH2CH2CH2CH2, CF3), (M-2099, H, F, CI, HOCH2CH2CH2CH2CH2, Br), (M-2100, H, F, CI,
HOCH2CH2CH2CH2CH2; CH3), (M-2101, H, F, CI, HOCH2CH2OCH2CH2; H)， (M-2102, H, F, CI, HOCH2CH2OCH2CH2, CI), (M-2103, H, F, CI,
HOCH2CH2OCH2CH2; F), (M-2104, H, F, CI, HOCH2CH2OCH2CH2, CFs), (M- 2105, H, F， CI, HOCH2CH2OCH2CH2, Br), (M-2106, H, F, CI,
HOCH2CH2OCH2CH2, CH3), (M-2107, H, F, CI, (Me)2N, H)， (M-2108, H, F, CI, (Me)2N， CI), (M-2109, H， F, CI, (Me)2N, F), (M-2110, H, F, CI, (Me)2N, CFs), (M-2111, H, F, CI, (Me)2N, Br), (M-2112, H, F, CI, (Me)2N, CH3), (M-2113, H, F, CI, piperidm-4-yl-methyl, H), (M-2114, H, F, CI, piperidin-4-yl-methyl, CI), (M-2115, H, F, CI, piperidin-4-yl-metliyl, F), (M-2116, H, F, CI, piperidin-4- yl-metliyl, CFs), (M-2117, H, F, CI, piperidin-4-yl-methyl, Br), (M-2118, H, F, CI, piperidin-4-yl-metliyl, CH3), (M-2119, H, F, CI, cyclohexylmethyl, H), (M- 2120， H' F, CI, cyclohexylmethyl, CI), (M-2121, H, F' CI, cyclohexylmethyl, F), (M-2122, H, F' CI, cyclohexylmethyl, CFs), (M-2123, H， F, CI, cyclohexylmethyl, Br), (M-2124, H, F, CI, cyclohexylmethyl, CHs), (M-2125, H, CHs, H, H, H), (M-2126, H, CHs, H, H， CI), (M-2127, H, CH3, H, H, F)， (M-2128, H, CH3, H， H， CFs), (M-2129, H, CHs, H, H， Br), (M-2130, H, CH3, H, H, CHs), (M-2131, H, CHs, H, F, H), (M-2132, H, CHa, H, F, CI), (M-2133, H, CHs, H, F, F)， (M-2134, H, CH3, H, F, CF3), (M-2135, H, CHs, H, F, Br), (M-2136, H, CHs, H, F, CHs), (M-2137, H, CHs, H, CI, H), (M-2138, H, CHs, H, CI, CI), (M-2139, H, CH3， H, Cl， F), (M-2140, H, CH3, H, CI, CFs), (M-2141, H, CHs, H, CI, Br), (M-2142, H, CH3, H, CI, CHs), (M-2143, H, CH3> H; CHs, H), (M-2144, H, CH3) H, CHs, CI), (M- 2145, H, CHs, H, CH3, F)，（M-2146, H, CH3, H, CHs, CFs), (M-2147, H, CHs, H, CHs, Br), (M-2148, H' CHs, H, CH3) CHs), (M-2149, H, CH3 ; H, Et, H), (M-2150, H, CHs, H, Et, CI), (M-2151, H, CHs, H, Et, F), (M-2152, H, CHs, H, Et, CFs), (M-2153, H, CHs, H, Et, Br), (M-2154, H, CHs, H, Et, CHs), (M-2155, H, CHs, H, n-Pr, H)， (M-2156, H, CHs, H, n-Pr, CI), (M-2157, H, CHs, H, n-Pr, F), (M-2158, H, CHs, H, n-Pr, CF3), (M-2159, H, CHs, H, n-Pr, Br), (M-2160, H, CHs, H, n- Pr, CHs), (M-2161, H, CHs, H, c-Pr, H), (M-2162, H, CHs, H, c-Pr, CI), (M-2163, H, CHs, H, c-Pr, F), (M-2164, H, CHs, H, c-Pr, CF3), (M-2165, H, CHs, H, c-Pr, Br), (M-2166, H， CHs, H, c-Pr, CH3), (M-2167, H， CH3, H, i-Pr, H), (M-2168, H， CHs, H, i-Pr, CI), (M-2169, H, CH3; H, i-Pr, F), (M-2170, H, CHs, H, i-Pr, CFs), (M-2171, H, CH3, H"i-Pr, Br), (M-2172, H' CH3, H, i-Pr, CHs), (M-2173, H, CH3, H, n-Bu, H), (M-2174, H, CHs, H, n-Bu, CI), (M-2175, H, CHs, H, n-Bu, F), (M-2176, H, CHs, H， n-Bu, CF3), (M-2177, H， CH3, H, n-Bu, Br), (M-2178, H, CHs, H, n-Bu, CHs), (M-2179, H, CH3, H, i-Bu, H), (M-2180, H, CHs, H, i-Bu, CI), (M-2181, H, CH3, H, i-Bu, F), (M-2182, H, CH3, H, i-Bu, CF3); (M-2183, H, CHs, H, i-Bu, Br), (M-2184, H, CHs, H, i-Bu, CHs), (M-2185, H, CHs, H, sec-Bu, H), (M-2186, H, CHs, H, sec-Bu, CI), (M-2187, H, CHs, H, sec-Bu, F)， (M-2188, H, CHs, H, sec-Bu, CF3), (M-2189, H, CH3, H, sec-Bu, Br), (M-2190, H, CHs, H, sec-Bu, CHs), (M-2191, H, CH3) H, n-Pen, H), (M-2192, H, CH3) H, n-Pen, CI), (M-2193, H, CHs, H, n-Pen, F), (M-2194, H, CHs, H, n-Pen, CFs), (M-2195, H, CHs, H, n-Pen, Br), (M-2196, H, CHs, H， n-Pen, CHs), (M-2197, H, GH3, H, c- Pen, H), (M-2198, H, CH3, H, c-Pen, CI), (M-2199, H， CHs, H, c-Pen, F), (M-2200, H, CH3， H, c-Pen, CFs), (M-2201, H, CHs, H, c-Pen, Br), (M-2202, H, CH3, H, c-Pen, CHs), (M-2203, H, CH3, H， n-Hex, H)，（M-2204, H， CH3, H, n-Hex, CI), (M-2205, H, CHs, H, n-Hex, F), (M-2206, H, CHs, H, n-Hex, CFs), (M-2207, H, CHs, H, n-Hex, Br), (M-2208, H, CHs, H, n-Hex, CHs), (M-2209, H, CH3, H, c- Hex, H), (M-2210, H, CHs, H, c-Hex, CI), (M-2211, H, CH3; H, c-Hex, F), (M- 2212' H， CHs, H, c-Hex, CFs), (M-2213, H, CHs, H, c-Hex, Br), (M-2214, H, CH3) H, c-Hex, CH3), (M-2215, H, CH3, H' OH, H), (M-2216, H, CHs, H, OH, CI), (M-2217, H, CHs, H, OH, F), (M-2218, H, CHs, H, OH, CFs), (M-2219, H, CH3, H, OH, Br), (M-2220, H， CHs, H, 01- I, CHs), (M-2221, H, CHs, H， EtO, H), (M-2222, H, CHs, H, EtO, CI), (M-2223, H, CHs, H, EtO, F), (M-2224, H, CHs, H' EtO, CFs), (M-2225, H, CHs, H, EtO, Br), (M-2226, H, CHs, H, EtO, CHs), (M-2227, H, CHs, H, n-PrO; H)， (M-2228, H, CH3， H, n-PrO, CI), (M-2229, H, CHs, H, n-PrO, F), (M-2230, H， CH3, H, n-PrO, CFs), (M-2231, H, CHs, H, n-PrO, Br), (M-2232, H, CHs, H, n-PrO; CHs), (M-2233, H, CHs, H, PhO, H), (M-2234, H, CHs, H, PhO, CI), (M-2235, H, CHs, H, PhO, F), (M-2236, H, CHs, H, PhO, CF3), (M-2237, H, CHs, H, PhO., Br), (M-2238, H, CHs, H, PhO, CH3)， (M-2239, H, CHs, H, BnO, H), (M-2240, H, CHs, H, BnO, CI), (M-2241, H, CH3> H, BnO, P), (M-2242, H, CHs, H, BnO, CF3); (M-2243, H, CHs, H, BnO, Br), (M-2244, H, CHs, H, BnO, CHs), (M-2245, H, CHs, H, PhCH2CH20, H), (M-2246, H, CHs, H, PliCH2CH20, CI), t
en 〇 n ),),,,,,,3 CH C C H H Bn 2304 HH H303 Br Bn 2
Ω
CO
Figure imgf000125_0001
(M-2305, H， CH3; H， 4-F-Bn, H) , (M-2306, H, CHs, H, 4-F-Bn, CI), (M-2307, H, CH3, H; 4-F-Bn, F), (M-2308, H, CH3; H, 4-F-Bn, CFs), (M-2309, H, CH3, H, 4- F-Bn, Br), (M-2310, H, CH3; H, 4-F-Bn, CHs), (M-2311, H, CH3, H, 2-Py, H), (M-2312, H, CH3， H, 2-Py, CI), (M-2313, H， CH3, H, 2-Py, F), (M-2314, H， CH3， H, 2-Py, CF3), (M-2315, H; CHs, H, 2-Py, Br), (M-2316, H, CHs, H, 2-Py, CHs), (M-2317, H, CH3, H, 3-Py, H), (M-2318, H, CHs, H, 3-Py, CI), (M-2319, H, CHs, H, 3-Py, F), (M-2320, H, CH3) H; 3-Py, CFs), (M-2321, H; CHs, H, 3 -Py, Br), (M-2322, H, CHs, H， 3-Py, CH3)， (M-2323, H, CHs, H, 4-Py, H), (M-2324, H, CHs, H, 4-Py, CI), (M-2325, H, CHs, H, 4-Py, F), (M-2326, H, CHs, H, 4-Py, CFs) , (M-2327, H, CHs, H, 4-Py, Br), (M-2328, H, CH3, H, 4-Py, CHs) , (M-2329, H, CHs, H, 2-Th, H), (M-2330, H, CH3, H， 2-Th, CI), (M-2331, H, CH3; H, 2-Th, F)， (M-2332, H, CHs, H, 2-Th, CFs), (M-2333, H, CH3, H, 2-Th, Br), (M- 2334, H, CHs, H, 2-Th, CHs), (M-2335, H, CH3) H, 3-Th, H), (M-2336, H, CHs, H, 3 -Th, CI), (M-2337, H, CH3, H, 3-Th, F), (M-2338, H, CH3, H, 3-Th, CFs), (M-2339, H, CH3) H; 3-Th, Br), (M-2340, H, CHs, H, 3-Th, CHs), (M-2341, H, CHs, H, pyrazol-2-yl, H), (M-2342, H， CH3) H, pyrazol-2-yl, CI), (M-2343, H, CHs, H， pyrazol-2-yl, F), (M-2344, H, CH3) H， pyrazol-2-yl, CFs), (M-2345, H, CHs, H, pyrazol-2-yl, Br), (M-2346, H, CH3> H， pyrazol-2-yl, CHs), (M-2347, H, CH3, H, pyrazol- 3-yl, H), (M-2348, H, CH3, H, pyrazol- 3 -yl; CI), (M-2349, H, CH3, H, pyrazol- 3-yl, F), (M-2350, H, CH3) H, pyrazol- 3-yl, CFs), (M-2351, H, CH3 ) H, pyrazol-3-yl, Br), (M-2352, H, CHs, H, pyrazol- 3-yl, CHs), (M-2353, H, CHs, H, pyrimidin-2-yl, H), (M-2354, H' CHs, H^. pyrimidin^-yl, CI), (M-2355, H, CHs, H， pyrimidm-2-yl, F)， (M-2356, H, CH3j H, pyrimidin-2-yl, CF3) , (M-2357, H, CHs, H, pyrimidin-2-yl, Br), (M-2358, H, CHs, H, pyrimidin-2-yl, CHs), (M- 2359, H, CHs, H, pyrimidin-4-yl, H), (M-2360, H, CHs, H, pyrimidin-4-yl, CI), (M-2361, H, CHs, H, pyrimidm-4-yl, F), (M-2362, H, CHs, H, pyrimidin-4-yl, CFs), (M-2363, H, CHs, H, pyrimidin-4-yl; Br), (M-2364, H， CHs, H,
pyrimidin-4-yl, CH3), (M-2365, H, CH3, H, pyrimidin-5-yl, H), (M-2366, H, CH3j H, pyrimidin-5-yl, CI), (M-2367, H, CHs, H, pyrimidin-5-yl, F)， (M-2368, H, CH3, H， pyrimidin-5-yl, CF3), (M-2369, H, CH3， H, pyrimidin-5-yl, Br), (M-2370, H, CH3> H, pyrimidin-5-yl, CHs), (M-2371, H, CHs, H, HOOCCH2CH2GH2) H)， (M-2372, H, CHs, H， HOOCCH2CH2CH2; CI), (M-2373, H, CH3, H,
HOOCCHaCHaCHa, F)， (M-2374, H, CH3, H, HOOCCH2CH2CH2, CFs), (M-2375, H, CHs, H, HOOCCH2CH2CH2> Br), (M-2376, H， CHs, H, HOOCCH2CH2CH2, CHs), (M-2377, H, CH3, H, HOOCCH2CH2CH2CH2， H), (M-2378, H, CHs, H, HOOCCH2CH2CH2CH2) CI), (M-2379, H, CHs, H, HOOCCH2CH2CH2CH2， F), (M-2380, H, CHs, H， HOOCCH2CH2CH2CH2, CFs), (M-2381, H, CHs, H,
HOOCCH2CH2CH2CH2) Br), (M-2382, H, CHs, H， HOOCCHsCHaCHaCHs, CH3)， (M-2383, H, CH3) H, (Me)2NCOCH2CH2CH2CH2, H), (M-2384, H, CH3; H, (Me)2NCOCH2CH2CH2CH2, CI), (M-2385, H, CHs, H,
(Me)2NCOCH2CH2CH2CH2, F)， (M-2386, H， CH3, H, (Me)2NGOCH2CH2CH2CH2' CFs), (M-2387, H, CH3, H, (Me)2NCOCH2CH2CH2CH2, Br), (M-2388, H, CH3) H, (Me)2NCOCH2CH2CH2CH2) CH3), (M-2389, H, CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2, H)， (M-2390, H, CH3, H，
(Me)2NCOCH2GH2CH2CH2CH2, CI), (M-2391, H, CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-2392, H， CHs, H，
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-2393, H, CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-2394, H, CH3) H， . .,
(Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-2395, H, CH3, H, MeOCH2, H), (M- 2396, H, CH3) H, MeOCH2; CI), (M-2397, H, CHs, H, MeOCH2) F), (M-2398, H, CH3; H, MeOCH2, CFs), (M-2399, H, CHs, H, MeOCH2， Br), (M-2400, H, CH3, H, MeOCH2, CHs), (M-2401, H, CH3; H, EtOCH2) H)， (M-2402, H, CHs, H, EtOCHa, CI), (M-2403, H, CHs, H, EtOCH2) F), (M-2404, H, CHs, H, EtOCH2, CFs), (M- 2405, H, CH3) H, EtOCH2, Br), (M-2406, H, CHs, H, EtOCH2; CHs), (M-2407, H， CH3， H, EtOCH2CH2, H), (M-2408, H， CHs, H， EtOCH2CH2) CI), (M-2409, H， CHs, H, EtOCH2CH2, F), (M-2410, H, CHg, H, EtOCH2CH2; CFs), (M-2411, H, CHs, H, EtOCH2CH2; Br), (M-2412, H, CHs, H, EtOCH2CH2; CHs), (M-2413, H, CHs, H, MeOCH2CH2OCH2CH2, H), (M-2414, H, CH3, H，
MeOCH2CH20CH2CH2; CI), (M-2415, H， CHs, H, MeOCH2CH2OCH2CH2) F)， (M-2416, H, CHs, H, MeOCHsCHsOCHsCH , CF3), (M-2417, H, CH3) H, MeOCH2CH20CH2CH2, Br), (M-2418, H, CHs, H, MeOCH2CH20CH2CH2, CHs), (M-2419, H, CH3) H; MeOCH2CH2; H); (M-2420, H, CH3l H, MeOCH2CH2, Cl)， (M-2421, H， CHs, H, MeOCH2CH2, F), (M-2422, H, CH3, H, MeOCH2CH2, CPs), (M-2423, H, CH3, H, MeOCH2CH2) Br), (M-2424, H, CH3, H, MeOCH2CH2, CHs), (M-2425, H， CHs, H, HOCH2, H), (M-2426, I-I, CHs, H, HO CHs, CI), (M-2427, H, CHs, H, HOCHs, F), (M-2428, H, CH3) H, HOCH2> CFs), (M-2429, H, CHs, H, HOCH2; Br), (M-2430, H, CHs, H, HOCH2, CHs), (M-2431, H' CHs, H,
HOCH2CH2) H)， (M-2432, H, CH3, H, HOCH2CH2, CI), (M-2433, H, CHs, H, HOCH2GH2, F), (M-2434, H， CHs, H, HOCHsCHa, CF3), (M-2435, H， CHs, H, HOCH2CH2, Br), (M-2436, H, CH3, H， HOCH2CH2, CHs), (M-2437, H, CHs, H, HOCH2CH2CH2， H)， (M-2438, H, CHs, H, HOCH2CH2CH2; CI), (M-2439, H， CHs, H, HOCH2CH2CH2, F), (M-2440, H， CHs, H, HOCH2CH2CH2, CFs), (M-2441, H, CHs, H, HOCH2CH2CH2, Br), (M-2442, H, CHs, H, HOCH2CH2CH2, CH3), (M- 2443, H' CHs, H, HOCH2GH2CH2CH2, H), (M-2444, H, CHs, H,
HOCH2CH2CH2CH2， CI), (M-2445, H, CHs, H, HOCH2CH2CH2C F); (M-2446, H, CHs, H, HOCH2CH2CH2CH2; CFs), (M-2447, H， CH3, H' HOCH2CH2CH2CH2, Br), (M-2448, H, CH3, H, HOCH2CH2CH2CH2, CH3), (M-2449, H, CH3) H,
HOCH2CH2CH2CH2CH2) H), (M-2450, H, CHs, H, HOCH2CH2CH2CH2CH2, CI), (M-2451, H， CHs, H, HOCH2CH2CH2CH2CH2, F), (M-2452, H, CHs, H,
HO CH2CH2CH2CH2CH2, CFs), (M-2453, H， CHs, H, HO CH2CH2CH2CH2CH2, Br), (M-2454, H, CHs, H, HOCH2CH2CH2CH2CH2, CHs), (M-2455, H, CHs, H, HOCH2CH2O CH2CH2, H), (M-2456, H, CH3) H, HOCH2CH2OCH2CH2, CI), (M- 2457, H, CHs, H, HO CH2CH2O CH2CH2, F), (M-2458, H' CH3, H,
HO CH2CH2OCH2CH2, CF3), (M-2459, H, CHs, H, HOCH2CH20CH2CH2; Br), (M-2460, H, CH3, H, HOCH2CH2OCH2CH2, CHs), (M-2461, H, CH3) H, (Me)2N, H), (M-2462, H, CH3， H, (Me)2N， CI), (M-2463, H, CHs, H, (Me)2N, F), (M-2464, H, CH3, H, (Me)2N, CFs), (M-2465, H， CH3, H, (Me)2N, Br), (M-2466, H, CHs, H, (Me)2N, CH3), (M-2467, H， CHs, H, piperidm-4-yl-metliyl, H)， (M-2468, H, CHs, H, piperidin-4-yl-metliyl, CI), (M-2469, H, CHs, H, piperidin-4-yl-methyl, F)， (M-2470, H, CHs, H, piperidin-4-yレ methyl, CF3)， (M-2471, H, CHs, H, piperidin-4-yl-metliyl, Br), (M-2472, H， CHs, H, piperidm-4-yl-meth.yl, CH3), (M-2473, H, CH3' H, cyclohexylmethyl, H)， (M-2474, H, CHs, H,
cyclohexylmetliyl, CI), (M-2475, H, CH3, H, cyclohexylmethyl, F), (M-2476, H, CHs, H, cyclohexylmethyl, CFs), (M-2477, H' CHs, H， cyclohexylmethyl, Br), (M-2478, H, CHs, H, cyclohexylmethyl, CHs), (M-2479, H, CHs, F, H, H), (M- 2480, H, CHs, F, H, CI), (M-2481, H, CHs, F, H, F), (M-2482, H, CH3, F, H， CF3), (M-2483, H, CHa, F, H, Br), (M-2484, H, CH3> F, H, CH3), (M-2485, H, CHs, F, F, H), (M-2486, H, CH3, F' F, CI), (M-2487, H, CH3, F, F, F), (M-2488, H, CH3, P, F, CF3), (M-2489, H, CH3, F, F, Br), (M-2490, H, CHs, F, F, CHa), (M-2491, H, C F, CI, H), (M-2492, H， CHs, F, CI, CI), (M-2493, H, CHs, F, CI, F), (M-2494, H, CH3 ) F, CI, CFs), (M-2495, H, CHs, F, CI, Br), (M-2496, H, CH3, F, CI, CHs), (M-2497, H， CHs, F, CHs, H), (M-2498, H, CHs, F, CHs, CI), (M-2499, H, CH3, F, CH3; F), (M-2500, H, CHs, F, CH3, CF3), (M-2501, H, CH3, F, CH3, Br), (M-2502, H, CHs, F, CH3, CHs), (M-2503, H, CHs, F, Et, H), (M-2504, H, CHs, F, Et, CI), 〇 ),),,,,,,,,,3 O3 C C569 HH C cHeH F cex 2 CH F Fx Br8 HH 56-- ),,,),,,,,,,33 C H566 C F cHexF567565 H C 2 H!H 2 2H F ce FHx--
M J
l— -l ),:),,,,,,,,356 C F ce CH cHe4 HHex CI Hx 2563 C Fx H 2H HH-- f
o
O οο ω
o
),,,,,,,,,s C3 C Br538 HH536 H537 HH Fu 2 2 CM F 2
),,),,S 3CT C FH F Bu F B Hu
),),,,,,,,333 C Fu CH533 H 0 52 HH n 2H F nBu Br-- ),,,,,,,,S3 C C50 HH FuF F nBu 59 H CH F nBu 2 nB2---
Figure imgf000130_0001
)),,,,,,33 0 Hi 〇H 6 CCT 7H F nBus 2 PrH 2 2 CH F- ,,,,,,,,,,3 Q33s Q55 HH C F iP C F iPrF 22 FH 4 HH--
H), (M-2570, H, CHs, F, OH, CI), (M-2571, H, CHs, F, OH, F), (M-2572, H, CH3, F, OH, CF3), (M-2573, H, CHs, F, OH, Br), (M-2574, H, CHs, F, OH, CHs), (M- 2575, H, CHs, F, EtO, H), (M-2576, H， CHs, F, EtO, CI), (M-2577, H, CH3, F, EtO, F), (M-2578, H, CH3, F, EtO, CF3), (M-2579, H, CH3; F， EtO, Br), (M-2580, H, CHs, F' EtO, CHs), (M-2581, H, CH3) F, n-PrO, H), (M-2582, H, CH3) F, n- PrO, CI), (M-2583, H, CHs, F, n-PrO, P), (M-2584, H, CHs, F, n-PrO, CF3), (M-2585, H, CHs, F, n-PrO, Br), (M-2586, H, CH3) F， n-PrO, CHs), (M-2587, H, CHs, F， PhO, H), (M-2588, H; CH3) F, PhO, CI), (M-2589, H; CHs, F, PhO, F), (M-2590, H, CHs, F, PhO, CFs), (M-2591, H' CHs, F, PhO, Br), (M-2592, H, CHs, F, PhO, CHs), (M-2593, H, CH3) F, BnO, H), (M-2594, H, CHs, F, BnO, CI),
(M-2595, H, CH3) F, BnO, F), (M-2596, H, CHs, F, BnO, CFs), (M-2597, H, CHs, F, BnO, Br), (M-2598, H， CHs, F, BnO, CHs), (M-2599, H， CHs, F' PI1CH2CH2O, H), (M-2600, H, CHs, F, PhCH2CH20, CI), (M-2601, H, CHs, F, PI1CH2CH2O, F), (M-2602, H， CH3, F, PhCH2CH20; CFs), (M-2603, H, CH3, F， PI1CH2CH2O, Br), (M-2604, H, CHs, F, PI1CH2CH2O, CH3)，（M-2605, H, CHs, F, CF30, H), (M-2606, H, CHs, F, CFsO, CI), (M-2607, H, CH3, F， CFsO, F), (M-2608, H， CHs, F, CF3O, CFa), (M-2609, H, CH3 ; F, CFsO, Br), (M-2610, H, CHs, P, CFsO, CHs), (M-2611, H, CH3; F， Ph, H), (M-2612, H, CHs, P, Ph, CI), (M-2613, H, CHs, F, Ph, F), (M-2614, H, CH3, F' Ph, GF3), (M-2615, H, CHs, F, Ph, Br), (M-2616, H, CHs, F, Ph, CHs), (M-2617, H, CH3) F, 4-F-Ph, H), (M-2618, H, CHs, F, 4-F-Ph, CI),
(M-2619, H, CHs, F, 4-F-Ph, F), (M-2620, H, CHs, F, 4-F-Ph, CFs), (M-2621, H, CH3; F, 4-F-Ph, Br), (M-2622, H, CHs, F, 4-F-Ph, CHs), (M-2623, H, CH3) F, 4-CFa-Pli, H), (M-2624, H, CH3, F, 4-CF3-Ph, CI), (M-2625, H， CHs, F, 4- CF3- P , F), (M-2626, H, CH3; F, 4-CPVPh, CFs), (M-2627, H, CHs, F, 4-CF3-Pli, Br), (M-2628, H, CHs, F， 4-CFs-Pli, CH3), (M-2629, H, CHs, F, 4-(Me)2N-Ph, H), (M-2630, H, CHs, F, 4-(Me)2N-Ph, CI), (M-2631, H, CH3, F, 4- (Me)2N-Ph, F), (M-2632, H, CHs, F, 4- (Me)2N-Ph, CF3), (M-2633, H, CHs, F, 4- (Me)2N-Ph, Br), (M-2634, H, CH3) F, 4- (Me)2N-Ph; CHs), (M-2635, H, CHs, F, 4-OH-Ph, H), (M- 2636, H, CHs, F, 4-OH-Ph, CI) , (M-2637, H， CH3, F, 4-OH-Ph, F), (M-2638, H， CHs, F, 4- OH-Ph, CFs), (M-2639, H, CHs, F, 4- OH-Ph, Br), (M-2640, H, CH3, F, 4-OH-Ph, CHs), (M-2641, H, CHs, F; 3, 4-di-F-Ph, H), (M-2642, H, CH3， F, 3, 4-di-F-Pli, CI), (M-2643, H， CHs, F, 3, 4-di-F-Pli, F) , (M-2644, H, CHs, F， 3, 4-di-F-Ph, CFs), (M-2645, H， CHs, F, 3, 4-di-F-Ph, Br), (M-2646, H, CHs, F， 3, 4-di-F-Ph, CHs), (M-2647, H, CHs, F, 4- CO OH-Ph, H), (M-2648, H, CH3, F, 4- CO OH-Pli, CI), (M-2649, H, CHs, F, 4- CO OH-Pli, F), (M-2650, H, CHs, F， 4- COOH-Ph, CFs), (M-2651, H, CHs, F, 4- COOH-Ph, Br), (M-2652, H, CHs, F, 4- COOH-Ph, CHs), (M-2653, H, CHs, P, Bn, H), (M-2654, H, CH3 ) F, Bn, CI), (M-2655, H, CH3, F, Bn, F)， (M-2656, H, CHs, F， Bn, CFs), (M-2657, H, CHs, F, Bn, Br); (M-2658, H, CHs, P, Bn, CH3), (M-2659, H, C F, 4-F-Bn, H), (M-2660, H, CHs, F, 4-F-Bn, CI), (M-2661, H, CHs, F, 4-F-Bn, F)， (M-2662, H, CH3; F, 4-F-Bn, CFs), (M-2663, H, CHs, F, 4-F-Bn, Br), (M-2664, H, CHs, F, 4-F-Bn, CH3), (M-2665, H, CH3, F, 2-Py, H), (M-2666, H, CHs, F, 2-Py, CI), (M-2667, H, CHs, F, 2-Py, F), (M-2668, H, CHs, F, 2-Py, CFs), (M- 2669, H, CHs, F, 2-Py, Br), (M-2670, H, CHs, F, 2-Py, CHs), (M-2671, H， CHs, F, 3-Py, H), (M-2672, H， CH3) F, 3-Py, CI), (M-2673, H, CH3, F, 3-Py, F), (M-2674, H, CH3, F, 3-Py, CF3), (M-2675, H, CH3) F, 3-Py, Br), (M-2676, H, CHs, F, 3-Py, CHs), (M-2677, H, CHs, F, 4-Py, H), (M-2678, H, CHs, F, 4-Py, CI), (M-2679, H, CHs, F, 4-Py, F), (M- 2680, H, CHs, E,- 4-Py, CFs), (M-2681, H, CHs, F, 4-Py, Br), (M-2682, H, CHs, F, 4-Py, CH3), (M-2683, H, CH3, P, 2-Th, H), (M-2684, H, CHs, F, 2-Th, CI), (M- 2685, H, CH3, F, 2-Th, F), (M-2686, H, CHs, F, 2-Th, CFs), (M-2687, H, CHs, F, 2-Th, Br), (M-2688, H, CHs, F, 2-Th, CH3) , (M-2689, H, CHs, F, 3-Tli, H) , (M- 2690, H, CH3; F, 3-Th, CI), (M-2691, H; CHs, F, 3 -Th, F), (M-2692, H, CHs, F, 3-Th, CFs), (M-2693, H, CH3, F， 3-T , Br), (M-2694, H, CHs, F, 3-Th， CHs), (M-2695, H, CHa, F, pyrazol-2-yl, H), (M-2696, H, CHs, F, pyrazol-2-yl, CI), (M-2697, H, CHs, F, pyrazol-2-yl, F), (M-2698, H, CHs, F, pyrazol-2-yl, CF3), (M-2699, H, CH3, F, pyrazol-2-yl, Br), (M-2700, H, CH3, F, pyrazol-2-yl, CHs), (M-2701, H, CHs, F, pyrazol-3-yl, H)， (M-2702, H, CH3, F， pyrazol-3-yl, CI), (M-2703, H, CHs, F, pyrazol-3-yl, F), (M-2704, H, CH3, F, pyrazol-3-yl, CFs), (M-2705, H, CH3) F, pyrazol-3-yl, Br), (M-2706, H, CHs, F, pyrazol-3-yl, CH3), (M-2707, H, CHs, F, pyrimidin-2-yl, H); (M-2708, H, CHs, F, pyrimidin-2-yl, CI), (M-2709, H, CHs, F, pyrimidin-2-yl, F), (M-2710, H， CHs, F, pyrimidin-2-yl, CF3), (M-2711, H, CH3) F, pyrimidin-2-yl, Br), (M-2712, H, CH3, F，
pyrimidin-2-yl, CH3), (M-2713, H, CH3; F, pyrimidin-4-yl, H), (M-2714, H' CHa, F, pyrimidin-4-yl, CI), (M-2715, H, CH3> F, pyrimidin-4-yl, F)， (M-2716, H, CH3; F, pyrimidin-4-yl, CFa), (M-2717, H, CHs, F, pyrimidin-4-yl, Br), (M-2718, H, CHs, F, pyrimidin-4-yl, CHs), (M-2719, H， CH3) F, pyrimidin-5-yl, H), (M-2720, H， CHs, F, pyrimidin-5-yl, CI), (M-2721, H' CHs, F, pyrimidm-5-yl, F), (M-2722, H， CHs, F, pyrimidin-5-yl, CPs), (M-2723, H, CH3, F, pyrimidm-5-yl, Br), (M- 2724, H, CH3> F, pyrimidin-5-yl, CH3), (M-2725, H, CHs, F, HOOCCH2CH2CH2, H), (M-2726, H, CHs, F, HOOCCH2CH2CH2, CI), (M-2727, H, CHs, F,
HOOCCH2CH2CH2; F), (M-2728, H, CHs, F, HOOCCH2CH2CH2， CFs), (M-2729, H, CH3) F, HOOCCH2CH2CH2, Br), (M-2730, H， CHs, F, HOOCCH2CH2CH2, CHs), (M-2731, H, CH3, F, HOOCCH2CH2CH2CH2, H)， (M-2732, H, CHs, F, HOOCCH2CH2CH2CH2; CI), (M-2733, H, CH3) F, HOOCCH2CH2CH2CH2, F), (M-2734, H' CH3, F, HOOCCH2CH2CH2CH2, CFs), (M-2735, H, CHa, F,
HOOCCH2CH2CH2CH2, Br), (M-2736, H, CHs, F, HOOCCH2CH2CH2CH2, CHs), (M-2737, H, CHs, F, (Me)2NCOCH2CH2CH2CH2, H), (M-2738, H, CH3, F, (Me)2NCOCH2CH2CH2CH2, CI), (M-2739, H, CH3, F, (Me)2NCOCH2CH2CH2CH2， F), (M-2740, H, CH3， F, (Me)2NCOCH2CH2CH2CH2, CFs), (M-2741, H， CH3, P, (Me)2NCOCH2CH2CH2CH2, Br), (M-2742, H, CHs, F, (Me)2NCOCH2CH2CH2CH2， CH3), (M-2743, H, CHa, F,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-2744, H, CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-2745, H, CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-2746, H, CH3) F，
(Me)2NCOCH2CH2CH2CH2CH2, CF3), (M-2747, H， CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2， Br), (M-2748, H, CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2, CHa), (M-2749, H, CHs, F, MeOCH2， H)， (M- 2750, H, CHa, F, MeOCH2; CI), (M-2751, H, CHs, F, MeOCH2) F), (M-2752, H, CHs, P, MeOCHa, CFs), (M-2753, H, CH3, F, MeOCH2, Br), (M-2754, H, CHs, F, MeOCHa, CHa), (M-2755, H, CH3, F, EtOCH2, H), (M-2756, H, CHs, F, EtOCHa, CI), (M-2757, H, CHa, F, EtOCH2, F), (M-2758, H, CHs, F, EtOCH2， CPs), (M- 2759, H, CHs, F, EtOCH2; Br), (M-2760, H, CHs, F, EtOCHs, CHs), (M-2761, H， CH3) F' EtOCH2CH2; H), (M-2762, H, CH3; F, EtOCH2CH2; CI), (M-2763, H, CHs, P, EtOCH2CH2) F), (M-2764, H, CHs, F, EtOCH2CH2, CFs), (M-2765, H, CHs, F, EtOCH2CH2, Br), (M-2766, H, CH3, F, EtOCH2CH2, CHs), (M-2767, H, CHs, F, MeOCH2CH2OCH2CH2; H), (M-2768, H, CH3, F， MeOCH2CH2OCH2CH2, CI), (M-2769, H, CH3, F, MeOCH2CH2OCH2CH2, F), (M-2770, H， CHs, F, MeOCH2CH2OCH2CH2, CFs), (M-2771, H, CH3, F, MeOCH2CH2OCH2CH2) Br), (M-2772, H, CHs, F, MeOCHsCHsOCEbCH ' CHa), (M-2773, H， CHs, F,
MeOCH2CH2, H)， (M-2774, H, CH8> F， MeOCH2CH2) CI), (M-2775, H, CHs, F， MeOCHaCHs, F), (M-2776, H, CH3, F, MeOCH2CH2, CF3), (M-2777, H, CHs, F, MeOCH2CH2， Br), (M-2778, H, CHa, F' MeOCH2CH2, CHs), (M-2779, H, CHs, F, HOCH2, H)， (M-2780, H, CHs, F, HOCH2, CI), (M-2781, H, CHs, P, HOCH2) F)， (M-2782, H, CH3, F, HOCH2, CPs), (M-2783, H, CHs, F, HOCH2, Br), (M-2784, H, CHs, F, HOCH2) CHs), (M-2785, H, CHs, F, HOCH2CH2, H), (M-2786, H， CHs, F, HOCH2CH2, CI), (M-2787, H, CHs, F, HOCH2CH2) F), (M-2788, H， CH3, F, HOCHaCHa, CFs), (M-2789, H, CH3, F， HOCH2CH2) Br), (M-2790, H, CHs, F, HOCH2CH2, CHs), (M-2791, H， CH3; F, HOCH2CH2CH2, H), (M-2792, H， CH3, F, HOCHaCHsCHa, CI), (M-2793, H, CHs, F, HOCH2CH2CH2; F), (M-2794, H, CHs, F, HOCH2CH2CH2) CF3)， (M-2795, H, CHs, F, HOCH2CH2CH2, Br), (M-2796, H, CH3, F, HOCH2CH2CH2, CH3), (M-2797, H, CH3, F, HOCH2CH2CH2CH2; H), (M-2798, H， CHs, F, HOCH2CH2CH2CH2, CI), (M-2799, H, CH3, F,
HOCH2CH2CH2CH2) F), (M-2800, H, CHs, F, HOCH2CH2CH2CH2, CF3), (M- 2801, H, CHs, F, HOCH2CH2CH2CH2) Br), (M-2802, H, CHs, F,
HOCH2CH2CH2CH2) CHs), (M-2803, H, CH3, F, HOCHsCHsCHsCHsCHs, H), (M-2804, H, CHs, F， HOCH2CH2CH2CH2CH2, CI), (M-2805, H, CH3, F,
HOCH2CH2CH2CH2CH2) F), (M-2806, H, CH3, F; HOCHsCHbCHsCH CE , CFs), (M-2807, H, CHs, F, HOCH2CH2CH2CH2CH2, Br), (M-2808, H' CH3) F,
HOCH2CH2CH2CH2CH2, CHs), (M-2809, H, CH3, F, HOCH2CH2OCH2CH2, H), (M-2810, H, CHs, F, HOCH2CH2OCH2CH2l CI), (M-2811, H, CHs, F,
HOCH2CH2OCH2CH2, F), (M-2812/ H, CH3) F, HOCH2CH2OCH2CII2, CFs), (M-2813, H, CHs, F, HOCH2CH2OCH2CH2, Br), (M-2814, H, CHs, F,
HOCH2CH2OCH2CH2, CH3), (M-2815, H, CHs, F, (Me)2N, H), (M-2816, H, CH3, F, (Me)2N, CI), (M-2817, H, CH3, F, (Me)aN, F), (M-2818, H, CHs, F, (Me)2N, CFs), (M-2819, H， CH3, F， (Me)2N, Br), (M-2820, H, CH3, F, (Me)2N; CHs), (M-2821, H, CHs, F, piperidm-4-.yl-metliyl, H), (M-2822, H, CHs, F, piperidin- 4-yレ methyl, . CI), (M-2823, H' CH3) F, piperidin-4-yレ methyl, F), (M-2824, H, CHs, F, piperidin-4-yl-methyl, CFs), (M-2825, H, CHs, P; piperidin-4-yl-metliyl, Br), (M-2826, H, CH3) F， piperidin-4-yl-methyl, CHs), (M-2827, H, CHs, F, cyclohexylmethyl, H), (M-2828, H, CH3, P, cyclohexylmethyl, CI), (M-2829, H, CH3, F, cyclohexylmethyl, F); (M-2830, H， CH3> F, cyclohexylmethyl, CFs), (M-2831, H, CHs, F, cyclohexylmethyl, Br), (M-2832, H, CHs, F,
cyclohexylmethyl, CH3), (M-2833, H, CHs, Cl, H, H), (M-2834, H, CH3, Cl, H, Cl), (M-2835, H, CH3> Cl, H, F)， (M-2836, H, CH3) Cl, H, CFs), (M-2837, H, CH3; Cl, H, Br), (M-2838, H, CHs, Cl, H, CHs), (M-2839, H, CH3> Cl, F, H), (M-2840, H, CH3, Cl, F, Cl), (M-2841, H, CH3) Cl, F, F), (M-2842, H, CH3, Cl, F, CF3), (M-2843, H, CH3) Cl, F, Br), (M-2844, H, CH3) Cl, F, CHs), (M-2845, H, CH3, Cl, Cl, H), (M-2846, H, CH3, Cl, Cl, Cl), (M-2847, H, CHs, Cl, Cl, F), (M-2848, H, CHs, Cl, Cl, CFs), (M-2849, H， CHs, Cl, Cl, Br), (M-2850, H, CH3, Cl, Cl, CHs), (M-2851, H, CHs, Cl, CH3, H), (M-2852, H, CH3, Cl, CHs, Cl), (M-2853, H, CH3) Cl, CH3) F), (M-2854, H, CHs, Cl, CHs, CFs), (M-2855, H, CH3; Cl, CH3) Br), (M-2856, H, CH3, Cl, CH3, CH3), (M-2857, H, CHs, Cl, Et, H), (M-2858, CH3, Cl, Et, Cl), (M-2859, H, CH3) Cl, Et, F), (M-2860, H， CH3) Cl, Et, CFs), (M-2861, H, CHs, Cl, Et, Br), (M-2862, H, CHs, Cl, Et, CHs), (M-2863, H, CHs, Cl, n-Pr, H), (M-2864, H， CH3, Cl, n-Pr, Cl), (M-2865, H， CH3) Cl, n-Pr, F), (M-2866, H, CH3; Cl, n-Pr, CFs), (M-2867, H, CH3) Cl, n-Pr, Br), (M-2868, H, CHs, Cl, n-Pr, CH3), (M-2869, H, CHs, Cl, c-Pr, H), (M-2870, H, CH3, Cl, c-Pr, Cl), (M-2871, H, CH3, Cl, c-Pr, F), (M-2872, H, CHs, Cl, c-Pr, CFs), (M-2873, H, CHs, Cl, c-Pr, Br), (M-2874, H, CHs, Cl, c-Pr, CHs), (M-2875, H, CHs, Cl, i-Pr, H)， (M-2876, H, CH3, Cl, i-Pr, Cl), (M-2877, H, CHs, Cl, i-Pr; F), (M-2878, H, CHs, Cl, i-Pr, CFs), (M-2879, H, CHs, Cl, i-Pr, Br), (M-2880, H, CHs, Cl, i-Pr, CH3)， (M-2881, H, CHs, .Cl, n-Bu, H), (M-2882, H, CH3, Cl, n-Bu, Cl), (M-2883, H, CHs, Cl, n-Bu; F), (M-2884, H, CH3, Cl, n-Bu, CFs), (M-2885, H, CH3, Cl, n-Bu, Br), (M-2886, H, CHs, Cl, n-Bu, CHs), (M-2887, H, CHs, Cl, i-Bu, H), (M-2888, H, CH3; Cl, i-Bu, Cl), (M-2889, H, CHs, Cl, i-Bu, F), (M-2890, H， CHs, Cl, i-Bu, CFs), (M-2891, H, CHs, Cl, i-Bu, Br), (M-2892, H, CH3, Cl, i-Bu, CH3), (M-2893, H, CHs, Cl, sec- Bu, H), (M-2894, H, CH3; CI, sec-Bu, CI), (M-2895, H, CH3' CI, sec-Bu, F), (M-2896, H, CHs, CI, sec-Bu, CFs), (M-2897, H, CHs, CI, sec-Bu, Br), (M-2898, H, CHs, CI, sec-Bu, CHs), (M-2899, H, CHs, CI, n-Pen, H), (M-2900, H， CH3) CI, n-Pen, CI), (M-2901, H, CHs, CI, n-Pen, F), (M-2902, H, CH3> CI, n-Pen, CFs), (M-2903, H, CHa, CI, n-Pen, Br), (M-2904, H, CH3, CI, n-Pen, CHs), (M-2905, H, CHs, CI, c-Pen, H)， (M-2906, H, CHs, CI, c-Pen, CI), (M-2907, H, CH3, CI, c-Pen, F), (M-2908, H, CHs, CI, c-Pen, CFs), (M-2909, H， CHs, CI, c-Pen, Br), (M-2910, H, CHs, CI, c-Pen, CH3), (M-2911, H, CHs, CI, n-Hex, H), (M-2912, H, CH3j CI, n-Hex, CI), (M-2913, H, CH3) CI, n-Hex, F), (M-2914, H, CHs, CI, n-Hex, CF3), (M-2915, H, CHs, CI, n-Hex, Br), (M-2916, H， CH3> CI, n-Hex, CH3), (M-2917, H, CHs, CI, c-Hex, H); (M-2918, H, CHs, CI, c-Hex, CI), (M-2919, H, CHs, CI, c-Hex, F), (M-2920, H, CHs, CI, c-Hex, CF3)， (M-2921, H, CHs, CI, c-Hex, Br), (M-2922, H, CHs, CI, c-Hex, CH3), (M-2923, H, CHs, CI, OH, H), (M-2924, H, CH3, CI, OH, CI), (M-2925, H, CHs, CI, OH, F), (M-2926, H, CHs, CI, OH, CF3), (M-2927, H, CH3, CI, OH, Br), (M-2928, H， CH3, CI, OH, CH3), (M-2929, H, CHs, CI, EtO, H)， (M-2930, H, CHs, CI, EtO, CI), (M-2931, H, CHs, CI, EtO, F), (M-2932, H， CH3, CI, EtO, CFs), (M-2933, H， CHs, CI, EtO, Br), (M-2934, H, CHs, CI, EtO, CHs), (M-2935, H, CH3, CI, n-PrO, H), (M-2936, H, CHs, CI, n-PrO, CI), (M-2937, H, CHs, CI, n-PrO, F), (M-2938, H, CH3, CI, n-PrO, CFs), (M-2939, H, CHs, CI, n- PrO, Br), (M-2940, H, CHs, CI, n-PrO, CH3), (M-2941, H， CH3, CI, PhO, H),
(M-2942, H, CHs, CI, PhO, CI), (M-2943, H, CHs, CI, PhO, F)， (M-2944, H, CHs, CI, PhO, CFs), (M-2945, H, CH3> CI, PhO, Br), (M-2946, H, CH3, CI, PhO, CH3), (M-2947, H, CHs, CI, BnO, H), (M-2948, H, CHs, CI, BnO, CI), (M-2949, H, CHs, CI, BnO, F), (M-2950, H, CH3, CI, BnO, CF3), (M-2951, H, CH3, CI, BnO, Br), (M-2952, H, CHs, CI, BnO, CHs), (M-2953, H; CHs, CI, PhCHaCHsO, H); (M- 2954, H, CHs, CI, PhCH2CH20, CI), (M-2955, H, CHs, CI, PhCH2CH20, F), (M-2956, H, CHs, CI, PhCHsCHzO, CFs), (M-2957, H, CHs, CI, PhCHsCHsO, Br), (M-2958, H, CHs, CI, PhCHsCH O, CH3); (M-2959, H, CH3) CI, CF30; H)， (M- 2960, H， CHs, CI, CFsO, CI), (M-2961, H, CH3, CI, CP30, F), (M-2962, H, CHs, CI, CFsO, CFs), (M-2963, H, CHs, CI, CFsO, Br), (M-2964, H, CHs, CI, CFaO, CH3), (M-2965, H, CHs, CI, Ph, H)， (M-2966, H, CHs, CI, Ph, CI), (M-2967, H, CHs, CI, Fh, F), (M-2968, H, CHs, CI, Ph, CFs), (M-2969, H, CH3; CI, Ph, Br), (M-2970, H; CHs, CI, Ph, CHs), (M-2971, H, CHs, CI, 4-F-Ph, H), (M-2972, H, CHs, CI, 4-F- Ph, CI), (M-2973, H, CHa, CI, 4-F-Ph, F), (M-2974, H， CH3, CI, 4-F-Ph, CFs), (M-2975, H, CHs, CI, 4-F-Ph, Br), (M-2976, H, CHs, CI, 4-F-Ph, CHs), (M-2977, H, CHs, CI, 4-CFs-Pli, H), (M-2978, H， CHs, CI, 4-CFs-Ph, CI), (M-2979, H, CHs, CI, 4-CFs-Pli, F), (M-2980, H, CHs, CI, 4-CPs-Pli, CF3), (M-2981, H, CHs, CI, 4-CF3-P11, Br), (M-2982, H, CHs, CI, 4-CFs-Ph, CH3), (M-2983, H， CH3, CI, - (Me)2N-Ph, H), (M-2984, H, CH3, CI, 4-(Me)2N-Ph, CI), (M-2985, H， CH3, CI, 4-(Me)2N-Ph, F), (M-2986, H, CHs, CI, 4-(Me)2N-Pli) CFs), (M-2987, H， CHs, CI, 4-(Me)2N-Ph, Br), (M-2988, H, CH3, CI, 4-(Me)2N-Pli, CHs), (M-2989, H, CH3, CI, 4-OH-Ph, H), (M-2990, H, CHs, CI, 4-OH-Ph, CI), (M-2991, H, CHs, CI, 4- OH-Ph; F), (M-2992, H, CH3, CI, 4-OH-Ph, CFs), (M-2993, H, CHs, CI, 4-OH-Ph, Br), (M-2994, H, CHs, CI, 4-OH-Ph, CHs), (M-2995, H, CH3, CI, 3,4-di-F-Ph, H), (M-2996, H, CHs, CI, 3,4-di-F-Ph, CI), (M-2997, H, CHs, CI, 3,4-di-F-Ph, F); (M-2998, H, CHs, CI, 3,4-di-F-Ph, CFs), (M-2999, H, CH3， CI, 3,4-di-F-Ph, Br), (M-3000, H, CHs, CI, 3,4-di-F-Pli, CHs), (M-3001, H, CH3, CI, 4-COOH-Ph, H), (M-3002, H, CHs, CI, 4-COOH-Ph, CI), (M-3003, H, CHs, CI, 4-COOH-Ph, F), (M-3004, H, CH3, CI, 4-COOH-Ph, CFs), (M-3005, H, CH3, CI, 4-COOH-Ph, Br), (M-3006, H, CHs, CI, 4-COOH-Ph, CHs), (M-3007, H, CHs, CI, Bn, H), (M-3008, H, CHs, CI, Bn, CI), (M-3009, H, CH3, CI, Bn, F), (M-3010, H， CHs, CI, Bn, CF3)， (M-3011, H, CHs, CI, Bn, Br), (M-3012, H, CH3, CI, Bn, CHs), (M-3013, H, CHs, CI, 4-F-Bn, H), (M-3014, H， CH3, CI, 4-F-Bn, CI), (M-3015, H, CH3, CI, 4-F-Bn, F)，（M-3016, H; CHs, CI, 4-F-Bn, CF3), (M-3017, H, CHs, CI, 4-F-Bn, Br), (M- 3018, H， CHs, CI, 4-F-Bn, CHs), (M-3019, H, CHs, CI, 2-Py, H), (M-3020, H, CH3, CI, 2-Py, CI), (M-3021, H, CHs, CI, 2-Py, F), (M-3022, H, CHs, CI, 2-Py, CFs), (M-3023, H, CHs, CI, 2-Py, Br), (M-3024, H, CH3, CI, 2-Py, CHs), (M-3025, H, CH3, CI, 3-Py, H), (M-3026, H, CHs, CI, 3-Py, CI), (M-3027, H, CHs, CI, 3-Py, F), (M-3028, H, CHs, CI, 3-Py, CF3)， (M-3029, H, CHs, CI, 3-Py, Br), (M-3030, H, CHs, CI, 3-Py, CHs), (M-3031, H, CHs, CI, 4-Py, H), (M-3032, H, CHs, CI, 4-Py' CI), (M-3033, H, CHs, CI, 4-Py, F), (M-3034, H, CHs, CI, 4-Py, CFa), (M-3035, H, CHs, CI, 4-Py, Br), (M-3036, H, CHs, CI, 4-Py, CHs), (M-3037, H, CHs, Cl， 2-Th, H), (M-3038, H, CHs, CI, 2-Th, CI), (M-3039, H, CHs, CI, 2-Th, F), (M-3040, H, CH3; CI, 2-Th, CFs), (M-3041, H, CH3, CI, 2-Th, Br), (M-3042, H， CH3, CI, 2-Th, CHs), (M-3043, H, CHs, CI, 3-Th, H), (M-3044, H, CHs, CI, 3-Th, CI), (M-3045, H, CHs, CI, 3-Th, F), (M-3046, H, CHs, CI, 3-Th, CF3), (M-3047, H, CH3) CI, 3-Th, Br), (M-3048, H, CHs, CI, 3-Th, CH3)，（M-3049, H, CH3) CI, pyrazol-2-yl, H), (M-3050, H, CHs, CI, pyrazol-2-yl, CI), (M-3051, H, CHs, CI, pyrazol-2-yl, F), (M-3052, H, CHs, CI, pyrazol-2-yl, CFs), (M-3053, H， CHs, CI, pyrazol-2-yl, Br), (M-3054, H， CHs, CI, pyrazol-2-yl, CHs), (M-3055, H, CHs, CI, pyrazol-3-yl' H), (M-3056, H, CHs, CI, pyrazol-3-yl, CI), (M-3057, H, CHs, CI, pyrazol-3-yl, F), (M-3058, H, CHs, CI, pyrazol-3-yl, CFs), (M-3059, H， CHs, CI, pyrazol-3-yl, Br), (M-3060, H, CHs, CI, pyrazol-3-yl, CHs), (M-3061, H, CHs, CI, pyrimidin-2-yl, H), (M-3062, H, CH3), CI, pyrimidin-2-yl, CI), (M-3063, H, CHs, CI, pyrimidin- . 2-yl, F), (M-3064, H, CHs, CI, pyrimidin-2-yl, CF3), (M-3065, H, CH3) CI, pyrimidin-2-yl, Br), (M-3066, H, CHs, CI, pyrimidin-2-yl, CHs), (M-3067, H， CH3) CI, pyrimidin-4-yl, H), (M-3068, H, CHs, CI, pyrimidin-4-yl, CI), (M-3069, H, CHs, CI, pyrimidin-4-yl, F), (M-3070, H, CH3, CI, pyrimidin-4-yl, CPs), (M- 3071, H, CHs, CI, pyrimidin-4-yl, Br), (M- 3072, H, CHs, CI, pyrimidin-4-yl, CHs), (M-3073, H, CHs, CI, pyrimidin-5-yl, H)， (M-3074, H, CH3, CI, pyrimidin-5-yl, CI), (M- 3075, H, CHs, CI, pyrimidin-5-yl, F), (M-3076, H, CH3, CI, pyrimidin- 5-yl; CF3), (M-3077, H, CH3， CI, pyrimidin-5-yl, Br), (M-3078, H, CHs, Cl， pyrimidin-5-yl, CH3), (M-3079, H, CH3, Cl， HOOCCH2CH2CH2, H), (M-3080, H, CHs, CI, HOOCCH2CH2CH2, CI), (M-3081, H, CH3) CI,
HOOCCH2CH2CH2, F), (M-3082, H, CH3, CI, HOOCCHaCHaCHs, CFs), (M- 3083, H, CHs, CI, HOO CCH2CH2CH2, Br), (M-3084, H, CH3, CI, HOOCCH2CH2CH2, CHs), (M-3085, H， CH3, CI, HOOCCHsCK CHsCHs, H)' (M-3086, H, CHs, CI, HOOCCH2CH2CH2CH2, CI), (M- 3087, H, CH3, CI, HOOCCH2CH2CH2CH2, F), (M-3088, H' CHs, CI, HOO CCHsCHsCHsCHs, CF3), (M-3089, H' CH3, CI, HOOC CH2 CH2CH2 CH2, Br), (M-3090, H， CHs, CI, HOOCCH2CH2CH2CH2， CHs), (M-3091, H， CHs, CI, (Me)2NCOCH2CH2CH2CH2， H), (M-3092, H, CHs, CI, (Me)2NCOCH2CH2CH2CH2) CI), (M-3093, H, CH3, CI,
(Me)2NCOCH2CH2CH2CH2， F), (M-3094, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2, CFs), (M-3095, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2, Br), (M- 3096, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2) CHs), (M-3097, H, CH3, CI,
(Me)2NCO CH2 CHs CH2 CH2 CH2; H), (M-3098, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2， CI), (M-3099, H, CH3, CI,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-3100, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CF3), (M-3101, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-3102, H, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-3103, H, CH3, CI, MeOCH2) H), (M- 3104, H, CHs, CI, MeO CH2, CI), (M-3105, H, CH3j CI, MeOCHa, F), (M-3106, H, CHs, CI, MeOCHs, CFs), (M-3107, H, CHs, CI, MeO CHa, Br), (M-3108, H, CHs, CI, MeOCH2, CHs), (M-3109, H， CHs, CI, EtOCHa, H), (M-3110, H, CH3, CI, EtOCH2, CI), (M-3111, H, CHs, CI, EtOCH2, F), (M-3112, H, CH3, CI, EtOCH2, CFs), (M-3113, H， CHs, CI, EtOCH2) Br), (M-3114, H, CH3, CI, EtOCH2, CHs), (M-3115, H, CH3) CI, EtOCH2CH2; H), (M-3116, H, CH3) CI, EtOCH2CH2, CI), (M-3117, H, CHs, CI, EtOCH2CH2) F), (M-3118, H, CH3, CI, EtOCH2CH2, CFs), (M-3119, H, CHs, CI, EtOCHaCHa, Br), (M-3120, H, CHs, CI, EtOCHsCHs, CHs), (M-3121, H, CHs, CI, MeOCH2CH20CH2CH2, H), (M-3122, H, CHs, CI,
MeOCH2CH20CH2CH2; CI), (M-3123, H， CH3, CI, MeOCH2CH20CH2CH2, F), (M-3124, H, CH3, CI, MeOCH2CH2OCH2CH2, CFs), (M-3125, H, CHs, CI, MeOCH2CH2OCH2CH2) Br), (M-3126, H, CHa, Cl， MeOCH2CH2OCH2CH2, CHs), (M-3127, H, CHs, CI, MeOCHaCHa, H), (M-3128, H， CH3> CI, MeOCH2CH2; CI), (M-3129, H, CH3) CI, MeOCH2CH2) F), (M-3130, H， CHs, CI, MeOCH2CH2, CF3), (M-3131, H, CHs, CI, MeOCH2CH2, Br), (M-3132, H, CHs, CI, MeOCH2CH2; CHs), (M-3133, H， CHs, CI, HOCHa, H), (M-3134, H, CH3) CI, HOCH2, CI), (M-3135, H, CHs, CI, HOCH2, F), (M-3136, H， CHs, CI, HOCH2, CFs), (M-3137, H, CH3) CI, HOCH2, Br), (M-3138, H, CH3, CI, HOCH2) CHs), (M-3139, H, CHs, CI, HOCH2CH2, H), (M-3140, H， CH3) CI, HOCH2CH2, CI), (M-3141, H, CHs, CI, HOCHaCHs, F), (M-3142, H, CHs, CI, HOCH2CH2, CFs), (M-3143, H, CHs, CI, HOCH2CH2, Br), (M-3144, H, CH3, CI, HOCH2CH2, CHs), (M-3145, H, CH3, CI, HOCH2CH2CH2; H), (M-3146, H, CH3, CI, ΗΟΟΗ2ΟΗ2ΟΗ2; CI), (M-3147, H, CHs, CI, HOCH2CH2CH2, F), (M-3148, H, CH3, CI, ΗΟΟΗ2ΟΗ2ΟΗ2) CPs), (M- 3149, H; CHs,. CI, HOCH2CH2CH2) Br), (M-3150, H, CHs, CI, HOCH2CH2CH2, CHs), (M-3151, H, CHa, CI, HOCH2CH2CH2CH2, H), (M-3152, H, CHs, CI, HOCH2CH2CH2CH2, CI), (M-3153, H, CHs, CI, HOCH2CH2CH2CH2, F), (M-3154, H, CH3) CI, HOCH2CH2CH2CH2) CF3), (M-3155, H, CHs, CI,
HOCH2CH2CH2CH2, Br), (M-3156, H， CHs, CI, HOCH2CH2CH2CH2, CHs), (M- 3157, H, CHs, CI, HOCH2CH2CH2GH2CH2， H)' (M-3158, H, CH3, CI,
HOCH2CH2CH2CH2CH2, CI), (M-3159, H, CHs, CI, HOCH2CH2CH2CH2CH2, F)， (M-3160, H, CH3) CI, HOCH2CH2CH2CH2CH2, 6F3), (M-3161, H, CHs, CI, HOCH2CH2CH2CH2CH2) Br), (M-3162, H, CH3, CI, HOCH2CH2CH2CH2CH2， CH3), (M-3163, H, CHs, CI, HOCH2CH2OCH2CH2; H), (M-3164, H, CHs, CI, HOCH2CH2OCH2CH2, CI), (M-3165, H, CH3; CI, HOCH2CH2OCH2CH2, F), (M- 3166, H, CHs, CI, HOCH2CH20CH2CH2， CFs), (M-3167, H, CHs, CI,
HOCHaCHaOCHaCHa, Br), (M-3168, H, CHs, CI, HOCH2CH2OCH2CH2, CHs), (M-3169, H, CHs, CI, (Me)2N, H), (M-3170, H， CHs, CI, (Me)2N, CI), (M-3171, H, CHs, CI, (Me)2N, F), (M-3172, H， CHs, CI, (Me N, CFs), (M-3173, H, CH3, CI, (Me)aN, Br), (M-3174, H, CHs, CI, (Me)2N, CHs), (M-3175, H, CHs, CI, piperidin-4-yl-metliyl, H), (M-3176, H, CH3, CI, piperidin-4-yl-methyl, CI), (M-3177, H, CH3) CI, piperidin-4-yレ methyl' F), (M-3178, H, CH3) CI, piperidm-4-yl-methyl, CFs), (M-3179, H, CHs, CI, piperidin-4-yl-metliyl, Br), (M-3180, H, CHs, CI, piperidin-4-yl-metliyl, CHs), (M-3181, H， CHs, CI, cyclohexylmethyl, H), (M-3182, H, CHs, CI, cyclohexylmethyl, CI), (M-3183, H, CHs, CI, cyclohexylmethyl, F), (M-3184, H, CHs, CI, cyclohexylmethyl, CPs), (M-3185, H， CH3, CI, cyclohexylmethyl, Br), (M-3186, H, CH3, CI,
cyclohexylmethyl, CHs), (M-3187, F, H, H, H, H)， (M-3188, F, H, H, H, CI), (M-3189, MeO, F， H, H, CFa), (M-3190, MeO, F， F, H, CFs), (M-3191, F, H, H， H， Br), (M-3192, F, H, H, H, CH3)， (M-3193, F, H, H, F, H), (M-3194, F, H， H, F, CI), (M-3195, F, H, H, F, F), (M-3196, F, H, H， ,F, CF3), (M-3197, F, H, H, F, Br), (M-3198, F, H, H, F, CH3), (M-3199, F, H, H, CI, H), (M-3200, MeO, F, H, H, n-Pr), (M-3201, F, H, H, CI, F), (M-3202, F, H, H， CI, CFs), (M-3203, F， H, H, CI, Br), (M-3204, F, H, H, CI, CHs), (M-3205, F, H, H, CH3, H), (M-3206, F, H, H, CHs, CI), (M-3207, F, H, H, CHs, F), (M-3208, F, H， H, CHs, CFs), (M-3209, F, H， H, CH3, Br), (M-3210, F, H, H, CHs, CHs), (M-3211, F, H, H, Et, H), (M-3212, F， H, H, Et, CI), (M-3213, F, H, H, Et, F), (M-3214, F， H, H, Et, CFs), (M- 3215, F, H, H, Et, Br), (M-3216, F， H， H, Et, CHs), (M-3217, F, H, H, n-Pr, H), (M-3218, F, H, H, n-Pr, CI), (M-3219, F, H, H, n-Pr, F), (M-3220, F, H, H, n-Pr, CFs), (M-3221, F, H' H， n-Pr, Br), (M-3222, F, H, H, n-Pr, CH3), (M-3223, F, H, H, c-Pr, H), (M-3224, F, H, H, c-Pr, CI), (M-3225, F, H, H， c-Pr, F), (M-3226, F, H, H, c-Pr, CFs), (M-3227, F, H, H, c-Pr, Br), (M-3228, F, H, H, c-Pr, CHs), (M- 3229, F, H, H, i-Pr, H), (M-3230, F, H, H, i-Pr, CI), (M-3231, F， H, H, i-Pr, F), (M-3232, F, H， H, i-Pr, CFs), (M- 3233, F, H， H, i-Pr, Br), (M-3234, F, H, H, i- Pr, CH3), (M-3235, F, H, H， n-Bu, H)， (M- 3236, F, H, H, n-Bu, CI), (M-3237, F， H, H, n-Bu, F), (M-3238, F, H， H, n-Bu, CFs), (M- 3239, F, H, H, n-Bu, Br), (M-3240, F, H, H, n-Bu, CHs), (M-3241, F, H, H, i-Bu, H), (M-3242, F' H, H, i-Bu, CI), (M-3243, F, H, H, i-Bu, P), (M-3244, F， H, H, i-Bu, CFs), (M-3245, F, H, H, i-Bu, Br), (M-3246, F， H, H, i-Bu, CHs), (M-3247, F, H, H, sec-Bu, H), (M- 3248, F, H, H， sec-Bu' CI), (M-3249, F, H, H, sec-Bu, F)， (M-3250, F, H, H， sec-Bu, CF3), (M-3251, F, H, H, sec-Bu, Br), (M-3252, F, H, H, sec-Bu, CHs), (M- 3253, F, H, H, n-Pen, H), (M-3254, F, H, H, n-Pen, CI), (M-3255, F, H, H, n-Pen, F), (M-3256, F, H, H, n-Pen, CFs), (M-3257, F, H， H, n-Pen, Br), (M-3258, F, H, H, n-Pen, CHs), (M-3259, F, H, H' c-Pen, H), (M-3260, F, H, H, c-Pen, CI), (M-3261, F, H, H, c-Pen, F), (M-3262, F, H, H, c-Pen, CFs), (M-3263, F, H, H, c-Pen, Br), (M-3264, F, H' H, c-Pen, CHs), (M- 3265, F, H, H, n-Hex, H), (M-3266, F, H， H, n-Hex, CI), (M-3267, F, H， H, n-Hex, F), (M-3268, F, H, H， n-Hex, CF3), (M-3269, F, H, H, n-Hex, Br), (M- 3270, F, H, H, n-Hex, CHs), (M-3271, F, H， H， c-Hex, H), (M-3272, P, H， H, c-Hex, CI), (M-3273, F, H, H, c-Hex, F), (M-3274, F, H' H, c-Hex, CFs), (M- 3275, F, H, H, c-Hex, Br), (M-3276, F, H, H, c-Hex, CHs), (M-3277, F, H, H, OH, H), (M-3278, F, H, H, OH, CI), (M-3279, F, H, H, OH, F), (M-3280, F, H, H, OH, CFs), (M-3281, F, H, H, OH, Br), (M-3282, F, H, H, OH, CH3); (M-3283, F, H, H, EtO, H), (M-3284, F, H， H， EtO, CI), (M-3285, F, H, H, EtO, F), (M-3286, F, H, H' EtO, CFs), (M-3287, F, H, H, EtO, Br), (M-3288, F, H, H, EtO, CHs), (M-3289, F, H， H, n-PrO, H)， (M-3290, F， H, H， n-PrO, CI), (M-3291, F， H, H, n-PrO, F), (M-3292, F, H, H, n-PrO, CFs), (M-3293, F, H, H， n-PrO, Br), (M-3294, F, H, H, n-PrO, CHs), (M-3295, F, H, H, PhO, H), (M-3296, F, H, H, PhO, CI), (M-3297, F, H, H, PhO, F)， (M-3298, F, H, H, PhO, CFs), (M-3299, F, H, H, PhO, Br), (M-3300, F, H, H, PhO, CH3)， (M-3301, P, H, H， BnO, H), (M-3302, F, H, H, BnO, CI), (M-3303, F, H, H, BnO, F), (M-3304, F, H， H， BnO, CF3), (M-3305, F, H， H, BnO, Br), (M-3306, F, H, H， BnO, CHs), (M- 3307, F, H, H， PI1CH2CH2O, H), (M-3308, F, H, H, PI1CH2CH2O, CI), (M-3309, F, H, H, PhCH2CH2。, F), (M-3310, F, H， H， PhCH2CH20; CFs), (M-3311, F, H, H, PhGH CHsO, Br), (M-3312, F, H， H, PhCH2CH20, CHs), (M-3313, MeO, H, H, CF30, CH3), (M-3314, F, H, H, CFaO, CI), (M-3315, F, H, H, CPsO, F), (M-3316, F， H, H, CF3O, CFs), (M-3317, F, H, H, CFsO, Br), (M-3318, F， H, H， GFsO, CH3), (M-3319, F, H, H, Ph, H), (M-3320, F, H' H, Ph, CI), (M-3321, F, H, H, Ph, F), (M-3322, F， H, H, Ph; CFs), (M-3323, F, H, H, Ph; Br), (M-3324, F, H, H, Ph, CHs), (M-3325, F, H, H, 4-F-Ph, H)' (M-3326, F, H, H， 4-F-Ph, CI), (M-3327, F, H, H， 4-F-Ph, F), (M-3328, F， H， H, 4-F-Ph, CFs), (M-3329, F, H, H, 4-F-Ph, Br), (M-3330, F, H, H, 4-F-Ph, CH3), (M-3331, F, H, H, 4-CFs-Pli, H), (M-3332, F, H, H, 4-CFs-Pli, CI), (M-3333, F, H, H, 4-CFs-P , F), (M-3334, F; H， H, 4-CFs-Ph, CFs), (M-3335, F， H, H, 4-CF3-Ph, Br), (M-3336, F, H, H， 4-CF3-Ph, CHs), (M- 3337, F, H, H, 4-(Me)2N-Ph, H)， (M-3338, F, H, H, 4-(Me)2N-Ph, CI), (M-3339, F， H, H, 4-(Me)2N-Ph; F), (M-3340, F, H, H, 4-(Me)2N-Pli) CFs), (M-3341, F, H, H, 4-(Me)2N-Ph, Br), (M-3342, F, H, H, 4-(Me)2N-Ph, CHs), (M-3343, F, H， H, 4- OH-Ph, H), (M-3344, F, H, H, 4-OH-Ph, CI), (M-3345, F, H, H, 4-OH-Pli, F), (M-3346, F， H， H, 4-OH-Ph, CFs), (M-3347, F, H, H, 4-OH-Ph, Br), (M-3348, F, H， H, 4-OH-Ph, CHs), (M-3349, F, H, H, 3,4-di-F-Ph, H), (M-3350, F, H, H， 3,4-di-F-Ph, CI), (M-3351, F, H, H, 3,4-di-F-Ph, F), (M-3352, F, H, H， 3,4-di- F-Ph, CFs), (M-3353, F, H, H, 3,4-di-F-Ph, Br), (M-3354, F, H, H, 3,4-di-F-Ph, CHs), (M-3355, F, H, H, 4-COOH-Ph, H), (M-3356, F; H， H， 4-COOH-Ph, CI), (M-3357, F, H, H, 4-COOH-Ph, F)， (M-3358, F, H， H， 4-COOH-Ph, CFs), (M- 3359, F, H, H, 4-COOH-Ph, Br), (M-3360, F, H, H, 4-COOH-Ph, CHs), (M-3361, F, H, H, Bn, H), (M-3362, F, H, H, Bn, CI), (M-3363, F， H, H, Bn, F), (M-3364, F, H, H, Bn, CFs), (M-3365, F, H, H, Bn, Br), (M-3366, F, H， H， Bn, CH3), (M- 3367' F， H, H, 4-F-Bn, H), (M-3368, F， H， H， 4-F-Bn, CI), (M-3369, F， H， H, 4- F-Bn, F), (M-3370, F， H, H， 4-F-Bn, CFs), (M-3371, F, H, H, 4-F-Bn, Br), (M- 3372, F, H, H, 4-F-Bn, CH3), (M-3373, F, H, H, 2-Py, H), (M-3374, F, H, H, 2- Py, CI), (M-3375, F， H, H, 2-Py, F), (M-3376, F, H, H, 2-Py, CFs), (M-3377, F， H, H, 2-Py, Br), (M-3378, F, H, H， 2-Py, CHs), (M-3379, F, H, H, 3-Py, H)， (M-3380, F, H, H, 3-Py, CI), (M-3381, F, H, H, 3-Py, F), (M-3382, F, H, H, 3-Py, CF3), (M-3383, F, H, H, 3-Py, Br), (M-3384, F， H, H, 3-Py, CHs), (M-3385, F, H, H， 4-Py, H), (M-3386, F, H, H, 4-Py, CI), (M-3387, F, H, H, 4-Py, F), (M-3388, F, H, H， 4-Py, CFs), (M-3389, F, H, H, 4-Py, Br), (M-3390, F， H, H, 4-Py, CHs), (M- 3391, F， H, H, 2-Th, H), (M-3392, P, H, H, 2-Th, CI), (M-3393, F， H, H, 2-Th, F), (M-3394, F, H, H, 2-Th, CFs), (M-3395, F, H, H， 2-Th, Br), (M-3396, F, H, H， 2-Th, CH3), (M-3397, F, H, H, 3-Th, H), (M-3398, F， H, H, 3-Th, CI), (M-3399, F， H, H' 3-Th, F), (M-3400, F, H， H, 3-Th, CFs), (M-3401, F, H, H, 3-Th, Br), (M- 3402, F, H, H, 3-Th, CHs), (M-3403, F, H, H, pyrazol-2-yl, H), (M-3404, F, H, H, pyrazoレ 2-yl， CI), (M-3405, F, H, H, pyrazol-2-yl, F), (M-3406, F, H, H, pyrazol-2-yl, CFs), (M-3407, F, H, H, pyrazol-2-yl, Br), (M-3408, F, H, H, pyrazol-2-yl, CHs), (M-3409, F, H, H, pyrazol-3-yl, H)， (M-3410, F, H, H, pyrazol-3-yl, CI), (M-3411, F, H, H, pyrazol-3-yl, F); (M- 3412, F, H, H, pyrazol- 3-yl, CFs), (M- 3413, F, H, H, pyrazol-3-yl, Br), (M-3414, F, H, H, pyrazol- 3-yl, CHs), (M-3415, F, H, H, pyrimidin-2-yl, H), (M-3416, F, H, H, pyrimidin-2-yl, CI), (M-3417, F, H, H, pyrimidin-2-yl, F), (M- 3418, F, H, H, pyrimidin-2-yl, CFs), (M-3419, F, H, H, pyrimidin-2-yl, Br), (M-3420, F, H, H， pyrimidin-2-yl; CHs), (M-3421, F, H, H, pyrimidin-4-yl, H), (M-3422, F, H, H, pyrimidin-4-yl, CI), (M-3423, F, H, H, pyrimidin-4-yl, F)， (M-3424, F， H, H, pyrimidin-4-yl; CFs), (M-3425, F, H, H， pyrimidin-4-yl, Br), (M-3426, F, H, H, pyrimidin-4-yl, CHs), (M-3427, F, H， H, pyrimidin-5-yl, H), (M-3428, F, H, H, pyrimxdin-5-yl, CI), (M-3429, F, H, H, pyrimidin-5-yl, F), (M-3430, F, H, H, pyrimidin-5-yl, CF3); (M-3431, F, H, H, pyrimidin-5-yl, Br), (M-3432, F, H, H, pyrimidin-5-yl, CHs), (M-3433, F, H' H, HOO CCH2CH2CH2, H)， (M- 3434, F, H' H, HOO CCH2CH2CH2, CI), (M-3435, F, H, H， HOOCCH2CH2CH2) F)， (M- 3436, F, H, H, HOO CCH2CH2CH2, CFs), (M-3437, F, H, H, HOO CCH2CH2CH2) Br), (M-3438, F， H, H, HOOCCH2CH2CH2) CHs), (M-3439, F, H, H,
HOOCCHaCHaCHaCHa, H), (M-3440, F, H, H, HOOCCH2CH2CH2CH2, CI), (M- 3441, F, H, H, HOO CCH2CH2CH2CH2, F), (M-3442, F, H， H，
HOO CCH2CH2CH2CH2) CFs), (M-3443, F, H, H, HOOCCH2CH2CH2CH2; Br), (M-3444, F, H, H, HOOCCH2CH2CH2CH2, CH3), (M-3445, F, H, H,
(Me)2NCO CH2CH2CH2CH2> H), (M-3446, F, H, H, (Me)2NCO CH2CH2CH2CH2, CI), (M-3447, F, H, H, (Me)2NCO CH2CH2CH2CH2, P), (M-3448, F, H, H, (Me)2NCOCH2CH2CH2CH2, CFs), (M-3449, F, H, H, (Me NCOCH CHsCHsCHs, Br), (M- 3450, F, H, H, (Me)2NCO CH2CH2CH2CH2, CHs), (M-3451, F, H, H, (Me)2NCOCH2CH2CH2CH2CH2) H), (M-3452, F, H, H,
(Me)2NCO CH2CH2CH2CH2CH2> CI), (M- 3453, F, H, H,
(Me)2NCOCH2CH2GH2CH2CH2， F), (M-3454, F， H, H, (Me)2NCO CH2CH2GH2CH2CH2, CF3), (M-3455, F, H, H,
(Me)2NCO CH2CH2CH2CH2CH2， Br), (M-3456, F, H, H,
(Me)2NCOCH2CH2CH2CH2CH2， CH3), (M- 3457, F, H, H， MeO CH2, H), (M-3458, F, H, H, MeOCH2, CI), (M-3459, F, H, H, MeO CHa, F), (M-3460, F, H, H, MeOCH2, CF3)，（M-3461, F, H' H， MeOCH2， Br), (M-3462, F, H, H, MeO CHs, CH3), (M-3463, F, H, H, EtOCH2, H), (M-3464, F, H, H, EtOCH2> CI), (M-3465, F, H, H, EtO CH2, F), (M- 3466, F, H, H， EtOCHs, CFs), (M-3467, F, H, H， EtOCH2, Br), (M-3468, F, H, H, EtO CH2, CH3), (M-3469, F， H, H, EtOCH2CH2; H), (M-3470, F， H' H, EtO CH2CH2> CI), (M-3471, F' H, H, EtO CH2CH2) F), (M-3472, F, H, H, EtOCH2CH2) CFs), (M- 3473, F, H, H, EtOCH2CH2' Br), (M- 3474, F， H, H, EtOCH2CH2) CH3), (M-3475, F, H, H, MeOCH2CH2OCH2CH2, H), (M-3476, F, H， H, MeOCH2CH2OCH2CH2， CI), (M-3477, F， H, H,
MeO CH2CH2O CH2CH2, F), (M-3478, F, H, H, MeOCH2CH20CH2CH2, CF3), (M-3479, F, H, H, MeOCH2CH2OCH2CH2, Br), (M-3480, F, H, H,
MeOCH2CH2O CH2CH2, CHs), (M-3481, F， H, H, MeOCH2CH2, H), (M-3482, F, H， H, MeOCH2CH2, CI), (M-3483, F, H, H, MeOCH2CH2) F), (M-3484, F, H, H, MeOCH2CH2) CFs), (M-3485, F, H, H, MeOCH2CH2, Br), (M-3486, F, H, H， MeOCH2CH2, CH3), (M-3487, F, H, H, HOCH2) H), (M-3488, F， H, H， HO CHs, CI), (M-3489, F, H, H, HOCH2, F), (M-3490, F' H， H, HOCH2, CFs), (M-3491, F, H, H, HO CH2, Br), (M-3492, F, H, H, HOCH2, CHs), (M- 3493, F, H, H,
HOCH2CH2) H), (M- 3494, F, H, H, HOCH2CH2, CI), (M-3495, F, H, H,
HO CH2CH2, F), (M-3496, F, H, H, HOCH2CH2, CFs), .(Mr3497, F, H, H, HOCH2CH2) Br), (M-3498, F, H, H, HOCH2CH2, CH3), (M-3499, P, H, H, HOCH2CH2CH2) H), (M- 3500, F, H, H, HOCH2CH2CH2, Cl)， (M-3501, F， H, H, HO CH2CH2CH2, F), (M-3502, F, H, H, HOCH2CH2CH2, CFs), (M-3503, F, H, H, HOCH2CH2CH2, Br), (M-3504, F, H, H, HO CH2CH2CH2, CH3), (M-3505, F, H， H, HOCH2CH2CH2CH2, H), (M-3506, F; H, H, HOCH2CH2CH2CH2) CI), (M-3507, F, H， H， HOCH2CH2CH2CH2， F), (M-3508, F， H, H, HOCH2CH2CH2CH2, CFs), (M-3509, F, H， H， HOCH2CH2CH2CH2, Br), (M-3510, F， H, H,
HOCH2CH2CH2CH2, CHs), (M-3511, F, H， H, HOCH2CH2CH2CH2CH2， H), (M- 3512, F, H， H， HOCH2CH2CH2CH2CH2, CI), (M-3513, F, H, H,
HOCH2CH2CH2CH2CH2, F), (M-3514, F, H, H, HOCH2CH2CH2CH2CH2, CF3), (M-3515, F, H， H, HOCH2CH2CH2CH2CH2, Br), (M-3516, F, H, H,
HOCH2CH2CH2CH2CH2, CHs), (M-3517, F, H, H, HOCH2CH2OCH2CH2, H), (M-3518, F, H, H, HOCH2CH2OCH2CH2, CI), (M-3519, F， H, H，
HOCH2CH2OCH2CH2) F), (M-3520, F, H, H, HOCH2CH2OCH2CH2， CFs), (M- 3521, F, H, H， HOCH2CH2OCH2CH2, Br), (M-3522, F, H, H，
HOCH2CH20CH2CH2) CHs), (M-3523, F, H, H, (Me)2N, H)' (M-3524, F, H， H, (Me)2N, CI), (M-3525, F, H， H， (Me)2N, F), (M-3526, F, H， H, (Me)2N' CF3), (M-3527, F, H， H, (Me)2N, Br), (M-3528, F, H, H, (Me)2N, CH3)， (M-3529, F， H, H, piperidin-4-yl-methyl, H), (M-3530, F, H, H， piperidin-4-yl-methyl, CI),
(M-3531, F, H, H, piperidin-4-yl-metliyl, F), (M-3532, F, H, H， piperidin-4-yl- methyl, CFs), (M-3533, F, H, H, piperidm-4-yl-methyl, Br), (M-3534, F, H, H, piperidm-4-yl-methyl, CHs), (M-3535, F, H, H， cyclohexylmethyl, H), (M-3536, F, H, H' cyclohexylmethyl, CI), (M-3537, F, H, H, cyclohexylmethyl, F), (M- 3538, F, H, H， cyclohexylmethyl, CFs), (M-3539, F, H， H, cyclohexylmethyl, Br), (M-3540, F, H， H, cyclohexylmethyl, CHs), (M-3541, F, H' F, H, H), (M-3542, F, H, F, H, CI), (M-3543, F; H, F, H, F), (M-3544, F, H, F, H, CFs), (M-3545, F, H, F, H, Br), (M.-3546, F, H, F, H, CHs), (M-3547, F, H, F, F, H), (M-3548, F, H, F, F' CI), (M-3549, F, H, F, F, F), (M-3550, F, H, F, F, CFs), (M-3551, F, H' F, F, Br), (M-3552, F, H, F, F, CHs), (M-3553, F, H, F, CI, H), (M-3554, F, H, F, CI, CI), (M-3555, F, H, F, CI, F), (M-3556, F, H， F, Cl， CF3), (M-3557, F, H, F, CI, Br), (M-3558, F' H, F, CI, CH3), (M-3559, F, H， F, CHs, H), (M- 3560, F, H, F, CHs, CI), (M-3561, F， H， F, CHs, F), (M-3562, F, H， F, CHs, CFs), (M-3563, F, H, F, CHs, Br), (M-3564, F, H, F, CH3, CHs), (M- 3565, F, H, F, Et, H), (M-3566, F, H, F, Et, CI), (M-3567, F, H, F, Et, F), (M-3568, F, H, F, Et, CF3), (M-3569, F, H， F， Et, Br), (M- 3570, P, H， F, Et, CHs), (M- 3571, F, H， F, n-Pr, H), (M-3572, F, H, F, n-Pr, CI), (M- 3573, F, H, F, n-Pr, F), (M-3574, F, H, F, n-Pr, CFs), (M-3575, F， H, P, n-Pr, Br), (M-3576, F, H, F, n-Pr, CHs), (M-3577, F, H, P, c-Pr, H)， (M-3578, F, H, F, c-Pr, CI), (M- 3579, F, H' F， c-Pr, F), (M- 3580, F, H, F， c-Pr, CFa), (M-3581, F, H, F, c-Pr, Br), (M-3582, F， H, F, c-Pr, CHs), (M-3583, F, H, F, i-Pr, H), (M-3584, F, H, F, i-Pr, CI), (M-3585, F, H, F, i-Pr, F), (M-3586, F, H, F, i-Pr, CFs), (M-3587, F, H, F, i-Pr, Br), (M-3588, F, H, F, i-Pr, CHs), (M-3589, F, H, F' n-Bu, H), (M-3590, F, H, F, n-Bu, CI), (M-3591, F, H, F, n-Bu, F), (M-3592, F, H, F, n-Bu, CFs), (M-3593, F, H, F, n-Bu, Br), (M- 3594, F, H, F, n-Bu, CH3), (M-3595, F, H, F, i-Bu, H), (M-3596, F, H, F， i-Bu, CI), (M- 3597, F, H, F, i-Bu, F), (M-3598, F， H, F, i-Bu, CFs), (M-3599, F, H, F, i-Bu, Br), (M-3600, F， H, F' i-Bu, CHs), (M-3601, F, H， F, sec-Bu, H), (M-3602, F, H, F, sec-Bu, CI), (M- 3603, F, H, F, sec-Bu, F), (M-3604, F, H, F, sec-Bu, CFs), (M-3605, F, H, F, sec-Bu, Br), (M-3606, F, H, F, sec-Bu, CH3), (M-3607, F, H, F, n-Pen, H), (M-3608, F, H, F, n-Pen, CI), (M-3609, F; H, F, n-Pen; F), (M-3610, F, H, F, n-Pen, CF3)， (M-3611, F, H, F, n-Pen, Br), (M-3612, P, H, F, n-Pen, CHs), (M-3613, F' H, F, c-Pen, H), (M-3614, F， H, F, c-Pen, CI), (M-3615, F， H, P, c-Pen, F), (M- 3616, F, H, F, c- Pen, CFs), (M-3617, F， H, F, c-Pen; Br), (M-3618, F, H, F, c-Pen, CH3), (M-3619, F, H, F, n-Hex, H), (M- 3620, F, H, F, n-Hex, CI), (M-3621, F, H, F; n-Hex, F), (M-3622, F, H, F, n-Hex, CF3), (M-3623, F, H， F, n-Hex, Br), (M-3624, F, H, F, n-Hex, CHs), (M- 3625, F, H, F, c-Hex, H), (M-3626, F, H, F， c-Hex, CI), (M- 3627, F, H, F, c-Hex, F)， (M-3628, F, H, F， c-Hex, CFs), (M-3629, F, H, F; c-Hex, Br), (M-3630, F, H, F' c-Hex, CHs), (M-3631, F, H, F, OH, H), (M-3632, F, H, F' OH, CI), (M-3633, F, H, F, OH, F), (M-3634, F, H, F, OH, CF3), (M-3635, F, H， F, OH, Br), (M-3636, F, H, F, OH, CH3), (M-3637, F， H, F, EtO, H), (M-3638, F, H, F, EtO, CI), (M-3639, F, H， F, EtO, P); (M-3640, F, H, F, EtO, CFs), (M-3641, F, H， P, EtO, Br), (M-3642, F, H， F, EtO, CH3), (M-3643, F, H, F, n-PrO, H), (M-3644, F, H, F, n-PrO, CI), (M-3645, F, H, F， n-PrO, F)， (M-3646, F, H, F， n-PrO, CF3), (M-3647, F， H, F, n-PrO, Br), (M-3648, F, H, F, n-PrO, CHs), (M-3649, P, H, F, PhO, H), (M-3650, F; H, F, PhO, CI), (M-3651, F， H; F, PhO, F), (M-3652, F, H, F, PhO, CF3), (M-3653, F， H, F, PhO, Br), (M-3654, F, H, F, PhO, CH3), (M-3655, F, H， F, BnO, H)' (M-3656, F， H, F, BnO, CI), (M-3657, F, H, F, BnO, F), (M- 3658, F， H, F, BnO, CFs), (M-3659, F, H, F, BnO, Br), (M-3660, F, H, F, BnO, CHs), (M-3661, F, H, F， PhCH2CH2。, H), (M-3662, F; H, F, PhCH2CH20, CI), (M-3663, P, H, F, PhCH2CH20; F), (M-3664, F, H， F, PI1CH2CH2O, CF3), (M- 3665, F, H， F， PhCH2CH20, Br), (M-3666, F, H, F, PhCH2CH20, CHs), (M-3667, F, H， F, CFsO, H), (M-3668, F, H， F, CFsO, CI), (M-3669, F， H, F, CFsO, F)， (M-3670, F, H, F, CFsO, CFs), (M-3671, F, H, F, CF3O, Br), (M-3672, F, H, F, CFsO, CHs), (M-3673, F, H, F, Ph, H), (M-3674, F, H， F， Ph, CI), (M-3675, F， H， F, Ph, F), (M-3676, F, H, F; Ph, CF3), (M-3677, F, H, F, Ph, Br), (M-3678, F, H, P, Ph, CHs), (M-3679, F, H, F, 4-F-Ph, H), (M-3680, F, H, F, 4-F-Ph, CI), (M- 3681, F, H, F; 4-F-Ph, F), (M-3682, F, H, F, 4-F-Ph, CFs), (M-3683, F, H， F, 4- F-Ph, Br), (M-3684, F， H, F, 4-F-Ph, CHs), (M-3685, F, H, F, 4-CP3-Pli, H), (M-3686, F, H, F， 4-CFa-Pli, CI), (M-3687, F， H, F, 4-CF3-Ph, F), (M-3688, F, .H, F, 4-CFs-Ph, CFs), (M-3689, F, H, F, 4-CFs-P , Br), (M-3690, F, H, F, 4-CF3-Ph, CHs), (M-3691, F， H, F, 4-(Me)2N-Ph) H), (M-3692, F, H, F, 4-(Me)2N-Ph) CI), (M-3693, F, H, F, 4-(Me)2N-Ph, P), (M-3694, F, H, F, 4-(Me)2N-Ph, CFs), (M- 3695, F, H， F, 4-(Me)2N-Ph, Br), (M-3696, F, H, F， 4-(Me)2N-Ph; CHs), (M-3697, F, H, F， 4-OH-Ph, H), (M-3698, F, H, F, 4-OH-Ph, CI), (M-3699' F, H, F， 4- OH-Ph, F), (M-3700, F, H, F, 4-OH-Ph, CFs), (M- 3701, F, H, F， 4-OH-Ph, Br), (M-3702, F, H, F, 4-OH-Ph, CHs), (M-3703, F, H, F, 3, 4-di-F-Pli, H), (M-3704, F, H, F, 3, 4-di-F-Pli, CI), (M-3705, F, H, F, 3, 4-di-F-Pli, F), (M-3706, F, H, F， 3, 4-di-F-Ph, CF3), (M-3707, F， H, F, 3' 4-di-F-Ph' Br), (M-3708, F, H, F, 3, 4-di- F-Ph, CHs), (M-3709, F， H, F, 4-COOH-Ph, H), (M-3710, F, H, F, 4-COOH-Ph, CI), (M-3711, F, H, F, 4-COOH-Ph, F), (M-3712, F, H， F, 4-COOH-Ph, CFs), (M-3713, F, H, P, 4-COOH-Ph, Br), (M-3714, F， H, F， 4-COOH-Pli, CHs), (M- 3715, P, H, F, Bn, H), (M-3716, F, H, F, Bn, CI), (M-3717, F, H, F, Bn, F), (M- 3718, F, H, F, Bn, CF3), (M-3719, F, H, F, Bn, Br), (M-3720, F, H, F, Bn, CHs), (M-3721, F, H， F, 4-F-Bn, H), (M-3722, F, H, F, 4-F-Bn, CI), (M-3723, F, H, F， 4-F-Bn, F), (M-3724, F, H, F, 4-F-Bn, CF3), (M-3725, F, H, F, 4-F-Bn, Br), (M- 3726, F, H, F, 4-F-Bn, CHs), (M- 3727, F, H, F, 2-Py, H), (M-3728, F, H, F, 2-Py, CI), (M-3729, F, H， F, 2-Py, F), (M-3730, F， H, F, 2-Py, CF3), (M-3731, F, H, F, 2-Py, Br), (M- 3732, F, H, F, 2-Py, CHs), (M-3733, F, H， F， 3-Py, H), (M-3734, F, H, F， 3-Py, CI), (M-3735, F, H, F, 3-Py, F)， (M-3736, F, H, F, 3-Py, CFs), (M-3737, F, H, F, 3-Py, Br), (M-3738, F, H, F， 3-Py, CH3), (M- 3739, F, H, F, 4-Py, H), (M-3740, F, H， P, 4-Py, CI), (M-3741, F， H, F, 4-Py, F), (M-3742, F, H, F, 4-Py, CFs), (M-3743, F, H, F, 4-Py, Br), (M-3744, F, H, F, 4-Py, CH3), (M-3745, F, H， F, 2-Th, H), (M-3746, F, H, F, 2-Th, CI), (M-3747, F, H， F, 2-Th, F), (M-3748, F, H, F, 2-Th, CFs), (M-3749, F, H, F, 2-Th, Br), (M-3750, F, H, F, 2-Th, CHs), (M-3751, F, H, F, 3-Th, H), (M-3752, F, H, .F' , 3-Tli, CI), (M-3753, F, H, F, 3-Th, F), (M-3754, F, H, F, 3-Th, CF3), (M-3755, F, H， F, 3-Th, Br), (M-3756, F， H, F, 3-Th, CHs), (M-3757, F, H, F, pyrazol-2-yl, H)， (M- 3758, F, H, F, pyrazol-2-yl, CI), (M-3759, F, H, F, pyrazol-2-yl, F), (M-3760, F, H, F, pyrazol-2-yl, CFs), (M-3761, F, H， F, pyrazol-2-yl, Br), (M-3762, F, H, P, pyrazol-2-yl, CHs), (M- 3763, F, H, F' pyrazol-3-yl, H), (M-3764, F, H, F, pyrazol-3-yl, CI), (M-3765, F' H， F, pyrazol-3-yl, F), (M-3766, F, H, F, pyrazol-3-yl, CFs), (M-3767, F, H, P, pyrazol-3-yl, Br), (M-3768, F, H， F, pyrazol-3-yl, CHs), (M-3769, F， H， F, pyrimidin-2-yl, H), (M-3770, F, H, F, pyrimidin-2-yl, CI), (M-3771, F, H, F, pyrimidin-2-yl, F), (M-3772, F, H， F, pyrimidin-2-yl, CFs), (M-3773, F， H, F， pyrimidin-2-yl, Br), (M-3774, F, H, F, pyrimidin-2-yl, CHs), (M-3775, F, H, F, pyrimidin-4-yl, H)， (M-3776, F, H, F, pyrimidin-4-yl, CI), (M-3777, F, H, F, pyrimidin-4-yl, F), (M-3778, F, H, F, pyrimidin-4-yl, CFs), (M-3779, F, H, F, pyrimidin-4-yl, Br), (M-3780, F, H, F， pyrimidin-4-yl, CHs), (M-3781, F, H， F， pyrimidin-5-yl, H), (M-3782, F, H， F, pyrimidin-5-yl, CI), (M-3783, F, H， F, pyrimidin-5-yl, F), (M-3784, F, H, F, pyrimidin-5-yl, CFs), (M-3785, F, H, F, pyrimidm-5-yl, Br), (M-3786, F, H, F, pyrimidin-5-yl, CHs), (M-3787, F, H, F, HOOCCH2CH2CH2, H)' (M-3788, F, H， F, HOOCCH2CH2CH2, CI), (M-3789, F' H, F; HOOCCH2CH2CH2; F)， (M-3790, F， H, F, HOOCCH2CH2CH2, CF3), (M- 3791, F, H' F, HOOCCH2CH2CH2, Br), (M-3792, F, H, F, HOOCCH2CH2CH2, CHs), (M-3793, F, H, F, H 00 C CHs CH2 CH2 CH2, H), (M-3794, F, H, F,
HOOCCH2CH2CH2CH2, CI), (M-3795, F, H, F, HOOCCH2CH2CH2CH2; F), (M- 3796, F, H; F, HOOCCH2CH2CH2CH2; CF3), (M-3797, P, H, F,
HOOCCH2CH2CH2CH2, Br), (M-3798, F, H， F， HOOCCH2CH2CH2CH2, CH3)， (M-3799, F， H, F, (Me)2NCOCH2CH2CH2CH2, H), (M-3800, F, H, F,
(Me)2NCOCH2CH2CH2CH2, CI), (M-3801, F, H, F, (Me)2NCOCH2CH2CH2CH2， F), (M-3802, .F; H, F, (Me)2NCOCH2CH2CH2CH2， CFs), (M-3803, P, H， F， (Me)2NCOCH2CH2CH2CH2, Br), (M-3804, F' H， F, (Me)2NCOCH2CH2CH2CH2, CHs), (M-3805, F， H, F, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-3806, F, H, F, (Me)2NCOCH2CH2CH2CH2CH2, CI), (M-3807, F, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, F); (M-3808, F, H, F, (Me)2NCOCH2GH2CH2CH2CH2, CF3), (M-3809, F, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-3810, F, H, F,
(Me)2NCOCH2CH2CH2CH2CH2， CH3), (M-3811, F, H, F, MeOCH2, H), (M-3812, F, H, F, MeOCH2, CI), (M-3813, F, H, F, MeOCHa, F), (M-3814, F, H, F, MeOCH2; CFs), (M-3815, F, H, F, MeOCH2, Br), (M-3816, F, H, F, MeOCH2, CH3), (M-3817, F, H, F, EtOCH2, H), (M-3818, F, H, F, EtOCHa, CI), (M-3819, F, H, F， EtOCH2, F), (M-3820, F, H, F, EtOCH2; CFs), (M-3821, F, H， F， EtOCHa, Br), (M-3822, F, H, F, EtOCH2, CH3), (M-3823, F, H, F, EtOCH2CH2; H), (M- 3824, F, H, F, EtOCH2CH2, CI), (M-3825, F, H, F, EtOCH2CH2, F), (M-3826, F, H, F, EtOCH2CH2, CF3), (M-3827, P, H, F, EtOCH2CH2, Br), (M-3828, F, H, F, EtOCH2CH2, CH3), (M-3829, F, H, F, MeOCH2CH2OCH2CH2, H), (M-3830, F, H, F， MeOCH2CH20CH2CH2, CI), (M-3831, F, H, F, MeOCH2CH20CH2CH2, F); (M-3832, F, H, F, MeOCH2CH2OCH2CH2, CF3)， (M-3833, F, H, F,
MeOCH2CH20CH2CH2) Br), (M-3834, F' H, F， MeOCH2CH2OCH2CH2, CH3), (M-3835, F， H, F, MeOCH2CH2, H), (M-3836, F, H, F, MeOCH2CH2, CI), (M- 3837, F, H, F, MeOCH2CH2, F), (M-3838, F' H, F, MeOCH2CH2, CF3), (M-3839, F, H, F, MeOCH2CH2, Br), (M-3840, F, H, F, MeOCH2CH2) CHs), (M-3841, F, H, F, HOCH2, H)' (M-3842, F, H, F, HOCH2, CI), (M-3843, F, H, F， HOCH2, F)， (M-3844, F, H, F, HOCH2, CF3)，（M-3845, F, H， F, HOCH2, Br), (M-3846, F, H, F, HOCH2, CHs), (M-3847, F, H, F, HOCH2CH2, H), (M-3848, F, H, F,
HOCH2CH2) CI), (M-3849, F, H, F, HOCH2CH2, F), (M-3850, F, H, F,
HOCH2CH2, CF3), (M-3851, P, H, F， HOCH2CH2, Br), (M-3852, F, H, F, HOCH2CH2) CHs), (M-3853, P, H, F, HOCH2CH2CH2, H), (M-3854, F, H， F, HOCH2CH2CH2, CI), (M-3855, F, H, F, HOCH2CH2CH2, F), (M-3856, F, H, F, HOCH2CH2CH2, CFs), (M-3857, F, H, F, HOCH2CH2CH2, Br), (M-3858, F, H, F, HOCH2CH2CH2， CH3), (M-3859, F, H, F, HOCH2CH2CH2CH2, H), (M-3860, F, H, F, HOCH2CH2CH2CH2; CI), (M-3861, F， H' F, HOCH2CH2CH2CH2' F)， (M-3862, P, H, F, HOCH2CH2CH2CH2, CFs), (M-3863, F, H, F， HOCH2CH2CH2CH2> Br), (M-3864, F, H, F, HOCH2CH2CH2CH2) CH3), (M-3865, P, H, F,
HOCH2CH2CH2CH2CH2， H), (M-3866, F, H, F, HOCH2CH2CH2CH2CH2, CI), (M-3867, F, H, F, HOCHsCHsCHsCH CHs, F), (M-3868, F, H, F,
HOCH2CH2CH2CH2CH2, CF3), (M-3869, F, H, F, HOCHsCHaCHsCHsCHs, Br), (M-3870, F, H, F， HOCH2CH2CH2CH2CH2, CH3), (M-3871, F, H, F，
HOCH2CH20CH2CH2; H), (M-3872, F， H, F, HOCH2CH2OCH2CH2, CI), (M-3873, P, H， F, HOCH2CH2OCH2CH2, F), (M-3874, F, H, F, HOCH2CH2OCH2CH2, CFs), (M-3875, F, H, F， HOCH2CH2OCH2CH2, Br), (M-3876, F, H, F，
HOCH2CH2OCH2CH2, CHs), (M-3877, F, H, F, (Me)sN, H), (M-3878, F, H, F, (Me)2N, CI), (M-3879, F, H, F, (Me)2N, F), (M-3880, F, H, F, (Me)2N, CFs), (M-3881, F， H' F, (Me)2N, Br), (M-3882, F, H, F, (Me)2N, CHs), (M-3883, F, H, F, piperidin-4-yl-methyl, H), (M-3884, F, H, F, piperidin-4-yl-metliyl, CI), (M- 3885, F， H, F, piperidin-4-yl-metliyl, F), (M-3886, F, H, F, piperidin-4-yl- methyl, CFs), (M-3887, F, H, F, piperidin-4-yl-methyl, Br), (M-3888, F, H, F， piperidin-4-yl-metliyl, CHs), (M-3889, F, H, F, cyclohexylmethyl, H), (M-3890, F, H, F, cyclohexylmethyl, CI), (M-3891, F, H, F, cyclohexylmethyl, F), (M-3892, F, H, F, cyclohexylmethyl, CFs), (M-3893, F, H, F, cyclohexylmethyl, Br), (M- 3894, F, H, F, cyclohexylmethyl, CHs), (M-3895, F, H， CI, H, H), (M-3896, F, H, CI, H' CI), (M-3897, F, H, CI, H, F), (M-3898, F, H, CI, H, CF3), (M-3899, F, H, C1 H, Br), (M-3900, F' H, CI, H, CHs), (M-3901, F, H， CI, F, H), (M-3902, F, H, CI, F, CI), (M-3903, F, H, CI, F， F), (M-3904, F, H, CI, F, CF3), (M-3905, F, H, CI, P, Br), (M-3906, F, H, CI, F, CH3), (M-3907, F， H, CI, CI, H), (M-3908, F, H, CI, CI, CI), (M-3909, F, H, CI, CI, F), (M-3910, F, H, CI, CI, CFs), (M-3911, F, H, CI, CI, Br), (M-3912, F， H, CI, CI, CHs), (M-3913, F, H, CI, CHs, H), (M-3914, F, H, CI, CHs, CI), (M-3915, F, H, CI, CH3> F), (M-3916, P, H， CI, CH3) CFs), (M-3917, F, H, CI, CH3; Br), (M- 3918, F, H, CI, CHs, CHs), (M-3919, F, H, CI, Et, H), (M-3920, F, H, CI, Et, CI), (M- 3921, F, H， CI, Et, F), (M-3922, F, H, CI, Et, CFs), (M-3923, F, H, CI, Et, Br), (M-3924, F, H, CI, Et, CHs), (M-3925, P, H, CI, n-Pr, H)， (M-3926, F, H, CI, n-Pr, CI), (M- 3927, F, H， CI, n-Pr, F), (M-3928, F, H, CI, n-Pr, CFs), (M-3929, F, H, CI, n-Pr, Br), (M-3930, F, H, CI, n-Pr, CHs), (M-3931, F, H, CI, c-Pr, H), (M-3932, F, H, CI, c-Pr, CI), (M-3933, F， H, CI, c-Pr, F); (M-3934, F, H, CI, c-Pr, CFs), (M-3935, F, H， CI, c-Pr, Br), (M-3936, F, H， Cl， c-Pr, CHs), (M-3937, F, H, CI, i-Pr, H), (M-3938, F， H, CI, i-Pr, CI), (M-3939, F, H, CI, i-Pr, F), (M-3940, F, H, CI, i-Pr, CFg), (M-3941, F, H, CI, i-Pr, Br), (M- 3942, F; H, Cl， i-Pr, CH3)， (M-3943, F, H, CI, n-Bu, H), (M-3944, F, H, CI, n-Bu, CI), (M- 3945, F, H, CI, n-Bu, F), (M-3946, F, H, CI, n-Bu, CFs), (M- 3947, F, H, CI, n-Bu, Br), (M-3948, F， H, CI, n-Bu, CHs), (M- 3949, F, H, CI, i-Bu, H), (M- 3950, F, H, CI, i-Bu, CI), (M-3951, F, H， CI, i-Bu, F), (M-3952, F, H, CI, i-Bu, CF3), (M-3953, F, H, CI, i-Bu, Br), (M-3954, F, H， CI, i-Bu, CHs), (M- 3955, F, H， CI, sec-Bu, H), (M-3956, F, H, CI, sec-Bu, CI), (M-3957, F， H， CI, sec-Bu, F), (M-3958, F, H， CI, sec-Bu, CFs), (M-3959, F, H, CI, sec-Bu, Br), (M-3960, F， H, CI, sec-Bu, CH3), (M-3961, F, H, CI, n-Pen, H), (M-3962, F, H， CI, n-Pen, CI), (M-3963, F, H, CI, n-Pen, F), (M-3964, F, H， CI, n-Pen, CF3), (M-3965, F, H, CI, n-Pen, Br), (M-3966, F, H, CI, n-Pen, CHs), (M-3967, F， H, CI, c-Pen, H), (M- 3968, F, H, CI, c-Pen, CI), (M-3969, F, H, CI, c-Pen, F), (M-3970, F, H, CI, c-Pen, CF3)， (M-3971, F, H, CI, c-Pen, Br), (M-3972, F, H, CI, c-Pen, CHs), (M-3973, F, H, CI, n-Hex, H), (M-3974, F, H, CI, n-Hex, CI), (M-3975, F, H, CI, n-Hex, F)， (M-3976, F, H, CI, n-Hex, CFs), (M-3977, F, H, CI, n-Hex, Br), (M-3978, F, H, CI, n-Hex, CH3), (M- 3979, F, H, CI, c-Hex, H), (M-3980, F, H, CI, c-Hex, CI), (M- 3981, F, H, CI, c-Hex, F), (M- 3982, F, H, CI, c-Hex, CFs), (M-3983, F, H, CI, c- Hex, Br), (M- 3984, F, H, CI, c-Hex, CHs), (M- 3985, F, H, CI, OH, H), (M- 3986, F, H, CI, OH, CI), (M- 3987, F, H, CI, OH, F), (M- 3988, F, H, CI, OH, CFs), (M- 3989, P, H, CI, OH, Br) , (M- 3990, F, H, CI, OH, CH3), (M-3991, F, H, CI, EtO, H) , (M- 3992, F, H' CI, EtO, CI), (M- 3993, F， H， CI, EtO, F), (M- 3994, F, H, CI, EtO, CFs), (M- 3995, F， H, CI, EtO, Br) , (M- 3996, F， H, CI, EtO, CHs), (M- 3997, F, H, CI, n-PrO, H), (M- 3998, F, H, CI, n-PrO, CI), (M- 3999, F, H, CI, n-PrO, F), (M-4000, F, H, CI, n-PrO, CFs), (M-4001, F, H, CI, n-PrO, Br), (M-4002, F， H， CI, n-PrO, CHs), (M-4003, F, H， CI, PhO, H), (M-4004, F, H, CI, PhO, CI), (M-4005, F, H, CI, PhO, F), (M-4006, F, H， CI, PhO, CFa), (M-4007, F, H, CI, PhO, Br), (M-4008, F, H, CI, PhO, CH3), (M-4009, F, H, CI, BnO, H), (M- 4010, F, H， CI, BnO, CI), (M-4011, F, H, CI, BnO, F), (M-4012, F， H, CI, BnO , CFs), (M-4013, F, H, CI, BnO, Br), (M-4014, F, H, CI, BnO, CHs), (M-4015, F, H, CI, PI1CH2CH2O, H), (M-4016, F, H， CI, PhCH2CH20, CI), (M-4017, F, H, CI, PI1CH2CH2O, F)， (M-4018, F, H, CI, PhCHsCBbO, CF3)， (M-4019, F, H， CI, PI1CH2CH2O, Br), (M-4020, F, H， CI, PhCH2 CH20 , CH3), (M-4021, F' H, CI, CFsO, H), (M-4022, F, H, CI, CFsO, CI) , (M-4023, F, H, CI, CF30, F), (M-4024, F， H, CI, CF3O, CF3), (M-4025, F, H, CI, CFsO, Br), (M-4026, F, H, CI, CFsO, CHs), (M-4027, F, H， CI, Ph, H), (M-4028, F, H, CI, Ph, CI), (M-4029, F, H, CI, Ph, F); (M-4030, F, H, CI, Ph, CF3); (M-4031, F， H， CI, Ph, Br), (M-4032, F, H, CI, Ph, CH3)，（M-4033, F, H， CI, 4-F-Ph, H), (M- 4034, F, H, CI, 4-F-Ph, CI) , (M-4035, F, H, CI, 4-F-Ph, F), (M-4036, F, H， CI, 4-F-Ph, CF3), (M-4037, F, H, CI, 4-F-Ph, Br), (M-4038, F, H, CI, 4-F-Ph, CHs), (M-4039, F, H, CI, 4- CFs-Ph, H), (M-4040, F, H, CI, 4- CF3-Ph, CI), (M-4041, F, H' .Cl, 4- CFs-Pli, F), (M-4042, F, H, CI, 4- CF3-Pli, CFs), (M-4043, F, H, CI, 4- CFs-Ph, Br), (M-4044, F, H, CI, 4-CF3-Ph, CH3), (M-4045, F, H, CI, 4- (Me)2N-Ph, H)， (M-4046, P, H, CI, 4- (Me)2N-Ph, CI), (M-4047, F, H, CI, 4- (Me)2N-Ph; F), (M-4048, F, H, CI, 4- (Me)2N-Ph; CFs), (M-4049, F, H, CI, 4- (Me)2N-Ph! Br), (M-4050, F, H, CI, 4-(Me)2N-Ph; CHs), (M-4051, F, H, CI, 4- OH-Ph, H), (M-4052, F, H, CI, 4-OH-Ph, CI), (M-4053, F, H, CI, 4-OH-Ph, F)， (M-4054, F, H, CI, 4-OH-Ph; CFs), (M-4055, F, H, CI, 4-OH-Ph, Br), (M-4056, F, H, CI, 4-OH-Ph, CHs), (M-4057, F， H, CI, 3,4-di-F-Ph, H), (M-4058, F， H， CI, 3,4-di-F-Ph, CI), (M-4059, F, H, CI, 3,4-di-F-Ph, F), (M-4060, F' H, CI, 3,4-di- F-Ph, CFs), (M-4061, F, H, CI, 3,4-di-F-Ph, Br), (M-4062, F, H, CI, 3,4-di-F-Ph, CH3)， (M-4063, F, H, CI, 4-COOH-Ph, H), (M-4064, F, H, CI, 4-COOH-Ph, CI), (M-4065, F, H, CI, 4-COOH-Ph, F), (M-4066, F, H, Cl; 4-COOH-Ph, CF3), (M- 4067， F， H, CI, 4-COOH-Ph, Br), (M-4068, F， H, CI, 4-COOH-Ph, CH3), (M-4069, F, H, CI, Bn, H), (M-4070, F, H, CI, Bn, CI), (M-4071, F, H, CI, Bn, F), (M-4072, F, H, CI, Bn, CF3), (M-4073, F, H, CI, Bn, Br), (M-4074, F, H, CI, Bn, CHs), (M-4075, F， H, CI, 4-F-Bn, H), (M-4076, F， H, CI, 4-F-Bn, CI), (M-4077, F, H, CI, 4-F-Bn, F), (M-4078, F, H， CI, 4-F-Bn, CFs), (M-4079, F, H, CI, 4-F-Bn, Br), (M-4080, F, H, CI, 4-F-Bn, CH3), (M-4081, F, H, CI, 2-Py, H), (M-4082, F， H, CI, 2-Py, CI), (M-4083, F, H, CI, 2-Py, F), (M-4084, F, H, CI, 2-Py, CFs), (M-4085, F, H, CI, 2-Py, Br), (M-4086, F, H, CI, 2-Py, CH3), (M-4087, F, H, CI, 3-Py, H), (M-4088, F, H, CI, 3-Py, CI), (M-4089, F, H, CI, 3-Py, F), (M-4090, F, H, CI, 3- Py, CFs), (M-4091, F, H, CI, 3-Py, Br), (M-4092, F, H, CI, 3-Py, CHs), (M-4093, F, H, CI, 4-Py, H), (M-4094, F, H, CI, 4-Py, CI), (M-4095, F, H, CI, 4-Py, F), (M-4096, F, H, CI, 4-Py, CFs), (M-4097, F, H, CI, 4-Py, Br), (M-4098, F， H, CI, 4-Py, CH3), (M-4099, F, H, CI, 2-Th, H), (M-4100, F, H, CI, 2-Th, CI), (M-4101, F， H, CI, 2-Th, F), (M-4102, F, H, CI, 2-Th, CFs), (M-4103, F, H, CI, 2-Th, Br),. (M-4104, F, H, CI, 2-T.h, CH3), (M-4105, F, H, CI, 3-Th, H), (M-4106, F, H, CI, 3-Th, CI), (M-4107, F, H， CI, 3-Th, F), (M-4108, F, H, CI, 3-Th, CFs), (M-4109, F, H， CI, 3-Th, Br), (M-4110, F, H, CI, 3-Th, CHs), (M-4111, F, H, CI, pyrazol-2- yl, H), (M-4112, F, H, CI, pyrazol-2-yl, CI), (M-4113, F, H, CI, pyrazol-2-yl; F), (M-4114, F, H, CI, pyrazol-2-yl, CFs), (M-4115, F, H, CI, pyrazol-2-yl, Br), (M-4116, F, H, CI, pyrazol-2-yl, CHs), (M-4117, F, H, Cl; yrazol-3-yl, H), (M- 4118, F, H, CI, pyrazoレ 3-yl, CI), (M-4119, F， H, CI, pyrazoレ 3-yl' F), (M-4120, F, H, CI, pyrazol-3-yl, CF3), (M-4121, F, H, CI, pyrazol-3-yl, Br), (M-4122, F, H, CI, pyrazol-3-yl, CH3), (M-4123, F, H, CI, pyrimidin-2-yl, H), (M-4124, F, H, CI, pyrimidm-2-yl; CI), (M-4125, F, H, CI, pyrimidin-2-yl, F), (M-4126, F, H, CI, pyrimidin-2-yl, CPs), (M-4127, P, H, CI, pyrimidin-2-yl, Br), (M-4128, F, H, CI, pyrimidin-2-yl, CHs), (M-4129, F, H, CI, pyrimidin-4-yl, H), (M-4130, F, H, CI, pyrimidm-4-yl, CI), (M-4131, F, H, CI, pyrimidm-4-yl, F), (M-4132, F, H, CI, pyrimidin-4-yl, CFs), (M-4133, F, H, CI, pyrimidin-4-yl, Br), (M-4134, F' H, CI, pyrimidin-4-yl, CHs), (M-4135, F, H, CI, pyrimidin-5-yl, H), (M-4136, F, H, CI, pyrimidin-5-yl, CI), (M-4137, F' H, CI, pyrimidin-5-yl, F), (M-4138, F, H, CI, pyrimidin-5-yl, CFs), (M-4139, F, H, CI, pyrimidin-5-yl, Br), (M-4140, F, H, CI, pyrimidin-5-yl; CHs), (M-4141, F, H, CI, HOOCCH2CH2CH2; H), (M-4142, F, H, CI, HOOCCH2CH2CH2, CI), (M-4143, F, H, CI, HOOCCH2CH2CH2, F); (M-4144, F, H, CI, HOOCCH2CH2CH2) CF3), (M-4145, F, H, CI, HOOCCH2CH2CH2, Br), (M-4146, F, H， CI, HOOCCH2CH2CH2, CHs), (M-4147, F, H， CI,
HOOCCH2CH2CH2CH2, H), (M-4148, F, H, CI, HOOCCH2CH2CH2CH2' CI), (M-4149, F, H， CI, HOOCCH2CH2CH2CH2> F), (M-4150, F, H, CI,
HOOCCH2CH2CH2CH2; CF3), (M-4151, F, H, CI, HOOCCH2CH2CH2CH2, Br), (M-4152, F, H， CI, HOOCCH2CH2CH2CH2, CH3), (M-4153, F, H, CI,
(Me)2NCOCH2CH2CH2CH2， H)， (M-4154, F, H, CI, (Me)2NCOCH2CH2CH2CH2, CI), (M-4155, F, H, CI, (Me)2NCOCH2CH2CH2CH2, F), (M-4156, F, H, CI, (Me)2NCOCH2CH2CH2CH2， CF3), (M-4157, F, H, CI, (Me)2NCOCH2CH2CH2CH2, Br), (M-4158, F, H, CI, (Me)2NCOCH2CH2CH2CH2, CH3)， (M-4159, F, H, CI, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-4160, F, H, CI, (Me)2NCOCH2CH2CH2CH2CH2, Cl)， (M-4161, F, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-4162, F, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CPs), (M-4163, F， H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-4164, F, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-4165, F, H, CI, MeOCH2, H), (M-4166, F, H; CI, MeOCH2) CI), (M-4167, F, H, CI, MeOCHs, F), (M-4168, F, H, CI, MeOCH2, CFs), (M-4169, F, H, CI, MeOC Br), (M-4170, F, H, CI, MeOCH2, CHs), (M-4171, F, H, CI, EtOCH2; H), (M-4172, F, H, CI, EtOCHz, CI), (M-4173, F, H， CI, EtOCH2, F), (M-4174, F, H, CI, EtOCH2; CFs), (M-4175, F, H, CI, EtOCH2) Br), (M-4176, P; H' CI, EtOCHs, CH3), (M-4177, F, H, CI, EtOCH2CH2) H), (M-4178, F, H, CI, EtOCH2CH2， CI), (M-4179, F, H, CI, EtOCH2CH2) F), (M-4180, F, H, CI, EtOCH2CH2, CF3), (M-4181, F, H, CI, EtOCH2CH2, Br), (M-4182, F, H, CI, EtOCH2CH2, CHs), (M-4183, F, H, CI, MeOCH2CH20CH2CH2, H), (M-4184, F, H, CI, Me 0 CH2 CH20 CH2 CH2, CI), (M-4185, F, H, CI,
MeOCH2CH2OCH2CH2, F)，（M-4186, F, H, CI, MeOCH2CH2OCH2CH2, CFs), (M-4187, F, H, CI, MeOCH2CH2OCH2CH2, Br), (M-4188, F, H, CI,
MeOCH2CH2OCH2CH2， CHs), (M-4189, F, H, CI, MeOCH2CH2， H), (M-4190, F， H, CI, MeOCH2CH2; CI), (M-4191, F, H, CI, MeOCH2CH2) F), (M-4192, F, H, CI, MeOCH2CH2; CFs), (M-4193, F, H; CI, MeOCH2CH2, Br), (M-4194, F, H, CI, MeOCH2CH2, CH3), (M-4195, F, H, CI, HOCH2> H), (M-4196, F, H, CI, HOCH2) CI), (M-4197, F, H, CI, HOCH2, F)' (M-4198, F, H, CI, HOCH2, CFs), (M-4199, F, H, CI, HO CH2, Br), (M-4200, F, H, CI, HOCH2) CHs), (M-4201, F, H， CI, ,..
HOCH2CH2; H), (M-4202, F, H, CI, HOCH2CH2; CI), (M-4203, F; H, CI,
HOCH2CH2, F); (M-4204, F, H, CI, HOCH2CH2) CFs), (M-4205, F, H, CI, HOCH2CH2, Br), (M-4206, F, H, CI, HOCH2CH2) CH3), (M-4207, F, H, CI,
HOCH2CH2CH2, H), (M-4208, F, H, CI, HOCH2CH2CH2, CI), (M-4209, F, H, CI, HOCH2CH2CH2, F)， (M-4210, F， H, CI, HO CH2CH2CH2， CF3), (M-4211, F， H, CI, HOCH2CH2CH2, Br), (M-4212, F, H, CI, HO CH2CH2CH2, CHs), (M-4213, F, H， CI, HO CH2CH2CH2CH2， H), (M-4214, F, H, CI, HOCH2CH2CH2CH2, CI), (M- 4215, F, H, CI, HOCH2CH2CH2C , F), (M-4216, F， H, CI, HOCH2CH2CH2CH2; CF3), (M-4217, F, H, CI, HOCH2CH2CH2CH2; Br), (M-4218, F, H, CI,
HO CH2CH2CH2CH2, CHs), (M-4219, F, H, CI, HO CH2CH2CH2CH2CH2, H)， (M-4220, F, H, CI, HOCH2CH2CH2CH2CH2, CI), (M-4221, F, H, CI,
HOCH2CH2CH2CH2CH2, F), (M-4222, F， H, CI, HO CH2CH2CH2CH2CH2> CFs), (M-4223, F, H, CI, HOCH2CH2CH2CH2CH2, Br), (M-4224, F; H, CI,
HOCH2CH2CH2CH2CH2) CHs), (M-4225, F, H, CI, HO CH2CH2OCH2CH2; H)， (M-4226, F, PI, CI, HO CH2CH2O CH2CH2, CI), (M-4227, F, H, CI,
HO CH2CI- I2OCH2CH2, F), (M-4228, F, H， CI, HOCH2CH2O CH2CH2, CFs), (M- 4229, F, H, CI, HO CH2CH2O CH2CH2， Br), (M-4230, F, H, CI,
HOCH2CH2OCH2CH2, CHs), (M-4231, F, H, CI, (Me)2N, H)' (M-4232, F, H, CI, (Me)2N, CI), (M-4233, F, H, CI, (Me)2N; F), (M-4234, F, H， CI, (Me)2N) CFs), (M-4235, F， H, CI, (Me)2N, Br), (M-4236, F, H, CI, (Me)2N, CHs), (M-4237, F, H, CI, piperidin-4-yl-methyl, H), (M-4238, F, H, CI, piperidin-4-yl-methyl, CI), (M-4239, F, H， CI, piperidin-4-yl-metliyl; P), (M-4240, F, H, CI, piperidin-4- yl-methyl, CF3), (M-4241, F, H, CI, piperidin-4-yレ methyl, Br), (M-4242, F， H, CI, piperidin-4-yレ methyl, CHs), (M-4243, F, H, CI, cyclohexylmethyl, H), (M- 4244, F， H, CI, cyclohexylmethyl, CI), (M-4245, F, H, CI, cyclohexylmethyl, F), (M-4246, F, H, CI, cyclohexylmethyl, CF.3) , (M-4247, F, H， CI, cyclohexylmethyl, Br), (M-4248, F, H, CI, cyclohexylmethyl, CHs), (M-4249, F, F, H, H, H), (M- 4250, P; F, H, H, CI), (M-4251, F, F, H, H, F), (M-4252, F; F, H, H, CF3), (M-4253, F, F, H, H, Br), (M-4254, F, F, H, H, CHs), (M-4255, F, F, H, P, H), (M-4256, F, F， H, P, CI), (M-4257, F, F， H, F, F), (M-4258, F, F, H, F, CFs), (M-4259, F, F, H, F， Br), (M-4260, F, F, H, F, CHs), (M-4261, F, F, H, CI, H), (M-4262, F, F， H, CI, CI), (M-4263, F, F, H, CI, F); (M-4264, F, F, H, CI, CFs), (M-4265, F, F, H, CI, Br), (M-4266, F, F, H, CI, CHs), (M-4267, F' F, H, CHs, H), (M-4268, F, F, H， CH3, CI), (M-4269, F, F, H' CHs, F), (M-4270, F' F, H, CHs, CFs), (M-4271, F, F, H, CH3, Br), (M-4272, F, F' H, CHs, CHs), (M-4273, F, F, H, Et, H), (M-4274, F, F' H, Et, CI), (M-4275, F, F， H, Et, F), (M-4276, F, F, H， Et, CFs), (M-4277, F， F， H, Et, Br), (M-4278, F, F, H, Et, CH3), (M-4279, F, F, H, n-Pr, H), (M-4280, F, F, H, n-Pr, CI), (M-4281, F, F, H, n-Pr, F), (M-4282, F, F, H, n-Pr, CFs), (M-4283, F, F, H, n-Pr, Br), (M-4284, F, F, H; n-Pr, CHs), (M-4285, F, F, H, c-Pr, H), (M-4286, F, F, H, c-Pr, CI), (M-4287, F, F, H' c-Pr, F), (M-4288, F, F, H, c-Pr, CF3), (M-4289, F, F, H， c-Pr, Br), (M-4290, F, F, H' c-Pr, CHs), (M-4291, F, F, H, i-Pr, H)， (M-4292, F, F, H, i-Pr, CI), (M-4293, F， F， H' i-Pr, F), (M-4294, F' F, H, i-Pr, CFs), (M-4295, F, F, H' i-Pr, Br), (M-4296, F, F, H, i-Pr, CH3), (M-4297, F, F, H, n-Bu, H)， (M-4298, F, F, H, n-Bu, CI), (M-4299, F， F, H, n-Bu, F), (M-4300, F, F, H, n-Bu, CFs), (M-4301, F, F, H, n-Bu, Br), (M-4302, F; F, H, n-Bu, CH3), (M-4303, F, F, H, i-Bu, H), (M-4304, F, F， H， i-Bu, CI), (M-4305, F, F, H, i-Bu, F), (M-4306, F， F, H, i-Bu, CFs), (M-4307, F, F, H, i-Bu, Br), (M-4308, F, F, H, i-Bu, CHs), (M-4309, F, F, H, sec-Bu, H), (M-4310, F, F, H, sec-Bu, CI), (M-4311, F, F, H, sec-Bu, F), (M-4312, F， P, H, sec-Bu, CFs), (M-4313, F， F, H, sec-Bu, Br), (M-4314, F, F, H, sec-Bu, CHs), (M-4315, F, F, H, n-Pen, H), (M-4316, F, F, H, n-Pen, CI), (M-4317, F, F, H, n-Pen, F), (M-4318, F， F, H, n-Pen, CFs), (M-4319, F, F, H; , n-Pen, Br), (M-4320, F, F, H, n-Pen, CHs), (M-4321, F, F H, c-Pen, H), (M-4322, F, F, H, c-Pen, CI), (M-4323, F， F, H, c-Pen, F), (M-4324, F, F， H, c- Pen, CFs), (M-4325, F, F, H, c-Pen, Br), (M-4326, F, F, H, c-Pen, CHs), (M-4327, F, F, H, n-Hex, H), (M-4328, F, F, H, n-Hex, CI), (M-4329, F, F, H, n-Hex, F), (M-4330, F, F， H, n-Hex, CF3), (M-4331, F, F, H, n-Hex, Br), (M-4332, F, F, H, n-Hex, CHs), (M-4333, F， F， H, c-Hex, H)， (M-4334, F， F; H, c-Hex, CI), (M-4335, F, F, H, c-Hex, F), (M-4336, F, F, H， c-Hex, CFs), (M-4337, P, F, H, c-Hex, Br), (M-4338, F, F, H, c-Hex, CHs), (M-4339, F, F, H, OH, H), (M-4340, F, F, H, OH, CI), (M-4341, F, F, H, OH, F), (M-4342, F; F, H, OH, CF3), (M-4343, F, F, H, OH, Br), (M-4344, F; F, H, OH, CHs), (M-4345, F, F, H, EtO, H), (M-4346, F, F, H, EtO, CI), (M-4347, F, P, H, EtO, F), (M-4348, F， F' H, EtO, CFs), (M-4349, F, F, H, EtO, Br), (M-4350, F, F, H, EtO, CHs), (M-4351, F, F, H, n-PrO, H); (M-4352, F, F, H, n-PrO, CI), (M-4353, F, F, H, n-PrO, F)， (M-4354, F, F, H, n-PrO, CFs), (M-4355, F, F, H, n-PrO, Br), (M-4356, F, F, H， n-PrO, CHs), (M-4357, F, F, H， PhO, H), (M-4358, F, P, H, PhO, CI), (M-4359, F, F， H, PhO, F), (M-4360, F, F， H, PhO, CF3), (M-4361, F, F, H, PhO, Br), (M-4362, F' F, H, PhO, CHs), (M-4363, F, F, H, BnO, H), (M-4364, F, F, H, BnO, CI), (M-4365, F， F, H, BnO, F), (M- 4366, F, F, H, BnO, CFs), (M-4367, F, F, H, BnO, Br), (M-4368, F， F, H, BnO, CHs), (M-4369, F, F, H, PhCH2CH20; H), (M-4370, F， F， H, PI1CH2CH2O, CI), (M-4371, F, F， H, PI1CH2CH2O, F), (M-4372, F, F, H, PI1CH2CH2O, CF3), (M- 4373, F, F, H, PhCHaCHaO, Br), (M-4374, F, F, H, PhCH2CH20, CHs), (M-4375, P, F, H, CPsO, H)， (M-4376, F, F, H, CF3O, CI), (M-4377, F, F, H, CF30, F), (M-4378, F, F, H, CFaO, CFs), (M-4379, F, F, H, CFsO, Br), (M-4380, F, F， H, CFsO, CHs), (M-4381, F, F, H' Ph, H), (M-4382, F, F, H, Ph, CI), (M-4383, F, F, H, Ph, F), (M-4384, F, F, H， Ph, CFs), (M-4385, F, F, H, Ph, Br), (M-4386, F， F, H, Ph, CHs), (M-4387, F, F, H, 4-F-Ph, H), (M-4388, F, F, H, 4-F-Ph, CI), (M- 4389, F, F, H, 4-F-Ph, F), (M-4390, F, F, H; 4-F-Ph, CFs), (M-4391, F, F, H, 4- F-Ph, Br), (M-4392, F, F, H, 4-F-Ph, CH3), (M-4393, F, F, H, 4-CF3-Pli; H), (M-4394, F, F, H, 4-CF3-Ph, CI), (M-4395, F, F， H， 4-CFs-Ph, F), (M-4396, F, F, H， 4-CF3-Ph; CFs), (M-4397, F, F, H, 4-CF3-Ph， Br), (M-4398, F, F， H, 4-CF3-Ph; CHs), (M-4399, F, F, H, 4-(Me)2N-Ph, H)， (M-4400, F, F, H, 4-(Me)2N-Ph; CI), (M-4401' F, F, H, 4-(Me)2N-P , F), (M-4402, F, F, H, 4-(Me)2N-Ph, CFs), (M- 4403, F, F， H, 4-(Me)2N-Ph, Br), (M-4404, F, F, H, 4-(Me)2N-Ph; CHs), (M-4405, F, F， H， 4-OH-Ph, H), (M-4406, F, F, H, 4-OH-Ph, Cl)， (M-4407, P, F, H, 4- OH-Ph, F), (M-4408, F, F, H， 4-OH-Ph, CF3), (M-4409, F, F, H, 4-OH-Ph, Br), (M-4410, F, F, H, 4-OH-Ph, CHs), (M-4411, F, F, H, 3,4-di-F-Ph, H), (M-4412, F, F, H, 3,4-di-F-Pli, CI), (M-4413, F, F， H, 3, 4-di-F-Ph, F)， (M-4414, F, F, H, 3,4-di-F-Ph, CFs), (M-4415, F; F， H, 3,4-di-F-Ph, Br), (M-4416, F, F， H， 3,4-di- F-Ph, CHs), (M-4417, F, F, H， 4-COOH-Ph, H), (M-4418, F, F, H, 4-COOH-Ph, CI), (M-4419, F' F, H, 4-COOH-Ph, F), (M-4420, P, F, H， 4-COOH-Ph, CFs), (M-4421, F, F, H, 4-COOH-Ph, Br), (M-4422, F, F, H， 4-COOH-Ph, CHs), (M- 4423, F, F, H, Bn, H), (M-4424, F, F, H, Bn, CI), (M-4425, F, F, H， Bn, F), (M- 4426, F, F, H, Bn, CF3), (M-4427, F, F, H, Bn, Br), (M-4428, F, F, H, Bn, CHs), (M-4429, F, F, H, 4-F-Bn, H), (M-4430, F, F, H, 4-F-Bn, CI), (M-4431, F, F, H， 4-F-Bn, F), (M-4432, F, F, H, 4-F-Bn, CFs), (M-4433, F, F, H, 4-F-Bn, Br); (M- 4434, F, F， H, 4-F-Bn, CHs), (M-4435, F, F， H， 2-Py, H), (M-4436, F, F, H, 2-Py, CI), (M-4437, F, F, H, 2-Py, F), (M-4438, F， F, H, 2-Py, CFs), (M-4439, F, F, H,
2- Py, Br), (M-4440, F, F, H, 2-Py, CH3), (M-4441, F; F, H, 3-Py, H), (M-4442, F, F, H, 3-Py, CI), (M-4443, F, F, H, 3-Py, F), (M-4444, F, F, H, 3-Py, CFs), (M-4445, F, F, H, 3-Py, Br), (M-4446, F, F, H, 3-Py, CH3), (M-4447, F, F, H, 4-Py, H), (M-4448, F, F, H' 4-Py, CI), (M-4449, F, F, H, 4-Py, F), (M-4450, F, F, H, 4-Py, CFs), (M-4451, F, P, H, 4-Py, Br), (M-4452, F, F, H, 4-Py, CHs), (M-4453, F, F, H, 2-Th, H), (M-4454, F, F, H, 2-Th, CI), (M-4455, F, F, H,.2-.Th; F), (M-4456, F, F, H, 2-Th, CFs), (M-4457, F, F, H, 2-Th, Br), (M-4458, F, F, H, 2-Th, CHs), (M-4459, F, F, H, 3-Th, H), (M-4460, F, F, H, 3-Th, CI), (M-4461, F, F, H, 3-Th, F), (M-4462, F, F, H, 3-Th, CF3), (M-4463, F, F， H， 3-Th, Br), (M-4464, F, F, H，
3- Th, CHs), (M-4465, F, F, H, pyrazol-2-yl, H), (M-4466, F, F, H, pyrazol-2-yl, CI), (M-4467, F, F, H; pyrazol-2-yl, F), (M-4468, F, F' H, pyrazol-2-yl, CF3), (M-4469, F, F, H, pyrazol-2-yl, Br), (M-4470, F, F, H, pyrazol-2-yl, CHs), (M- 4471, F, F, H, pyrazol-3-yl, H), (M-4472, F, F， H, pyrazol-3-yl, CI), (M-4473, F, F, H, pyrazol-3-yl, F), (M-4474, F, F, H, pyrazol-3-yl, CFs), (M-4475, F, F, H, pyrazol-3-yl, Br), (M-4476, F, F, H, pyrazol-3-yl, CHs), (M-4477, P, F, H, pyrimidin-2-yl, H)， (M-4478, F, F, H, pyrimidin-2-yl, CI), (M-4479, F, F, H, pyrimidin-2-yl, F), (M-4480, F, F, H, pyrimidin-2-yl, CFs), (M-4481, F, F, H, pyrimidin-2-yl, Br), (M-4482, F, F, H, pyrimidin-2-yl, CHs), (M-4483, F, F, H, pyrimidin-4-yl, H), (M-4484, F, F, H， pyrimidin-4-yl, CI), (M-4485, F， F, H, pyrimidin-4-yl, F)， (M-4486, F, F， H, pyrimidin-4-yl, CF3), (M-4487, F, F, H, pyrimidin-4-yl, Br), (M-4488, F, F, H, pyrimidin-4-yl, CHa), (M-4489, F, F， H, pyrimidin-5-yl, H), (M-4490, F, F, H, pyrimidin-5-yl, CI), (M-4491, F, F, H, pyrimidin-5-yl, F)， (M-4492, F, F, H, pyrimidin-5-yl, CFs), (M-4493, F， F, H, pyrimidin-5-yl, Br), (M-4494, F, F, H, pyrimidin-5-yl, CHs), (M-4495, F, P, H， HOOCCH2CH2CH2; H), (M-4496, F, F' H, HOOCCH2CH2CH2) CI), (M-4497, F, F, H, HOOCCH2CH2CH2) F), (M-4498, F, F, H, HOOCCH2CH2CH2, CFs), (M-4499, F, F, H, HOOCCH2CH2CH2, Br), (M-4500, F, F, H, HOOCCH2CH2CH2, CHs), (M-4501, F, F, H, HOOCCH2CH2CH2CH2, H)，（M-4502, F, F, H,
HOOCCHaCHsCHsCHs, CI), (M-4503, F, F, H, HOOCCH2CH2CH2CH2, F), (M- 4504, F， F, H, HOOCCH2CH2CH2CH2) CF3)， (M-4505, F, P, H,
HOOCCH2CH2CH2CH2) Br), (M-4506, F, P, H, HOOCCH2CH2CH2CH2) CHs), (M-4507, F, F' H, (Me)2NCOCH2CH2CH2CH2, H), (M-4508, F, F, H,
(Me)2NCOCH2CH2CH2CH2) CI), (M-4509, P, F, H, (Me)2NCOCH2CH2CH2CH2, F), (M-4510, F, F, H, (Me)2NCOGH2CH2CH2CH2, CFs), (M-4511, F, F, H, (Me)2NCOCH2CH2CH2CH2; Br), (M-4512, F, F, H，（Me)2NCOCH2CH2CH2CH2, CHs), (M-4513, F, F' H, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-4514, F, F, H， (Me)2NCOCH2CH2CH2CH2CH2, CI), (M-4515, F, F, H,
(Me)2NC0CH2CH2CH2CH2CH2> F), (M-4516, F, F， H, 。 (Me)2NCOCH2CH2CH2CH2CH2， CPs), (M-4517, F, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-4518, F， F' H,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-4519, F, F, H, MeOCH2) H), (M-4520, F, F， H, MeOCH2, CI), (M-4521, F' F, H, MeOCHa, F), (M-4522, F, F, H, MeOCHs, CFs), (M-4523, F, F, H, MeOCH2, Br), (M-4524, F， F, H, MeOCH2) CHs), (M-4525, F， F, H， EtOCHs, H), (M-4526, F, F， H, EtOCH2; CI), (M-4527, F, F, H, EtOCH2; F), (M-4528, F; P, H, EtOCH2, CF3), (M-4529, F, F， H, EtOCH2' Br), (M-4530, F， F, H， EtOCH2, CHs), (M-4531, F, F, H, EtOCH2CH2) H), (M- 4532, F, F' H, EtOCH2CH2, CI), (M-4533, F， F， H, EtOCH2CH2, F), (M-4534, F, F, H, EtOCH2CH2; CF3), (M-4535, F, F, H, EtOCH2CH2, Br), (M-4536, F, F, H, EtOCH2CH2, CH3), (M-4537, F, F, H, MeOCH2CH2〇CH2CH2, H), (M-4538, F, F, H, Me 0 CHs CHsO CH2 CH2, CI), (M-4539, F, F, H, MeOCH2CH2OCH2CH2, F), (M-4540, F, F, H, MeOCH2CH2OCH2CH2) CFs), (M-4541, F, F, H，
MeOCH2CH2OCH2CH2， Br), (M-4542, F, F, H， MeOCH2CH2OCH2CH2, CH3)， (M-4543, F, F; H, MeOCH2CH2; H)， (M-4544, F, F, H, MeOCH2CH2) CI), (M- 4545, F, F, H, MeOCH2CH2, F), (M-4546, F, F, H， MeOCHsCHs, CFa), (M-4547, F, F, H, MeOCH2CH2, Br), (M-4548, F, F, H, MeOCH2CH2) CHs), (M-4549, F' F, H, HOCH2, H), (M-4550, F, F, H, HOCH2, CI), (M-4551, F, F, H; HOCH2, F), (M-4552, F, F, H, HOCH2, CF3), (M-4553, F, F; H， HOCH2) Br), (M-4554, F, F, H, HOCH2, CHs), (M-4565, F, F, H, HOCH2CH2, H), (M-4556, F, F, H, HOCH2CH2, CI), (M-4557,. F, F; H, HOCH2CH2, F), (M-4558, F', F, H, HOCH2CH2, CFS) , (M-4559, F, F, H, HOCH2CH2' Br), (M-4560, F, F, H, HOCH2CH2, CHs), (M- 4561, F, F, H, HOCH2CH2CH2> H), (M-4562, F, F, H, HOCH2CH2CH2) CI), (M- 4563, F' F, H, HOCH2CH2CH2, F)， (M-4564, F, F, H, HOCH2CH2CH2, CF3); (M-4565, F, F, H, HOCH2CH2CH2, Br), (M-4566, F, F, H, HOCH2CH2CH2, CHs), (M-4567, P, F, H, HOCH2CH2CH2CH2, H), (M-4568, F, F; H'
HOCH2CH2CH2CH2, CI), (M-4569, F, F, H, HOCH2CH2CH2CH2, F), (M-4570, F, F, H, HOCH2CH2CH2CH2) CF3), (M-4571, F, F, H, HOCH2CH2CH2CH2) Br), (M-4572, F, F, H， HOCH2CH2CH2CH2, CH3), (M-4573, F' F, H,
HOCH2CH2CH2CH2CH2, H), (M-4574, F， F， H, HOCH2CH2CH2CH2CH2， CI), (M-4575, F, F, H, HOCH2CH2CH2CH2CH2， F), (M-4576, F, F, H,
HOCH2CH2CH2CH2CH2; CFs), (M-4577, F, F, H, HOCH2CH2CH2CH2CH2, Br), (M-4578, F， F, H， HOCH2CH2CH2CH2CH2, CH3), (M-4579, F, F, H，
HOCH2CH20CH2CH2) H), (M-4580, F, F, H, HOCH2CH2OCH2CH2, CI), (M-4581, F, F, H, HOCH2CH2OCH2CH2， F)， (M-4582, F, F, H, HOCH2CH2OCH2CH2; CF3), (M-4583, F, F, H, HOCH2CH2OCH2CH2, Br), (M-4584, F, F, H,
HOCH2CH2OCH2CH2, CH3), (M-4585, F, F, H, (Me)2N, H), (M-4586, F, F, H, (Me)2N, CI), (M-4587, F， F， H, (Me)2N; F), (M-4588, F, F, H, (Me)2N, CPs), (M-4589, F, F, H, (Me)2N, Br), (M-4590, F, F, H, (Me)2N, CH3), (M-4591, P, F, H, piperidin-4-yl-metliyl, H), (M-4592, F, F, H, piperidin-4-yレ methyl' CI), (M- 4593, F， F, H, piperidin-4-yl-methyl, F), (M-4594, F, F, H, piperidin-4-yl- methyl, CFs), (M-4595, F, F, H, piperidin-4-yl-methyl, Br), (M-4596, F, F, H, piperidin-4-yl-methyl, CH3)， (M-4597, F， F, H, cyclohexylmethyl, H), (M-4598, F, F, H, cyclohexylmethyl, CI), (M-4599, F, F， H, cyclohexylmethyl, F), (M-4600, F, F, H, cyclohexylmethyl, CF3), (M-4601, F, F, H, cyclohexylmethyl, Br), (M- 4602, F, F, H, cyclohexylmethyl, CHs), (M-4603, F, F, F, H, H), (M-4604, F， F, F, H, CI), (M-4605, F, F, F， H, F)' (M-4606, F, F, F, H, CF3), (M-4607, F, F， F, H, Br), (M-4608, F, F, F, H, CH3), (M-4609, F, F, F, F, H), (M-4610, F, F, F, F， CI), (M-4611, F, F, F, F, F), (M-4612, F, F， F, F, CF3), (M-4613, F, F, F, F, Br), (M-4614, F, F, F, F, CHs), (M-4615, F, F, F, CI, H), (M-4616, F, F， F, CI, CI), (M-4617, F, F， F; Cl, F), (M-4618, F， F, F, Cl, CFs), (M-4619, F, F， F, Cl, Br), (M-4620, F' F, F, Cl, CH3), (M-4621, F, F, F, CHs, H), (M-4622, F, F, F, CHs, Cl), (M-4623, F, F, F, CH3) F), (M-4624, F, F, F, CH3, CFs), (M-4625, F, F, F, CHs, Br), (M-4626, F, F; F, CHs, CH3)， (M-4627, F, F， F, Et, H), (M-4628, F, F， F' Et, Cl), (M-4629, F, F, F, Et, F), (M-4630, F, F, F, Et, CFs), (M-4631, F, F, F, Et, Br), (M-4632, F, F， F, Et, CHs), (M-4633, F, F, F, n-Pr, H), (M-4634, F, F, F, n-Pr, Cl), (M-4635, F, F, F, n-Pr, F), (M-4636, F, F, F, n-Pr, CFs), (M-4637, F, F, F, n-Pr, Br), (M-4638, F， F， F, n-Pr, CHs), (M-4639, F， F, F, c-Pr, H), (M-4640, F, F, F， c-Pr, Cl), (M-4641, F, F, F, c-Pr, F), (M-4642, F, F, F, c-Pr, CFs), (M-4643, F, F, F, c-Pr, Br), (M-4644, F, F, F, c-Pr, CH3), (M-4645, F, F, F, i-Pr, H), (M-4646, F, P, F, i-Pr, Cl), (M-4647, F， F, F, i-Pr, F), (M-4648, F, F, F, i-Pr, CFs), (M-4649, F， F， F, i-Pr, Br), (M-4650, F, F, F， i-Pr, CH3), (M-4651, F, F, F， n-Bu, H), (M- 4652, F, F, F, n-Bu, Cl), (M-4653, F, F, F, n-Bu, F), (M-4654, F, F, F, n-Bu, CFs), (M-4655, F, F, F, n-Bu, Br), (M-4656, F， F, F， n-Bu, CH3), (M-4657, F, F, F, i- Bu, H), (M-4658, F, F, F, i-Bu, Cl), (M-4659, F, F, F, i-Bu, F)， (M-4660, F, F， F, i-Bu, CF3), (M-4661, F; F, F, i-Bu, Br), (M-4662, F, F， F, i-Bu, CHs), (M-4663, F, F, F, sec-Bu, H), (M-4664, F, F, F, sec-Bu, Cl), (M-4665, F, F, F, sec-Bu, F), (M-4666, F, F, F, sec-Bu, CFs), (M-4667, F, F, F, sec-Bu, Br), (M-4668, F, F, F, sec-Bu, CH3)， (M-4669, F, F, F, n-Pen, H), (M-4670, F, F, F, n-Pen, Cl), (M-4671, F, F, F, n-Pen, F), (M-4672, F, F, F, n-Pen, CFs), (M-4673, F, F, F， n-Pen, Br), (M-4674, F， F, F, n-Pen, CHs), (M-4675, F, F, F, c-Pen, H), (M-4676, F, F, F, c-Pen, Cl), (M-4677, F, F, F, c-Pen, F), (M-4678, F, F, F, c-Pen, CFs), (M-4679, F， F， F, c-Pen, Br), (M-4680, F, F， F, c-Pen, CH3), (M-4681, F, F, F, n-Hex, H)， (M-4682, F， F, F; n-Hex, Cl), (M-4683, F, F, F, n-Hex, F), (M-4684, F， F, F, n- Hex, CFs), (M-4685, F, F, F' n-Hex, Br), (M-4686, F, F, F, n-Hex, CH3), (M-4687, F, F, F， c-Hex, H)， (M-4688, F, F, F, c-Hex, Cl), (M-4689, F, F， F, c-Hex, F), (M-4690, F, F, F， c-Hex, CF3), (M-4691, F, F, F, c-Hex, Br), (M-4692, F, F, F, c-Hex, CHs), (M-4693, F, F, F, OH, H), (M-4694, P, F, F, OH, CI), (M-4695, F, F， F, OH, F), (M-4696, F, F, F, OH, CFs), (M-4697, F, F, F, OH, Br), (M-4698, F, F, F, OH, CHs), (M-4699, F, F, F, EtO, H), (M-4700, F, F， F, EtO, CI), (M-4701, F, F， F, EtO, F), (M-4702, F， F, F, EtO, CFs), (M-4703, F, F, F, EtO, Br), (M-4704, F, F， F, EtO, CH3), (M-4705, F, F, F， n-PrO, H), (M-4706, F， F, F, n-PrO, CI), (M-4707, F， F, F, n-PrO, F), (M-4708, F, F, F, n-PrO, CFs), (M-4709, F, F， F, n-PrO, Br), (M-4710, F, F, F, n-PrO, CH3), (M-4711, F, F, F, PhO, H), (M-4712, F, F， F, PhO, CI), (M-4713, F, F, F, PhO, F)，（M-4714, P, F, F, PhO, CFs), (M- 4715, F， F, F, PhO, Br), (M-4716, F, F, F, PhO, CHs), (M-4717, F, F， F, BnO, H), (M-4718, F, F, F, BnO, CI), (M-4719, F, F, F, BnO, F), (M-4720, F, F, F, BnO, CFs), (M-4721, F, F, F, BnO, Br), (M-4722, F, F, P, BnO, CHs), (M-4723, F, F, F, PhCH2CH20, H)， (M-4724, F, F, F, PI1CH2CH2O, CI), (M-4725, F, F, F,
PhCH2CH20) P), (M-4726, P, F, F, PhCHaCHaO, CFs), (M-4727, F, F, F,
PI1CH2CH2O, Br), (M-4728, F, F， F,； PI1CH2CH2O, CHs), (M-4729, F, F, F, CF30, H), (M-4730, F, F, F, CF30, CI), (M-4731, F, F, F, CFsO, F), (M-4732, F， F, F, CFsO, CFs), (M-4733, F, F, P, CFsO, Br), (M-4734, F, F, F' CF3O, CHs), (M-4735, F， F, F, Ph, H), (M-4736, F, F, F, Ph, CI), (M-4737, F， F, F, Ph, F), (M-4738, F, F, F, Ph, CFs), (M-4739, F, F, F, Ph, Br), (M-4740, F, F, F, Ph, CHs), (M-4741, F, F, F, 4-F-Ph, H), (M-4742, F， F， F, 4-F-Ph, CI), (M-4743, F, F, F, 4-F-Ph, F), (M-4744, F， F, F, 4-F-Ph, CF3)， (M-4745, F, F, F, 4-F-Ph, Br), (M-4746, F, F, F, 4-F-Ph, CH3)"(M-4747, F, F, F, 4-CPVPh, H),- (M-4748, F, F, F, 4-CF3.-Ph, CI), (M-4749, F, F, F, 4-CFs-Pli, F), (M-4750, F, F' F, 4-CPVPh, CFs), (M-4751, F, F, P, 4-CPs-Ph, Br), (M-4752, F, F, F, 4-CF3-Ph, CH3), (M-4753, F, F, F, 4- (Me)2N-Ph, H), (M-4754, F, F, F, 4-(Me)2N-Ph, CI), (M-4755, F, F, F, 4- (Me)2N-Ph, F), (M-4756, F, F, F, 4-(Me)2N-P ) CF3), (M-4757, F, F, F, 4- (Me)2N-Ph, Br), (M-4758, F, F, F, 4- (Me)2N-Ph, CHs), (M-4759, F, F， F, 4-OH- Ph, H), (M-4760, F, F, F, 4- OH-Ph, CI), (M-4761, F, F, F, 4-OH-Ph, F), (M-4762, F, F, F， 4-OH-Ph, CFs), (M-4763, F, F, F, 4-OH-Ph, Br), (M-4764, F, F, F, 4- OH-Ph, CHs), (M-4765, F， F, F, 3, 4- di-F-Ph, H), (M-4766, F, F, F, 3, 4-di-F-Ph, CI), (M-4767, F, F, F, 3, 4- di-F-Ph, F), (M-4768, F, F, F, 3, 4-di-F-Pli, CFs) , (M- 4769, F， F， F, 3, 4-di-F-Ph, Br), (M-4770, F, F, F, 3, 4-di-F-Ph, CHs), (M-4771, F， F, F, 4- COOH-Ph, H), (M- 4772, F, F, F, 4- COOH-Ph, Cl)， (M-4773, F, F, F， 4- CO OH-Ph, F)， (M-4774, F, P, F， 4-COOH-Ph, CF3), (M-4775, F， F, F, 4- COOH- Ph, Br), (M-4776, F, F, F, 4- CO OH-Ph' CHs), (M-4777, F, F, F, Bn, H)，（M-4778, F, F， F, Bn, CI), (M-4779, F, F, F, Bn, F), (M-4780, F, F, F, Bn, CFs), (M-4781, F, F, F' Bn, Br), (M-4782, F, F, F, Bn, CHs), (M-4783, F, F' F, 4-F-Bn' H), (M-4784, F, F, F, 4-F-Bn, CI), (M-4785, F, F, F, 4-F-Bn, F), (M-4786, F, F' F, 4-P-Bn, CFs), (M-4787, F， F, F, 4-F-Bn, Br), (M-4788, F, F, F, 4-F-Bn, CHs), (M-4789, F, F, F, 2-Py, H), (M-4790, F, F, F, 2-Py, CI), (M-4791, F, F, F, 2-Py, F), (M-4792, F, F, F, 2-Py, CFs), (M-4793, F, F, F, 2-Py, Br), (M-4794, F, F, F, 2-Py, CHs), (M-4795, F, F, F， 3-Py, H), (M- 4796, F, F, F, 3 -Py, CI), (M-4797, F, F, F, 3-Py, F), (M-4798, F, F, F, 3-Py, CF3)， (M-4799, F, F, F, 3-Py, Br) , (M-4800, F, F, F, 3-Py, CHs), (M-4801, F, F, F, 4-Py, H), (M-4802, F, F, F, 4-Py, CI), (M-4803, F, F, F, 4-Py, F), (M-4804, F, F, F, 4-Py, CF3), (M-4805, F, F， F, 4-Py, Br), (M-4806, F, F, F, 4-Py, CHs), (M-4807, F， F, F， 2-Th, H) , (M-4808, F, F, F, 2-Th, CI), (M-4809, F， F， F, 2-Th, F), (M-4810, F, F, F, 2-Th, CF3), (M-4811, F, F, F, 2-Th, Br), (M-4812, P, F, F, 2-Th, CHs), (M-4813, F, F， F, 3-Th, H), (M-4814, F, F, F, 3-Th, CI), (M-4815, F, F, F, 3 -Th, F), (M-4816, F， F， F, 3-Th, CF3), (M-4817, F， F, F, 3-Th, Br), (M-4818, F, F, F, 3 -Th, CH3), (M-4819, F, F, F, pyrazol-2-yl, H), (M-4820, F, F, F, pyrazol-2-yl, CI), (M-4821, F, F, F, pyrazol-2-yl, F), (M-4822, F, P, F, pyrazoレ 2-yl' CFs), (M-4823, F, F, F, pyrazol-2-yl, Br), (M-4824, F, F, F, pyrazol-2-yl; CHs), (M-4825, F, F, F, pyrazol-3-yl; H), (M-4826, F, P, F， pyrazol-3-yl, CI), (M-4827, F, F, F, pyrazol- 3-yl, F), (M-4828, F, F, F, pyrazol- 3-yl, CFs), (M-4829, F, F, F, pyrazol- 3-yl, Br), (M-4830, F, F, F， pyrazol-3-yl, CHs), (M-4831, F, F, F, pyrimidin-2-yl, H), (M-4832, F, F, F， pyrimidin-2-yl, CI), (M-4833, F, F, F, pyrimidin-2-yl, F), (M-4834, F, F, F, pyrimidin-2-yl, CFs), (M-4835, F, F， F, pyrimidin-2-yl, Br), (M-4836, F, F, F, pyrimidin-2-yl, CH3)， (M-4837, F, F， F, pyrimidin-4-yl, H), (M-4838, F, F, F, pyrimidin-4-yl, CI), (M-4839, F, F, F, pyrimidm-4-yl, F), (M-4840, F, F, F, pyrimidin-4-yl, CF3), (M-4841, F, F， F, pyrimidin-4-yl, Br), (M-4842, F, F, F, pyrimidin-4-yl, CHs), (M-4843, F, F, F, pyrimidin-5-yl, H), (M-4844, F, F, F, pyrimidin-5-yl, CI), (M-4845, F, F, F, pyrimidin-5-yl, F), (M-4846, F, F, F, pyrimidin-5-yl, CF3), (M-4847, F， F, F, pyrimidin-5-yl, Br), (M-4848, F, F, F, pyrimidin-5-yl, CHs), (M-4849, F, F， F, HOOCCH2CH2CH2, H), (M-4850, F, F, F, HOOCCH2CH2CH2' CI), (M-4851, F, F' F, HOOCCHaCHaCHs, F), (M-4852, F, F, F，
HOO CCH2CH2CH2) CFs), (M-4853, F， F, F， HOO CCH2CH2CH2, Br), (M-4854, F, F, F, HOOCCH2CH2CH2, CHs), (M-4855, F, F, F, HOO CCH2CH2CH2CH2, H), (M-4856, F, F, F' HOOCCH2CH2CH2CH2, CI), (M-4857, F, F, F,
HOO CCH2CH2CH2CH2, F), (M-4858, F, F, F, HOOCCH2CH2CH2CH2, CFs), (M-4859, F, F' F, HOOCCH2CH2CH2CH2， Br), (M-4860, F, F, F,
HOO CCH2CH2CH2CH2, CHs), (M-4861, F, F, F, (Me)2NCOCH2CH2CH2CH2, H), (M-4862, F, F, F, (Me)2NCOCH2CH2CH2CH2， CI), (M-4863, F, F, F,
(Me)2NCOCH2CH2CH2GH2, F), (M-4864, F, F, P, (Me)2NCOCH2CH2CH2CH2， CFs), (M-4865, F' F' F, (Me)2NCO CH2CH2CH2CH2; Br), (M-4866, F, F, F, (Me)2NCOCH2CH2CH2CH2, CHs), (M-4867, F, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-4868, F, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-4869, F, F, F, (Me)2NCOCH2CH2CH2CH2CH2, F), (M-4870, F, F, F,
(Me)2NCOCH2G CH2CH2CH2, CF3), (M-4871, F, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-4872, F, F, F,
(Me)2NCOCH2CH2CH2CH2CH2) CH3), (M-4873, F, F, F, MeOCH2) H), (M-4874, F, F, F, MeOCH2) CI), (M-4875, F, F, F, MeOCH2) F), (M-4876, F, F, F, MeOCH2， CF3), (M-4877, F, P, P, MeOCH2, Br), (M-4878, F, F, F, MeOCH2) CHa), (M-4879, F, F, F, EtOCHa, H)' (M-4880, F， F, F, EtOCH2j CI), (M-4881, F， F, F, EtOCH2, F), (M-4882, F, F, F, EtOCH2, CF3), (M-4883, F, F, F, EtOCH2' Br), (M-4884, F， F, F, EtOCH2> CH3), (M-4885, F, F， F, EtOCH2CH2, H), (M-4886, F, F, F， EtOCH2CH2, CI), (M-4887, F, F, F， EtOCH2CH2) F)， (M-4888, F, F, P,
EtOCH2CH2, CFs), (M-4889, F, F, F, EtOCH2CH2) Br), (M-4890, F, F, F, EtOCH2CH2) CH3), (M-4891, F, F, F, MeOCH2CH20CH2CH2, H), (M-4892, F， F, F, MeOCH2CH20CH2CH2; CI), (M-4893, F, F, F, MeOCH2CH2OCH2CH2, F), (M-4894, F, F, F, MeOCHaCHsOCHsCHs, CFs), (M-4895, F, F, F,
MeOCH2CH20GH2CH2, Br), (M-4896, F, F, F, MeOCH2CH2OCH2CH2, CH3),
(M-4897, F, F, F, MeOCH2CH2, H)， (M-4898, F, F, F, MeOCH2CH2, CI), (M-4899, F, F, F, MeOCH2CH2) F), (M-4900, F, F, F, MeOCH2CH2; CF3), (M-4901, F, F, F, MeOCH2CH2) Br), (M-4902, F, F, F, MeOCH2CH2, CH3), (M-4903, F, F, F， HOCH2) H), (M-4904, F, F, F, HOCH2, CI), (M-4905, F, F, F, HOCH2, F), (M- 4906, F, F, F, HOCH2) CF3), (M-4907, F, F, F, HOCH2) Br), (M-4908, F, F, F, HOCH2, CH3), (M-4909, F, F, F, HOCH2CH2' H), (M-4910, F, F, F, HOCH2CH2, CI), (M-4911, F, F, F, HOCH2CH2, F), (M-4912, F, F, F, HOCH2CH2' CF3), (M- 4913, F, F, F;. HOCH2CH2) Br), (M-4914, F, F, F, HOCH2CH2; CHs), (M-4915, F, F, F, HOCH2CH2CH2) H), (M-4916, F; F, F, HOCH2CH2CH2， CI), (M-4917, F, F, F, HOCH2CH2CH2， F)，（M-4918, F, F, F, HOCH2CH2CH2, CF3), (M-4919, F, F, F, HOCH2CH2CH2, Br), (M-4920, F， F, F, HOCH2CH2CH2, CHs), (M-4921, F, F, F， HOCH2CH2CH2CH2, H)， (M-4922, F， F, F, HOCH2GH2CH2CH2, CI), (M-4923, F, F, F, HOCH2CH2CH2CH2, F), (M-4924, F, F， F, HOCH2CH2GH2CH2, CF3), (M- 4925, F, F, F, HOCH2CH2CH2CH2, Br), (M-4926, F, F, F, HOCHsCHsCHsCHs, CHs), (M-4927, F, F, F, HOCH2CH2CH2CH2CH2， H), (M-4928, F, F, F，
HOCH2CH2CH2CH2CH2j CI), (M-4929, F, F, F, HOCH2CH2CH2CH2CH2, F), (M-4930, F， P, F, HOCH2CH2CH2CH2CH2, CFs), (M-4931, F, F, F;
HOCH2CH2CH2CH2CH2, Br), (M-4932, F, F, F, HOCH2CH2CH2CH2CH2, CHs), (M-4933, F, F' F, HOCH2CH2OCH2GH2， H), (M-4934, F, F, F，
HOCH2CH2OCH2CH2, CI), (M-4935, F, F, F, HOCH2CH2OCH2CH2, F), (M-4936, F, F, F, HOCH2CH2OCH2CH2, CFs), (M-4937, F, F, F, HOCHsCHsOCHsCHs, Br), (M-4938, F, F, F, HOCH2CH2OCH2CH2, CHs), (M-4939, F, F, F, (Me)2N, H), (M-4940, F, F, F, (Me)2N, CI), (M-4941, F, F, F, (Me)2N, F)， (M-4942, F, F, F, (Me)2N， CFs), (M-4943, F, F, F, (Me)2N; Br), (M-4944, F, F, F, (Me)2N, CHs), (M-4945, F, F, F, piperidin-4-yl-methyl, H), (M-4946, F, F, F, piperidin-4-yl- methyl, CI), (M-4947, F, F, F, piperidin-4-yl-metliyl, F), (M-4948, F， F， F, piperidm-4-yl-methyl, CFs), (M-4949, F, F, F, piperidin-4-yレ methyl, Br), (M- 4950, F, F, F, piperidin-4-yl-metliyl, CHs), (M-4951, F, F, F, cyclohexylmethyl, H)， (M-4952, F, F, F, cyclohexylmethyl, CI), (M-4953, F, F， F, cyclohexylmethyl, F), (M-4954, F, F, F, cyclohexylmethyl, CFs), (M-4955, F, F, F,
cyclohexylmethyl, Br), (M-4956, F, F, F, cyclohexylmethyl, CHs), (M-4957, F, F, CI, H, H), (M-4958, F, F, CI, H， CI), (M-4959, F, F, CI, H, F)， (M-4960, F, F, CI, H, CFs), (M-4961, F; P, CI, H, Br), (M-4962, F, F, CI, H, CHs),. (M-4963, F, F, CI, F, H), (M-4964, F, F, CI,. F, CI), (M-4965, F, F, CI, F, P), (M-4966, F, F, CI, F, CFs), (M-4967, F, F, CI, F, Br), (M-4968, F, F, CI, F, CHs), (M-4969, F, F, CI, CI, H), (M-4970, F, F, CI, CI, CI), (M-4971, F, F, CI, CI, F); (M-4972, F, F, CI, CI, CF3), (M-4973, F, F, CI, CI, Br), (M-4974, F, F, CI, CI, CHs), (M-4975, P, F, CI, CH3, H); (M-4976, F, F, CI, CH3) CI), (M-4977, F, F, CI, CHs, F), (M-4978, F, F， CI, CHs, CFs), (M-4979, F, F, CI, CH3, Br), (M-4980, F, F, CI, CH3) CHs), (M- 4981, F, F, CI, Et, H), (M-4982, F, F, CI, Et, CI), (M-4983, F, F, CI, Et, F), (M- 4984， F, F, CI, Et, CFs), (M-4985, F, F, CI, Et, Br), (M-4986, F, F, CI, Et, CHs), (M-4987, F, F, CI, n-Pr, H), (M-4988, F, F, CI, n-Pr, CI), (M-4989, F, F, CI, n- Pr, F), (M-4990, F, F， CI, n-Pr, CFs), (M-4991, F, F, CI, n-Pr, Br), (M-4992, F, F, CI, n-Pr, CHs), (M-4993, F， F, CI, c-Pr, H), (M-4994, F, F, CI, c-Pr, CI), (M-4995, F, F, CI, c-Pr, F)， (M-4996, F, F, CI, c-Pr, CFs), (M-4997, F, F， CI, c-Pr, Br), (M-4998, F, F, CI, c-Pr, CH3), (M-4999, F, F, CI, i-Pr, H)， (M-5000, F, F, CI, i- Pr, CI), (M-5001, F， F, CI, i-Pr, F), (M- 5002, F, F， CI, i-Pr, CFs), (M-5003, F' F， CI, i-Pr, Br), (M-5004, F, F, CI, i-Pr, CHs), (M- 5005, F, F, CI, n-Bu, H)， (M-5006, F, F, CI, n-Bu, CI), (M-5007, F, F, CI, n-Bu, F), (M-5008, F, F, CI, n-Bu, CF3), (M- 5009, F, F, CI, n-Bu, Br), (M-5010, F, F, CI, n-Bu, CH3), (M-5011, F， F, CI, i-Bu, H), (M-5012, F, F, CI, i-Bu, CI), (M-5013, F; F, CI, i-Bu, F)， (M-5014, F, F， CI, i-Bu, CFs), (M-5015, F, F, CI, i-Bu, Br), (M-5016, F, F， CI, i-Bu, CHs), (M- 5017, F, F, CI, sec-Bu, H), (M-5018, F; F, CI, sec-Bu, CI), (M-5019, F' F, CI, sec-Bu, F), (M-5020, F, F, CI, sec-Bu, CFs), (M-5021, F， F, CI, sec-Bu, Br), (M-5022, F, F, CI, sec-Bu, CHs), (M-5023, F， F, CI, n-Pen, H)， (M-5024, F, F, CI, n-Pen, CI), (M-5025, F, F, CI, n-Pen, F), (M-5026, F, F, CI, n-Pen, CFs), (M-5027, F, F, CI, n-Pen, Br), (M- 5028, F, F, CI, n-Pen, CH3), (M-5029, F, F, CI, c-Pen, H), (M-5030, P, F, CI, c-Pen, CI), (M-5031, F, F, CI, c-Pen, F), (M-5032, F, F， CI, c-Pen, CFs), (M-5033, F， F, CI, c-Pen, Br), (M-5034, F, F, CI, c-Pen, CHs), (M- 5035, F, F, CI, n-Hex, H), (M- 5036, F, F, CI, n-Hex, CI), (M- 5037, F, F, CI, n- Hex, F), (M-5038, F, F, CI, n-Hex, CF3), (M-5039, P, F, CI, n-Hex, Br), (M-5040, F, F, CI, n-Hex, CHs), (M-5041, F, F, CI, c-Hex, H), (M-5042, F, F, CI, c-Hex, CI), (M- 5043, F, F, CI, c-Hex, F), (M-5044, F, , CI, c-Hex, CF3), (M-5045, F, F, CI, c-Hex, Br), (M-5046, F, P, Cl, c-Hex, CH3)， (M-5047, F; F, Cl, OH, H), (M-5048, F, F, Cl, OH, Cl), (M-5049, F, F, Cl, OH, F), (M-5050, F, F, Cl, OH, CF3), (M- 5051， P, F, Cl, OH, Br), (M- 5052, F, F, Cl, OH, CH3), (M-5053, F, F, Cl, EtO, H), (M-5054, F, F, Cl, EtO, Cl), (M-5055, F, F, Cl, EtO, F), (M-5056, F， F, Cl, EtO, CFs), (M-5057, F, F, Cl, EtO, Br), (M-5058, F, F, Cl, EtO, CHs), (M-5059, F, F, Cl, n-PrO, H), (M-5060, F, F, Cl, n-PrO, Cl), (M-5061, F， F， Cl, n-PrO, F), (M- 5062, F, F, Cl, n-PrO, CFs), (M-5063, F, F, Cl, n-PrO, Br), (M-5064, F, F, Cl, n-PrO, CHs), (M-5065, F, F, Cl, PhO, H), (M- 5066, P, F, Cl, PhO, Cl), (M- 5067, F， F, Cl, PhO, F), (M-5068, F, F, Cl, PhO, CF3), (M-5069, F, F, Cl, PhO, Br), (M-5070, F, F， Cl, PhO, CHs), (M-5071, F, F， Cl, BnO, H), (M-5072, F, F, Cl, BnO, Cl), (M-5073, F, F, Cl, BnO, F), (M-5074, F, F, Cl, BnO, CFs), (M-5075, F, F, Cl, BnO, Br), (M-5076, F, F, Cl, BnO, CHs), (M-5077, F, F, Cl, PhCH2CH20, H), (M-5078, F， F, Cl, PhCHsCHsO, Cl), (M-5079, F, F， Cl, PI1CH2CH2O, F), (M-5080, F， F, Cl, PI1CH2CH2O, CF3); (M-5081, F, F, Cl, PhCHaCHaO, Br), (M-5082, F, F, Cl, PhCHaCHaO, CH3)，（M-5083, F, F, Cl, CFaO, H)， (M- 5084, F, F, Cl, CF3O, Cl), (M-5085, F, F, Cl, CFsO, F), (M-5086, F, F, Cl, CFsO, CFs), (M-5087, F， F, Cl, CFsO, Br), (M-5088, F, F, Cl, CFsO, CH3), (M-5089, F, F, Cl, Ph, H)， (M-5090, F, F, Cl, Ph, Cl), (M-5091, F, F, Cl, Ph, F), (M-5092, F, F, Cl, Ph, CF3), (M-5093, F, F, Cl, Ph, Br), (M-5094, F, F， Cl, Ph, CH3), (M-5095, F, F, Cl, 4-F-Ph, H), (M-5096, F, F, Cl, 4-F-Ph, Cl), (M-5097, F, F， Cl, 4-F-Ph, F),
(M-5098, F, F, Cl, 4-F-Ph, CFs), (M-5099, F, F, Cl, 4-F-Ph, Br), (M-5100, F, F, Cl, 4-F-Ph, CHs), (M-5101, F, F, Cl, 4- CPVPh, H), (M.-5102, F, F, Cl, 4-CFs-Pli, Cl), (M-5103, F, F， Cl, 4-CFs-Ph, F); (M-5104, F, F， Cl, 4-CFs-Ph, CFs), (M-5105, F, F, Cl, 4-CFs-Pli, Br), (M-5106, F, F, Cl, 4-CF3-Ph, CH3), (M-5107, F, F, Cl, 4- (Me)2N-Ph, H), (M-5108, F, F, Cl, 4-(Me)2N-Ph, Cl), (M-5109, F， F, Cl, 4- (Me)2N-Ph, F), (M-5110, F, F, Cl, 4-(Me)2N-Pli; CF3), (M-5111, F; F, Cl, - 〇 o
o
Figure imgf000175_0001
,,)),,,,,,,, 5116 C 4〇ll CS117 F FIipiF 5 F COPr FI 4Hh B---- ,,,,),,,,,, CO 5114 FIHh C5 F C0Pli F 4PI 511 FI 4H F---- )),)),,,,,2 eNp2S Chr ep C 513 FI BNhH1 F 4-- F, F, CI, pyrazoレ 2-yl, CFs), (M-5177, F, F, CI, pyrazol-2-yl, Br), (M-5178, F, F, CI, pyrazol-2-yl, CHs), (M-5179, P, F, CI, pyrazol-3-yl; H), (M-5180, F, F, CI, pyrazol- 3-yl, CI), (M-5181, F, F, CI, pyrazol-3-yl, F), (M-5182, F, F， CI, pyrazol-3-yl, CPs), (M-5183, F, F, CI, pyrazol-3-yl, Br), (M- 5184, F， F， CI, pyrazol-3-yl; CHs), (M-5185, F, F, CI, pyrimidin-2-yl, H), (M-5186, F， F, CI, pyrimidin-2-yl, CI), (M-5187, F, P, CI, pyrimidin-2-yl, F), (M-5188, F, F, CI, pyrimidin-2-yl, CF3)，（M-5189, F, F, CI, pyrimidin-2-yl, Br), (M-5190, F, F, CI, pyrimidin-2-yl, CHs), (M-5191, F, F, CI, pyrimidin-4-yl, H), (M-5192, F, F， CI, pyrimidin-4-yl, CI), (M-5193, F, F, CI, pyrimidin-4-yl, F), (M-5194, F， F, CI, pyrimidin-4-yl, CF3)， (M- 5195, F， F, CI, pyrimidin-4-yl, Br), (M-5196, F, F， CI, pyrimidin-4-yl, CHs), (M-5197, F, F, CI, pyrimidin-5-yl, H)， (M-5198, F, F, CI, pyrimidin- 5-yl, CI), (M-5199, F, F, CI, pyrimidin-5-yl, F), (M-5200, F, F, CI, pyrimidin-5-yl, CFs), (M- 5201, F, F, CI, pyrimidin-5-yl, Br), (M-5202, F, F, CI, pyrimidin-5-yl, CH3), (M-5203, F， F, CI, HOOCCH2CH2CH2, H)， (M-5204, F, F, CI, HOO CCH2CH2CH2, CI), (M-5205, F, F, Cl， HOO CCH2CH2CH2, F), (M-5206, F， F, CI, HOOCCH2CH2CH2, CFs), (M-5207, F， F, CI, HOO CCH2CH2CH2, Br), (M-5208, F, F, CI, HOOCCH2CH2CH2, CHs), (M-5209, F, F, CI,
HOOCCH2CH2CH2CH2) H), (M- 5210, F, F, CI, HOOCCHaCHaCHaCHa, CI), (M-5211, F, F， CI, HOOCCH2CH2CH2CH2， F), (M-5212, F, F, CI,
HOO CCH2CH2CH2CH2; CF3), (M-5213, F, P, CI, HOO CCH2CH2CH2CH2, Br), (M-5214, F, F, CI, HOO CC^CHzCHsCtb, CHs), (M- 5215, F, F, CI,
(Me)2NCOCH2CH2CH2CH2， H)， (M-5216, F, F, CI, (Me)2NCO CH2CH2CH2CH2, CI), (M-5217, F, F' CI, (Me)2NCOCH2CH2CH2CH2' F), (M-5218, F, F, CI, (Me)2NCO CH2CH2CH2CH2， CFs), (M-5219, F, F, CI, (Me)2NCOCH2CH2CH2CH2， Br), (M-5220, F， F, CI, (Me)2NCO CH2CH2CH2CH2' CHs), (M-5221, F, F, CI, (Me)2NCO CH2CH2CH2CH2CH2, H), (M-5222, P, F, CI, (Me)2NCOCH2CH2CH2CH2CH2, CI), (M-5223, F, F, Cl，
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-5224, F, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2> CFs), (M-5225, F, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-5226, F, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-5227, F, F' CI, MeOCH2, H), (M-5228, F, F, CI, MeOCHs, CI), (M-5229, F, F, CI, MeOCH2) F), (M-5230, F, F， CI, MeOCHs, CFs), (M-5231, F, F, CI, MeOCHa, Br), (M-5232, F, F， CI, MeOCH2) CH3), (M-5233, F, F, CI, EtOCHa, H), (M-5234, F, F, CI, EtOCH2, CI), (M-5235, F, F, CI, EtOCH2; F), (M-5236, F, F, CI, EtOCHa, CFs), (M-5237, F, F, CI, EtOCH2; Br), (M-5238, F, F， CI, EtOCH2， CH3), (M-5239, F, F, CI, EtOCH2CH2; H), (M-5240, F， F, CI, EtOCH2CH2; CI), (M-5241, F, F, CI, EtOCH2CH2; F), (M-5242, F, F， CI, EtOCH2CH2, CFs), (M-5243, P, F, CI, EtOCH2CH2; Br), (M- 5244, F, F, CI, EtOCH2CH2, CHs), (M-5245, F, F, CI, MeOCHaCHaOCHsCHa, H), (M-5246, F, F, CI, MeOCH2CH2OCH2CH2, CI), (M-5247, F' F, CI,
MeOCH2CH2OCH2CH2) F), (M-5248, F, F, CI, MeOCH2CH2OCH2CH2, CF3), (M-5249, F, F, CI, MeOCH2CH2OCH2C Br), (M-5250, F, F, CI,
MeOCH2CH20CH2CH2> CH3), (M-5251, F, F, CI, MeOCH2CH2, H), (M-5252, F' F, CI, MeOCH2CH2) CI), (M-5253, F, F, CI, MeOCH2CH2) F), (M-5254, F, F, CI, MeOCHsCHs, CFs), (M-5255, F, F, CI, MeOCH2CH2) Br), (M-5256, F' F, CI, MeOCH2CH2; CHs), (M-5257, F， F, CI, HOCHa, H), (M-5258, P, F， CI, HOCH2, CI), (M-5259, F, F, CI, HOCH2, F), (M-5260, F, F, CI, HOCHs, CFs), (M-5261, F, P, CI, HOCH2, Br), (M-5262, F, F, CI, HOCHs, CHs), (M-5263, F, F, CI,
HOCH2CH2, H), (M-5264, F, F, CI, ΗΟΟΗ2ΟΗ2) CI), (M-5265, F, F, CI,
HOCH2CH2， F), (M-5266, F, F, CI, HOCH2CH2, CFs), (M-5267, F, F, CI, HOCH2CH2; Br), (M-5268, F, CI, HOCH2CH2) CHs), (M-5269, F, F, CI,
HOCH2CH2CH2j H), (M-5270, F, F， CI, HOCH2CH2CH2) CI), (M-5271, F, F, CI, HOCH2CH2CH2, F), (M-5272, F, F, CI, HOCH2CH2CH2, CFs), (M-5273, F, F, CI, HOCH2CH2CH2, Br), (M-5274, F, F, CI, HOCH2CH2CH2) CHs), (M-5275, F, F， CI, HOCH2CH2CH2CH2, H)， (M-5276, F, F, Cl， HOCH2CH2CH2CH2, CI), (M- 5277, F, F, CI, HOCH2CH2CH2CH2, F), (M-5278, F, F, CI, HOCH2CH2CH2CH2， CFs), (M-5279, F, F, CI, HOCH2CH2CH2CH2, Br), (M-5280, F, F, CI,
HOCH2CH2CH2CH2, CH3), (M-5281, F, F, CI, HOCH2CH2CH2CH2CH2, H), (M- 5282, F, F, CI, HOCH2CH2CH2CH2CH2, CI), (M-5283, F, F, CI,
HOCH2CH2CH2CH2CH2) F), (M-5284, F, F, CI, HOCH2CH2CH2CH2CH2) CFs), (M-5285, F, F, CI, HOCH2CH2CH2CH2CH2, Br), (M-5286, F, F, CI,
HOCH2CH2CH2CH2CH2, CH3); (M-5287, F, F, CI, HOCH2CH2OCH2CH2, H), (M-5288, F， F, CI, HOCH2CH2OCH2CH2, CI), (M-5289, F, F， CI,
HOCH2CH20CH2CH2) P), (M-5290, F, F, CI, HOCH2CH2OCH2CH2, CFs), (M- 5291, F， F, CI, HOCIiaCHzOCHzCHs, Br), (M-5292, F, F, CI,
HOCH2CH2OCH2CH2; CHs), (M-5293, F, F, CI, (Me)2N, H), (M-5294, F, F, CI, (Me)2N, CI), (M-5295, F, F, CI, (Me)2N, F), (M-5296, F, F, CI, (Me)2N, CFs),
(M-5297, F, F, CI, (Me)2N, Br), (M-5298, F, F, CI, (Me)2N, CH3), (M-5299, F, F, CI, piperidin-4-yl-methyl, H), (M-5300, F， F, CI, piperidin-4-yl-methyl, CI), (M-5301, F, F, CI, piperidin-4-yl-metliyl, F), (M-5302, F, F, CI, piperidin-4-yl- methyl, CPs), (M-5303, F, F, CI, piperidin-4-yl-methyl, Br), (M-5304, F， F, CI, piperidm-4-yl-methyl, CH3), (M-5305, F, F, CI, cyclohexylmetliyl, H), (M-5306, F, F' CI, cyclohexylmethyl, CI), (M-5307, F, F, CI, cyclohexylmethyl, F), (M- 5308, F, F, CI, cyclohexylmetliyl, CFs), (M-5309, F, F, CI, cyclohexylmethyl, Br), (M-5310, F, F, CI, cyclohexylmethyl, CHs), (M-5311, F, CHs, H， H, H)，（M-5312, F, CH3) H, H, CI), (M-5313, P, CHs, H， H， F), (M-5314, F, CHs, H, H, CF3), (M-5315, F, CHs, H, H, Br), (M-5316, F, CHs, H, H, CH3), (M-5317, F, CHs, H, F, H), (M-5318, F, CHs, H, F, CI), (M-5319, F, CH3, H, F, F), (M-5320, F, CHs, H, F, CFs), (M-5321, F, CHs, H, F, Br), (M-5322, F， CHs, H, F, CHs), (M-5323, F, CHs, H, CI, H), (M-5324, F, CH3, H, CI, CI), (M-5325, F, CHs, H, CI, F), (M-5326, F, CHs, H, CI, CPs), (M-5327, F; CHs, H, CI, Br), (M-5328, P, CH3, H' CI, CH3), (M-5329, F, CHs, H, CHs, H), (M-5330, F, CHs, H, CHs, CI), (M-5331, F, CHs, H, CHs, F), (M-5332, F, CH3, H, CH3; CF3), (M-5333, F， CH3) H, CH3; Br), (M-5334, F, CHs, H, CHs, CH3); (M-5335, F, CHs, H, Et, H)， (M-5336, F, CHs, H， Et, CI), (M-5337, F, CHs, H， Et, F), (M-5338, F, CHs, H, Et, CF3), (M-5339, F, CH3, H' Et, Br), (M-5340, F, CHs, H, Et, CHs), (M-5341, F, CHs, H, n-Pr; H), (M-5342, F, CHs, H, n-Pr, CI), (M-5343, F, CHs, H, n-Pr, F), (M-5344, F, CH3, H, n-Pr, CFs), (M-5345, F, CHs, H, n-Pr, Br), (M-5346, F, CHs, H, n-Pr, CHs), (M-5347, F, CHs, H' c-Pr, H), (M-5348, F, CH3) H， c-Pr, CI), (M-5349, F, CHs, H, c-Pr, F), (M-5350, F, CH3) H， c-Pr, CF3), (M-5351, F, CH3) H, c-Pr, Br), (M-5352, F, CH3, H， c-Pr, CHs), (M-5353, F, CH3) H， i-Pr, H), (M-5354, F， CHs, H, i-Pr, CI), (M-5355, F, CHs, H， i-Pr, F), (M-5356, F, CHs, H, i-Pr, CFs), (M-5357, F， CHs, H, i-Pr, Br), (M-5358, F, CHs, H, i-Pr， CH3), (M-5359, F, CHs, H, n-Bu, H), (M-5360, P, CH3, H, n-Bu, CI), (M-5361, F, CHs, H, n-Bu, F), (M-5362, F, CH3, H, n-Bu, CFs), (M-5363, F, CHs, H， n-Bu, Br), (M-5364, F, CHs, H, n-Bu, CHs), (M-5365, F, CHs, H, i-Bu, H), (M-5366, F, CHs, H, i-Bu, CI), (M-5367, F, CHs, H, i-Bu, F), (M-5368, F, CHs, H, i-Bu, CF3), (M-5369, F, CH3, H' i-Bu, Br), (M-5370, F, CH3, H, i-Bu, CHs), (M-5371, F, CHs, H, sec-Bu, H), (M-5372, F, CHs, H, sec-Bu, CI), (M-5373, F, CH3) H, sec-Bu, F), (M-5374, F, CH3, H, sec-Bu, CFs), (M-5375, F, CHs, H, sec-Bu, Br), (M-5376, F, CHs, H' sec-Bu, CH3), (M-5377, F, CHs, H, n-Pen, H), (M-5378, F, CHs, H, n-Pen; CI), (M-5379, F, CHs, H, n-Pen, F), (M- 5380, F, CHs, H, n-Pen, CFs), (M-5381, F, CHs, H, n-Pen, Br), (M-5382, F, CH3) H, n-Pen, CHs), (M-5383, F, CHs, H, c-Pen, H), (M-5384, F, CHs, H, c-Pen, CI), (M-5385, F, CHs, H, c-Pen, F), (M-5386, F, CHs, H, c-Pen, CFs), (M-5387, F， CHs, t t
o
Figure imgf000180_0001
),¾ (:,,,,, C3 57H 9 F C H Hex53 Cs〇39 HM96 FH H Hex1- ,)),,,,,,,3 HHe 393 F 93e nx CF CH H nffie Br cffi:HCxx F n--- ,:,,,,,,,,),, 3903 F CH HHe C 531 Ce 39 F CH nxI9 FH H nHx F2-- ),,),,,,,,s,, cPe8 H Hn M 538 F C cen c9 CexrHP 38 FH H nH--- t to
o
Figure imgf000181_0001
)),(,,,,),,2SeO68 C tMNh CH 467 F CH H 4HPh H 4 FHp--- )),,)),,,,,22 C36 Cs ep 566 F CH eNPF 45 FH H 4Nh Br4-- ),):,,(),,,223 Ce6 CHeNp。1 56H H 4M:NP F 44 F :h4 F--- ))(,,,,,,,2s6 C cpll CH6 F cffi 4eNh H2 FH 4 Hp 4--- )),,,,,,333CP C 9 F Q 50 CH 4F1IF^H H Br46 F.- ,,,,,,),,,,,,s C Hs33CFs58H CHCFp CI57 F S Hh F 4 F F H 4h 44P---.
),,, 5565s JH4 544 F CH ),))¾,,,,,,3 s G 553 F C H 4FPh Br FPh F 452 F CHF4---. o o
Figure imgf000182_0001
HOOCCH2CH2CH2CH2, H), (M-5564, F, CH3, H, HOOCCH2CH2CH2CH2, CI), (M-5565, F, CH3, H, HOOCCH2CH2CH2CH2, F), (M-5566, F, CH3, H,
HOOCCH2CH2CH2CH2, CF3); (M-5567, F， CH3, H， HOOCCH2CH2CH2CH2, Br), (M-5568, F, CH3, H, HOOCCH2CH2CH2CH2) CHs), (M-5569, F, CH3, H, (Me)2NCOCH2CH2CH2CH2, H), (M-5570, F, CH3; H, (Me)2NCOCH2CH2GH2CH2, CI), (M-5571, F, CHs, H, (Me)2NCOCH2CH2CH2CH2, F), (M-5572, F, C H， (Me)2NCOCH2CH2CH2CH2, CF3)， (M-5573, F, CH3, H,
(Me)2NCOCH2CH2CH2CH2， Br), (M-5574, F, CHs, H,
(Me)2NCOCH2CH2CH2CH2, CH3), (M-5575, F, CHs, H,
(Me)2NCOCH2CH2CH2CH2C¾, H), (M-5576, F, CH3, H,
(Me)2NCOCH2CH2CH2CH2CH2， CI), (M-5577, F, CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2' F), (M-5578, F， CH3， H，
(Me)2NCOCH2CH2CH2CH2CH2, CF3), (M-5579, F， CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2> Br), (M-5580, F, CH3， H,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-5581, F, CH3， H, MeOCHs, H), (M- 5582, F, CHs, H, MeOCHa, CI), (M-5583, F, CHs, H, MeOCHa, F), (M-5584, F, CH3, H, MeOCH2, CF3), (M-5585, F, CH3, H, MeOCH2, Br), (M-5586, F, CHs, H, MeOCHs, CHs), (M-5587, F, CHs, H, EtOCHs, H), (M-5588, F, CHs, H, EtOCHs, CI), (M-5589, F, CHs, H, EtOCH2) F), (M-5590, F, CHs, H, EtOCHs, CF3), (M- 5591' F, CH3, H, EtOCH2, Br), (M-5592, F, CH3, H, EtOCH2; CHs), (M-5593, F, CH3) H, EtOCH2CH2, H), (M-5594, F, CHs, H, EtOCH2CH2' CI), (M-5595, F, CHs, H, EtOCH2CH2; F), (M-5596, F, CH3, H, EtOCH2CH2; CFs), (M-5597, F, CHs, H, EtOCH2CH2, Br), (M-5598, F, CH3, H, EtOCH2CH2, CHs), (M-5599, F, CHs, H, MeOCH2CH2OCH2CH2, H), (M-5600, F, CH3; H, MeOCH2CH2OCH2CH2, CI), (M-5601, F; CHs, H, MeOCH2CH2OCH2CH2， F), (M-5602, F, CH3) H,
MeOCH2CH2OCH2CH2, CF3), (M-5603, F, CH3, H, MeOCH2CH2OCH2CH2, Br), (M-5604, F, CHs, H, MeOGH2CH2OCH2CH2， CHs), (M-5605, P, CHs, H，
MeOCH2CH2, H), (M-5606, F, CH3, H, MeOCH2CH2) CI), (M-5607, F, CH3, H, MeOCH2CH2, F), (M-5608, F, CH3, H, MeOCHaCHa, CF3), (M-5609, F, CH3, H, MeOCH2CH2, Br), (M-5610, F, CHs, H, MeOCH2CH2) CHs), (M-5611, F, CHs, H， HOCH2, H)， (M-5612, F, CHs, H, HOCH2, CI), (M-5613, F, CH3， H, HOCH2, F), (M-5614, F, CH3, H, HOC CFs), (M-5615, F, CHs, H, HOCHs, Br), (M-5616, F, CHs, H, HOCH2; CH3)， (M-5617, F, GH3, H, HOCH2CH2, H)， (M-5618, F, CH3, H, HOCH2CH2) CI), (M-5619, F, CH3) H, HOCH2CH2, F), (M-5620, F, CH3) H, HOCHaCHs, CPs), (M-5621, F, CH3, H, HOCH2CH2, Br), (M-5622, F, CH3) H, HOCH2CH2) CHs), (M-5623, F, CHs, H, HOCH2CH2CH2, H), (M-5624, F, CHs, H, HOCH2CH2CH2, CI), (M-5625, F, CHs, H， HOCHsCHsCK , F), (M-5626, F, CH3, H, HOCH2CH2CH2) CF3), (M-5627, F, CH3, H, HOCH2CH2CH2, Br), (M-5628, F; CHs, H, HOCH CH2CH2, CHs), (M-5629, F, CHs, H, HOCH2CH2CH2CH2, H), (M-5630, F， CHs, H' HOCH2CH2CH2CH2) CI), (M-5631, F, CH3, H,
HOCH2CH2CH2CH2) F), (M-5632, F, CH3, H, HOCH2CH2CH2CH2' CFs), (M- 5633, F, CHs, H, HOCHaCHaCHaCHs, Br), (M-5634, F, CH3) H,
HOCH2CH2CH2CH2, CH3)， (M-5635, F, CHs, H, HOCH2CH2CH2CH2CH2， H), (M-5636, F, CH3; H, HO CH2 CH2 CH2 CH2 CH2) CI), (M-5637, F, CHs, H,
HOCH2CH2CH2CH2CH2, F)，（M-5638, F， CH3) H, HOCH2CH2CH2CH2CH2, CFs), (M-5639, F, CH3; H, HOCH2CH2CH2GH2CH2, Br), (M-5640, F, CH3, H,
HOCH2CH2CH2CH2CH2, CH3), (M-5641, F, CHs, H， HOCH2CH2OCH2CH2, H), (M-5642, F, CH3; H, HOCHsCHsOCHzCHa, CI), (M-5643, F, CH3, H, . ,. . HOCH2CH2OCH2GH2, F)， (M-5644, F, CHs, H, HOCH2CH2OCH2CH2, CF3), (M-5645, F， CH3, H, HOCH2CH2OCH2CH2, Br), (M-5646, F, CH3, H,
HOCH2CH2OCH2CH2, CH3), (M-5647, F, CHs, H, (Me)2N, H), (M-5648, F, CH3, H, (Me)2N, CI), (M-5649, F, CHs, H, (Me)2N; F), (M-5650, F, CHs, H, (Me)2N， CFs), (M- 5651, F, CHs, H, (Me)2N， Br), (M- 5652, F, CHs, H, (Me)2N， CH3), (M-5653, F, CHs, H， piperidin-4-yl-metliyl, H), (M-5654, F, CHs, H, piperidin- 4-yl-metliyl, CI), (M- 5655, F, CH3, H, piperidin-4-yレ methyl, F), (M-5656, F, CH8) H, piperidin-4-yl-metliyl, CFs), (M-5657, F' CHs, H, piperidin-4-yl-metliyl, Br), (M-5658, F, CHs, H, piperidm-4-yl-methyl, CHs), (M-5659, F, CHs, H, cyclohexylmethyl, H), (M-5660, ¥, CHs, H, cyclohexylmethyl, CI), (M-5661, F, CHs, H, cyclohexylmethyl, F), (M-5662, F, CHs, H, cyclohexylmethyl, CF3), (M-5663, F, CHs, H, cyclohexylmethyl, Br), (M-5664, F, CHs, H;
cyclohexylmethyl, CHs), (M-5665, F, CHs, F, H, H), (M-5666, F, CHs, F, H, CI), (M- 5667, F, CHs, F， H, F), (M-5668, F, CH3, F, H, CFs), (M-5669, F， CHs, F, H, Br), (M- 5670, F, CHs, F, H, CHs), (M-5671, F， CH3, F, F, H), (M-5672, F, CHs, F, F, CI), (M-5673, F, CH3, F, F, F), (M-5674, F, CHs, F, F, CFs), (M-5675, F, CH3, F, F, Br), (M-5676, F, CH3) F, F, CH3), (M- 5677, P, CH3; F, CI, H), (M-5678, F, CHs, F, CI, CI), (M-5679, F, CHs, F, CI, F), (M-5680, F， CH3, F, CI, CFs), (M- 5681, F, CHs, F, CI, Br), (M-5682, F, CHs, F, CI, CH3), (M-5683, F, CHs, F, CH3, H), (M-5684, F， CH3, F, CH3, CI), (M-5685, F, CHs, F, CHs, F); (M-5686, F, CHs, F, CH3, CF3), (M-5687, F, CHs, F, CH3; Br), (M-5688, F, CH3; F, CHs, CH3), (M-5689, F, CHs, F, Et, H), (M-5690, F, CHs, F, Et, CI), (M-5691, F， CHs, F, Et, F), (M-5692, F, CHs, F, Et, CFs), (M-5693, F, CHs, F, Et, Br), (M-5694, F, CHs, F, Et, CHs), (M-5695, F, CHs, F, n-Pr, H), (M- 5696, F, CH3, F, n-Pr; CI), (M- 5697, F, CHs, F, n-Pr, F), (M-5698, F, CH3; F, n-Pr, CFs), (M-5699, F, CHs, F, n-Pr, Br), (M-5700, F， CH3; F, n-Pr, CHs), (M- 57.01, F, CHs, F, c-Pr, H), (M- 5702, F, CHs, F, c-Pr, CI), (M-5703, F, CHs, F, c-Pr, F), (M-5704, F, CHs, F, c-Pr, CFs), (M-5705, F, CHs, F, c-Pr, Br), (M-5706, F， CHs, F, c-Pr, CHs), (M-5707, F, CHs, F, i-Pr, H), (M- 5708, F, CH3) F, i-Pr, CI), (M-5709, F, CHs, F, i-Pr, F), (M-5710, F, CH3) F, i-Pr, CFs), (M-5711, F, CHs, F, i-Pr, Br), (M-5712, F, CHs, F, i-Pr, CH3), (M-5713, F, CHs, F, n-Bu, H), (M-5714, F, CH3， F; n-Bu, CI), (M- 5715, F, CH3, F, n-Bu, F), (M-5716, F, CHs, F, n-Bu, CFs), (M-5717, F, CHs, F, n-Bu, Br), (M-5718, F, CHs, F, n-Bu, CHs), (M-5719, F, CHs, F, i-Bu, H)， (M-5720, F, CH3, F, i-Bu, CI), (M-5721, F, CHs, F, i-Bu, F), (M-5722, F, CH3, F, i-Bu, CFs), (M- 5723, F, CH3, F, i-Bu, Br), (M-5724, F, CH3, F, i-Bu, CHs), (M-5725, F, CH3, F, sec-Bu, H)， (M-5726, F, CHs, F， sec-Bu, CI), (M- 5727, F, CHs, F, sec-Bu, F), (M-5728, F, CH3, F, sec-Bu, CFs), (M-5729, F, CHa, F, sec-Bu, Br), (M-5730, F, CHs, F, sec-Bu, CHs), (M-5731, F, CH3, F, n-Pen, H), (M-5732, F, CHs, F, n-Pen, CI), (M- 5733, F, CHs, F, n-Pen, F), (M-5734, F, CH3) F, n-Pen, CFs), (M-5735, F, CH3, F, n-Pen, Br), (M-5736, F， CH3, F, n-Pen, CH3), (M-5737, F, CH3, F, c-Pen, H), (M-5738, F, CH3, F, c-Pen, CI), (M-5739, F, CHs, F, c-Pen, F), (M- 5740, F, CH3) F, c-Pen, CFs), (M-5741, F, CHa, F, c-Pen, Br), (M-5742, F, CH3, F, c-Pen, CH3), (M-5743, F, CH3, F, n-Hex, H), (M-5744, F, CH3, F, n-Hex, CI), (M-5745, F， CHs, F, n-Hex, F), (M-5746, F, CH3; F, n-Hex, CFs), (M-5747, F, CHa, P, n- Hex, Br), (M-5748, F， CHs, F， n-Hex, CHs), (M-5749, F， CHs, F, c-Hex, H),
(M-5750, F, CHs, F, c-Hex, CI), (M-5751, F， CHs, F, c-Hex, F), (M- 5752, F, CHa, F, c-Hex, CFs), (M-5753, F， CH3, F, c-Hex, Br), (M-5754, F, CHs, F, c-Hex, CH3), (M-5755, F, CHs, F, OH, H), (M-5756, F, CH3) F, OH, CI), (M-5757, F， CH3， F, OH, F)， (M-5758, F, CHs, F, OH, CPs), (M-5759, F, CHa, F, OH, Br), (M-5760, F, CHs, F, OH, CH3), (M-5761, F, CHs, F' EtO, H), (M-5762, F, CH3, F' EtO, Cl)， (M-5763, F, CHs, F, EtO, F), (M-5764, F, CHs, F, EtO, CF3), (M-5765, F, CH3) F, EtO, Br), (M-5766, F, CHs, F, EtO, CHs), (M-5767, F, CH3, F, n-PrO„ H), (M- 5768, F, CHs, F, n-PrO, CI), (M-5769, F, CHs, F, n-PrO, F), (M-5770, F, CH3, F， n-PrO, CFs), (M-5771, F; CHs, F, n-PrO; Br), (M- 5772, F, CHs, F, n-PrO, CHs), (M-5773, F, CHs, P, PhO, H), (M-5774, F, CH3， F, PhO, CI), (M-5775, F, CH3, F, PhO, F), (M-5776, F, CHa, F, PhO, CFs), (M-5777, F, CHs, F, PhO, Br), (M- 5778, F, CH3) F, PhO; CHs), (M-5779, F, CH3; F, BnO, H), (M-5780, F， CHs, F, BnO, CI), (M-5781, F， CH3> F, BnO, F), (M-5782, F, CH3, F, BnO, CFs), (M-5783, P, CH3) F, BnO, Br), (M-5784, F, CH3> F, BnO, CHs), (M-5785, F， CHs, F,
PhCH2CH20; H), (M-5786, F, CH3， F, PhCHaCHaO, CI), (M-5787, F, CHs, F, PhCH2CH20; F), (M-5788, F, CH3, F, PI1CH2CH2O, CFs), (M-5789, F, CH3, F， PhCH2CH20, Br), (M-5790, F, CH3, F, PhCH2CH20, CHs), (M-5791, F， CHs, F, CFsO, H), (M-5792, F, CHs, F, CFsO, CI), (M-5793, F, CHs, F, CFsO, F)' (M-5794, F' CHs, F, CFsO, CF3), (M-5795, F, CH3, F, CFsO, Br), (M-5796, F, CHs, F, CFsO, CHs), (M-5797, F, CH3) F, Ph, H), (M-5798, F, CH3) F, Ph, CI), (M-5799, F, CH3, F， Ph, F), (M-5800, F， CHs, F， Ph, CFs), (M-5801, F, CH3， F, Ph, Br), (M-5802, F, CHs, F， Ph, CHs), (M-5803, F, CHs, F, 4-F-Ph, H), (M-5804, F, CHs, F, 4-F-Ph, CI), (M-5805, F, CH3) F, 4-F-Ph, F), (M-5806, F， CHs, F, 4-F-Ph, CFs), (M-5807, F, CHs, F, 4-F-Ph, Br), (M-5808, F, CHs, F, 4-F-Ph, CHs), (M-5809, F， CHs, F, 4-CFa-Pli, H), (M-5810, F， CH3, F, 4-CFs-Ph, CI), (M-5811, F, CH3， F, 4-CFa-Ph, F), (M-5812, F, CHs, F, 4-CF3-Pli， CFs), (M-5813, F, CH3) F, 4-CF3-Ph, Br), (M-5814, F, CHs, F, 4-CFs-Pli, CH3), (M-5815, F, CHs, F, 4-(Me)2N-Pli, H), (M-5816, F, CHs, F, 4-(Me)2N-Ph, CI), (M-5817, F， CHs, F, 4-(Me)2N-Ph, F), (M-5818, F, CHs, F, 4-(Me)2N-Pli> CFs), (M-5819, F, CHs, F, 4-(Me)2N-Ph, Br), (M-5820, F, CHs, F, 4-(Me)2N-P ; CHs), (M-5821, F, CH3, F, 4-OH-Ph, H), (M- 5822, F, CHs, F, 4-OH-Ph, CI), (M-5823, F, CHs, F， 4-OH-Ph, F); (M-5824, F, CH3, F, 4-OH-Ph, CFs), (M-5825, F, CHs, F, 4-OH-Ph, Br), (M-5826, F, CH3, F, 4-OH-Ph, CHs), (M-5827, F, CH3, F, 3,4-di-F-Ph, H), (M-5828, F, CHs, F, 3,4- di-F-Ph, Cl)" .(M-5829, F, CHs, F, 3, 4-di-F-Pli, F), (M-5830, F, CHs, F, 3,4-di- F-Ph, CF3), (M-5831, P, CH3， F, 3,4-di-F-Ph, Br), (M-5832, F, CH3, F, 3, 4-di- F-Ph, CHs), (M-5833, F, CH3, F, 4-COOH-Ph, H), (M-5834, F, CH3) F, 4-
COOH-P , CI), (M-5835, F, CH3, F, 4-COOH-Ph, F), (M-5836, F; CH3, F, 4- COOH-Ph, CFs), (M-5837, F, CHs, F, 4-COOH-Ph, Br), (M-5838, F， CHs, F, 4- COOH-Ph, CHs), (M-5839, F, CHs, F, Bn; H), (M-5840, F, CHs, F, Bn, CI), (M- 5841, F, CHs, F， Bn, F), (M-5842, F, CHs, F, Bn, CFs), (M- 5843, P, CHs, F, Bn, Br), (M-5844, F, CHs, F, Bn, CHs), (M-5845, F' CHs, F, 4-F-Bn, H), (M-5846, P, CHs, F, 4-F-Bn, CI), (M-5847, F, CH3, F， 4-F-Bn, F), (M-5848, F, C F, 4-F- Bn, CFs), (M-5849, F, CHs, F， 4-F-Bn, Br), (M-5850, F, CH3) F, 4-F-Bn, CHs), (M-5851, F, CHs, F， 2-Py, H), (M-5852, F, CHs, F, 2-Py, CI), (M- 5853, F, CH3, F, 2-Py, F), (M-5854, F, CHs, F, 2-Py, CFs), (M-5855, F, CHs, F, 2-Py, Br), (M-5856, F, CHs, F, 2-Py, CHs), (M- 5857, F, CHs, F, 3-Py, H), (M-5858, F, CH3; F, 3-Py, CI), (M-5859, F, CHs, F, 3-Py, F), (M-5860, F， CH3， F， 3-Py, CFs), (M-5861, F, CHs, F, 3-Py, Br), (M-5862, F， CH3> F, 3-Py, CHs), (M-5863, F, CH3, F, 4-Py, H), (M-5864, F, CHs, F, 4-Py, CI), (M-5865, F, CHs, F, 4-Py; F), (M- 5866, F; CHs, F, 4-Py, CFa), (M-5867, F, CHs, F, 4-Py, Br), (M-5868, P, CH3, F; 4-Py, CHs), (M- 5869, F, CHs, F, 2-Th, H), (M-5870, F, CHs, F, 2-Th, CI), (M-5871, F, CHs, F, 2-Th, F), (M-5872, F, CHs, F, 2-Tli, CFs), (M-5873, F, CH3, F, 2-Th, Br), (M-5874, F, CHs, F， 2-Th, CHs), (M- 5875, F， CH3, P, 3-Th, H), (M-5876, F, CHs, F， 3-Th, CI), (M-5877, F, CHs, F， 3-Th, F), (M-5878, F, CHs, F, 3-Th, CFs) (M-5879, F, CH3) F, 3-Th, Br), (M- 5880, F, CH3, F, 3-Th, CH3), (M-5881, F, CH3) F，
pyrazol-2-yl, H), (M-5882, F, CHs, F, pyrazol-2-yl, CI), (M-5883, F, CH3) F, pyrazol-2-yl, F), (M- 5884, F, CHs, F, pyrazol-2-yl, CFs), (M-5885, F, CHs, F， pyrazol-2-yl, Br), (M-5886, P, CHs, F, pyrazol-2-yl, CHs), (M- 5887, F, CHs, F， pyrazo 3.，yl, H), (M-5888, F, CH3, F, pyrazol-3-yl, CI), (M-5889, E, CH3, F, pyrazol-3-yl, F), (M- 5890, F, CHs, F, pyrazol- 3-yl, CFs), (M-5891, F, CH3, F, pyrazol-3-yl, Br), (M-5892, F, CHs, F, pyrazol-3-yl, CHs), (M-5893, F, CHs, F, pyrimidin-2-yl, H), (M-5894, F, C F, pyrimidin-2-yl, CI), (M-5895, F, CH3, F, pyrimidin-2-yl, F), (M-5896, F, CHs, F, pyrimidin-2-yl, CF3); (M-5897, F, CHs, F, pyrimidin-2-yl, Br), (M-5898, F, CHs, F, pyrimidin-2-yl, CH3), (M-5899, F, CHs, F, pyrimidin-4-yl; H), (M-5900, F, CH3, F, pyrimidin-4-yl, CI), (M-5901, F, CH3; F, pyrimidin-4-yl, F), (M-5902, F, CHa, F, pyrimidin-4-yl, CFs), (M-5903, F, CB.3, F, pyrimidin-4-yl, Br), (M-5904, F, CH3, F, pyrimidin-4-yl, CHs), (M- 5905, F， CHs, F, pyrimidin-5-yl, H)， (M-5906, F， CHs, F, pyrimidin-5-yl, CI), (M-5907, F, CHs, F， pyrimidin-5-yl, F)， (M-5908, F, CHa, F, pyrimidin-5-yl, CFs), (M-5909, F, CHs, F, pyrimidin-5-yl, Br), (M-5910, F, CHs, F, pyrimidin- 5-yl, CH3), (M-5911, F, CH3, F, HOOCCH2CH2CH2; H), (M-5912, F， CHs, F, HOOCCH2CH2CH2, CI), (M-5913, F, CHs, F, HOOCCH2CH2CH2, F), (M-5914, F, CH3, F, HOO CCH2CH2CH2, CFs), (M-5915, F, CHa, F， HOO CCH2CH2CH2, Br), (M-5916, F, CH3) F, ΗΟΟΟΟΗ2ΟΗ2ΟΗ2> CH3), (M-5917, F, CH3, F,
HOOCCH2CH2CH2CH2, H), (M-5918, F, CHs, F， HOOCCH2CH2CH2CH2, CI), (M-5919, F, CHs, F, HOOCCH2CH2CH2CH2, F), (M-5920, F, CH3, F,
HOO CCH2CH2CH2CH2, CF3), (M-5921, F， CHs, F, HOOCCH2CH2CH2CH2, Br), (M-5922, F, CH3, F, HOOCCH2CH2CH2CH2, CHs), (M-5923, F, CH3; F,
(Me)2NCOCH2CH2CH2CH2, H), (M-5924, F, CHa, F, (Me)2NCOCH2CH2CH2CH2, CI), (M-5925, F， CHs, F, (Me)2NCOCH2CH:2CH2CH2， F)， (M-5926, F, CHs, F， (Me)2NCOCH2CH2CH2CH2, CFs), (M-5927, F, CHa, F,
(Me)2NCO CH2CH2CH2CH2> Br), (M-5928, F, CHs, F,
(Me)2NCOCH2CH2CH2CH2, CHs), (M-5929, F, CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-5930, F, CH3, F;
(Me)2NCO CH2CH2CH2CH2CH2, CL), (M-5931, F, CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-5932, F, CH3; F,
(Me)2NCOCH2CH2CH2CH2CH2, CPs), (M-5933, F, CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-5934, F, CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-5935, F, CHs, F, MeOCH2, H), (M- 5936, F, CH3) F, MeOCH2, CI), (M-5937, F， CH3) F, MeOCH2> F), (M-5938, F, CHs, F, MeOCH2) CFs), (M-5939, F, CHs, F, MeOCH2, Br), (M-5940, F, CHs, F, MeOCHa, CH3), (M-5941, F, CHs, F, EtOCH2, H), (M-5942, F, CHs, F， EtOCHa, CI), (M-5943, F, CHs, F, EtOCH2， F)，（M-5944, F, CHs, F, EtOCH2, CPs), (M- 5945, F, CHs, F， EtOCH2; Br), (M-5946, F, CHs, F, EtOCH2, CHs), (M-5947, F, CHs, F, EtOCH2CH2; H)， (M-5948, F, CH3, F, EtOCHsCHs, CI), (M-5949, F, CHs, F, EtOCH2CH2, F), (M-5950, F, CHs, F, EtOCH2CH2) CFs), (M-5951, F, CHs, F, EtOCH2CH2, Br), (M-5952, F, CH3， F, EtOCH2CH2! CHs), (M-5953, F, CHs, F, MeOCH2CH2OCH2CH2) H), (M-5954, F, CHs, F, MeOCH2CH2OCH2CH2) CI), (M-5955, F， GH3, F, MeO CH2CH2O CH2CH2; F), (M-5956, F, CHs, F，
MeOCH2CH2OCH2CH2, CFs), (M-5957, F, CHs, F, MeOCH2CH20CH2CH2, Br), (M-5958, F, CH3, F, MeOCHsCB OCE CHs, CHs), (M-5959, F, CHs, F,
MeOCH2CH2， H), (M-5960, F' CH3, F, MeOCH2CH2, CI), (M-5961, F, CHs, F， MeOCHsCHs, F), (M-5962, F, CHs, F, MeOCH2CH2; CFs), (M-5963, F, CHs, F, MeOCH2CH2, Br), (M-5964, F, CH3, F, MeOCH2CH2, CHs), (M-5965, F, CH3, F, HOCH2, H), (M-5966, F, CH3, F, HOCH2, CI), (M-5967, F, CHs, F, HOCH2, F), (M-5'968, F, CH3) F, HOCH2， CFs), (M-5969, F; CHs, F, HOCH2, Br), (M-5970, F, CHs, F, HOCH2) CH3)， (M-5971, F, CH3, F' HOCH2CH2; H), (M-5972, F, CHs, F， HOCH2CH2> CI), (M-5973, F， CHs, F, HOCH2CH2) F)， (M-5974, F， CH3, F, HOCH2CH2, CF3), (M-5975, F, CH3, F， HOCH2CH2; Br), (M-5976, F, CHs, F, HOCH2CH2, CHs), (M-5977, F, CHs, F, HOCH2CH2CH2, H), (M-5978, F, CHs, F， HOCH2CH2CH2, CI), (M-5979, F, CHs, F, HOCH2CH2CH2, E), (M-5980, F, CHs, F, HOCH2CH2CH2, CFs), (M-5981, F, CHs, F, HOCH2CH2CH2) Br), (M-5982, F, CH3; F, HOCH2CH2CH2, CH3), (M-5983, F, CH3, F, HOCH2CH2CH2CH2, H), (M-5984, F, CH3, F, H〇CH2CH2CH2CH2, CI), (M-5985, F; CHs, F,
HOCH2CH2CH2CH2, F), (M-5986, F, CHs, F, HOCH2CH2CH2CH2, CFs), (M- 5987, F, CH3, F， HOCH2CH2CH2CH2) Br), (M-5988, F, CHs, F, HOCH2CH2CH2CH2) CHs), (M-5989, F， CH3, F; HOCH2CH2CH2CH2CH2, H), (M-5990, F, CH3) F, HOCII2CH2CH2CU2CU2, CI), (M-5991, F, CH3; F，
HOGH2CH2CH2CH2CH2, F), (M-5992, F, CH3, F, HOCH2CH2CH2CH2CH2， CFs), (M-5993, F, CHs, F, HOCH2CH2CH2CH2CH2, Br), (M-5994, F, CH3, F,
HOCH2CH2CH2CH2CH2, CH3), (M-5995, F, CH3, F, HOCH2CH2OCH2CH2, H), (M-5996, F, CHs, F, HOC CH2OCH2CH2, CI), (M-5997, F, CHs, F,
HOCH2CH2OCH2CH2， F), (M-5998, F, CHs, F, HOCH2CH2OCH2CH2' CFs), (M-5999, F, CH3) F, HOCH2CH2OCH2CH2， Br), (M-6000, F, CH3; F,
HOCH2CH2OCH2CH2, CH3), (M-6001, F， CHs, F, (Me)2N, H)， (M-6002, F, CH3， F' (Me)2N, CI), (M-6003, F, CHs, P, (Me)2N, F)， (M-6004, F, CHs, F， (Me)2N, CFs), (M-6005, F, CH3, F, (Me)aN, Br), (M-6006, F, CH3, P, (Me)2N, CHs), (M- 6007, F, CHs, F, piperidm-4-yl-methyl, H), (M-6008, F, CH8) F, piperidin-4- yl-methyl, CI), (M-6009, F, CHs, F, piperidm-4-yl-methyl; F), (M-6010, F, CHs, F, piperidin-4-yl-metliyl, CF3), (M-6011, F, CHs, F， piperidm-4-yl-methyl; Br), (M-6012, F， CH3) F, piperidin-4-yl-metliyl, CH3), (M-6013, F, CH3, F, cyclohexylmethyl, H), (M-6014, F, CH3, F, cyclohexylmethyl, CI), (M-6015, F, CH3, F, cyclohexylmethyl, F), (M-6016, F， CH3， F, cyclohexylmethyl, CFs), (M-6017, F, CHs, F, cyclohexylmethyl, Br), (M-6018, F, CHs, F,
cyclohexylmethyl, CHs), (M-6019, F, CH3, CI, H, H), (M-6020, F, CH3, CI, H, CI), (M-6021, F, CHs, CI, H, F), (M-6022, F, CHs, CI, H, CFs), (M-6023, F, CHs, CI, H, Br), (M-6024, F， CHs, CI, H, CHs), (M-6025, F， CH3; CI, F, H), (M-6026, F, CHs, CI, F, CI), (M-6027, F, CHs, CI, F, F), (M-6028, F, CH3; CI, F, CFs), (M-6029, F, CH3) CI, F, Br), (M-6030, F, CHs, CI, F, CHs), (M-6031, F， CHs, CI, CI, H), (M-6032, F， CHs, CI, CI, CI), (M-6033, F, CHs, CI, CI, F), (M-6034, F, CHs, CI, CI, CFs), (M-6035, F, CH3, CI, CI, Br), (M-6036, F, CH3) CI, CI, CHs), (M-6037, F, CH3) CI, CH3; H), (M-6038, F, CHs, CI, CHs, CI), (M-6039, F, CHs, CI, CHs, F), (M-6040, F, CHs, CI, CHs, CFs), (M-6041, F, CH3， CI, CH3> Br), (M-6042, F, CH3; CI, CH3> CHs), (M-6043, F, CH3) CI, Et, H), (M-6044, F, CH3, CI, Et, CI), (M- 6045, F, CH3， CI, Et, F), (M-6046, F， CHs, CI, Et, CF3), (M-6047, F, CH3, CI, Et, Br), (M-6048, F, CHs, CI, Et, CH3), (M-6049, F, CH3, CI, n-Pr, H), (M-6050, F, CHs, CI, n-Pr, CI), (M-6051, F， CH3j CI, n-Pr, F), (M-6052, F, CHs, CI, n-Pr, CFs), (M-6053, F, CHs, CI, n-Pr, Br), (M-6054, F, CH3， CI, n-Pr, CHs), (M-6055, F, CHs, CI, c-Pr, H), (M-6056, F, CH3; CI, c-Pr, CI), (M-6057, F， CH3, CI, c-Pr, F), (M-6058, F, CHs, CI, c-Pr, CFs), (M-6059, F, CH3, CI, c-Pr, Br), (M-6060, F, CHs, CI, c-Pr, CHs), (M-6061, F, CH3, CI, i-Pr, H), (M-6062, F, CHa, CI, i-Pr, CI),
(M-6063, F, CH3, CI, i-Pr, F), (M-6064, F, CH3; CI, i-Pr, CFs), (M-6065, F, CHs, CI, i-Pr, Br), (M-6066, F, CHs, CI, i-Pr, CH3)， (M-6067, F, CH3) CI, n-Bu, H), (M-6068, F, CHs, CI, n-Bu, CI), (M-6069, F, CHs, CI, n-Bu, F), (M-6070, F, CHs, CI, n-Bu, CFs), (M-6071, F, CHs, CI, n-Bu, Br), (M-6072, F, CH3) CI, n-Bu, CH3), (M-6073, F, CH3> CI, i-Bu, H), (M-6074, F， CH3, CI, i-Bu, CI), (M-6075, F, CHs, CI, i-Bu, F), (M-6076, F, CHa> CI, i-Bu, CF3)， (M-6077, F; CH3, CI, i-Bu, Br), (M-6078, F, CHs, CI, i-Bu, CH3), (M-6079, F, CHs, CI, sec-Bu, H), (M-6080, F， CHs, CI, sec-Bu, CI), (M-6081, F, CH3, CI, sec-Bu, F), (M-6082, F, CHs, CI, sec-Bu, CFs), (M-6083, P, CHs, CI, sec-Bu， Br), (M-6084, F, CHs, CI, sec-Bu, CH3), (M-6085, F, CHs, CI, n-Pen, H), (M-6086, F, CH3, CI, n-Pen, CI), (M-6087, F, CHa, CI, n-Pen, F); (M-6088, F, CHs, CI, n-Pen, CFs), (M-6089, F， CH3, CI, n-Pen, Br), (M-6090, F; CHs, CI, n-Pen, CHs), (M-609.1, F, CHs, CI, c-Pen, H), (M-6092, F, CH3, CI, c-Pen, CI), (M-6093, F; CHs, CI, c-Pen, F), (M-6094, F, CHs, CI, c-Pen, CF3), (M-6095, F, CHs, CI, c-Pen, Br), (M-6096, F, CH3; CI, c-Pen, CHs), (M-6097, F, CH3, CI, n-Hex, H), (M-6098, F, CHs, CI, n-Hex, CI), (M-6099, F, CH3) CI, n-Hex, F), (M-6100, F, CHs, CI, n-Hex, GF3), (M-6101, F, CH3j CI, n-Hex, Br), (M-6102, F， CHs, CI, n-Hex, CHs), (M-6103, F, CH3, CI, c-Hex, H), (M-6104, F, CH3; CI, c-Hex, CI), (M-6105, F, CHs, CI, c-Hex, F), (M-6106, F, CH3) CI, c-Hex, CFs), (M-6107, F, CH3, CI, c-Hex, Br), (M-6108, F, CHs, CI, c-Hex, CHs), (M-6109, F, CHs, CI, OH, H), (M-6110, F, CH3, CI, OH, CI), (M-6111, F, CHs, CI, OH, F), (M-6112, F, CH3, CI, OH, CFs), (M-6113, F, CHs, CI, OH, Br), (M-6114, F, CH3, CI, OH, CH3), (M-6115, F, CHs, CI, EtO, H), (M-6116, F, CHs, CI, EtO, CI), (M-6117, F, CH3; CI, EtO, F), (M-6118, F, CH3, CI, EtO, CFs), (M-6119, F, CH3, CI, EtO, Br), (M-6120, F, CHs, CI, EtO, CHs), (M-6121, F, CHs, CI, n-PrO, H), (M-6122, F， CHs, CI, n-PrO, CI), (M-6123, F, CH3, CI, n-PrO, F), (M-6124, F， CH3, CI, n-PrO, CFs), (M-6125, F, CHs, CI, n-PrO, Br), (M-6126, F, CHs, CI, n-PrO, CHs), (M-6127, F; CH3, CI, PhO, H), (M-6128, F, CHs, CI, PhO, CI), (M-6129, F, CH3; CI, PhO, F)， (M-6130, F， CHs, CI, PhO, CFs), (M-6131, F, CHs, CI,： PhO, Br), (M-6132, F, CH3, CI, PhO, CHs), (M-6133, F, CH3, CI, BnO, H), (M-6134, F, CH3, CI, BnO, CI), (M-6135, F, CH3, CI, BnO, F), (M-6136, F, CHs, CI, BnO, CFs), (M-6137, F, CHs, CI, BnO, Br), (M-6138, F, CHs, CI, BnO, CHs), (M-6139, F, CHs, CI, PhCH2CH20, H), (M-6140, F, CH3) CI, PhCH2CH20, CI), (M-6141, , CHs, CI, PhCH2CH20; F), (M-6142, F, CHs, CI, P CHsCHsO, CF3), (M-6143, P, CHs, CI, PhCH2CH20, Br), (M-6144, F, CHs, CI, PhCH2CH20, CHs), (M-6145, F, CHs, CI, CF30, H), (M-6146, F, CHs, CI, CFsO, CI), (M-6147, F, CH3) CI, CFsO, F), (M-6148, F, CH3) CI, CFsO, CPs), (M-6149, F, CHs, CI, CFsO, Br), (M-6150, F, CH3; CI, CFsO, CH3), (M-6151, F， CH3) CI, Ph, H), (M- 6152, F, CHs, CI, Ph,. CI), (M-6153, F, CH3) CI, Ph, P), (M-6154, F, CHs, CI, Ph,ノ CFs), (M-6155, F, CHs, CI, Ph, Br), (M-6156, F, CHs, CI, Ph, CHs), (M-6157, F, CHs, CI, 4-P-Pli, H), (M-6158, F， CHs, CI, 4-F-Ph, CI), (M-6159, F, CHs, CI, - F-Ph, F), (M-6160, F, CHs, CI, 4-F-Ph, CFs), (M-6161, F, CHs, CI, 4-F-Ph, Br), (M-6162, F, CH3; CI, 4-F-Ph, CHs), (M-6163, F, CHs, CI, 4-CF3-Ph; H)， (M-6164, F, CHs, CI, 4-CF3-Ph, CI), (M-6165, F, CHs, CI, 4-CFs-Ph, F), (M-6166, F, CHs, CI, 4-CFs-Ph, CFs), (M-6167, F, CHs, CI, 4-CFs-Ph, Br), (M-6168, F, CH3, CI, 4-CF3-Ph, CHs), (M-6169, F, CHs, CI, 4-(Me)2N-Ph) H), (M-6170, F， CH3) CI, 4-(Me)2N-Ph, CI), (M-6171, F, CHs, CI, 4-(Me)2N-Pli! F), (M-6172, F, CHs, CI, 4-(Me)2N-Ph, CFs), (M-6173, P; CH3> CI, 4-(Me)2N-Ph, Br), (M-6174, F, CH3， CI, 4-(Me)2N-Ph, CHs), (M-6175, F， CH3, CI, 4-0H-Ph; H); (M-6176, F, CHs, CI, 4- OH-Ph, CI), (M-6177, F， CHs, CI, 4-OH-P , F), (M-6178, F, CH3; CI, 4-OH-P , CFs), (M-6179, F， CHs' CI, 4-OH-Ph, Br), (M-6180, F, CHs, CI, 4-OH-Ph, CH3), (M-6181, F， CHs, CI, 3,4-di-F-Ph, H), (M-6182, F, CHs, CI, 3,4-di-F-Ph, CI), (M-6183, F, CHs, CI, 3,4-di-F-Ph, F), (M-6184, F, CH3, CI, 3,4-di-F-Ph, CFs), (M-6185, P, CH3) CI, 3,4-di-F-Ph, Br), (M-6186, F, CH3> CI, 3,4-di-F-Ph, CH3)， (M-6187, F, CHs, CI, 4-COOH-Ph, H), (M-6188, F, CH3) CI, 4-COOH-Ph, CI), (M-6189, F, CH3, CI, 4-COOH-Ph, F), (M-6190, F, CHs, CI, 4-COOH-Ph, CF3), (M-6191, F, CHs, CI, 4-COOH-Ph, Br), (M-6192, F, CHs, CI, 4-COOH-Ph, CHs), (M-6193, F, CH3; CI, Bn, H), (M-6194, F, CH3; CI, Bn, CI), (M-6195, F， CHs, CI, Bn, F)， (M-6196, F, CHs, CI, Bn, CFs), (M-6197, F, CHs, CI, Bn, Br), (M-6198, F, CHs, CI, Bn, CH3), (M-6199, F, CHs, CI, 4-F-Bn, Ή), (M-6200, F, CHs, CI, 4-F- Bn, CI), (M-6201, F, CHs, CI, 4-F-Bn, F), (M-6202, F, CHs, CI, 4-F-Bn, CFs), (M-6203, F， CHs, CI, 4-F-Bn, Br), (M-6204, F, CH3) CI, 4-F-Bn, CHs), (M-6205, F, CHs, CI, 2-Py, H), (M-6206, F, CH3, CI, 2-Py, CI), (M-6207, F, CHs, CI, 2-Py, F)，（M-6208, F, CHs, CI, 2-Py, CFs), (M-6209, F, CH3) CI, 2-Py, Br), (M-6210, F, CHs, CI, 2-Py, CHs), (M-6211, F, CHs, CI, 3-Py, H), (M-6212, F, CH3, CI, 3-Py, CI), (M-6213, F, CHs, CI, 3-Py, F), (M-6214, F, CH3， CI, 3-Py, CFs), (M-6215, F, CH3, CI, 3-Py, Br), (M-6216, F, CHs, CI, 3-Py, CH3), (M-6217, F, CHs, CI, 4-Py, H), (M-6218, F, CHs, CI, 4-Py, CI), (M-6219, F， CH3) CI, 4-Py, F), (M-6220, F, CHs, CI, 4-Py, CFs), (M-6221, F, CHs, CI, 4-Py, Br), (M-6222, F, CHs, CI, 4-Py, CHs), (M-6223, F, CHs, CI, 2-Th, H), (M-6224, F, CHs, CI, 2-Th, CI), (M-6225, F, CHs, CI, 2-Th, F), (M-6226, P, CHs, CI, 2-Th, CFs), (M-6227, F, CH3; CI, 2-Th, Br), (M-6228, F, CHs, CI, 2-Th, CHs), (M-6229, F, CH3, CI, 3-Th, H), (M-6230, F, CH3> CI, 3-Th, CI), (M-6231, F, CHs, CI, 3-Th, F), (M-6232, F, CHs, CI, 3-Th, CFs), (M-6233, F, CHs, CI, 3-Th, Br), (M-6234, F， CH3) CI, 3-Th, CHs), (M-6235, F, CHs, CI, pyrazol-2-yl, H), (M-6236, F, CHs, CI, pyrazol-2-yl, CI), (M-6237, F, CHs, CI, pyrazol-2-yl; F)，（M-6238, F, CHs, CI, pyrazol-2-yl, CF3)， (M-6239, F, CHs, CI, pyrazol-2-yl, Br), (M-6240, F, CHs, CI, pyrazol-2-yl; CHs), (M-6241, F, CHs, Cl; pyrazol-3-yl, H), (M-6242, F, CH3, CI, pyrazol-3-yl; CI), (M-6243, F, CH3, CI, pyrazol-3.yl, F), (M-6244, F, CHs, CI, pyrazol-3-yl, CF3), (M-6245, F, CHs, CI, pyrazol-3-yl, Br), (M-6246, F, CH3, CI, pyrazol-3-yl, CHs), (M-6247, F, CH3; CI, pyrimidin-2-yl, H), (M-6248, F, CHs, CI, pyrimidin-2-yl, CI), (M-6249, F, CHs, CI, pyrimidin-2-yl, F), (M-6250, F, CH3) CI, pyrimidin-2-yl, CFs), (M- 6251, F, CHs, CI, pyrimidin-2-yl, Br), (M-6252, P, CHs, CI, pyrimidin-2-yl, CHs), (M-6253, F, CHs, CI, pyrimidin-4-yl, H), (M-6254, F' CHs, CI, pyrimidin-4-yl, CI), (M-6255, F, CHs, CI, pyrimidin-4-yl, F), (M-6256, F, CHs, CI, pyrimidin- 4-yl, CFs), (M-6257, F, CHs, CI, pyrimidin-4-yl, Br), (M-6258, F, CHs, CI, pyrimidin-4-yl, CHs), (M-6259, F, CH3) CI, pyrimidin-5-yl, H), (M-6260, F, CH3) CI, pyrimidin-5-yl, CI), (M-6261, F， CH3; CI, pyrimidin-5-yl, F), (M-6262, F, CHs, CI, pyrimidin- 5 -yl, CFs), (M-6263, F, CHs, CI, pyrimidin-5-yl, Br), (M- 6264, F, CHs, CI, pyrimidin-5-yl, CHs), (M-6265, F, CH3， CI, ΗΟΟ00Η20Η20Η2; H), (M-6266, F, CHs, CI, HOOCCH2CH2CH2, CI), (M-6267, F, CHs, CI,
HOOCCH2CH2CH2) F), (M-6268, F, CH3, CI, HOOCCH2CH2CH2, CFs), (M-6269, F， CHs, CI, HOOCCH2CH2C Br), (M-6270, F, CHs, CI, HOOCCH2CH2CH2, CHs), (M-6271, F, GHs, CI, HOOCCHsCHsCB CHs, H), (M-6272, F, CH3, CI, HOOCCH2CH2CH2CH2; CI), (M-6273, F, CH3) CI, HOOCCH2CH2CH2CU2, F), (M-6274, F; CHs, CI, HOOCCH2CH2CH2CH2' CF3), (M-6275, F, CH3, CI, HOOCCH2CH2CH2CH2' Br), (M-6276, F, CH3) CI, HOOCCHsCHsCHsCHs, CHs), (M-6277, F, CHs, CI, (Me)2NCOCH2CH2CH2CH2, H), (M-6278, F, CHs, CI, (Me)2NCOCH2CH2CH2CH2, CI), (M-6279, F, CHs, CI,
(Me)2NCOCH2CH2CH2CH2, F), (M-6280, F, CH3, CI, (Me)2NCOCH2CH2CH2CH2, CFs), (M-6281, F, CH3, CI, (Me^NCOCHsCHsCHsCH ' Br), (M-6282, F, CHs, Cl， (Me)2NCOCH2CH2CH2CH2> CHs), (M-6283, F, CH3) CI,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-6284, F, CH3, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-6285, F, CH3， CI,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-6286, F, CHs, CI,
(Me)2NCOCH2CI-l2CH2CH2CH2， CFs), (M-6287, F, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2; Br), (M-6288, F, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2) CH3), (M-6289, F， CHs, CI, MeOCH2; H), (M- 6290, F, CH3) CI, MeOCH2; CI), (M-6291, F, CH3, CI, MeOCH2) F), (M-6292, F, CH3, CI, MeOCH2, CF3), (M-6293, F, CHs, CI, MeOCH2, Br), (M-6294, F， CH3, CI, MeOCH2, CH3), (M-6295, F， CHs, CI, EtOCH2) H), (M-6296, F, CHs, CI, EtOCH2) CI), (M-6297, F, CHs, CI, EtOCHs, F), (M-6298, F， CH3> CI, EtOCHa, CF3), (M-6299, F, CHs, CI, EtOCH2, Br), (M-6300, F, CHs' CI, EtOCH2; CHs), (M-6301, F, CHs, CI, EtOCH2CH2, H), (M-6302, F, CH3, CI, EtOCH2CH2, CI), (M-6303, F, CHs, CI, EtOCHsCHa, F), (M-6304, F, CHs, CI, EtOCH2CH2, CF3), (M-6305, F, CH3, CI, EtOCH2CH2, Br), (M-6306, F， CH3, CI, EtOCHaCHa, CH3), (M-6307, F, CHs, CI, MeOCH2CH2OCH2CH2> H), (M-6308, F, CHs, CI,
MeOCH2CH20CH2CH2, CI), (M-6309, F, CHs, CI, MeOCHsCHsOCHsCHs, F), (M-6310, F, CH3, CI, MeOCH2CH2OCH2CH2， CFs), (M-6311, F, CHs, CI,
MeOCH2CH2OCH2CH2, Br), (M-6312, F， CH3, CI, MeOCH2CH2OCH2CH2, CHs), (M-6313, F, CH3) CI, MeOCH2CH2j H), (M-6314, F, CH3) CI, MeOCH2CH2) CI), (M-6315, F, CHs, CI, MeOCH2CH2) F), (M-6316, F, CH3， CI, MeOCH2CH2) CFs), (M-6317, F, CHs, CI, MeOCH2CH2, Br), (M-6318, F, CHs, CI, MeOCH2CH2, CHs), (M-6319, F, CH3, CI, HOCH2, H), (M-6320, F, CH3， CI, HOCH2， CI), (M-6321, F, CH3) CI, HOCHa, F)， (M-6322, F, CHs, CI, HOCHs, CF3)， (M-6323, F, CHs, CI, HOCH2; Br), (M-6324, F, CH3, Cl; HOCH2, CHs), (M-6325, F' CH3) CI,
H0CH2CH2, H), (M-6326, F, CH3> CI, HOCH2CH2; CI), (M-6327, F, CH3, CI, HOCHaCHa, F), (M-6328, F, CH3; CI, HOCB CHs, CF3), (M-6329, F， CH3) CI, HOCHsCHa, Br), (M-6330, F, CHs, CI, HOCH2CH2, CHs), (M-6331, F, CH3) CI, HOCH2CH2CH2; H), (M-6332, F, CH3, CI, HOCH2CH2CH2, CI), (M-6333, F, CH3, CI, HOCH2CH2CH2) F), (M-6334, F， CH3, CI, HOCH2CH2CH2, CF3), (M-6335, F; CHs, CI, HOCH2CH2CH2, Br), (M-6336, F, CHs, CI, HOCH2CH2CH2; CH3)， (M- 6337, F, CHs, CI, HOCH2CH2CH2CH2; H), (M-6338, F， CHs, CI,
HOCH2CH2CH2CH2, CI), (M-6339, F, CH3' CI, HOCH2CH2CH2CH2, F), (M-6340, F， CHs, CI, HOCH2CH2CH2CH2, CF3), (M-6341, F, CH3， CI, HOCH2CH2CH2CH2) Br), (M-6342, F, CHs, CI, HOCH2CH2CH2CH2, CHs), (M-6343, F, CHs, CI,
HOCH2CH2CH2CH2CH2， H), (M-6344, F, CH3, CI, HOCH2CH2CH2CH2CH2, CI), (M-6345, F, CHs, CI, HOCH2CH2CH2CH2CH2, F), (M-6346, F, CH3, CI,
HOCH2CH2CH2CH2CH2, CFs), (M-6347, F, CHs, CI, HOCH2CH2CH2CH2CH2, Br), (M-6348, F, CHs, CI, HOCH2CH2CH2CH2CH2, CHs), (M-6349, F, CHs, CI, HOCH2CH2OCH2CH2, H)， (M-6350, F， CHs, CI, HOCHsCHaOCHaCHa, CI), (M- 6351, F, CH3, CI, HOCH^CH OCHhCHs, F), (M-6352, F, CHs, CI,
HOCH2CH2OCH2CH2, CFs), (M-6353, F, CH3) CI, ΗΟΟΗ2ΟΗ2ΟΟΉ2θΗ2> Br), (M-6354, F, CH3, CI, HOCHsCHsOCHbCHs, CH3), (M-6355, F, CH3) CI, (Me)2N, H)， (M-6356, F， CHs, CI, (Me)2N, CI), (M-6357, F, CHs, CI, (Me)2N, P), (M-6358, F, CH3, CI, (Me)2N, CF3), (M-6359, F, CHs, CI, (Me)2N, Br), (M-6360, F, CH3; CI, (Me)2N, CH3), (M-6361, F, CH3, CI, piperidin-4-yl-methyl, H), (M-6362, F, CHs, CI, piperidin-4-yl-metliyl, CI), (M-6363, F, CHs, CI, piperidin-4-yl-methyl, F), (M-6364, F, CHs, CI, piperidin-4-yl-methyl, CF3), (M-6365, F, CHs, CI, piperidin-4-yl-metliyl, Br), (M-6366, F, CHs, CI, piperidin-4-yl-metliyl, CH3), (M-6367, F, CH3, CI, cyclohexylmethyl, H), (M-6368, F, CHs, CI,
cyclohexylmethyl, CI), (M-6369, F, CHs, CI, cyclohexylmethyl, F), (M-6370, F, CHs, CI, cyclohexyhnethyl, CFs), (M-6371, P, CHs, CI, cyclohexylmethyl, Br), (M-6372, F, CH3) CI, cyclohexylmethyl, CH3), (M-6373, CI, H, H, H, H), (M- 6374, CI, H, H, H, CI), (M-6375, MeO, F, H, H， F), (M-6376, MeO, F, H, H, c-Pr), (M-6377, CI, H, H, H, Br), (M-6378, CI, H, H, H, CHs), (M-6379, MeO, H, H， F， c-Pr), (M-6380, CI, H, H， F, CI), (M-6381, MeO, H, H, F, F), (M-6382, CI, H, H, F, CFs), (M-6383, CI, H' H, F, Br), (M-6384, CI, H, H, F' CH3), (M-6385, CI, H， H, CI, H), (M-6386, MeO, F， H, H, Et)，（M-6387, MeO, H, H, CI, ), (M-6388, CI, H, H, CI, CFs), (M-6389, CI, H， H, CI, Br), (M-6390, CI, H, H, CI, CHs), (M-6391, CI, H, H, CHs, H), (M-6392, Cl， H, H, CH3, CI), (M-6393, CI, H, H, CH3, F), (M-6394, CI, H, H, CHs, CFs), (M-6395, CI, H, H, CHs, Br), (M-6396, CI, H, H, CHs, CH3), (M-6397, CI, H， H, Et, H)， (M-6398, CI, H, H, Et, CI), (M-6399, CI, H, H, Et, F), (M-6400, CI, H， H, Et, CF3), (M-6401, CI, H, H, Et, Br), (M-6402, CI, H, H, Et, CH3), (M-6403, CI, H, H, n-Pr, H), (M-6404, CI, H, H, n-Pr, CI), (M- 6405, CI, H, H, n-Pr, P), (M-6406, CI, H, H, n-Pr, CFs), (M-6407, CI, H, H, n- Pr, Br), (M-6408, CI, H, H, n-Pr, CHs), (M-6409, CI, H, H, c-Pr, H), (M-6410, CI, H, H， c-Pr, CI), (M-6411, CI, H, H, c-Pr, F)，（M-6412, CI, H, H, c-Pr, CF3)， (M- 6413, CI, H, H, c-Pr, Br), (M-6414, CI, H, H, c-Pr, CHa), (M-6415, CI, H, H, i- Pr, H), (M-6416, Cl， H, H， i-Pr, CI), (M-6417, CI, H, H, i-Pr, F), (M-6418, CI, H, H, i-Pr, CFs), (M-6419, CI, H, H, i-Pr, Br), (M-6420, CI, H, H, i-Pr, CHs), (M- 6421, MeO, H, H, n-Bu; H), (M-6422, CI, H, H, n-Bu, CI), (M-6423, CI, H, H, n-Bu, F)， (M-6424, CI, H, H, n-Bu, CFs), (M-6425, CI, H, H, n- u, Br), (M-6426, CI, H, H， n-Bu, CHs), (M-6427, CI, H, H, i-Bu, H), (M-6428, CI, H, H, i-Bu, CI), (M-6429, CI, H, H, i-Bu, F), (M-6430, CI, H, H, i-Bu, CF3), (M-6431, CI, H, H, i-Bu, Br), (M-6432, CI, H, H, i-Bu, CHs), (M-6433, CI, H, H, sec-Bu, H); (M-6434, CI, H, H, sec-Bu, CI), (M-6435, CI, H， H, sec-Bu, F), (M-6436, CI, H, H， sec-Bu, CFs), (M-6437, CI, H, H, sec-Bu, Br), (M-6438, CI, H, H, sec-Bu, CH3), (M-6439, CI, H, H' n-Pen, H), (M-6440, CI, H, H, n-Pen, CI), (M-6441, MeO, H, H, n-Pen, F), (M-6442, CI, H, H, n-Pen, CFs), (M-6443, CI, H, H, n-Pen, Br), (M-6444, CI, H, H, n-Pen, CHs), (M-6445, CI, H, H, c-Pen, H)， (M-6446, CI, H, H, c-Pen, CI), (M-6447, CI, H, H, c-Pen, F), (M-6448, CI, H, H, c-Pen, CFs), (M-6449, CI, H, H， c-Pen, Br), (M-6450, CI, H, H, c-Pen, CHs), (M-6451, CI, H, H, n-Hex, H)， (M- 6452, CI, H， H' n-Hex, CI), (M-6453, CI, H, H, n-Hex, F), (M-6454, CI, H, H, n-Hex, CFs), (M-6455, CI, H， H, n-Hex, Br), (M-6456, CI, H, H, n-Hex, CHs), (M-6457, CI, H, H, c-Hex, H), (M-6458, CI, H, H, c-Hex, CI), (M-6459, CI, H, H, c-Hex, F), (M-6460, CI, H, H, c-Hex, CF3), (M-6461, CI, H, H, c-Hex, Br), CM- 6462, CI, H, H, c-Hex, CHs), (M-6463, CI, H, H, OH, H), (M-6464, CI, H， H, OH, CI), (M-6465, CI, H, H， OH, F), (M-6466, CI, H， H, OH, CFs), (M-6467, CI, H, H， OH, Br), (M-6468, CI, H, H, OH, CHs), (M-6469, CI, H， H， EtO, H), (M-6470, CI, H, H, EtO, CI), (M-6471, CI, H, H, EtO, F), (M-6472, CI, H, H, EtO, CFs), (M- 6473, CI, H, H, EtO, Br), (M-6474, CI, H, H， EtO, CHs), (M-6475, CI, H, H, n- PrO, H), (M-6476, CI, H, H, n-PrO, CI), (M-6477, CI, H, H, n-PrO, F), (M-6478, CI, H, H, n-PrO, CF3), (M-6479, CI, H, H, n-PrO, Br), (M-6480, CI, H, H, n-PrO, CHa), (M-6481, Cl， H， H, PhO, H), (M-6482, CI, H, H, PhO, CI), (M-6483, CI, H, H, PhO, F), (M-6484, CI, H, H, PhO, CFs), (M-6485, CI, H, H, PhO, Br), (M-6486, CI, H, H, PhO, CHs), (M-6487, CI, H, H, BnO, H), (M-6488, CI, H, H, BnO, CI), (M-6489, CI, H, H, BnO, F), (M-6490, CI, H, H, BnO, CF3), (M-6491, CI, H, H, BnO, Br), (M-6492, CI, H, H, BnO, CHs), (M-6493, CI, H, H, PhCH2CH20, H), (M-6494, CI, H, H, PhCH2CH20, CI), (M-6495, CI, H, H， PhCH2CH20, F), (M- ' 6496, CI, H, H, PhCHaCHaO, CF3)， (M-6497, CI, H, H， PI1CH2CH2O, Br), (M- 6498, CI, H, H, PI1CH2CH2O, CH3)， (M-6499, MeO, H， H, CF3O, CFs), (M-6500, CI, H, H, CFaO, CI), (M-6501, CI, H, H, CFsO, F), (M-6502, CI, H， H, CF30, CF3), (M-6503, CI, H, H, CF3O, Br), (M-6504, CI, H, H, CFsO, CHs), (M-6505, MeO, H' H， Ph, H), (M-6506, CI, H， H， Ph, CI), (M-6507, CI, H， H, Ph, F), (M-6508, CI, H, H, Ph, CFs), (M-6509, CI, H, H, Ph, Br), (M-6510, CI, H, H, Ph, CH3), (M-6511, CI, H, H, 4-F-Ph, H), (M-6512, CI, H， H, 4-F-Ph, CI), (M-6513, CI, H, H, 4-F-Ph, P), (M-6514, CI, H, H， 4-F-Ph, CFs), (M-6515, CI, H, H, 4-F-Ph, Br), (M-6516, CI, H, H, 4-F-Ph, CHs), (M-6517, CI, H, H， 4-CFVPh, H), (M-6518, CI, H, H, 4-
CPVPh, CI), (M-6519, CI, H, H, 4-CF3-Pli， F), (M-6520, CI, H, H, 4-CPVPh, CF3), (M-6521, CI, H, H, 4-CF3-Ph, Br), (M-6522, CI, H, H, 4-CFs-Pli, CHs), (M-6523, CI, H, H, 4-(Me)2N-Ph, H), (M-6524, CI, H, H, 4-(Me)2N-Ph; CI), (M-6525, CI, H, H' 4-(Me)2N-Ph, F), (M-6526, CI, H, H, 4-(Me)2N-Ph; CFs), (M-6527, CI, H, H, 4-(Me)2N-Ph, Br), (M-6528, CI, H, H, 4-(Me)2N-Ph, CH3), (M-6529, CI, H' H, 4-OH-Ph, H), (M-6530, CI, H, H, 4-OH-Pli, CI), (M-6531, CI, H, H, 4-OH-Ph, F), (M-6532, CI, H, H, 4-OH-Ph, CF3), (M-6533, CI, H， H, 4-OH-Ph, Br), (M-6534, CI, H, H, 4-OH-Ph, CH3), (M-6535, CI, H, H, 3,4-di-F-Ph, H), (M-6536, CI, H， H 3,4-di-F-Ph, CI), (M-6537, CI, H, H, 3,4-di-F-Ph, F), (M-6538, CI, H, H, 3,4-di- F-Ph, CFs), (M-6539, CI, H, H， 3,4-di-F-Ph, Br), (M-6540, CI, H' H， 3,4-di-F-Ph, CHs), (M-6541, CI, H, H, 4-COOH-Ph, H), (M-6542, CI, H， H, 4-COOH-Ph, CI), (M-6543, CI, H， H, 4-COOH,Ph, F), (M-6544, CI, H, H, 4-COOH-Ph, CFa), (M- 6545, CI, H, H, 4-COOH-Ph, Br), (M-6546, CI, H, H, 4-COOH-Ph, CHs), (M-6547, CI, H, H， Bn, H), (M-6548, CI, H, H， Bn, CI), (M-6549, CI, H, H, Bn, F), (M-6550, CI, H, H, Bn, CFs), (M-6551, CI, H, H, Bn, Br), (M-6552, CI, H, H, Bn, CH3), (M-6553, CI, H, H, 4-P-Bn, H), (M-6554, CI, H, H, 4-F-Bn, CI), (M-6555, CI, H, H, 4-F-Bn, F), (M-6556, CI, H, H, 4-F-Bn, CPs), (M-6557, CI, H, H, 4-F-Bn, Br), (M-6558, CI, H, H, 4-F-Bn, CHs), (M-6559, CI, H, H, 2-Py, H), (M-6560, CI, H， H,
2- Py, CI), (M-6561, CI, H， H, 2-Py, F); (M-6562, CI, H, H, 2-Py, CF3), (M-6563, CI, H, H, 2-Py, Br), (M-6564, CI, H, H, 2-Py, CHa), (M-6565, CI, H, H, 3-Py, H),
5 (M-6566, CI, H, H， 3-Py, CI), (M-6567, CI, H， H' 3-Py, F), (M-6568, CI, H, H,
3- Py, CFs), (M-6569, CI, H, H， 3-Py, Br), (M-6570, CI, H, H, 3-Py, CHs), (M-6571, CI, H, H, 4-Py, H), (M-6572, CI, H, H, 4-Py, CI), (M-6573, CI, H, H, 4-Py, F), (M-6574, CI, H, H, 4-Py, CFs), (M-6575, CI, H, H, 4-Py, Br), (M-6576, CI, H, H,
4- Py, CHs), (M-6577, CI, H, H, 2-Th, H), (M-6578, CI, H, H, 2-Th, CI), (M-6579, CI, H, H, 2-Th, F), (M-6580, CI, H, H, 2-Th, CFs), (M-6581, CI, H, H, 2-Th, Br),
(M-6582, CI, H, H, 2-Th, CH3), (M-6583, CI, H, H, 3-Th, H), (M-6584, CI, H, H, 3-Th, CI), (M-6585, CI, H, H, 3-Th, F), (M-6586, CI, H, H, 3-Th, CF3), (M-6587, CI, H, H, 3-Th, Br), (M-6588, CI, H, H， 3-Th, CH3), (M-6589, CI, H, H, pyrazoレ 2-yl, H)， (M-6590, CI, H; H, pyrazol-2-yl, CI), (M-6591, CI, H, H, pyrazol-2-yl, F), (M-6592, CI, H, H, pyrazol-2-yl, CFs), (M-6593, CI, H, H, pyrazol-2-yl; Br), (M-6594, CI, H, H, pyrazol-2-yl, CHs), (M-6595, CI, H, H, pyrazol-3-yl, H), (M-6596, CI, H, H, pyrazol-3-yl, CI), (M-6597, CI, H, H, pyrazol-3-yl, F), (M-6598, CI, H, H， pyrazol-3-yl, CFs), (M-6599, CI, H, H, pyrazol-3-yl, Br), (M-6600, CI, H, H, pyrazoレ 3-yl' CH3), (M-6601, CI, H, H, pyrimidin-2-yl, H), (M-6602, CI, H, H, pyrimidm-2-yl; CI), (M-6603, CI, H, H, pyrimidin-2-yl, F), (M-6604, CI, H, H, pyrimidin-2-yl, CFs), (M-6605, CI, H, H, , . , pyrimidin-2-yl, Br), (M-6606, CI, H, H, pyrimidin-2-yl, CHs), (M-6607, CI, H, H, pyrimidin-4-yl, H), (M-6608, CI, H, H, pyrimidin-4-yl, CI), (M-6609, CI, H, H, pyrimidin-4-yl, F), (M-6610, CI, H' H, pyrimidin-4-yl, CFs), (M-6611, CI, H, H, pyrimidin-4-yl, Br), (M-6612, CI, H, H, pyrimidin-4-yl, CHs), (M-6613, CI, H, H, pyrimidin-5-yl, H), (M-6614, CI, H， H, pyrimidin-5-yl, CI), (M-6615, CI, H, H, pyrimidin-5-yl, F), (M-6616, CI, H, H, pyrimidm-5-yl, CFs), (M-6617, CI, H, H, pyrimidin-5-yl, Br), (M-6618, CI, H, H, pyrimidin-5-yl, CHs), (M-6619, CI, H, H， HOOCCH2CH2CH2) H), (M-6620, CI, H， H, HOOCCH2CH2CH2; CI), (M-6621, CI, H， H, HOOCCH2CH2CH2, F)， (M-6622, CI, H， H, HOOCCH2CH2CH2， CF3), (M- 6623, CI, H, H, HOOCCH2CH2CH2, Br), (M-6624, CI, H, H, HOOCCH2CH2CH2, CHs), (M-6625, CI, H, H, HOOCCH2CH2CH2CH2; H), (M-6626, CI, H, H, HOOCCH2CH2CH2CH2， CI), (M-6627, CI, H, H, HOOCCH2CH2CH2CH2, F)， (M-6628, CI, H, H, HOOCCHaCHaCHaCHs, CPs), (M-6629, CI, H, H,
HOOCCH2CH2CH2CH2, Br), (M-6630, CI, H, H， HOOCCHsCHsCHsCHs, CH3)， (M-6631, CI, H， H, (Me)2NCOCH2CH2CH2CH2, H), (M-6632, CI, H, H，
(Me)2NCOCH2CH2CH2CH2, CI), (M-6633, CI, H, H, (Me)2NCOCH2CH2CH2CH2， F)，（M-6634, CI, H, H，（Me)2NCOCH2CH2CH2CH2, CF3), (M-6635, CI, H, H, (Me)2NCOCH2CH2CH CH2, Br), (M-6636, CI, H, H, (Me)2NCOCH2CH2CH2CH2, CHs), (M-6637, CI, H， H, (Me)2NCOCH2CH2CH2CH2CH2， H), (M-6638, CI, H, H, (Me)2NCOCH2CH2CH2CH2CH2, CI), (M-6639, CI, H' H,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-6640, CI, H, H,
(Me)2NCOCH2GH2CH2CH2CH2, CFs), (M-6641, CI, H' H,
(Me)2NCOCH2GH2CH2CH2CH2, Br), (M-6642, CI, H, H,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-6643, CI, H, H, MeOCH2) H), (M-6644, CI, H, H, MeOCH2; CI), (M-6645, CI, H, H, MeOCHs, F), (M-6646, CI, H, H,
MeOCHa, CFs), (M-6647, CI, H, H, MeOCH2> Br), (M-6648, CI, H, H, MeOCHa, CHs), (M-6649, CI, H, H, EtOCH2， H), (M-6650, CI, H, H, EtOCH2) CI), (M-6651, CI, H, H, EtOCHa, F), (M-6652, CI, H, H, EtOCH2) CF3), (M-6653, CI, H, H, EtOCH , Br), (M-6654, CI, H, H, EtOCH2, CH3), (M-6655, CI, H, H, EtOCH2CH2, H), (M-6656, CI, H， H, EtOCH2CH2) CI), (M-6657, CI, H, H, EtOCH2CH2; F), (M-6658, CI, H, H， EtOCH2CH2, CFs), (M-6659, CI, H, H, EtOCH2CH2; Br), (M-6660, CI, H, H， EtOCH2CH2, CHs), (M-6661, CI, H, H，
MeOCH2CH2OCH2CH2, H), (M-6662, CI, H, H, MeOCHaCHsOCHaCHa, Gl), (M-6663, CI, H, H, MeOGH CHsOCH CHs, F), (M-6664, CI, H， H,
MeOCH2CH2OCH2CH2, CF3), (M-6665, CI, H, H, MeOCH2CH2OCH2CH2, Br), (M-6666, CI, H, H, MeOCH2CH2OCH2CH2, CHs), (M-6667, CI, H, H,
MeOCH2CH2; H), (M-6668, CI, H, H, MeOCH2CH2; CI), (M-6669, CI, H, H, MeOCH2CH2) F), (M-6670, CI, H, H, MeOCH2CH2) CFs), (M-6671, CI, H, H， MeOCHsCHa, Br), (M-6672, CI, H, H, MeOCH2CH2, CH3), (M-6673, CI, H, H, HOCH2; H), (M-6674, CI, H, H, HOCH2, CI), (M-6675, CI, H, H, HOCH2, F), (M-6676, CI, H, H， HOCH2, CFa), (M-6677, CI, H, H, H0CH2) Br), (M-6678, CI, H, H, HOCH2; CH3); (M-6679, CI, H, H, HOCH2CH2, H), (M-6680, CI, H, H, HOCH2CH2, Gl), (M-6681, CI, H, H, HOCH2CH2, F), (M-6682, CI, H, H, HOCH2CH2, CF3), (M-6683, CI, H, H, HOCH2CH2, Br), (M-6684, CI, H, H， HOCH2CH2> CHs), (M-6685, CI, H, H, HOCH2CH2CH2) H), (M-6686, CI, H, H, HOCH2CH2CH2, CI), (M-6687, CI, H， H, HOCH2CH2CH2; F), (M-6688, CI, H, H, HOCH2CH2CH2, CFs), (M-6689, CI, H, H, HOCHsCHsCHs, Br), (M-6690, CI, H， H, HOCH2CH2CH2) CHs), (M-6691, CI, H, H， HOCH2CH2CH2CH2， H)， (M-6692, CI, H, H, HOCH2CH2CH2CH2, CI), (M-6693, CI, H, H, HOCH2CH2CH2CH2, F)， (M-6694, CI, H, H, HOCH2CH2CH2CH2, CFa), (M-6695, CI, H, H,
HOCH2CH2CH2CH2, Br), (M-6696, CI, H, H， HOCH2CH2CH2CH2， CH3), (M- 6697, CI, H, H, HOCH2CH2CH2CH2CH2, H), (M-6698, CI, H, H,
HOCH2CH2CH2CH2CH2, CI), (M-6699, Cl， H, H, HOCH2CH2CH2CH2CH2, F), (M-6700, Cl'.H, H， HOCH2CH2CH2CH2CH2, CFs), (M-6701, CI, H, H,
HOCH2CH2CH2CH2CH2, Br), (M-6702, CI, H, H' HOCH2CH2CH2CH2CH2, CHs), (M-67Q3, CI, H, H, HOCH2CH2OCH2CH2, H), (M-6704, CI, H, H,
HOCH2CH2OCH2CH2, CI), (M-6705, CI, H, H, HOCH2CH2OCH2CH2, F), (M- t
〇
Figure imgf000204_0001
(),,,,,2CM222223 M〇cH0MC08C2 CjCHjvl 67 CI H H0CH0CHCH ,),,,,,,2 66 C22370I H HOCHC0C c0 HHCHH¾ 677 CI H H CI, H， F, c-Pr, CHs), (M-6769, CI, H, F, i-Pr, H), (M-6770, CI, H, F, i-Pr, CI), (M-6771, CI, H， F, i-Pr, F), (M-6772, CI, H, F' i-Pr, CFs), (M-6773, CI, H， F, i- Pr, Br), (M-6774, CI, H, F, i-Pr, CHs), (M-6775, MeO, H, F, n-Bu, H), (M-6776, CI, H， F, n-Bu, CI), (M-6777, CI, H， F， n-Bu, F), (M-6778, CI, H, F, n-Bu, CF3), (M-6779, CI, H, F， n-Bu, Br), (M-6780, CI, H, F, n-Bu, CHs), (M-6781, CI, H, F, i-Bu, H), (M-6782, CI, H, F, i-Bu, CI), (M-6783, CI, H, F, i-Bu, F), (M-6784, CI, H, F, i-Bu, CF3), (M-6785, CI, H, P, i-Bu, Br), (M-6786, CI, H, F, i-Bu, CH3)， (M-6787, CI, H, F, sec-Bu, H), (M-6788, CI, H， F, sec-Bu, CI), (M-6789, CI, H， F, sec-Bu, F), (M-6790, CI, H, F, sec-Bu, CFs), (M-6791, CI, H, F, sec-Bu, Br), (M-6792, CI, H, F, sec-Bu, CHs), (M-6793, MeO, H， F, n-Pen, H), (M-6794, CI, H, F， n-Pen, CI), (M-6795, MeO, H, F, n-Pen, F), (M-6796, CI, H, F, n-Pen, CFs), (M-6797, CI, H, F， n-Pen, Br), (M-6798, CI, H, F, n-Pen, CHs), (M-6799, CI, H, F， c-Pen, H), (M-6800, CI, H, F, c-Pen, CI), (M-6801, CI, H, F, c-Pen, F), (M-6802, CI, H, F, c-Pen, CFs), (M-6803, CI, H， F, c-Pen, Br), (M-6804, CI, H, F, c-Pen, CHs), (M-6805, MeO, H, F, n-Hex, H), (M-6806, CI, H， F, n-Hex, CI), (M-6807, CI, H， F, n-Hex, F), (M-6808, CI, H, F， n-Hex, CFs), (M-6809, CI, H， F, n-Hex, Br), (M-6810, CI, H' F, n-Hex, CHs), (M-6811, MeO, H, F, c-Hex, H), (M-6812, CI, H, F, c-Hex, CI), (M-6813, CI, H, F, c-Hex, F), (M-6814, CI, H, F, c-Hex, CF3), (M-6815, CI, H, F, c-Hex, Br), (M-6816, CI, H， F, c-Hex, CHs), (M-6817, CI, H, F， OH, H), (M-6818, CI, H, F, OH, CI), (M-6819, CI, H' F, OH, F), (M-6820, CI, H, F, OH, CFs), (M-6821, CI, H, F, OH, Br), (M-6822, CI, H, F, OH, CHs), (M-6823, MeO, H, F, EtO, H)， (M-6824, CI, H, F, EtO, CI), (M-6825, CI, H, F, EtO, F), (M-6826, C1"H, F, EtO, CFs), (M-6827, CI, H, F, EtO, Br), (M-6828, CI, H, F, EtO, CHs), (M-6829, CI, H, F, n-PrO, H), (M-6830, CI, H, F, n-PrO, CI), (M-6831, CI, H, F, n-PrO, F), (M-6832, CI, H, F, n-PrO, CFs), (M-6833, CI, H, F, n-PrO, Br), (M-6834, CI, H, F， n-PrO, CH3), (M-6835, CI, H， F, PhO, H)， (M-6836, CI, H, F, PhO, CI), (M-6837, CI, H, F, PhO, F), (M-6838, CI, H, F, PhO, CF3)， (M-6839, CI, H, F, PhO, Br), (M-6840, CI, H, F, PhO, CHs), (M-6841, CI, H, F, BnO, H), (M-6842, CI, H， F, BnO, CI), (M-6843, CI, H, F, BnO, F), (M-6844, CI, H, F， BnO, CFs), (M-6845, CI, H, F, BnO, Br), (M-6846, CI, H, F， BnO, CH3)， (M-6847, CI, H， F, PhCH2CH20， H), (M-6848, CI, H， F, PhCH2CH20, Cl)，（M-6849, CI, H, F, P CH2CH20, F), (M-6850, CI, H, F， PhCH2CH20, CF3), (M-6851, CI, H, F， PhCHaCHaO, Br), (M-6852, CI, H, F， P CHaCHaO, CHs), (M-6853, CI, H， F， CFsO, H), (M-6854, CI, H， F, CF30, CI), (M-6855, CI, H, F， CFsO, F)，（M-6856, CI, H, F， CFsO, CFs), (M-6857, CI, H, F, CFsO, Br), (M-6858, CI, H， F, CF30, CH3), (M-6859, MeO, H, F, Ph, H), (M-6860, CI, H, F, Ph, CI), (M-6861, MeO, H, F, Ph, F), (M-6862, CI, H， F, Ph, CFs), (M-6863, CI, H, F, Ph, Br), (M-6864, CI, H, F, Pli, CHs), (M-6865, MeO, H, F, 4-F-Ph, H), (M-6866, CI, H, F, 4-F-Ph, CI), (M-6867, CI, H, F, 4-F-Ph, F), (M-6868, CI, H, F, 4-F-Ph, CFs), (M-6869, CI, H， F, 4-F-Ph, Br), (M-6870, CI, H, F， 4-F-Ph, CH3), (M-6871, CI, H， F, 4-CF3-Ph, H), (M-6872, CI, H, F, 4-CF3-Ph, CI), (M-6873, CI, H, F， 4-CF3-P , F), (M-6874, CI, H, F, 4-CF3-PI1, CF3), (M-6875, CI, H, F, 4-CF3-Ph， Br), (M-6876, CI, H, F, 4- CFs-Ph, CHs), (M-6877, CI, H, F， 4-(Me)2N-Ph; H), (M-6878, CI, H， F, 4- (Me)2N-Ph， CI), (M-6879, CI, H， F, 4-(Me)2N-Ph, F), (M-6880, CI, H, F, 4- (Me)2N-Ph; CF3), (M-6881, CI, H, F, 4-(Me)2N-Pli) Br), (M-6882, CI, H, F, 4- (Me)2N-Ph, CH3)， (M-6883, CI, H, F， 4-OH-Ph, H), (M-6884, CI, H, F, 4-OH-3Ph, CI), (M-6885, CI, H, F, 4-OH-Ph, F), (M-6886, CI, H, F, 4-OH-Ph, CFs), (M-6887, CI, H, F, 4-OH-Ph, Br), (M-6888, CI, H, F, 4-OH-Ph, CH3), (M-6889, CI, H, F, 3, 4-di-F-Ph, H), (M-6890, CI, H, F, 3, 4-di-F-Ph, CI), (M-6891, CI, H， F, 3, 4-di- F-Ph, F), (M-6892, CI, H, F, 3, 4-di-F-Pli, CFs), (M-6893, CI, H, F, 3,4-di-F-Ph, Br), (M-6894, CI, H, F, 3, 4-di-F-Ph, CHs), (M-6895, CI, H, F, 4-COOH-Ph, H), (M-6896, CI, H, F, 4-COOH-Ph, CI), (M-6897, CI, H, F, 4-COOH-Ph, F), (M-6898, CI, H, F, 4-COOH-Ph, CF3), (M-6899, CI, H, F, 4-COOH-Ph, Br), (M-6900, CI, H, F, 4-COOH-Ph, CHs), (M-6901, MeO, H, F, Bn, H), (M-6902, CI, H, F, Bn, CI), (M-6903, CI, H, F, Bn, F)， (M-6904, CI, H, F; Bn, CFs), (M-6905, CI, H, F， Bn, Br), (M-6906, CI, H, F, Bn, CHs), (M-6907, CI, H, F, 4-F-Bn, H), (M-6908, CI, H, F， 4-F-Bn, CI), (M-6909, CI, H， F, 4-F-Bn, F), (M-6910, CI, H, F, 4-F-Bn, CFs), (M-6911, CI, H， F, 4-F-Bn, Br), (M-6912, CI, H, F, 4-F-Bn, CH3)， (M-6913, CI, H， F, 2-Py, H), (M-6914, CI, H, F, 2-Py, CI), (M-6915, CI, H, F, 2-Py, F), (M-6916, CI, H， F, 2-Py, CFs), (M-6917, CI, H, F, 2-Py, Br), (M-6918, CI, H, F, 2-Py, CHs), (M-6919, MeO, H, F' 3-Py, H), (M-6920, CI, H， F, 3-Py, CI), (M-6921, CI, H, F, 3-Py, F), (M-6922, CI, H, F, 3-Py, CFs), (M-6923, CI, H, F, 3-Py, Br), (M-6924, CI, H, F, 3-Py, CH3), (M-6925, CI, H, F, 4-Py, H)， (M-6926, CI, H, F, 4-Py, CI), (M-6927, CI, H, F, 4-Py, F), (M-6928, CI, H, F, 4-Py, CF3), (M-6929, CI, H, F， 4-Py, Br), (M-6930, CI, H, F, 4-Py, CHs), (M-6931, CI, H, F, 2-Th, H), (M-6932, CI, H, F, 2-Th, CI), (M-6933, CI, H, F, 2-Th, F), (M-6934, CI, H, F, 2-Th, CFs), (M-6935, CI, H, F, 2-Th, Br), (M-6936, CI, H, F, 2-Th, CHs), (M-6937, CI, H, F, 3-Th, H), (M-6938, CI, H, F， 3-Th, CI), (M-6939, CI, H, F， 3-Th, F), (M-6940, CI, H, F, 3-Th, CFs), (M-6941, CI, H, F, 3-Tli, Br), (M-6942, CI, H, F, 3-Th, CHs), (M-6943, CI, H, F, pyrazol-2-yl; H), (M-6944, CI, H, F, pyrazol-2-yl, CI), (M- 6945, CI, H, F, pyrazol-2-yl, F), (M-6946, CI, H, F, pyrazol-2-yl, CFs), (M-6947, CI, H, F, pyrazol-2-yl, Br), (M-6948, CI, H, F, pyrazol-2-yl, CHs), (M-6949, CI, H, F， pyrazol-3-yl, H), (M-6950, CI, H, F, pyrazol-3-yl, CI), (M-6951, CI, H， F, pyrazol-3-yl, F), (M-6952, CI, H, F, pyrazol-3-yl, CFs), (M-6953, CI, H, F, pyrazol-3-yl, Br), (M-6954, CI, H, F, pyrazol-3-yl, CH3), (M-6955, CI, H， F, pyrimidin-2-yl, H), (M-6956, CI, H, F， pyrimidin-2-yl, CI), (M-6957, CI, H, F, pyrimidin-2-yl, F), (M-6958, CI, H, F, pyrimidin-2-yl, CFs), (M-6959, CI, H, F, pyrimidm-2-yl, Br), (M-6960, CI, H, F, pyrimidin-2-yl, CH3), (M-6961, CI, H, F, pyrimidin-4-yl, H), (M-6962, CI, H, F, pyrimidin-4-yl, CI), (M-6963, CI, H' F, pyrimidin-4-yl, F), (M-6964, CI, H, F, pyrimidin-4-yl, CFs), (M-6965, CI, H, F' pyrimidin-4-yl, Br), (M-6966, CI, H， F, pyrimidin-4-yl, CH3), (M-6967, CI, H， F, pyrimidin-5-yl, H), (M-6968, CI, H, F, pyrimidin-5-yl; CI), (M-6969, CI, H, F, pyrimidin-5-yl, F), (M-6970, CI, H, F' pyrimidin-5-yl, CF3), (M-6971, CI, H, F, pyrimidin-5-yl, Br), (M-6972, CI, H, F, pyrimidm-5-yl, CH3), (M-6973, CI, H, F, HOOCCH2CH2CH2) H)， (M-6974, CI, H, F, HOOCCH2CH2CH2, CI), (M-6975, CI, H， F， HOOCCH2CH2CH2, F)，（M-6976, CI, H, F, HOOCCH2CH2CH2, CFs), (M- 6977, Cl， H, F， HOOCCH2CH2CH2, Br), (M-6978, CI, H, F， HOOCCH2CH2CH2; CH3)， (M-6979, CI, H, F, HOOCCH2CH2CH2CH2， H), (M-6980, CI, H, F，
HOOCCH2CH2CH2CH2, CI), (M-6981, CI, H, F, HO 0 C CHs CH2 CHs CH2, F), (M-6982, CI, H, F, HOOCCE CH CEbCHs, CFs), (M-6983, CI, H, F,
HOOCCH2CH2CH2CH2, Br), (M-6984, CI, H, F, HOOCCH2CH2CH2CH2, CH3)， (M-6985, CI, H, F, (Me)2NCOCH2CH2CH2C H), (M-6986, CI, H, F，
(Me)2NCOCH2CH2CH2CH2; CI), (M-6987, CI, H, F, (Me)2NCOCH2CH2CH2CH2' F), (M-6988, CI, H, F, (Me)2NCOCH2CH2CH2CH2， CF3), (M-6989, CI, H, F, (Me)2NCOCH2CH2CH2CH2, Br), (M-6990, CI, H, F, (Me)2NCOCH2CH2CH2CH2, CH3), (M-6991, CI, H, F, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-6992, CI, H, F, (Me)2NCOCH2CH2CH2CH2CH2, CI), (M-6993, CI, H, F，
(Me)2NCOCH2CH2CH2CH2CH2， F), (M-6994, CI, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-6995, CI, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-6996, CI, H, F， , .
(Me)2NCOCH2CH2CH2CH2CH2, CH3)， (M-6997, CI, H, F, MeOCH2, H), (M-6998, CI, H, F， MeOCHa, CI), (M-6999, CI, H, F, MeOCH2) F), (M-7000, CI, H, F, MeOCH2, CFs), (M-7001, CI, H， F, MeOCH2, Br), (M-7002, CI, H, F, MeOCH2) CH3), (M-7003, CI, H, F, EtOCH2, H), (M-7004, CI, H, F, EtOCHs, CI), (M-7005, CI, H, F, EtOCH2) F), (M-7006, CI, H, F, EtOCH2, CFs), (M-7007, CI, H, F, EtOCHa, Br), (M-7008, CI, H, F, EtOCHa, CHs), (M-7009, MeO, H, F,
EtOCH2CH2, H), (M-7010, CI, H, F, EtOCH2CH2; CI), (M-7011, CI, H, F, EtOCH2CH2) F)，（M-7012, CI, H, F， EtOCH2CH2; CFs), (M-7013, CI, H, F, EtOCH2CH2, Br), (M-7014, CI, H, F, EtOCH2CH2) CHs), (M-7015, CI, H, F, MeOCH2CH20CH2CH2; H), (M-7016, CI, H, F' MeOCH2CH2OCH2CH2; CI), (M-7017, Cl; H, F, MeOCH2CH20CH2CH2) F), (M-7018, CI, H, F，
MeOCH2CH20CH2CH2， CF3), (M-7019, CI, H, F, MeOCH2CH2OCH2CH2, Br), (M-7020, CI, H, F, MeOCH2CH2OCH2CH2; CHs), (M-7021, CI, H， F,
MeOCH2CH2> H), (M-7022, CI, H, F, MeOCH2CH2; CI), (M-7023, CI, H, F， MeOCH2CH2) F), (M-7024, CI, H, F, MeOCH2CH2) CFs), (M-7025, CI, H, F， MeOCH2CH2, Br), (M-7026, CI, H, F， MeOCH2CH2) CHs), (M-7027, CI, H, F, HOCHa, H), (M-7028, CI, H, F, HOCHs, CI), (M-7029, CI, H, F, HOCH2, F)， (M-7030, CI, H, F, HO CHs, CF3), (M-7031, CI, H, F, HOCH2, Br), (M-7032, CI, H, F, HOCHs, CHs), (M-7033, CI, H, F, HOCH2CH2) H), (M-7034, CI, H, F, HOCH2CH2, CI), (M-7035, CI, H, F, HOCH2CH2, F), (M-7036, CI, H, F,
HOCH2CH2, CF3), (M-7037, CI, H， F， HOCH2CH2, Br), (M-7038, CI, H, F, HOCH2CH2) CHs), (M-7039, CI, H, F, HOCHsCHsCB^ H), (M-7040, CI, H, F, HOCH2CH2CH2, CI), (M-7041, CI, H, F, HOCH2CH2CH2, F), (M-7042, CI, H, F, HOCH2CH2CH2, CF3), (M-7043, CI, H, F, HOCH2CH2CH2, Br), (M-7044, CI, H， F, HOCH2CH2CH2, CH3), (M-7045, CI, H, F, HOCH2CH2CH2CH2, H), (M-7046, CI, H, F, HOCH2CH2CH2CH2, CI), (M-7047, CI, H, F, HOCH2CH2CH2CH2， F)， (M-7048, CI, H， F, HOCH2CH2CH2CH2, CF3), (M-7049, CI, H, F;
HOCH2CH2CH2CH2, Br), (M-7050, CI, H, F, HOCH2CH2CH2CH2， CHs), (M- 7051, CI, H, F, HOCH2CH2CH2CH2CH2) H)， (M-7052, CI, H, F,
HOCH2CH2CH2CH2CH2, CI), (M-7053, CI, H, F, HOCH2CH2CH2CH2CH2, F), (M-7054, CI, H, F, HOCB GH2CH2CH2CH2, CF3), (M-7055, CI, H, F，
HOCH2CH2CH2CH2CH2, Br), (M-7056, CI, H, F, HOCH2CH2CH2CH2CH2, CHs), (M-7057, CI, H， F, HOCH2CH2OCH2CH2, H), (M-7058, CI, H, F,
HOCH2CH2OCH2CH2, CI), (M-7059, CI, H, F; HOCH2CH2OCH2CH2; F), (M- 7060, CI, H, F, HOCH2CH2OCH2CH2, CF3)， (M-7061, CI, H, F，
HOCH2CH2OCH2CH2, Br), (M-7062, CI, H, F, HOCH2CH2OCH2CH2) CH3), (M-7063, CI, H， F, (Me)2N, H)， (M-7064, CI, H, F; (Me)2N, Cl)，（M-7065, CI, H, F， (Me)2N, F), (M-7066, CI, H, F, (Me)2N, CFs), (M-7067, CI, H, F, (Me)aN, Br), (M-7068, CI, H, F, (Me)2N, CH3), (M-7069, CI, H， F, piperidin-4-yレ methyl' H), (M-7070, CI, H, F, piperidin-4-yレ methyl, CI), (M-7071, CI, H， F, piperidin-4- yl-methyl, F), (M-7072, CI, H， F, piperidm-4-yl-methyl, CFs), (M-7073, CI, H, F， piperidin-4-yl-methyl; Br), (M-7074, CI, H, F, piperidin-4-yl-methyl, CH3)， (M-7075, CI, H， F, cyclohexylmethyl, H), (M-7076, CI, H, F， cyclohexylmethyl, CI), (M-7077, CI, H, F, cyclohexylmethyl, F)， (M-7078, CI, H， F,
cyclohexylmethyl, CFs), (M-7079, CI, H, F, cyclohexylmethyl, Br), (M-7080, CI, H, F, cyclohexylmethyl, CHs), (M-7081, CI, H, CI, H, H), (M-7082, CI, H, CI, H, CI), (M-7083, CI, H, CI, H, F), (M-7084, CI, H， CI, H， CFs), (M-7085, CI, H, CI, H, Br), (M-7086, CI, H, CI, H, CHs), (M-7087, CI, H, CI, F, H), (M-7088, CI, H, CI, F, CI), (M-7089, CI, H， CI, F, F), (M-7090, CI, H, CI, F, CFs), (M-7091, CI, H, CI, F, Br), (M-7092, CI, H, CI, F, CHs), (M-7093, MeO, H, CI, CI, H), (M-7094, CI, H, CI, CI, CI), (M-7095, CI, H, CI, CI, F)， (M-7096, CI, H, CI, CI, CFs), (M-7097, CI, H, CI, CI, Br), (M-7098, CI, H, CI, CI, CH3)， （M-7099, CI, H, CI, CH3, H), (M- 7100, CI, H' .Cl, CHs, CI), (M-7101, CI, H, CI, CHs, F), (M-7102, CI, H, CI, CH3, CFs), (M-7103, CI, H, CI, CHs, Br), (M-7104, CI, H, CI, CH3) CHs), (M-7105, CI, H， CI, Et, H), (M-7106, CI, H, CI, Et, CI), (M-7107, CI, H, CI, Et, F), (M-7108, CI, H, CI, Et, CFs), (M-7109, CI, H, CI, Et, Br), (M-7110, CI, H, CI, Et, CHs), (M- 7111, CI, H, CI, n-Pr, H)， (M-7112, CI, H, CI, n-Pr, CI), (M-7113, CI, H, CI, n- Pr, F), (M-7114, CI, H, Cl， n-Pr, CFs), (M-7115, CI, H， Cl， n-Pr, Br), (M-7116, CI, H, CI, n-Pr, CHs), (M-7117, CI, H, CI, c-Pr, H), (M-7118, CI, H, CI, c-Pr, CI), (M-7119, CI, H, CI, c-Pr, F), (M-7120, CI, H, CI, c-Pr, CF3), (M-7121, CI, H, CI, c-Pr, Br), (M-7122, CI, H， CI, c-Pr, CHs), (M-7123, CI, H, CI, i-Pr, H), (M-7124, CI, H, CI, i-Pr, CI), (M-7125, CI, H, CI, i-Pr, F), (M-7126, CI, H, CI, i-Pr, CF3); (M-7127, CI, H， CI, i-Pr, Br), (M-7128, Cl， H, CI, i-Pr, CHs), (M-7129, CI, H, CI, n-Bu, H), (M-7130, CI, H, Cl， n-Bu, CI), (M-7131, CI, H, CI, n-Bu, F), (M-7132, CI, H, CI, n-Bu, CFs), (M-7133, CI, H, CI, n-Bu, Br), (M-7134, CI, H, CI, n-Bu, CHs), (M-7135, CI, H， CI, i-Bu, H)， (M-7136, CI, H, CI, i-Bu, CI), (M-7137, CI, H, CI, i-Bu, F)， (M-7138, CI, H, CI, i-Bu, CF3)， (M-7139, CI, H, CI, i-Bu, Br), (M- 7140, CI, H, CI, i-Bu, CHs), (M-7141, CI, H, CI, sec-Bu, H), (M-7142, CI, H, CI, sec-Bu, CI), (M-7143, CI, H, CI, sec-Bu, F), (M-7144, CI, H, CI, sec-Bu, CFs), (M-7145, CI, H, CI, sec-Bu, Br), (M-7146, CI, H, CI, sec-Bu, CH3), (M-7147, CI, H, CI, n-Pen, H), (M-7148, CI, H, CI, n-Pen, CI), (M-7149, CI, H, CI, n-Pen, F), (M-7150, CI, H, CI, n-Pen, CFs), (M-7151, CI, H, CI, n-Pen, Br), (M-7152, CI, H， CI, n-Pen, CHs), (M-7153, CI, H, CI, c-Pen, H), (M-7154, CI, H, CI, c-Pen, CI), (M-7155, CI, H, CI, c-Pen, F), (M-7156, CI, H, CI, c-Pen, CFa), (M-7157, CI, H, CI, c-Pen, Br), (M-7158, CI, H, CI, c-Pen, CH3), (M-7159, CI, H, CI, n-Hex, H)， (M-7160, CI, H, CI, n-Hex, CI), (M-7161, CI, H' CI, n-Hex, F), (M-7162, CI, H, CI, n-Hex, CFs), (M-7163, CI, H, CI, n-Hex, Br), (M-7164, CI, H, CI, n-Hex, CHs), (M-7165, CI, H, CI, c-Hex, H)， (M-7166, CI, H, CI, c-Hex, CI), (M-7167, CI, H, CI, c-Hex, F)' (M-7168, CI, H, CI, c-Hex, CF3), (M-7169, CI, H, CI, c-Hex, Br), (M- 7170, CI, H, CI, c-Hex, CHs), (M-7171, CI, H, CI, OH, H), (M-7172, CI, H, CI, OH, CI), (M-7173, CI, H, CI, OH, F), (M-7174, CI, H, CI, OH, CFs), (M-7175, CI, H, CI, OH, Br), (M-7176, CI, H， CI, OH, CHs), (M-7177, CI, H, CI, EtO, H), (M-7178, CI, H, CI, EtO, CI), (M-7179, CI, H, CI, EtO, F), (M-7180, CI, H' CI, EtO, CFs), (M-7181, CI, H, CI, EtO, Br), (M-7182, CI, H, CI, EtO, CHs), (M-7183, CI, H， CI, n-PrO, H), (M-7184, CI, H, CI, n-PrO, CI), (M-7185, CI, H, CI, n-PrO, F), (M- 7186, CI, H， CI, n-PrO, CFs), (M-7187, CI, H, CI, n-PrO, Br), (M-7188, CI, H, CI, n-PrO, CHs), (M-7189, CI, H, CI, PhO, H), (M-7190, CI, H, CI, PhO, CI), (M-7191, CI, H, CI, PhO, F), (M-7192, CI, H, CI, PhO, CFs), (M-7193, CI, H, CI, PhO, Br), (M-7194, CI, H， CI, PhO, CH3), (M-7195, CI, H, CI, BnO, H), (M-7196, CI, H, CI, BnO, CI), (M-7197, CI, H， CI, BnO, F)， (M-7198, CI, H, CI, BnO, CFs), (M-7199, CI, H, CI, BnO, Br), (M-7200, CI, H, CI, BnO, CHs), (M-7201, CI, H， CI,
PI1CH2CH2O, H), (M-7202, CI, H, CI, PhCH2CH20, CI), (M-7203, CI, H, CI, PliCHsCHsO, F); (M-7204, CI, H, CI, PhCH2CH20， CFs), (M-7205, CI, H, CI, PI1CH2CH2O, Br), (M-7206, CI, H, CI, PI1CH2CH2O, CHs), (M-7207, CI, H, CI, CF30， H), (M-7208, CI, H, CI, CFsO, CI), (M-7209, CI, H, CI, CFsO, F), (M-7210, CI, Η·， CI, CFsO, CF3), (M-7211, CI, H, CI, CFsO, Br), (M-7212, CI, H， CI, CFsO, CHs), (M-7213, CI, H, CI, Ph, H), (M-7214, CI, H, CI, Ph, CI), (M-7215, CI, H, CI, Ph, F), (M-7216, CI, H, CI, Ph, CFs), (M-7217, CI, H， CI, Ph, Br), (M-7218, CI, H, CI, Ph, CH3), (M-7219, CI, H, CI, 4-F-Ph, H), (M-7220, CI, H, CI, 4-F-Ph, CI), (M-7221, CI, H， CI, 4-F-Ph, F), (M-7222, CI, H, CI, 4-F-Ph, CF3), (M-7223, CI, H, CI, 4-F-Ph, Br), (M-7224, CI, H, CI, 4-F-Ph, CHs), (M-7225, CI, H, Gl, 4-CFs-Ph, H)， (M-7226, CI, H， CI, 4-CFs-Pli, CI), (M-7227, CI, H, CI, 4-CFs-Pli, F), (M-7228, CI, H, CI, 4-CF3-Ph, CFs), (M-7229, CI, H， CI, 4-CFs-Ph, Br), (M-7230, CI, H， CI, 4-CTVPh, CHs), (M-7231, CI, H, CI, 4-(Me)2N-Ph, H), (M-7232, CI, H, CI, 4- (Me)2N-P , CI), (M-.7233, CI, H, CI, 4-(Me)2N-Ph; F), (M-7234, CI, H, CI, 4- (Me)2N-Ph, CFs), (M-7235, CI, H, CI, 4-(Me)2N-Ph; Br), (M-7236, CI, H, CI, 4- (Me)2N-Ph, CHs), (M-7237, CI, H, CI, 4-OH-Ph, H), (M-7238, CI, H, CI, 4-OH- P , CI), (M-7239, CI, H, CI, 4-OH-Pli, F), (M-7240, CI, H, CI, 4-OH-Ph, CFs), (M-7241, CI, H, CI, 4-OH-Ph, Br), (M-7242, CI, H, CI, 4-OH-Ph, CHs), (M-7243, CI, H, CI, 3,4-di-F-Ph, H), (M-7244, CI, H, CI, 3,4-di-F-Ph, CI), (M-7245, CI, H, CI, 3,4-di-F-Pli, F), (M-7246, CI, H, CI, 3;4-di-F-P ; CFs), (M-7247, CI, H, CI, 3,4-di-F-Pli, Br), (M-7248, CI, H, CI, 3,4-di-F-Ph, CHs), (M-7249, CI, H, CI, 4- COOH-Ph, H), (M-7250, CI, H, CI, 4-COOH-Ph, CI), (M-7251, CI, H, CI, 4- COOH-Ph, F), (M-7252, CI, H， CI, 4-COOH-Ph, CF3), (M-7253, CI, H, CI, 4- COOH-Ph, Br), (M-7254, CI, H, CI, 4-COOH-Ph, CHs), (M-7255, CI, H, CI, Bn, H), (M-7256, CI, H,. CI, Bn, CI), (M-7257, CI, H, CI, Bn, F), (M-7258, CI, H， CI, Bn, CF3), (M-7259, CI, H, CI, Bn, Br), (M-7260, CI, H, CI, Bn, CHs), (M-7261, CI, H, CI, 4-F-Bn, H), (M-7262, CI, H， CI, 4-F-Bn, CI), (M-7263, CI, H, CI, 4-F-Bn, F), (M-7264, CI, H, CI, 4-F-Bn, CFs), (M-7265, CI, H, CI, 4-F-Bn, Br), (M-7266, CI, H, CI, 4-F-Bn, CHa), (M-7267, CI, H' CI, 2-Py, H), (M-7268, CI, H, CI, 2-Py, CI), (M-7269, CI, H, CI, 2-Py, F), (M-7270, CI, H， Cl， 2-Py, CFs), (M-7271, CI, H, CI, 2-Py, Br), (M-7272, CI, H, CI, 2-Py, CH3), (M-7273, CI, H, CI, 3-Py, H), (M-7274, CI, H, CI, 3-Py, CI), (M-7275, CI, H, CI, 3-Py, F), (M-7276, CI, H, CI, 3-Py, CFs), (M-7277, CI, H, CI, 3-Py, Br), (M-7278, CI, H, CI, 3-Py, CH3), (M- 7279, CI, H, CI, 4-Py, H), (M-7280, CI, H, CI, 4-Py, CI), (M-7281, CI, H; CI, 4- Py, F), (M-7282, CI, H, CI, 4-Py, CF3), (M-7283, CI, H, CI, 4-Py, Br), (M-7284, CI, H, CI, 4-Py, CHs), (M-7285, CI, H, CI, 2-Th, H), (M-7286, CI, H' CI, 2-Th, CI), (M-7287, CI, H, CI, 2-Th, F), (M-7288, CI, H, CI, 2-Th, CFs), (M-7289, CI, H, CI, 2-Th, Br), (M-7290, CI, H, CI, 2-Th, CH3), (M-7291, CI, H, CI, 3-Th, H)， (M-7292, CI, H, CI, 3-Th, CI), (M-7293, CI, H， Cl' 3-Th, F), (M-7294, CI, H, CI, 3-Th, .CFs), (M-7295, Cl, H, Cl, 3-Th, Br), (M-7296, Cl, H, Cl, 3-Th, CHs), (M-7297, Cl, H， Cl, pyrazol-2-yl, H), (M-7298, Cl, H, Cl, pyrazol-2-yl, Cl), (M-7299, Cl, H, Cl, pyrazoレ 2-yl, F), (M-7300, Cl, H, Cl, pyrazol-2-yl, CFs), (M-7301, Cl, H, Cl, pyrazol-2-yl, Br), (M-7302, Cl, H, Cl, pyrazol-2-yl, CHs), (M-7303, Cl, H, Cl, 〇
Figure imgf000214_0001
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Figure imgf000215_0001
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HOCH2CH2CH2) CFs), (M-7397, CI, H, CI, HOCH2CH2CH2, Br), (M-7398, CI, H, CI, HOCH2CH2CH2! CH3), (M-7399, CI, H, CI, HOCH2CH2CH2CH2, H), (M-7400, CI, H， CI, HOCH2CH2CH2CH2, CI), (M-7401, CI, H, CI, HOCH2CH2CH2CH2, F), (M-7402, Cl; H, CI, HOCH2GH2CH2CH2, CF3), (M-7403, CI, H, CI,
HOCH2CH2CH2CH2, Br), (M-7404, CI, H, CI, HOCH2CH2CH2CH2, CHs), (M- 7405, CI, H, CI, HOCH2CH2CH2CH2CH2, H), (M-7406, CI, H, CI,
HOCH2CH2CH2CH2CH2; CI), (M-7407, CI, H, CI, HOCH2CH2CH2CH2CH2) F), (M-7408, CI, H, CI, HOCH2CH2CH2CH2CH2, CFs), (M-7409, CI, H, CI,
HOCH2CH2CH2CH2CH2， Br), (M-7410, CI, H, CI, HOCH2CH2CH2CH2CH2, CHs), (M-7411, CI, H, CI, HOCH2CH2OCH2CH2, H), (M-7412, CI, H, CI,
HOCH2CH2OC CH2, CI), (M-7413, CI, H, CI, HOCH2CH2OCH2CH2; F), (M- 7414, CI, H, CI, HOCH2CH2OCH2CH2; CFs), (M-7415, CI, H, CI,
HOCH2CH2OCH2CH2, Br), (M-7416, CI, H, CI, HOCH2CH OCH2CH2, CHs), (M-7417, CI, H, CI, (Me)2N, H), (M-7418, CI, H, CI, (Me)2N, Cl)， (M-7419, CI, H, CI, (Me)2N, F), (M-7420, CI, H, CI, (Me)2N, CFs), (M-7421, CI, H， 1, (Me)2N, Br), (M-7422, CI, H, CI, (Me)2N, CHs), (M-7423, CI, H, CI, piperidin-4-yl- methyl, H), (M-7424, CI, H, CI, piperidin-4-yl-metliyl, CI), (M-7425, CI, H, CI, piperidin-4-yl-methyl, F), (M-7426, CI, H, CI, piperidin-4-yl-methyl, CFs), (M-7427, CI, H, CI, piperidin-4-yレ methyl, Br), (M-7428, CI, H, CI, piperidin- 4-yl-methyl, CHs), (M-7429, CI, H, CI, cyclohexylmethyl, H), (M-7430, CI, H, CI, cyclohexylmethyl, CI), (M-7431, CI, H, CI, cyclohexylmethyl, F)， (M-7432, CI, H, CI, cyclohexylmethyl, CF3), (M- 74.3.3, CI, H, CI, cyclohexylmethyl, Br), (M-7434, CI, H, CI, cyclohexylmethyl, CH3), (M-7435, CI, F, H, H, H), (M-7436, CI, F, H, H, CI), (M-7437, CI, F, H, H, F), (M-7438, CI, P, H, H, CFs), (M-7439, CI, F, H, H, Br), (M-7440, CI, F, H, H, CHs), (M-7441, CI, F， H' F, H), (M-7442, CI, F， H, F, CI), (M-7443, CI, F, H， F, F), (M-7444, CI, F, H, F, CFs), (M-7445, CI, P, H, F' Br), (M-7446, CI, F, H, F, CH3), (M-7447, CI, F, H, CI, H)， (M-7448, CI, F, H， CI, CI), (M-7449, CI, F, H, CI, F), (M-7450, CI, F, H, CI, CFs), (M-7451, CI, F, H, CI, Br), (M-7452, CI, F, H, CI, CHs), (M-7453, CI, F, H, CHs, H), (M-7454, CI, F， H， C CI), (M-7455, CI, F, H, CH3， F), (M-7456, CI, F, H, CH3, CFs), (M-7457, CI, F' H, CH3) Br), (M-7458, CI, F, H, CH3) CHs), (M-7459, CI, F, H, Et, H), (M-7460, CI, F， H, Et, CI), (M-7461, CI, F, H, Et, F)， (M-7462, CI, F, H, Et, CFs), (M-7463, CI, F, H, Et, Br), (M-7464, CI, F, H, Et, CHs), (M-7465, CI, F, H， n-Pr, H), (M- 7466, CI, F， H, n-Pr; CI), (M-7467, CI, F, H, n-Pr, F), (M-7468, CI, F, H， n-Pr, CFs), (M-7469, CI, F, H, n-Pr, Br), (M-7470, CI, F' H, n-Pr, CH3), (M-7471, CI, F, H, c-Pr, H), (M-7472, CI, F, H, c-Pr, CI), (M-7473, CI, F, H, c-Pr, F), (M-7474, CI, F, H, c-Pr, CFs), (M-7475, CI, F, H, c-Pr, Br), (M-7476, CI, F, H, c-Pr, CH3), (M-7477, CI, F， H, i-Pr, H), (M-7478, CI, F, H, i-Pr, CI), (M-7479, CI, F, H, i-Pr, F), (M-7480, CI, F， H, i-Pr, CFs), (M-7481, CI, F, H, i-Pr, Br), (M-7482, CI, F, H, i-Pr, CH3)， (M-7483, MeO, F, H, n-Bu, H), (M-7484, CI, F, H, n-Bu, CI), (M-7485, CI, F, H, n-Bu, F), (M-7486, CI, F, H, n-Bu, CFs), (M-7487, CI, F, H, n-Bu, Br), (M-7488, CI, F, H, n-Bu, CH3), (M-7489, CI, F, H, i-Bu, H), (M-7490, CI, F, H, i-Bu, CI), (M-7491, CI, F, H, i-Bu, F)， (M-7492, CI, F, H, i-Bu, CF3), (M-7493, CI, F, H, i-Bu, Br), (M-7494, CI, F, H, i-Bu, CHs), (M-7495, CI, F, H, sec-Bu, H), (M-7496, CI, F, H, sec-Bu, CI), (M-7497, CI, F, H, sec-Bu, F)， (M-7498, CI, F, H, sec-Bu, CFs), (M-7499, CI, F, H, sec-Bu, Br), (M-7500, CI, F, H, sec-Bu, CHs), (M-7501, CI, F, H, n-Pen, H), (M-7502, CI, F, H, n-Pen, CI), (M-7503, CI, F, H, n-Pen, F), (M-7504, CI, F, H, n-Pen, CF3), (M-7505, CI, F, H, n-Pen, Br), (M- 7506, CI, F, H, n-Pen, CHs), (M-7507, CI, F; H， c-Pen, H), (M-7508, CI, F, H, c-Pen, CI), (M-7509, CI, F, H, c-Pen, F), (M-7510, CI, F, H, c-Pen, CFs), (M-7511, CI, F, H, c-Pen, Br), (M-7512, CI, F, H, c-Pen, CHs), (M-7513, CI, F, H, n-Hex, H), (M-7514, CI, F, H, n-Hex, CI), (M-7515, CI, F, H, n-Hex, F)， (M-7516, CI, F, H, n-Hex, CF3), (M-7517, CI, F, H， n-Hex, Br), (M-7518, CI, P, H, n-Hex, CH3), (M-7519, CI, F, H, c-Hex, H)' (M-7520, CI, F, H, c-Hex, CI), (M-7521, CI, F, H, c-Hex, F)， (M-7522, CI, F, H, c-Hex, CFs), (M-7523, CI, F, H, c-Hex, Br), (M- 7524, Cl; F, H, c-Hex, CH3), (M-7525, CI, F， H, OH, H)， (M-7526, CI, F, H, OH, CI), (M-7527, CI, F, H， OH, F), (M-7528, CI, F， H， OH, CFs), (M-7529, CI, F， H, OH, Br), (M-7530, CI, F, H， OH, CH3)， (M-7531, CI, F， H, EtO, H), (M-7532, CI, F, H, EtO, CI), (M-7533, CI, F, H， EtO, F), (M-7534, CI, F, H, EtO, CPs), (M- 7535, CI, F, H， EtO, Br), (M-7536, CI, F, H， EtO, CHs), (M-7537, CI, F， H， n-PrO, H), (M-7538, CI, F, H, n-PrO, CI), (M-7539, CI, F, H, n-PrO, F), (M-7540, CI, F, H, n-PrO, CFa), (M-7541, CI, F, H， n-PrO, Br), (M-7542, CI, F, H, n-PrO, CH3), (M-7543, CI, F， H, PhO, H), (M-7544, CI, F, H, PhO, CI), (M-7545, CI, F, H, PhO, F), (M-7546, CI, F, H' PhO, CF3), (M-7547, CI, F, H, PhO, Br), (M-7548, CI, F, H， PhO, CHs), (M-7549, CI, F, H, BnO, H)， (M-7550, Cl， F, H, BnO, CI), (M-7551, CI, F, H, BnO, F), (M-7552, CI, F, H, BnO, CF3), (M-7553, CI, F, H, BnO, Br), (M- 7554, CI, F, H, BnO, CHs), (M-7555, CI, F, H， PhCHaCHaO, H), (M-7556, CI, F, H, PhCH2CH20; CI), (M-7557, CI, F， H, PhCHaCHaO, F), (M-7558, CI, F, H, PhCHaCHsO, CF3), (M-7559, CI, F, H, PhCH2CH20, Br), (M-7560, CI, F; H, PhCHsCHsO, CHs), (M-7561, CI, F, H' CFsO, H), (M-7562, CI, F, H, CFsO, CI), (M-7563, CI, F, H, CFsO, F), (M-7564, CI, F, H， CFsO, CF3)， (M-7565, CI, F, H, CFsO, Br), (M-7566, CI, F, H, CF30, CHs), (M-7567, CI, F, H, Ph, H), (M-7568, CI, F, H, Ph, CI), (M-7569, CI, F, H' Ph, F), (M-7570, CI, F, H, Ph, CF3), (M-7571, CI, F, H, Ph, Br), (M-7572, ,-Cl; F, H, Ph, CHs), (M-7573, CI, F， H, 4-F-Ph, H), (M-7574, C\, F, H, 4-F-Ph, CI), (M-7575, CI, F, H, 4-F-Ph, F), (M-7576, CI, F, H, 4-F-Ph, CFs), (M-7577, CI, F, H, 4-F-Ph, Br), (M-7578, CI, F, H, 4-F-Ph, CHs), (M-7579, CI, F, H, 4-CFs-Pli, H), (M-7580, CI, F, H, 4-CFs-Ph, CI), (M-7581, CI, F， H, 4-CF3-Ph, F), (M-7582, CI, F, H, 4-CF3-Ph, CF3), (M-7583, CI, F, H, 4- CFs-Pli, Br), (M-7584, CI, F; H, 4-CFs-Ph, CHs), (M-7585, CI, F, H, 4-(Me)2N- Ph, H), (M-7586, CI, F, H, 4-(Me)2N-Ph, CI), (M-7587, CI, F, H, 4-(Me)2N-Pli, F), (M-7588, CI, F, H, 4-(Me)2N-Ph; CFs), (M-7589, CI, F, H, 4-(Me)2N-Ph, Br), (M-7590, CI, F, H， 4-(Me)2N-Ph, CHs), (M-7591, CI, F, H， 4-OH-Ph, H), (M-7592, CI, F, H, 4-OH-Ph, CI), (M-7593, CI, F; H, 4-OH-Ph, F), (M-7594, CI, F, H, 4- OH-Ph, CFs), (M-7595, CI, F, H, 4-OH-Ph, Br), (M-7596, CI, F, H, 4-OH-Pli, CH3), (M-7597, CI, F, H, 3,4-di-P-Pli, H), (M-7598, CI, F， H， 3, 4-di-F-Pli, CI), (M-7599, CI, F, H, 3,4-di-F-Ph, P), (M-7600, CI, F, H, 3,4-di-F-Ph, CF3), (M- 7601， CI, F, H， 3, 4-di-F-Ph, Br), (M-7602, CI, F, H, 3,4-di-F-Ph, CHs), (M-7603, CI, F, H, 4-COOH-Ph, H), (M-7604, Cl， F, H， 4-COOH-Ph, CI), (M-7605, CI, F, H， 4-COOH-Ph, F), (M-7606, CI, F, H, 4-COOH-Ph, CFs), (M-7607, CI, F, H, 4- COOH-Ph, Br), (M-7608, CI, F, H, 4-COOH-Ph, CHs), (M-7609, CI, F, H, Bn, H)， (M-7610, CI, F， H， Bn, CI), (M-7611, CI, F， H, Bn, F), (M-7612, CI, P; H, Bn, CFs), (M-7613, CI, F, H, Bn, Br), (M-7614, CI, F, H, Bn, CH3), (M-7615, CI, F， H, 4- F-Bn, H)， (M-7616, CI, F, H, 4-F-Bn, CI), (M-7617, CI, F, H, 4-F-Bn, F)， (M-7618, CI, F， H, 4-F-Bn, CFs), (M-7619, CI, F, H， 4-F-Bn, Br), (M-7620, CI, F, H, 4-F- Bn, CHs), (M-7621, CI, F, H, 2-Py, H), (M-7622, CI, F, H, 2-Py, CI), (M-7623, CI, F, H， 2-Py, F), (M-7624, CI, F, H, 2-Py, CF3), (M-7625, CI, F， H， 2-Py, Br), (M-7626, CI, F' H, 2-Py, CHs), (M-7627, CI, F, H, 3-Py, H), (M-7628, CI, F, H， 3-Py, CI), (M-7629, CI, F, H, 3-Py, F), (M-7630, CI, F, H, 3-Py, CFs), (M-7631, CI, F, H, 3-Py, Br), (M-7632, CI, F, H, 3-Py, CH3), (M-7633, CI, F， H, 4-Py, H)' (M-7634, CI, F， H, 4-Py, CI), (M-7635, CI, F, H, 4-Py, F), (M-7636, CI, F, H, 4- Py, CFs), (M.7637, CI, , H, 4-Py, Br), (M-7638, CI, F, H, 4-Py, CHs), (M-7639, CI, F, H, 2-Th, H), (M-7640, CI, F, H, 2-Th, CI), (M-7641, CI, F, H, 2-Th, F), (M-7642, CI, F， H， 2-Th, CF3), (M-7643, CI, F, H， 2-Th, Br), (M-7644, CI, F, H, 2-Th, CHs), (M-7645, CI, F, H, 3-Th, H), (M-7646, CI, F, H, 3-Th, CI), (M-7647,
Figure imgf000220_0001
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ffiHON000HHQ〇¾ΗΗΗ:H Ή卜9
0 ΗΗ Hο H 10ΗΗί¾0 ΐfe 19696卜- - (Me)2NCOCH2CH2CH2CH2, CFs), (M-7697, CI, F, H, (Me)2NCOCH2CH2CH2CH2， Br), (M-7698, CI, F， H, (Me)2NCOCH2CH2CH2CH2, CH3), (M-7699, CI, F, H, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-7700, CI, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-7701, CI, F, H,
(Me)2NGOCH2CH2CH2CH2CH2, F), (M-7702, CI, F, H,
(Me)2NCOCH2CH2CH2CH2CH2; CFs), (M-7703, CI, F, H,
(Me)2NCOCH2CH2CH2CH2CH2， Br), (M-7704, CI, F， H, ' (Me)2NCOCH2CH2CH2CH2CH2， CH3), (M-7705, CI, F, H, MeOCHa, H), (M-7706, CI, F, H, MeOCH2; CI), (M-7707, CI, F, H, MeOCH2) F), (M-7708, CI, F, H, MeOCHa, CFs), (M-7709, CI, F, H, MeOCHa, Br), (M-7710, CI, F, H， MeOCH2, CHs), (M-7711, CI, F, H, EtOCH2) H), (M-7712, CI, F, H, EtOCHs, CI), (M-7713, CI, F, H, EtOCH2) F), (M-7714, CI, F, H, EtOCH2> CF3), (M-7715, CI, F, H, EtOCH2, Br), (M-7716, CI, F， H, EtOCH2) CH3), (M-7717, CI, F， H， EtOCH2CH2, H), (M-7718, CI, F, H, EtOCH2CH2, CI), (M-7719, CI, F, H, EtOCHsCHs, F), (M-7720, CI, F' H, EtOCH2CH2; CFs), (M-7721, CI, F, H, EtOCH2CH2, Br),
(M-7722, CI, F, H, EtOCH2CH2; CHs), (M-7723, CI, F, H, MeOCH2CH2OCH2CH2, H)， (M-7724, CI, F, H, MeOCH2CH2OCH2CH2, CI), (M-7725, CI, F, H,
MeOCH2CH2OCH2CH2, F)， (M-7726, CI, F, H, MeOCH2CH2OCK CH2, CF3), (M-7727, CI, F, H, MeOCH2CH2OCH2CH2, Br), (M-7728, CI, F, H,
MeOCH2CH2OCH2CH2> CH3), (M-7729, CI, F, H, MeOCH2CH2, H), (M-7730, CI, F, H, MeOCH2CH2; CI), (M-7731, CI, F, H, MeOCH2CH2) F), (M-7732, CI, F, H, MeOCH2CH2) CFs), (M-7733, CI, F， H, MeOCHaCHs, Br), (M-7734, CI, F, H; MeOCH2CH2; CHs), (M-7735, CI, F， H, HOCH2, H), (M-7736, CI, F, H, HOCH2, CI), (M-7737, CI, F, H， HOCH2, F), (M-7738, CI, F, H, HOCH2, CFs), (M-7739, CI, F, H, HOCH2, Br), (M-7740, CI, F, H, HOCH2， CHs), (M-7741, CI, F, H,
HOCH2CH2; H), (M-7742, CI, F, H, HOCH2CH2, CI), (M-7743, CI, F, H; HOCH2CH2, F), (M-7744, CI, F, H, HOCH2CH2, CFs), (M-7745, CI, F, H, HOCH2CH2) Br), (M-7746, CI, F, H, HOCH2CH2) CH3)， (M-7747, CI, F， H, HOCH2CH2CH2, H), (M-7748, CI, F, H, HOCH2CH2CH2; CI), (M-7749, CI, F, H, HOCH2CH2CH2, F), (M-7750, CI, F, H, HOCH2CH2CH2) CF3), (M-7751, CI, F, H, HOCH2CH2CH2) Br), (M-7752, CI, F, H, HOCH2CH2CH2, CHa), (M-7753, CI, F, H, HOCH2CH2CH2CH2, H), (M-7754, CI, F, H, HOCH2CH2CH2CH2) CI), (M- 7755, CI, F， H， HOCH2CH2CH2CH2, F), (M-7756, CI, F, H, HOCH2CH2CH2CH2, CFs), (M-7757, CI, F, H, HOCH2CH2CH2GH2, Br), (M-7758, Cl， F' H，
HOCH2CH2CH2CH2, CHa), (M-7759, CI, F， H， HOCH2CH2CH2CH2CH2， H), (M-7760, CI, F, H, HOCH2CH2CH2CH2CH2; CI), (M-7761, CI, F, H，
HOCH2CH2CH2CH2CH2, F), (M-7762, CI, F， H, HOCH2CH2CH2CH2CH2, CF3), (M-7763, CI, F, H, HOCHaCHsCHsCHaCHa, Br), (M-7764, CI, F, H,
HOCH2CH2CH2CH2CH2, CHs), (M-7765, CI, F， H, HOCH2CH2OCH2CH2, H)， (M-7766, CI, F, H， HOCH2CH2OCH2CH2, CI), (M-7767, CI, F, H，
HOCH2CH2OCH2CH2, F), (M-7768, CI, F, H, HOCH2CH2OCH2CH2, CFs), (M- 7769, CI, F, H, HOCH2CH2OCH2CH2, Br), (M-7770, CI, F, H，
HOCH2CH2OCH2CH2! CHs), (M-7771, CI, F, H, (Me)2N, H), (M-7772, CI, F， H, (Me)2N, CI), (M-7773, CI, F, H, (Me)2N, F), (M-7774, CI, F， H, (Me)2N, CFs), (M-7775, CI, F, H, (Me)2N, Br), (M-7776, CI, ; H' (Me)2N, CHs), (M-7777, CI, F, H, piperidin-4-yl-metliyl, H)， (M-7778, CI, F, H, piperidin-4-yl-methyl, CI), (M-7779, CI, F, H, piperidin-4-yl-met yl; F), (M-7780, CI, F, H, piperidin-4- yl-methyl, CFs), (M-7781, Cl' F, H, piperidin-4-yl-methyl, Br), (M-7782, ,C1; F, H, piperidm-4-yl-methyl, CHs), (M-7783, Cl, F, H, cyclohexylmethyl, H), (M- 7784, Cl, F, H, cyclohexylmethyl, Cl), (M-7785, Cl, F, H, cyclohexylmethyl, F), (M-7786, Cl, F, H, cyclohexylmethyl, CFs), (M-7787, Cl, F, H, cyclohexylmethyl, Br), (M-7788, Cl, F, H, cyclohexylmethyl, CHs), (M-7789, Cl, F, F, H, H), (M- 7790, CI, F' F, H, CI), (M-7791, CI, F, F, H, P), (M-7792, CI, F, F, H, CF3)，（M- 7793, CI, F, F, H, Br), (M-7794, CI, F, F， H， CH3), (M-7795, CI, F, F, F, H), (M-7796, CI, F, F, F, CI), (M-7797, CI, F, F， F, F), (M-7798, CI, F; F, F, CFs), (M-7799, CI, F, F, F, Br), (M-7800, CI, F, F， F， CHs), (M-7801, CI, F, F， CI, H), (M-7802, CI, F, F, CI, CI), (M-7803, CI, F, F, CI, F), (M-7804, CI, F, F, CI, CF3), (M-7805, CI, F, F, CI, Br), (M-7806, CI, F, F, CI, CHs), (M-7807, CI, F, P, CH3; H), (M-7808, CI, F, F， CHs, CI), (M-7809, CI, F, F, CHs, F)，（M-7810, CI, F, F， CH3, CFs), (M-7811, CI, F, F, CHa, Br), (M- 7812, CI, , F, CH3) CH3), (M-7813, CI, F, F, Et, H), (M-7814, CI, F, F, Et, CI), (M-7815, CI, F， F, Et, F), (M-7816, CI, F, F, Et, CF3)， (M-7817, CI, F, P, Et, Br), (M-7818, CI, F, F, Et, CHs), (M-7819, CI, , F, n-Pr, H), (M-7820, CI, F, F， n-Pr, CI), (M-7821, CI, F, F, n-Pr, F), (M-7822, CI, F, F, n-Pr, CFs), (M-7823, CI, F, F， n-Pr, Br), (M-7824, CI, F, F, n-Pr, CHs), (M-7825, CI, F, F, c-Pr, H), (M-7826, CI, F, F, c-Pr, CI), (M-7827, CI, F; F, c-Pr, F), (M-7828, CI, F, F, c-Pr, CFs), (M-7829, CI, F, F， c-Pr, Br), (M-7830, CI, F, F, c-Pr, CH3), (M-7831, CI, F, F, i-Pr, H), (M-7832, CI, F, F， i-Pr, CI),
(M-7833, CI, F, F, i-Pr, F), (M-7834, CI, F, F, i-Pr, CFs), (M-7835, CI, F， P, i-Pr, Br), (M-7836, CI, F, F, i-Pr, CHs), (M-7837, CI, F, F, n-Bu, H), (M-7838, CI, F, F, n-Bu, CI), (M-7839, CI, F, F, n-Bu, F), (M-7840, CI, F, F, n-Bu, CF3), (M-7841, CI, F, F, n-Bu, Br), (M-7842, CI, F, F, n-Bu, CHs), (M-7843, CI, F, F, i-Bu, H), (M-7844, CI, F, F, i-Bu, CI), (M-7845, CI, F, F, i-Bu, F), (M-7846, CI, F, F, i-Bu, CFs), (M-7847, CI, F, F, i-Bu, Br), (M-7848, CI, F, F' i-Bu, CH3), (M-7849, CI, F, F, sec-Bu, H), (M-7850, CI, F, F， sec-Bu, CI), (M-7851, CI, F， F, sec-Bu, F), (M-7852, Cl' .F, F, sec-Bu, CF3)， (M-7853, CI, F， F, sec-Bu, Br), (M-7854, CI, F, F, sec-Bu, CHs), (M-7855, CI, F, F, n-Pen, H)， (M-7856, CI, F, F, n-Pen, CI), (M-7857, CI, F, F, n-Pen, F), (M-7858, CI, F, F, n-Pen, CF3), (M-7859, CI, F, F, n-Pen, Br), (M-7860, CI, F, F, n-Pen, CHs), (M-7861, CI, F, F， c-Pen, H), (M- 7862, Cl, F, F, c-Pen, Cl), (M-7863, Cl, F, F, c-Pen, F), (M-7864, Cl, F, F, c-Pen, CFs), (M-7865, Cl, F, F, c-Pen, Br), (M-7866, Cl, F, F, c-Pen, CHs), (M-7867, Cl, F, F, n-Hex, H), (M-7868, Cl, F， F, n-Hex, Cl), (M-7869, Cl, F, F, n-Hex, F), (M-7870, Cl, F, F, n-Hex, CF3), (M-7871, Cl, F, F, n-Hex, Br), (M-7872, Cl, F, F, n-Hex, CH3); (M-7873, Cl, F, F, c-Hex, H), (M-7874, Cl, F， F, c-Hex, Cl), (M- 7875, Cl, F, F， c-Hex, F), (M-7876, Cl, F, F, c-Hex, CFs), (M-7877, Cl, F, F, c- Hex, Br), (M-7878, Cl, F; F, c-Hex, CHs), (M-7879, Cl, F, F, OH, H), (M-7880, Cl, F, F, OH, Cl), (M-7881, Cl, F, F, OH, F), (M-7882, Cl, F, F, OH, CF3), (M-7883, Cl, P, F, OH, Br), (M-7884, Cl, F, F, OH, CH3), (M-7885, Cl, F, F, EtO, H), (M-7886, Cl, F， F, EtO, Cl), (M-7887, Cl, F, P, EtO, F), (M-7888, Cl, F, F, EtO, CFs), (M-7889, Cl, F, F, EtO, Br), (M-7890, Cl, F, F, EtO, CH3), (M-7891, Cl, F, F, n-PrO, H)， (M-7892, Cl, F， F, n-PrO, Cl), (M-7893, Cl, F, F, n-PrO, F), (M- 7894, Cl, F, F, n-PrO, CFs), (M-7895, Cl, F, F, n-PrO, Br), (M-7896, Cl, F, F, n-PrO, CHs), (M-7897, Cl, F, F, PhO, H), (M-7898, Cl, F, F, PhO, Cl), (M-7899, Cl, F, F, PhO, F), (M-7900, Cl, F, F, PhO, CPs), (M-7901, Cl, F, F, PhO, Br), (M-7902, Cl, F, F, PhO, CHs), (M-7903, Cl, F, F, BnO, H), (M-7904, Cl, P, F, BnO, Cl), (M-7905, Cl, F, F, BnO, F), (M-7906, Cl, F, F, BnO, CF3)， (M-7907, Cl, F, F, BnO, Br), (M-7908, Cl, F, F, BnO, CHs), (M-7909, Cl, F, F, PI1CH2CH2O, H), (M-7910, Cl' P, F, PhCH2CH20, Cl), (M-7911, Cl, F, F, PhCHaCHaO, F), (M-7912, Cl, F, F， PhCH2CH20, CFs), (M-7913, Cl, F, F, P CHaC^O, Br),
(M-7914, Cl, F, F, PI1CH2CH2O, CH3), (M-7915, Cl, F, F, CF30, H), (M-7916, Cl, F， F, CFsO, Cl), (M-7917, Cl, F, F， CF30, F)' (M-7918, Cl, F, F;. CFsO, CFs), (M-7919, Cl, F, F, CF3O, Br), (M-7920, Cl, F, F， CFsO, CH3), (M-7921, Cl, F, F, Ph, H)， (M-7922, Cl, F， F, Ph, Cl), (M-7923, Cl, F, F, Ph, P), (M-7924, Cl, F, F, Ph, CFs), (M-7925, Cl, F, F, Ph, Br), (M-7926, Cl, , F, Ph, CH3)， (M-7927, Cl, F, F, 4-F-Ph, H), (M-7928, Cl, F, F， 4-F-Ph, Cl), (M-7929, Cl, F, F, 4-F-Ph, P), (M-7930, CI, F, F, 4-F-Ph, CF3)，（M-7931, CI, F, F, 4-F-Ph, Br), (M-7932, CI, F, F, 4-F-Pli, CHs), (M-7933, CI, F， F, 4-CFs-Ph, H), (M-7934, CI, F, F, 4-CF3-Ph, CI), (M-7935, CI, F， F, 4-CFs-Ph, F)， (M-7936, CI, F, F, 4-CFs-Ph, CF3)， (M-7937, CI, F, F， 4-CF3-Ph, Br), (M-7938, CI, F, F， 4-CF3-Ph, CH3), (M-7939, CI, F, F， 4-(Me)2N-Ph, H), (M-7940, CI, F, F, 4-(Me)2N-Ph, CI), (M-7941, CI, F, F, 4- (Me)2N-Ph; F)， (M-7942, CI, F, F, 4-(Me)2N-Ph, CF3), (M-7943, CI, F, F, 4- (Me)2N-Pli; Br), (M-7944, CI, F, F, 4-(Me)2N-Ph; CH3), (M-7945, CI, F， F， 4- OH-Ph, H), (M-7946, CI, F, F, 4-OH-Ph, CI), (M-7947, CI, F, F, 4-OH-Ph, F)， (M-7948, CI, F， F, 4-OH-Ph, CF3)， (M-7949, CI, F; F, 4-OH-Ph, Br), (M-7950, CI, F, F, 4-OH-Ph, CHs), (M-7951, CI, F, F， 3,4-di-F-Ph, H), (M-7952, CI, F, F， 3,4-di-F-Ph, CI), (M-7953, CI, F, F, 3,4-di-F-Ph, F), (M-7954, Cl， F， F, 3,4-di- F-Ph, CFs), (M-7955, CI, F; F, 3,4-di-F-Ph, Br), (M-7956, CI, F, F, 3,4-di-F-Ph, CHs), (M-7957, CI, F, F, 4-COOH-Ph, H), (M-7958, CI, F, F, 4-COOH-Ph, CI), (M-7959, CI, F, F, 4-COOH-Ph, F), (M-7960, CI, F, F, 4-COOH-Ph, CF3), (M- 7961, CI, F， F， 4-COOH-Ph, Br), (M-7962, CI, F, F, 4-COOH-Ph, CH3)， (M-7963, CI, F, F, Bn, H), (M-7964, CI, F, F, Bn, CI), (M-7965, CI, F, F, Bn, F), (M-7966, CI, F, F, Bn, CF3), (M-7967, CI, F, F, Bn, Br), (M-7968, CI, F, F, Bn, CHs), (M-7969, CI, F, F, 4-F-Bn, H), (M-7970, CI, F, F, 4-F-Bn, CI), (M-7971, CI, F, F, 4-F-Bn, F), (M-7972, CI, F; F, 4-F-Bn, CFs), (M-7973, CI, F, F, 4-F-Bn, Br), (M-7974, CI, F, F, 4-F-Bn, CHs), (M-7975, CI, F, F, 2-Py, H), (M-7976, CI, F, F, 2-Py, CI), (M-7977, CI, F, F, 2-Py, F), (M-7978, CI, F, F, 2-Py, CFs), (M-7979, CI, F, F, 2-Py, Br), (M-7980, CI, F, E, 2-Py, CHs), (M-7981, CI, F, F, 3-Py, H)， (M- 7982, CI, F, F, 3-Py, CI), (M-7983, CI, F, F, 3-Py, F), (M-7984, CI, F, F, 3-Py, CFs), (M-7985, CI, F, F, 3-Py, Br), (M-7986, CI, F, F, 3-Py, CH3)， (M-7987, CI, F, F， 4-Py, H), (M-7988, CI, F, F, 4-Py, CI), (M-7989, CI, F, F, 4-Py, F), (M-7990, CI, F, F, 4-Py, CFs), (M-7991, CI, F, F, 4-Py, Br), (M-7992, CI, F, F, 4-Py, CH3), (M-7993, CI, F, F, 2-Th, H), (M-7994, CI, F, F, 2-Th, CI), (M-7995, CI, F， F, 2- Th, F), (M-7996, CI, F, F, 2-Th, CFs), (M-7997, CI, F, F, 2-Th, Br), (M-7998, CI, F, F, 2-Th, CHa), (M-7999, CI, F, P, 3-Th, H)' (M-8000, CI, F, F; 3-Th, CI), (M- 8001， CI, F, F, 3-Th, F), (M-8002, CI, F, F, 3-Th, CF3), (M-8003, CI, F, F, 3-Th, Br), (M-8004, CI, F, F, 3-Th, CHs), (M-8005, CI, F, F, pyrazol-2-yl, H), (M-8006, CI, F, F, pyrazol-2-yl, CI), (M-8007, CI, F, F, pyrazol-2-yl, F), (M-8008, CI, F, F, pyrazoレ 2-yl, CF3), (M-8009, CI, F, F， pyrazol-2-yl, Br), (M-8010, CI, F, F, pyrazoレ 2-yl, CHs), (M-8011, CI, F， F, pyrazol-3-yl, H), (M-8012, CI, F, F, pyrazol-3-yl, CI), (M-8013, CI, F， F, pyrazoレ 3-yl, F), (M-8014, Cl' F, P, pyrazol-3-yl, CPs), (M-8015, Cl, F, F, pyrazol-3-yl, Br), (M-8016, Cl, ; F, pyrazol-3-yl, CHs), (M-8017, Cl, F, F, pyrimidin-2-yl, H), (M-8018, Cl, F, F, pyrimidin-2-yl, Cl), (M-8019, Cl, F, F, pyrimidin-2-yl, F), (M-8020, Cl, F, F, pyrimidin-2-yl, CFs), (M-8021, Cl, F, F, pyrimidin-2-yl, Br), (M-8022, Cl, F, F, pyrimidin-2-yl, CHs), (M-8023, Cl, F, F, pyrimidin-4-yl; H), (M-8024, Cl, F, F, pyrimidin-4-yl, Cl), (M-8025, Cl, F, F, pyrimidin-4-yl, F), (M-8026, Cl, F, F, pyrimidin-4-yl, CFs), (M-8027, Cl, F, F, pyrimidin-4-yl, Br), (M-8028, Cl, F, F, pyrimidin-4-yl, CH3), (M-8029, Cl, F, F, pyrimidin-5-yl, H), (M-8030, Cl, F, F, pyrimidin-5-yl, Cl), (M-8031, Cl, F, F, pyrimidin-5-yl, F), (M-8032, Cl, F, F, pyrimidin-5-yl, CFs), (M-8033, Cl, F, F, pyrimidin-5-yl, Br), (M-8034, Cl, F， F， pyrimidin-5-yl, CHs), (M-8035, Cl, F, F, HOOCCH2CH2CH2) H), (M-8036, Cl, F， F, HOOCCH2CH2CH2; Cl), (M-8037, Cl, F, F, HOOCCH2CH2CH2) F), (M-8038, Cl, F, P, HOO CCH2CH2CH2, CFs), (M-8039, Cl, F, F, HOOCCH2CH2CH2, Br), (M-8040, Cl, F, F, HOOCCH2CH2CH2, CH3), (M-8041, Cl, F, F,
HOOCCH2CH2CH2CH2, H), (M-8042, Cl, F, F， HOOCCH2CH2CH2CH2) Cl), (M-8043, Cl, F, F, HOOCCH2CH2CH2CH2, F), (M-8044, Cl, F, F,
HOOCCH2CH2CH2CH2, CFs), (M-8045, Cl, F, F, HOOCCH2CH2CH2CH2, Br), (M-8046, CI, F, F， HOOCCH2CH2CH2CH2, CHs), (M-8047, CI, F, F,
(Me)2NCOCH2CH2CH2CH2， H), (M-8048, CI, F, F, (Me)2NCOCH2CH2CH2CH2, CI), (M-8049, CI, F, F, (Me)2NCOGH2CH2CH2CH2, P); (M-8050, CI, F, F, (Me)2NCOCH2CH2CH2CH2, CFa), (M-8051, CI, F, F, (Me)2NCOCH2CH2CH2CH2, Br), (M-8052, CI, F, F, (Me)2NCOCH2CH2CH2CH2, CH3), (M-8053, CI, F, F, (Me)2NCOCH2CH2CH2CH2CH2, H), (M-8054, CI, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-8055, CI, F; F,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-8056, CI, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-8057, CI, F, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-8058, CI, F, F,
(Me)2NC0CH2CH2CH2CH2CH2j CH3), (M-8059, CI, F, F, MeOCH2, H), (M-8060, CI, F, F, MeOCH2, CI), (M-8061, Cl， F, F, MeOCH2, F), (M-8062, CI, F, F, MeOCH2, CFa), (M-8063, CI, F， F， MeOC¾ Br), (M-8064, CI, F， F, MeOCH2, CHs), (M-8065, CI, F, F， EtOCH2; H), (M-8066, CI, F, F, EtOCHs, CI), (M-8067, CI, F， F, EtOCHa, F), (M-8068, CI, F, F, EtOCHa, CPs), (M-8069, CI, F， F，
EtOCH2, Br), (M-8070, CI, F, F, EtOCH2, CH3), (M-8071, CI, F, F, EtOCH2CH2, H), (M-8072, CI, F, F， EtOCH2CH2) CI), (M-8073, CI, F, F, EtOCH2CIi2' F), (M-8074, CI, , F, EtOCHsCHs, CFs), (M-8075, CI, P, F, EtOCH2CH2, Br), (M- 8076, CI, F, F, EtOCH2CH2; CH3), (M-8077, CI, F, F, MeOCH2CH2OCH2CH2) H), (M-8078, CI, F, F， MeOCH2CH2OCH2CH2, CI), (M-8079, CI, F, F,
MeOCH2CH2OCH2CH2; F), (M-8080, CI, F, F, MeOCH2CH2OCH2CH2, CF3), (M-8081, CI, F, F, MeOCH2CH20CH2CH2) Br), (M-8082, CI, F, F,
MeOCH2CH2OCH2CH2, CHs), (M-8083, CI, F, F, MeOCH2CH2, H), (M-8084, CI, F, F, MeOCH2CH2, CI), (M-8085, CI, F, F, MeOCH2CH2) F), (M-8086, Cl; F, F, MeOCH2CH2) CFs), (M-8087, CI, P, F, MeOCH2CH2) Br), (M-8088, CI, F, F,
MeOCH2CH2, CHs), (M-8089, CI, F, F, HOCH2, H), (M-8090, CI, F, F, HOCH2, CI), (M-8091, CI, F, F， HOGH2, F), (M-8092, CI, F, F, HOCH2, CFs), (M-8093, CI, F, F, HO CH2, Br), (M-8094, Cl; F, F, HOCHa, CH3)， (M-8095, CI, F, F,
HOCH2CH2; H), (M-8096, CI, F, P, HOCH2CH2; CI), (M-8097, CI, F， F,
HOCH2CH2, F), (M-8098, CI, F, F, HOCH2CH2> CFs), (M-8099, CI, F, F, HOCH2CH2) Br), (M-8100, CI, F, F, HO CH2CH2) CH3)，（M-8101, CI, F, F，
HOCH2CH2CH2) H), (M-8102, CI, F, F, HOCH2CH2CH2, CI), (M-8103, CI, F， F, HO CH2CH2CH2， F), (M-8104, CI, F, F, HOCH2CH2CH2, CFs), (M-8105, CI, F, F, HOCH2CH2CH2; Br), (M-8106, CI, F, F, HOCH2CH2CH2, CH3)， (M-8107, CI, F, F， HOCH2CH2CH2CH2) H), (M-8108, CI, F, F, HOCH2CH2CH2CH2, CI), (M-8109, CI, F, F， HOCH2CH2CH2CH2, F), (M-8110, CI, F, F, HOCH2CH2CH2CH2, CF3), (M-8111, CI, F， F, HOCH2CH2CH2CH2, Br), (M-8112, CI, F, F,
HOCH2CH2CH2CH2, CHs), (M-8113, CI, F, F, HOCH2CH2CH2CH2CH2, H)' (M- 8114, CI, F, F, HOCH2CH2CH2CH2CH2, CI), (M-8115, CI, F, F,
HOCH2CH2CH2CH2CH2, F), (M-8116, CI, P, F， HO CH2CH2CH2CH2CH2, CFs), (M-8117, CI, F， F; HOCH2CH2CH2C CH2, Br), (M-8118, CI, F, F,
HO CH2CH2CH2CH2CH2; CHs), (M-8119, CI, F, F, HOCH2CH2OCH2CH2， H), (M-8120, CI, F， F， HOCH2CH2OCH2CH2, CI), (M-8121, CI, F, F，
HOCH2CH2OCH2CH2, F), (M-8122, CI, F, F， HOGH2CH2OCH2CH2, CP3), (M- 8123, CI, F; F, HOCH2CH20CH2CH2, Br), (M-8124, CI, F, F,
HOCH2CH2O CH2CH2, CHs), (M-8125, CI, F, F, (Me)2N, H)， (M-8126, CI, F, F, (Me)2N, CI), (M-8127, CI, F, F, (Me)2N; F)， (M-8128, CI, F, F, (Me)2N, CF3), (M-8129, CI, F, F, (Me)aN, Br), (M-8130, CI, F, E, (Me)2N, CH3), (M-8131, CI, F' F, piperidm-4-yl-met yl, H)， (M-8132, CI, F, F, piperidin-4-yl-methyl, CI), (M-8133, CI, F, F' piperidin-4-yl-methyl, F), (M-8134, CI, F, F, piperidin-4-yl- methyl, CFs), (M-8135, CI, F, F, piperidin-4-yl-methyl, Br), (M-8136, CI, P, F, piperidm-4-yl-met yl, CH3), (M-8137, CI, F, F, cyclohexylmethyl, H), (M-8138, CI, F, F, cyclohexylmethyl, CI), (M-8139, CI, F， F, cyclohexylmethyl, F)， (M- 8140, CI, F, F, cyclohexylmethyl, CFs), (M-8141, CI, F, F, cyclohexylmethyl, Br), (M-8142, CI, F, F, cyclohexylmethyl, CHs), (M-8143, CI, F, CI, H, H), (M-8144, Gl, F, CI, H, Gl), (M-8145, CI, F, CI, H， F), (M-8146, CI, F' CI, H, CFs), (M-8147, CI, F, CI, H, Br), (M-8148, CI, F, CI, H, CHs), (M-8149, CI, P, CI, F, H), (M-8150, CI, F, CI, F, CI), (M-8151, CI, F, CI, F, F), (M-8152, CI, F, CI, F， CFs), (M-8153, CI, F, CI, F, Br), (M-8154, CI, F' CI, F, CHs), (M-8155, CI, P, CI, CI, H), (M-8156, Cl， F, CI, CI, CI), (M-8157, CI, F, CI, CI, F), (M-8158, CI, F; CI, CI, CF3), (M-8159, CI, F, CI, CI, Br), (M-8160, CI, F' CI, CI, CHs), (M-8161, CI, F, CI, CH3, H), (M-8162, CI, F, CI, CHs, CI), (M-8163, CI, F, CI, CH3, F), (M-8164, CI, F, CI, CHs, CF3), (M-8165, CI, F, CI, CH3, Br), (M-8166, CI, F, CI, CH3, CH3), (M-8167, CI, F, CI, Et, H), (M-8168, CI, F, CI, Et, CI), (M-8169, CI, F, CI, Et, F), (M-8170, CI, F, CI, Et, CFs), (M-8171, CI, F, CI, Et, Br), (M-8172, CI, F, CI, Et, CHs), (M-8173, CI, F, CI, n-Pr, H)， (M-8174, CI, F, CI, n-Pr, CI), (M-8175, CI, F， CI, n-Pr, F), (M-8176, CI, F, CI, n-Pr, CFs), (M-8177, CI, F, CI, n-Pr, Br); (M-8178, CI, F, CI, n-Pr, CHs), (M-8179, CI, F, CI, c-Pr, H), (M-8180, CI, F, CI, c-Pr, CI), (M-8181, CI, F, CI, c-Pr, F)， (M-8182, CI, F, CI, c-Pr, CFs), (M-8183, CI, F, CI, c-Pr, Br), (M-8184, CI, F, CI, c-Pr, CH3), (M-8185, CI, F, CI, i-Pr, H), (M-8186, CI, F, CI, i-Pr, CI), (M-8187, CI, F, CI, i-Pr, F), (M-8188, CI, F， CI, i-Pr, CF3), (M-8189, CI, F, CI, i-Pr, Br), (M-8190, CI, F, CI, i-Pr, CHs), (M-8191, CI, F, CI, n-Bu, H), (M-8192, CI, F, CI, n-Bu, CI), (M-8193, CI, F, CI, n-Bu, F), (M-8194, CI, F, CI, n-Bu, CFs), (M-8195, CI, P, CI, n-Bu, Br), (M-8196, CI, F, CI, n-Bu, CHs), (M- 8197, CI, F, CI, i-Bu, H), (M-8198, CI, F, CI, i-Bu, CI), (M-8199, CI, F, CI, i-Bu, F), (M-8200, CI, F, Gl, i-Bu, CFs), (M-8201, CI, F, CI, i-Bu, Br), (M-8202, CI, F, CI, i-Bu, CHs), (M-8203, CI, F, CI, sec-Bu, H), (M-8204, CI, F, CI, sec-Bu, Cl)， (M-8205, CI, F, CI, sec-Bu, F), (M-8206, CI, F, CI, sec-Bu, CFs), (M-8207, CI, F, CI, sec-Bu, Br), (M-8208, CI, F, CI, sec-Bu, CHa), (M-8209, CI, F, CI, n-Pen, H), (M-8210, CI, F, CI, n-Pen, CI), (M-8211, CI, F, CI, n-Pen, F), (M-8212, CI, F, CI, n-Pen, CFs), (M-8213, CI, F, CI, n-Pen, Br), (M-8214, CI, F, CI, n-Pen, CHs), (M-8215, CI, F, CI, c-Pen, H), (M-8216, CI, F, CI, c-Pen, CI), (M-8217, CI, P, CI, c-Pen, F), (M-8218, CI, F， CI, c-Pen, CF3), (M-8219, CI, F, CI, c-Pen, Br), (M- 8220， CI, F, CI, c-Pen, CHs), (M-8221, CI, F, CI, n-Hex, H), (M-8222, CI, P, CI, n-Hex, CI), (M-8223, CI, F, CI, n-Hex, F), (M-8224, CI, F, CI, n-Hex, CFa), (M- 8225, Cl， F, CI, n-Hex, Br), (M-8226, CI, F, CI, n-Hex, CHs), (M-8227, CI, F, CI, c-Hex, H), (M-8228, CI, F, CI, c-Hex, CI), (M-8229, CI, F, CI, c-Hex, F), (M-8230, CI, F, CI, c-Hex, CFs), (M-8231, CI, F, CI, c-Hex, Br), (M-8232, CI, F, CI, c-Hex, CHs), (M-8233, CI, F, CI, OH, H)， (M-8234, Cl， F, CI, OH, CI), (M-8235, CI, F, CI, OH, F), (M-8236, CI, F, CI, OH, CF3), (M-8237, CI, F, CI, OH, Br), (M-8238, CI, F' CI, OH, CHs), (M-8239, CI, F, CI, EtO, H), (M-8240, CI, F, CI, EtO, CI), (M- 8241, CI, F, CI, EtO, F), (M-8242, CI, F, CI, EtO, CFs), (M-8243, CI, F, CI, EtO, Br), (M-8244, CI, F， CI, EtO, CH3), (M-8245, CI, F, CI, n-PrO, H), (M-8246, CI, F, CI, n-PrO, CI), (M-8247, CI, F, CI, n-PrO, F), (M-8248, CI, F, CI, n-PrO, CFs), (M-8249, CI, F, CI, n-PrO, Br), (M-8250, CI, F， CI, n-PrO, CHs), (M-8251, CI, F, CI, PhO, H), (M-8252, CI, F, CI, PhO, CI), (M-8253, CI, F, CI, PhO, F), (M-8254, CI, F, CI, PhO, CFs), (M-8255, CI, F, CI, PhO, Br), (M-8256, CI, F, CI, PhO, CH3), (M-8257, CI, F, CI, BnO, H), (M-8258, CI, F, CI, BnO, CI), (M-8259, CI, F, CI, BnO, F), (M-8260, CI, F, CI, BnO, CFs), (M-8261, CI, F, CI, BnO, Br), (M-8262, CI, F, CI, BnO, CHs), (M-8263, CI, F, Cl' PliCHsCHaO, H), (M-8264, CI, F, CI, PhCH2CH20, Cl), (M-8265, Cl; F, Cl, PhCH2CH20; F), (M-8266, Cl, F, Cl,
PI1CH2CH2O, CFs), (M-8267, Cl, F, Cl, PhCHsCHsO, Br), (M-8268, Cl, F, Cl, PhCH2CH20, CHs), (M-8269, Cl, F, Cl, CFaO, H), (M-8270, Cl, F, Cl, CFaO, Cl), (M-8271, Cl, F, Cl, CFsO, F), (M-8272, Cl, F, Cl, CFaO, CFs), (M-8273, Cl, F, Cl, CFsO, Br), (M-8274, CI, F， CI, CFsO, CHs), (M-8275, CI, F, CI, Ph, H)' (M-8276, CI, F, CI, Ph, CI), (M-8277, CI, F, CI, Ph, F), (M-8278, CI, F， CI, Fh, CFs), (M- 8279， CI, F, CI, Ph, Br), (M-8280, CI, F, CI, Ph, CHs), (M-8281, CI, F, CI, 4-F- Ph; H), (M-8282, CI, F, CI, 4-P-Ph, CI), (M-8283, CI, F, CI, 4-F-Pli, F), (M-8284, CI, F, CI, 4-F-Ph, CFs), (M-8285, CI, F， CI, 4-F-Ph, Br), (M-8286, CI, F, CI, 4- F-Ph, CHs), (M-8287, CI, F, CI, 4-CPVPh, H), (M-8288, CI, F, CI, 4-CFs-Pli, CI), (M-8289, CI, F, CI, 4-CPVPli, F), (M-8290, CI, F, CI, 4-CFs-Pli, CF3), (M-8291, CI, F, CI, 4-CFs-Pli, Br), (M-8292, CI, F, CI, 4-CF3-Pli, CHs), (M-8293, CI, F, CI, 4-(Me)2N-Ph, H), (M-8294, CI, F, CI, 4-(Me)2N-Ph, CI), (M-8295, CI, F, CI, 4- (Me)2N-Ph, F), (M-8296, CI, F， CI, 4-(Me)2N-Ph, CF3), (M-8297, CI, F, CI, 4- (Me)2N-Ph; Br), (M-8298, CI, F, CI, 4-(Me)2N-Ph, CHs), (M-8299, CI, F, CI, 4- OH-Ph, H), (M-8300, CI, F, CI, 4-OH-Ph, CI), (M-8301, CI, F， CI, 4-OH-Ph, F)， (M-8302, CI, F， CI, 4-OH-Ph, CFs), (M-8303, CI, F, CI, 4-OH-Ph, Br), (M-8304, CI, F， CI, 4-OH-Ph, CHs), (M-8305, CI, F, CI, 3,4-di-F-Ph, H)， (M-8306, CI, F, CI, 3,4-di-F-Ph, CI), (M-8307, CI, F, CI, 3,4-di-F-Ph, F)， (M-8308, CI, F， CI, 3,4- di-F-Ph, CF3), (M-8309, CI, F, CI, 3,4-di-F-Ph, Br), (M-8310, CI, F, CI, 3,4-di- F-Ph, CHs), (M-8311, CI, F, CI, 4-COOH-Ph, H), (M-8312, CI, F, CI, 4-COOH- Ph, CI), (M-8313, CI, F, CI, 4-COOH-Ph, F), (M-8314, CI, F, CI, 4-COOH-Ph, CFs), (M-8315, CI, F， CI, 4-COOH-Ph, Br); (M-8316, CI, P, CI, 4-COOH-Ph, CH3); (M-8317, CI, F, CI, Bn, H), (M-8318, CI, F, CI, Bn, CI), (M-8319, CI, F, CI, Bn, P), (M-8320, CI, F, CI, Bn, CF3), (M-8321, CI, F, CI, Bn, Br), (M-8322, CI, F, CI, Bn, CH3), (M-8323, CI, F, CI, 4-F-Bn, H), (M-8324, CI, F, CI, 4-F-Bn, CI), (M-8325, CI, F, CI, 4-F-Bn, F); (M-8326, CI, F, CI, 4-F-Bn, CFs), (M-8327, CI, P, CI, 4-F-Bn, Br), (M-8328, CI, F, CI, 4-F-Bn, CHs), (M-8329, CI, F, CI, 2-Py, H), (M-8330, CI, F, CI, 2-Py, CI), (M-8331, CI, F， CI, 2-Py, F)' (M-8332, CI, F, CI, 2-Py, CFs), (M-8333, CI, F， CI, 2-Py, Br), (M-8334, CI, F, CI, 2-Py, CHs), (M- 8335, CI, F, CI, 3-Py, H), (M-8336, CI, F, CI, 3-Py, CI), (M-8337, CI, F, CI, 3-Py, F), (M-8338, CI, F, CI, 3-Py, CF3), (M-8339, CI, F, CI, 3-Py, Br), (M-8340, CI, F, CI, 3-Py, CH3), (M-8341, CI, F, CI, 4-Py, H), (M-8342, CI, F, CI, 4-Py, CI), (M- 8343, CI, F, CI, 4-Py, F), (M-8344, CI, F, CI, 4-Py, CFs), (M-8345, CI, F, CI, 4- Py, Br), (M-8346, CI, F' CI, 4-Py, CHs), (M-8347, CI, F， CI, 2-Th, H), (M-8348, CI, F, CI, 2-Th, CI), (M-8349, CI, F, CI, 2-Th, P), (M-8350, CI, F, CI, 2-Th, CF3), (M-8351, CI, F, CI, 2-Th, Br), (M-8352, CI, F, CI, 2-Th, CH3), (M-8353, CI, F, CI, 3-Th, H), (M-8354, CI, F, CI, 3-Th, CI), (M-8355, CI, F, CI, 3-Th, F), (M-8356, CI, F, CI, 3-Th, CF3), (M-8357, CI, F, CI, 3-Th, Br), (M-8358, CI, F， CI, 3-Th, CH3)， (M-8359, CI, F, CI, pyrazol-2-yl, H), (M-8360, CI, F, CI, pyrazol-2-yl, CI), (M- 8361, CI, F, CI, pyrazol-2-yl, F), (M-8362, CI, F, CI, pyrazoレ 2-yl， CFs), (M-8363, CI, F' CI, pyrazol-2-yl, Br), (M-8364, CI, F, CI, pyrazoレ 2-yl' CHs), (M-8365, CI, F， CI, pyrazol-3-yl, H); (M-8366, CI, F, CI, pyrazol-3-yl, CI), (M-8367, CI, F, CI, pyrazol-3-yl, F), (M-8368, CI, F， CI, pyrazol-3-yl, CFa), (M-8369, CI, F, CI, pyrazol-3-yl, Br), (M-8370, CI, F, CI, pyrazol-3-yl, CHs), (M-8371, CI, F, CI, pyrimidin-2-yl, H), (M-8372, CI, F, CI, pyrimidin-2-yl, CI), (M-8373, CI, F, CI, pyrimidin-2-yl, F), (M-8374, CI, F, CI, pyrimidin-2-yl, CFs), (M-8375, CI, F， CI, pyrimidin-2-yl, Br), (M-8376, CI, F, CI, pyrimidin-2-yl, CH3), (M-8377, CI, F, CI, pyrimidin-4-yl, H), (M-8378, CI, F, CI, pyrimidin-4-yl, CI), (M-8379, CI, F' CI, pyrimidin-4-yl, F), (M-8380, CI, F, CI, pyrimidin-4-yl, CFs), (M-8381, CI, F， CI, pyrimidin-4-yl, Br), (M-8382, CI, F, CI, pyrimidin-4-yl, CH3), (M-8383, CI, F, CI, pyrimidm-5-yl, H); (M-8384, CI, P, CI, pyrimidin-5-yl, CI), (M-8385, CI, F, CI, pyrimidin-5-yl, F), (M-8386, CI, P, CI, pyrimidin-5-yl, CFs), (M-8387, CI, F, CI, pyrimidin-5-yl, Br), (M-8388, CI, P, CI, pyrimidin-5-yl, CHs), (M-8389, CI, F, CI, HOOCCH2CH2CH2) H), (M-8390, CI, F, CI, HOOCCH2CH2CH2) CI), (M-8391, CI, F, CI, HOOCCH2CH2CH2, F), (M-8392, CI, F, CI, HOOCCH2CH2CH2) CF3)， (M-8393, CI, F, CI, HOO CCH2CH2CH2, Br), (M-8394, CI, F， CI, HOOCCH2CH2CH2; CHs), (M-8395, CI, F， CI, HOOCCH2CH2CH2CH2， H), (M- 8396， CI, F， CI, HOO CCH2CH2CH2CH2, CI), (M-8397, CI, F, CI,
HOOCCH2CH2CH2CH2, F)， (M-8398, CI, F, Cl， HOO CCH2CH2CH2CH2， CFs), (M-8399, CI, F' CI, HOOCCH2CH2CH2CH2, Br), (M-8400, CI, F, CI,
HOO CCH2CH2CH2CH2, CH3)，（M-8401, CI, F, CI, (Me)2NCO CH2CH2CH2CH2, H), (M-8402, CI, F, CI, (Me NCOCH2CH2C CH2， CI), (M-8403, CI, F, CI, (Me)2NCOCH2CH2CH2CH2, F), (M-8404, CI, F, CI, (Me)2NCOCH2CH2CH2CH2, CFs), (M-8405, CI, F， CI, (Me)2NCOCH2CH2CH2CH2, Br), (M-8406, CI, F, CI, (Me)2NCOCH2CH2CH2CH2; CHs), (M-8407, CI, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-8408, CI, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-8409, CI, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-8410, CI, F, CI,
(Me)2NC0CH2CH2CH2CH2CH2; CFs), (M-8411, CI, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-8412, CI, F' CI,
(Me)2NCOCH2CH2CH2CH2CH2, CH3); (M-8413, CI, F, CI, MeOCH2) H); (M-8414, CI, F, CI, MeO CH2, CI), (M-8415, CI, F, CI, MeO CHa, F), (M-8416, CI, F, CI, MeOCH2, CFs), (M-8417, CI, F, CI, MeOCH2, Br), (M-8418, CI, F, CI, MeOCH , CHs), (M-8419, CI, F, CI, EtOCHb, H)， (M-8420, CI, F, CI, EtO CH2) CI), (M-8421, CI, F, CI, EtOCH2) F), (M-8422, CI, F， CI, EtOCH2) CF3), (M-8423, CI, F， CI, EtO C¾ Br), (M-8424, CI, F, CI, EtO CH2) CH3), (M-8425, CI, F, CI,
EtOCH2CH2, .H), (M-8426, CI, F, CI, EtOCH2CH2; CI), (M-8427, CI, F, .CI, EtOCH2CH2; F), (M-8428, CI, F, CI, EtOCH2CH2, CFs), (M-8429, CI, F, CI, EtO CH2C¾ Br), (M-8430, CI, F, CI, EtO CH2CH2; CH3), (M-8431, CI, F, CI, MeOCH2CH2OCH2CH2, H), (M-8432, CI, , CI, MeO CH2CH2O CH2CH2, CI), (M-8433, CI, , CI, MeO CHsCHsO CHaCHs, F), (M-8434, CI, F, CI, MeOCH2CH2OCH2CH2) CFs), (M-8435, Cl, F， Cl, MeOCH2CH2OCH2CH2， Br), (M-8436, Cl, F, Cl, MeOCH2CH2OCH2CH2, CH3); (M-8437, Cl, F, Cl,
MeOCH2CH2; H), (M-8438, Cl, F, Cl, MeOCH2CH2) Cl), (M-8439, Cl, F, Cl, MeOCH2CH2， F), (M-8440, Cl, F, Cl, MeOCH2CH2, CFs), (M-8441, Cl, F， Cl, MeOCH2CH2, Br), (M-8442, Cl, F, Cl, MeOCH2CH2; CHs), (M-8443, Cl, F, Cl, HOCH2, H), (M-8444, Cl, F, Cl, HOCH2, Cl), (M-8445, Cl, F, Cl, HOCH2, F), (M-8446, Cl, F, Cl, HOCH2) CFs), (M-8447, Cl, F, Cl, HOCH2' Br), (M-8448, Cl, F, Cl, HOCHa, CH3), (M-8449, Cl, F, Cl, HOCH2CH2) H), (M-8450, Cl, F, Cl, HOCH2CH2, Cl), (M-8451, Cl, F, Cl, HOCHaCHa, F), (M-8452, Cl, F, Cl, HOCH2CH2; CF3), (M-8453, Cl, F, Cl, HOCH2CH2) Br), (M-8454, Cl, F, Cl,
HOCH2CH2l CH3), (M-8455, Cl, F, Cl, ΗΟ0Η20Η20Η2) H), (M-8456, Cl, F, Cl, HOCH2CIi2CH2! Cl), (M-8457, Cl, F， Cl, HOCH2CH2CH2) F)， (M-8458, Cl, F, Cl, HOCHaCHaCHs, CFs), (M-8459, Cl, F, Cl, HOCH2CH2CH2, Br), (M-8460, Cl, F, Cl, HOCH2CH2CH2) CHs), (M-8461, Cl' F, Cl, HOCH2CH2CH2CH2) H), (M-8462, Cl, F, Cl, HOCH2CH2CH2CH2, Cl), (M-8463, Cl, F, Cl, HOCH2CH2CH2CH2) F), (M-8464, Cl, F, Cl, HOCHsCHsCHsCB , CF3), (M-8465, Cl, F, Cl,
HOCH2CH2CH2CH2, Br), (M-8466, Cl, F, Cl, HOCH2CH2CH2CH2, CHs), (M- 8467, Cl, F, Cl, HOCH2CH2CH2CH2CH2, H), (M-8468, Cl, F, Cl,
HOCH2CH2CH2CH2CH2, Cl), (M-8469, Cl, F, Cl, ΗΟΟΗ2ΟΗ2θΗ2ΟΗ2θΗ2) F), (M-8470, Cl, F, Cl, HOCH2CH2CH2CH2CH2, CF3), (M-8471, Cl, F, Cl,
HOCH2CH2CH2CH2CH2, Br), (M-8472, Cl, F, Cl, HOCH2CH2CH2CH2CH2, CH3), (M-8473, Cl, F, Cl, HOCH2CH2OCH2GH2, H), (M-8474, Cl, F, Cl,
HOCH2CH2OCH2CH2) Cl), (M-8475, Cl, F, Cl, HOCH2CH2OCH2CH2; F); (M- 8476, Cl, F, Cl, HOCH2CH2OCH2CH2, CFa), (M-8477, Cl, F, Cl,
HOCH2CH2OCH2CH2, Br), (M-8478, Cl, F' Cl, HOCH2CH2OCH2CH2, CH3),
(M-8479, Cl, F, Cl, (Me)2N, H)， (M-8480, Cl, F, Cl, (Me)2N, Cl), (M-8481, Cl, F, CI, (Me N, F), (M-8482, CI, F' CI, (Me)2N, CF3), (M-8483, CI, , CI, (Me)2N, Br), (M-8484, CI, F, CI, (Me)2N; CHs), (M-8485, CI, F, CI, piperidin-4-yl-methyl, H), (M-8486, CI, F, CI, piperidin-4-yレ： methyl' CI), (M-8487, CI, F, CI, piperidin-4- yl-metliyl, F), (M-8488, CI, F, CI, piperidin-4-yレ methyl, CFs), (M-8489, CI, P, CI, piperidm-4-yl-met yl; Br), (M-8490, CI, F, CI, piperidm-4-yl-methyl, CH3), (M-8491, CI, F, CI, cyclohexylmethyl, H), (M-8492, CI, F, CI, cyclohexylmethyl, CI), (M-8493, CI, F, CI, cyclohexylmethyl, F), (M-8494, CI, F, CI,
cyclohexylmethyl, CFs), (M-8495, CI, F, CI, cyclohexylmethyl, Br), (M-8496, CI, F, Cl; cyclohexylmethyl CH3), (M-8497, CI, CH3) H, H, H), (M-8498, CI, CH3, H, H, CI), (M-8499, CI, CH3 ) H, H, F), (M-8500, CI, CH3, H, H, CF3), (M-8501, CI, CH3, H, H, Br), (M-8502, Cl， CH3; H, H, CHs), (M-8503, CI, CHs, H， F, H)， (M-8504, CI, CH3; H, F, Cl), (M-8505, CI, CH3, H, F, F), (M-8506, CI, CH3, H, F, CFs), (M-8507, Cl, CHs, H, F, Br), (M-8508, Cl, CHs, H， F, CH3), (M-8509, Cl, CH3) H, Cl, H), (M-8510, Cl, CHs, H, Cl, Cl), (M-8511, Cl, CH3, H, Cl, F), (M- 8512, Cl, CH3, H， Cl, CFs), (M-8513, Cl, CHs, H, Cl, Br), (M-8514, Cl, CH3, H, Cl, CHs), (M-8515, Cl, CHs, H, CHs, H)， (M-8516, Cl, CHs, H, C Cl), (M-8517, Cl, CH3) H, CH3) F), (M-8518, Cl, CH3; H, CH3, CF3), (M-8519, Cl, CH3, H, CHs, Br), (M-8520, Cl, CH3, H, CHs, CHs), (M-8521, Cl, CHs, H, Et, H), (M-8522, Cl, CH3, H, Et, Cl), (M-8523, Cl, CH3, H， Et, F), (M-8524, Cl, CH3> H, Et, CFs), (M-8525, Cl, CHs, H, Et, Br), (M-8526, Cl, CHs, H, Et, CHs), (M-8527, Cl, CHs, H， n-Pr, H), (M-8528, Cl, CHs, H, n-Pr, Cl), (M-8529, Cl, CH3, H, n-Pr, F), (M-8530, Cl, CHs, H, n-Pr, CFs), (M-8531, Cl, CHs, H, n-Pr, Br), (M-8532, Cl, CHs, H, n-Pr, CHs), (M-8533, Cl, CHs, H, c-Pr, H), (M-8534, Cl, CH3; H, c-Pr, Cl), (M-8535, Cl, CHs, H, c-Pr, F), (M-8536, Cl, CH3) H, c-Pr, CFs), (M-8537, Cl, CHs, H, c-Pr, Br), (M-8538, Cl, CHs, H, c-Pr, CHs), (M-8539, Cl, CHs, H, i-Pr, H), (M-8540, Cl, CHs, H, i-Pr, Cl), (M-8541, Cl, CH3, H, i-Pr, P), (M-8542, Cl, CHs, H, i-Pr, CFs), (M-8543, CI, CHs, H, i-Pr, Br), (M-8544, CI, CHs, H, i-Pr, CHs), (M-8545, CI, CH3, H, n-Bu, H), (M-8546, CI, CHs, H, n-Bu, CI), (M-8547, CI, CH3, H, n-Bu, F), (M-8548, CI, CHs, H, n-Bu, CFs), (M-8549, CI, CHs, H, n-Bu, Br), (M-8550, CI, CHs, H, n-Bu, CHs), (M-8551, CI, CH3) H, i-Bu, H), (M-8552, CI, CHs, H, i-Bu, CI), (M-8553, CI, CH3, H， i-Bu, F), (M-8554, CI, CHs, H, i-Bu, CFa), (M-8555, CI, CHs, H， i-Bu, Br), (M-8556, CI, CHs, H, i-Bu, CHs), (M-8557, CI, CHs, H， sec- Bu, H), (M-8558, CI, CHs, H, sec-Bu, CI), (M-8559, CI, CH3, H, sec-Bu, F), (M-8560, CI, CHs, H, sec-Bu, CPs), (M-8561, CI, CHs, H, sec-Bu, Br), (M-8562, CI, CH3, H, sec-Bu, CH3), (M-8563, CI, CH3, H, n-Pen, H), (M-8564, CI, CHs, H, n-Pen, CI), (M-8565, CI, CH3, H， n-Pen, F), (M-8566, CI, CH3) H, n-Pen, CFa), (M-8567, CI, CHs, H， n-Pen, Br), (M-8568, CI, CH3, H' n-Pen, CHs), (M-8569, CI, CH3, H, c-Pen, H), (M-8570, CI, CH3) H; c-Pen, CI), (M-8571, CI, CHs, H, c-Pen, F), (M-8572, CI, CHs, H, c-Pen, CF3), (M-8573, CI, CHs, H, c-Pen, Br), (M-8574, CI, CHs, H, c-Pen, CHs), (M-8575, CI, CHs, H, n-Hex, H), (M-8576, CI, CH3, H, n-Hex, CI), (M-8577, CI, CH3, H, n-Hex, F), (M-8578, CI, CHs, H, n-Hex, CFs), (M-8579, CI, CH3, H, n-Hex, Br), (M-8580, CI, CHa, H, n-Hex, CHs), (M-8581, CI, CHs, H, c-Hex, H), (M-8582, CI, CH3, H, c-Hex, CI), (M-8583, CI, CHs, H' c-Hex, F), (M-8584, CI, CHs, H, c-Hex, CFs), (M-8585, CI, CHs, H, c-Hex, Br), (M-8586, CI, CH3) H， c-Hex, CHs), (M-8587, CI, CH3, H, OH, H), (M-8588, CI, CH3) H, OH, CI), (M-8589, CI, CHs, H, OH, F), (M-8590, CI, CHs, H, OH, CFs), (M-8591, CI, CH3) H, OH, Br), (M-8592, CI, CH3) H, OH, CHs), (M-8593, CI, CH3, H, EtO, H)' (M-8594, CI, CHs, H, EtO, CI), (M.8595, CI, CHa, H, EtO, F), (M-8596, CI, CHs, H, EtO, CFs), (M-8597, CI, CHs, H, EtO, Br), (M-8598, CI, CHs, H, EtO, CHs), (M-8599, CI, CHs, H, n-PrO, H), (M-8600, CI, CH3, H, n-PrO, CI), (M-8601, CI, CH3, H, n-PrO, F), (M-8602, CI, CHs, H, n-PrO, CFs), (M-8603, CI, CHs, H, n- PrO, Br), (M-8604, CI, CHa, H, n-PrO, CHs), (M-8605, CI, CHs, H, PhO, H), (M-8606, CI, CH3, H, PhO, CI), (M-8607, CI, CH3, H, PhO, F), (M-8608, CI, CHs, H, PhO, CP3); (M-8609, CI, CHs, H, PhO, Br), (M-8610, CI, CHs, H, PhO, CHs), (M-8611, CI, CHs, H, BnO, H), (M-8612, CI, CHs, H， BnO, CI), (M-8613, CI, CHs, H, BnO, F), (M-8614, CI, CHs, H, BnO, CF3)， (M-8615, CI, CH3> H, BnO, Br), (M-8616, CI, CHs, H, BnO, CHs), (M-8617, CI, CH3, H, PhCHaCHaO, H), (M- 8618, CI, CH3, H, PI1CH2CH2O, CI), (M-8619, CI, CHs, H, PI1CH2CH2O, F), (M-8620, CI, CHs, H, PhCH2CH20' CF3), (M-8621, CI, CH3， H, PhCH2CH20; Br), (M-8622, CI, CH3, H, PhCH2CH20, CH3)，（M-8623, CI, CH3, H， CFsO, H), (M- 8624, Cl， CHs, H, CFsO, CI), (M-8625, CI, CH3) H, CFsO, F), (M-8626, CI, CH3) H, CF3O, CFs), (M-8627, CI, CHs, H, CFsO, Br), (M-8628, CI, CHs, H, CFsO, CHs), (M-8629, CI, CHs, H， Ph, H), (M-8630, CI, CHa, H， Ph, CI), (M-8631, CI, CH3) H, Ph, F), (M-8632, CI, CHs, H, Ph, CFs), (M-8633, CI, CH3, H, Ph, Br), (M-8634, CI, CHs, H, Ph, CHs), (M-8635, CI, CHs, H, 4-F-Ph, H), (M-8636, CI, CHa, H, 4-F-Ph, CI), (M-8637, CI, CHa, H, 4-F-Ph, F), (M-8638, CI, CH3; H, 4- F-Pli, CFs), (M-8639, CI, CHa, H, 4-F-Ph, Br); (M-8640, Cl' CH3, H, 4-F-Ph, CHs), (M-8641, Cl, CHs, H, 4-CFs-Ph, H), (M-8642, Cl, CHs, H, 4-CF3-Ph, Cl), (M-8643, Cl, CHs, H, 4-CFa-Ph, F), (M-8644, Cl, CHs, H, 4-CFs-Ph, CF3)， (M- 8645, Cl, CHs, H, 4-CF3-Ph' Br), (M-8646, Cl, CH3， H, 4-CFs-Ph, CHa), (M-8647, Cl, CH3, H, 4-(Me)2N-Ph; H), (M-8648, Cl, CH3) H, 4-(Me)2N-Ph; Cl), (M-8649, Cl, CHs, H, 4-(Me)2N-Ph) F), (M-8650, Cl, CHs, H, 4-(Me)2N-Ph, CFs), (M-8651, Cl, CHs, H' 4-(Me)2N-Ph, Br), (M-8652, Cl, CHa, H, 4-(Me)2N-Pli) CH3), (M- 8653, Cl, CHs, H, 4-OH-Ph, H), (M-8654, Cl; CH3, H, 4-OH-Eh, Cl), (M-8655, Cl, CH3, H, 4-OH-Ph, F)， (M-8656, Cl, CHs, H, 4-OH-Ph, CF3), (M-8657, Cl, CH3, H, 4-OH-Ph, Br), (M-8658, Cl, CHs, H, 4-OH-Ph, CHs), (M-8659, Cl, CHs, H, 3,4- di-F-Ph, H)， (M-8660, Cl, CHs, H, 3,4-di-F-Pli, Cl), (M-8661, Cl, CH3, H, 3,4- di-F-Ph, F), (M-8662, Cl, CHs, H, 3,4-di-F-Ph, CFs), (M-8663, Cl, CHs, H, 3,4- di-F-Ph, Br), (M-8664, Cl, CHs, H, 3,4-di-F-Pli, CHs), (M-8665, Cl, CH3, H, 4- COOH-Ph, H), (M-8666, Cl, CHs, H, 4-COOH-Ph, Cl), (M-8667, Cl, CHs, H; 4- COOH-Ph, F), (M-8668, Cl, CH3, H, 4-COOH-Ph, CF3), (M-8669, Cl, CHs, H; 4-COOH-Ph, Br), (M-8670, Cl, CHs, H, 4-COOH-Pli, CH3)， (M-8671, Cl, CHs, H, Bn, H)， (M-8672, Cl, CH3, H, Bn, Cl), (M-8673, Cl, CHs, H, Bn, F), (M-8674, Cl, CHs, H, Bn, CFs), (M-8675, Cl, CHs, H, Bn, Br), (M-8676, Cl, CHs, H， Bn, CH3), (M-8677, Cl, CHs, H, 4-F-Bn, H), (M-8678, Cl, CHs, H, 4-F-Bn, Cl), (M-8679, Cl, CH3) H， 4-F-Bn, F), (M-8680, Cl, CH3, H, 4-F-Bn, CFs), (M-8681, Cl, CHs, H, 4-F-Bn, Br), (M-8682, Cl, CHs, H, 4-F-Bn, CHs), (M-8683, Cl, CH3> H, 2-Py, H), (M-8684, Cl, CHs, H, 2-Py, Cl), (M-8685, Cl, CHs, H, 2-Py, F), (M-8686, Cl, CHs, H, 2-Py, CFs), (M-8687, Cl, CHs, H, 2-Py, Br), (M-8688, Cl, CHs, H, 2-Py, CH3), (M-8689, Cl, CHs, H, 3-Py, H)， (M-8690, Cl, CHs, H, 3-Py, Cl), (M-8691, Cl, CHs, H, 3-Py, F), (M-8692, Cl, CHs, H, 3-Py, CFs), (M-8693, Cl, CH3, H, 3-Py, Br), (M-8694, Cl, CHs, H, 3-Py, CH3), (M-8695, Cl, CHs, H, 4-Py, H), (M-8696, Cl, CH3> H, 4-Py, Cl), (M-8697, Cl, CH3; H, 4-Py, F), (M-8698, Cl, CH3) H, 4-Py, CPs), (M-8699, Cl, CHs, H' 4-Py, Br), (M-8700, Cl, CHs, H， 4-Py, CHs), (M-8701, Cl, CH3, H, 2-Th, H), (M-8702, Cl, CHs, H, 2-Th, Cl), (M-8703, Cl, CHs, H, 2- Th, F), (M-8704, Cl, CHs, H, 2-Th, CFa), (M-8705, Cl, CHs, H, 2-Th, Br), (M- 8706， Cl, CHs, H, 2-Th, CHs), (M-8707, Cl, CHs, H, 3-Th, H), (M-8708, Cl, CH3; H, 3-Th, Cl), (M-8709, Cl, CH3， H, 3-Th, P), (M-8710, Cl, CHs, H, 3-Th, CFs), (M-8711, Cl, CHs, H, 3-Th, Br), (M-8712, Cl, CHs, H, 3-Th, CHs), (M-8713, Cl, CHs, H, pyrazoレ 2-yl， H), (M-8714, Cl, CH3; H, pyrazol-2-yl, Cl), (M-8715, Cl, CHs, H, pyrazol-2-yl, F), (M-8716, Cl, CH3, H, pyrazol-2-yl, CF3), (M-8717, Cl, CHs, H, pyrazol-2-yl, Br), (M-8718, Cl, CH3, H, pyrazol-2-yl, CH3), (M-8719, Cl, CHs, H, pyrazol-3-yl, H), (M-8720, Cl, CH3, H, pyrazol-3-yl, Cl), (M-8721, Cl, CHs, H, pyrazol-3-yl, F), (M-8722, Cl, CH3> H, pyrazol-3-yl, CFs), (M-8723, Cl, CHs, H, pyrazol-3-yl, Br), (M-8724, CI, CHs, H, pyrazol-3-yl, CHs), (M-8725, CI, CHs, H, pyrimidin-2-yl; H), (M-8726, CI, C , H, pyrimidin-2-yl, CI), (M-8727, CI, CHs, H, pyrimidin-2-yl; F), (M-8728, CI, CH3, H, pyrimidin-2-yl, CF3), (M- 8729, CI, CHs, H, pyrimidin-2-yl, Br), (M-8730, CI, CHs, H, pyrimidin-2-yl; CH3), (M-8731, CI, CHs, H, pyrimidin-4-yl, H), (M-8732, CI, CH3) H,
pyrimidin-4-yl; CI), (M-8733, CI, CHs, H, pyrimidin-4-yl, F), (M-8734, CI, CH3， H, pyrimidin-4-yl, CFs), (M-8735, CI, CHs, H, pyrimidin-4-yl, Br), (M-8736, CI, CHs, H, pyrimidin-4-yl, CHs), (M-8737, CI, CHs, H, pyrimidin-5-yl, H), (M-8738, CI, CHs, H, pyrimidin-5-yl, CI), (M-8739, CI, CH3, H, pyrimidin-5-yl, F), (M- 8740, CI, CH3, H, pyrimidin-5-yl, CFs), (M-8741, CI, CH3) H, pyrimidin-5-yl, Br), (M-8742, CI, CHs, H, pyrimidin-5-yl, CHs), (M-8743, CI, CH3; H,
HOOCCH2CH2CH2, H), (M-8744, CI, CH3, H, HOOCCH2CH2CH2) CI), (M-8745, CI, CHs, H, HOOCCH2CH2CH2, F), (M-8746, CI, CHs, H， HOOCCH2CH2CH2, CFs), (M-8747, CI, CHs, H， HOOCCH2CH2CH2, Br), (M-8748, CI, CH3, H，
HOOCCH2CH2CH2, CHs), (M-8749, CI, CHs, H, HOOCCH2CH2CH2CH2, H)， (M-8750, CI, CH3> H, HOOCCH2CH2CH2CH2, CI), (M-8751, CI, CH3, H,
HOOCCH2CH2CH2CH2, F), (M-8752, CI, CH3, H, HOOCCH2CH2CH2CH2' CF3), (M-8753, CI, CH3, H, HOOCCH2CH2CH2CH2, Br), (M-8754, CI, CHa, H，
HOOCCH2CH2CH2CH2， CHs), (M-8755, CI, CHs, H, (Me)2NCOCH2CH2CH2CH2, H)， (M-8756, CI, CHs, H, (Me)2NCOCH2CH2CH2CH2, CI), (M-8757, CI, CHs, H， (Me)2NCOCH2CH2CH2CH2， F), (M-8758, CI, CH3) H,
(Me)2NCOCH2CH2CH2CH2, CF3), (M-8759, CI, CH3) H,
(Me)2NGOCH2CH2CH2CH2, Br), (M-8760, CI, CHs, H,
(Me)2NCOCH2CH2CH2CH2, CH3)， (M-8761, CI, CH3, H,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-8762, CI, CH3, H,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-8763, CI, CH3, H, (Me)2NCOCH2CH2CH2CH2CH2, F), (M-8764, CI, CH3) H,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-8765, CI, CH3, H,
(Me)2NCOCH2CH2CH2CH2CH2; Br), (M-8766, CI, CHa, H，
(Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-8767, CI, CHs, H, MeOCH2, H), (M- 8768, CI, CHs, H, MeOCHa, CI), (M-8769, CI, CH3, H, MeOCH2, F), (M-8770, CI, CH3; H, MeOCHa, CFs), (M-8771, CI, CHs, H, MeOCH2， Br), (M-8772, CI, CH3; H, MeOCH2, CHs), (M-8773, CI, CH3, H, EtOCHa, H), (M-8774, CI, CHs, H, EtOCHa, CI), (M-8775, CI, CH3, H, EtOCH2， F), (M-8776, CI, CH3, H, EtOCH2) CFs), (M-8777, CI, CHa, H, EtOCH2) Br), (M-8778, CI, CHs, H, EtOCHs, CH3), (M-8779, CI, CH3; H, EtOCHsCHs' H), (M-8780, CI, CHs, H, EtOCH2CH2; CI), (M-8781, CI, CHs, H' EtOCHaCHa, F), (M-8782, CI, CH3; H, EtOCH2CH2) CFs), (M-8783, CI, CHs, H, EtOCHaCHa, Br), (M-8784, CI, CH3, H， EtOCH2CH2) CH3), (M-8785, CI, CH3) H, MeOCH2CH2OCH2CH2, H)， (M-8786, CI, CHs, H,
MeOCH2CH2DCH2CH2! CI), (M-8787, CI, CH3, H, MeOCH2CH2OCH2CH2, F), (M-8788, CI, CHs, H, MeOCH2GH20CH2CH2, CF3)，（M-8789, CI, CH3, H，
MeOCH2CH2OCH2CH2, Br), (M-8790, Cl; CHs, H, MeOCH2CH20CH2CH2, CHs), (M-8791, CI, CHs, H, MeOCH2CH2> H), (M-8792, CI, CHs, H, MeOCH2CH2; CI), (M-8793, CI, CHs, H, MeOCH2CH2, P), (M-8794, CI, CHs, H, MeOCH2CH2) CFs), (M-8795, CI, CHa, H, MeOCH2CH2; Br), (M-8796, CI, CH3, H, MeOCH2CH2, CHa), (M-8797, CI, CH3) H, HOCH2) H), (M-8798, CI, CHs, H, HOCH2, CI),
(M-8799, CI, CHs, H， HOCHs, F), (M-8800, CI, CH3, H, HOCH2) CF3), (M-8801, CI, CHs, H, HOCH2, Br), (M-8802, CI, CH3, H, HOC CHs), (M-8803, CI, CHs, H, HOCH2CH2, H), (M-8804, CI, CH3; H, HOCH2CH2, CI), (M-8805, CI, CHs, H, HOCH2CH2, F), (M-8806, CI, CH3) H, HOCH2CH2' CPs), (M-8807, CI, CH3, H， HOCH2CH2) Br), (M-8808, CI, CHs, H, HOCH2CH2, CHs), (M-8809, CI, CHs, H, HOCH2CH2CH2' H), (M-8810, CI, CHs, H, HOCH2CH2CH2, CI), (M-8811, CI, CHs, H, HOCH2CH2CH2， F), (M-8812, Cl' CHs, H, HOCH2CH2CH2, CPs), (M- 8813, Cl, CH3, H， HOCH2GH2CH2, Br), (M-8814, Cl, CHs, H， HOCH2CH2CH2; CH3), (M-8815, Cl, CHs, H, H0CH2CH2CH2CH2) H), (M-8816, Cl, CHs, H, HOCH2CH2CH2CH2, Cl), (M-8817, Cl, CH3, H, HOCH2CH2CH2CH2, F), (M-8818, Cl, CHs, H, HOCH2CH2CH2CH2; CFs), (M-8819, Cl, CHs, H,
HOCH2CH2CH2CH2> Br), (M-8820, Cl, CHs, H, HOCH2C CH2CH2, CH3), (M- 8821, Cl, CHs, H, HOCH2CH2CH2CH2CB , H), (M-8822, Cl, CH3， H，
HOCH2CH2CH2CH2CH2) Cl), (M-8823, Cl, CH3, H, HOCH2CH2CH2CH2CH2, F)， (M-8824, Cl, CH3， H, HOCH2CH2CH2CH2CH2, CFs), (M-8825, Cl, CHs, H, HOCH2CH2CH2CH2CH2, Br), (M-8826, Cl, CHs, H, HOCH2CH2CH2CH2CH2, CH3), (M-8827, Cl, CHs, H, HOCH2CH2OCH2CH2, H)，（M-8828, Cl, CH3, H, HOCH2CH2OCH2CH2, Cl), (M-8829, Cl, CHs, H, HOCH2CH2OGH2CH2, F), (M- 8830, Cl, CHs, H, HOCH2CH2OCH2CH2) CFs), (M-8831, Cl, CH3) H,
H0CH2CH20CH2CH2, Br), (M-8832, Cl, CHs, H, HOCH2CH2OCH2CH2, CHs), (M-8833, Cl, CH3' H， (Me)2N; H), (M-8834, Cl, CH3, H, (Me)2N, Cl), (M-8835, Cl, CHs, H, (Me)2N; F), (M-8836, Cl, CH3) H, (Me)2N, CFs), (M-8837, Cl, CHs, H, (Me)2N, Br), (M-8838, Cl, CH3, H, (Me)2N, CH3), (M-8839, Cl, CHs, H, piperidin-4-yl-metliyl, H), (M-8840, Cl, CHs, H, piperidm-4-yl-metliyl, Cl), (M-8841, Cl, CH3, H, piperidin-4-yl-methyl, F)， (M-8842, Cl, CH3, H, piperidin-4-yl-methyl, CF3), (M-8843, Cl, CHs, H, piperidin-4-yl-methyl, Br), (M-8844, Cl, CHs, H, piperidin-4-yl-metliyl; CH3), (M-8845, Cl, CHs, H, cyclohexylmethyl, H), (M-8846, Cl, CHa, H, cyclohexylmethyl, Cl), (M-8847, Cl, CH3, H, cyclohexylmethyl, F), (M-8848, Cl, CH3) H, cyclohexylmethyl, CF3), (M-8849, Cl, CHs, H, cyclohexylmethyl, Br), (M-8850, Cl, CH3, H,
cyclohexylmethyl, CHs), (M-8851, Cl, CH3, F, H, H), (M-8852, Cl, CHs, F, H, Cl), (M-8853, MeO, CHs, F, H, F), (M-8854, Cl, CH3, F, H, CF3), (M-8855, Cl, CH3, F, H, Br), (M-8856, Cl, CH3， P, H, CHs), (M- 8857, Cl, CHs, F, F, H), (M-8858, Cl, CHs, F, F, Cl), (M-8859, Cl, CHs, F, F, F), (M-8860, Cl, CHs, F, F, CFs), (M-8861, Cl, CH3, F， F, Br), (M-8862, Cl' CH3; F, F, CHs), (M-8863, Cl, CH3) F， Cl, H), (M-8864, Cl, CH3) F， Cl, Cl), (M- 8865, Cl, CHs, F, Cl, F)， (M-8866, Cl, CHs, F， Cl, CFs), (M-8867, Cl, CHs, F, Cl, Br), (M-8868, Cl, CHs, F, Cl, CHs), (M-8869, Cl, CH3l F' CH3; H), (M-8870, Cl, CH3, F, CH3) Cl), (M-8871, Cl, CHs, F, CHs, F) , (M-8872, Cl, CH3) F, CHs, CFs), (M-8873, Cl, CHs, F, CH3 ) Br), (M-8874, Cl, CHs, F, CH8) CHs), (M-8875, Cl, CH3, F， Et, H), (M- 8876, Cl, CH3j F, Et, Cl), (M-8877, Cl, CHs, F, Et, F), (M-8878, Cl, CHs, F, Et, CFs), (M-8879, Cl, CHs, F, Et, Br), (M-8880, Cl, CHs, F, Et, CH3), (M-8881, Cl, CH3) F, n-Pr, H)， (M-8882, Cl, CHs, F, n-Pr, Cl), (M-8883, Cl, CH3, F, n-Pr, F) , (M-8884, Cl, CHs, F, n-Pr, CFs), (M-8885, Cl, CHs, F, n-Pr, Br), (M-8886, Cl, CHa, F, n-Pr, CHs), (M-8887, Cl, CHs, F, c-Pr, H) , (M-8888, Cl, CHs, F， c-Pr, Cl), (M-8889, Cl, CHs, F, c-Pr, F), (M-8890, Cl, CHs, F, c-Pr, CFs), (M-8891, Cl, C F, c-Pr, Br), (M-8892, Cl, CH3) F, c-Pr, CHs), (M-8893, Cl, CH3， F, i-Pr, H)，（M-8894, Cl, CHs, F, i-Pr, Cl), (M-8895, Cl, CHs, P, i-Pr, F)， (M-8896, Cl, CHs, F, i-Pr, CP3), (M-8897, Cl, CHs, F, i-Pr, Br), (M-8898, Cl, CHs, F, i-Pr, CH3), (M- 8899, Cl, CHs, F， n-Bu, H) , (M-8900, Cl, CHs, F, n-Bu, Cl) , (M-8901, Cl, CHs, F， n-Bu, F)， (M-8902, Cl, CHs, F, n-Bu, CFs), (M-8903, Cl' CHs, F, n-Bu, Br), (M-8904, Cl, CH3, F, n-Bu, CHs), (M-8905, Cl, CH3, F， i-Bu, H), (M-8906, Cl, CHs, F, i-Bu, Cl), (M-8907, Cl, CH3, F, i-Bu, F), (M-8908, Cl, CHs, F， i-Bu, CFs), (M-8909, Cl, CHs, F, i-Bu, Br), (M- 8910, Cl, CH3, ,F, . i-Bu, CHs), (M- 8911, Cl, CHs, F, sec -Bu, H), (M-8912, Cl, CH3, F, sec-Bu, Cl), (M-8913, Cl, CH3) F, sec-Bu, F) , (M-8914, Cl, CH3) F, sec- Bu, CFs), (M-8915, Cl, CH3, F, sec-Bu, Br), (M-8916, Cl, CHs, F, sec-Bu, CH3) , (M-8917, Cl, CHs, F， n-Pen, H), (M-8918, Cl, CH3, F, n-Pen, Cl), (M-8919, Cl, CHs, F, n-Pen, F), (M-8920, Cl, CHs, F, n-Pen, CFs), (M-8921, Cl, CH3, F, n-Pen, Br), (M-8922, Cl, CH3; F, n-Pen, CH3), (M-8923, Cl, CH3, F, c-Pen, H), (M-8924, Cl, CH3) F, c-Pen, Cl), (M-8925, Cl, CH3, F, c-Pen, F), (M-8926, Cl, CH3, F， c- Pen, CFs), (M-8927, Cl, CHs, F, c-Pen, Br), (M-8928, Cl, CH3; F, c-Pen, CH3), (M-8929, Cl, CHs, F, n-Hex, H), (M-8930, Cl, CHs, F, n-Hex, Cl), (M-8931, Cl, CH3, F, n-Hex, F), (M-8932, Cl, CH3) F, n-Hex, CF3), (M-8933, Cl, CHs, F， n- Hex, Br), (M-8934, Cl, CH3; F, n-Hex, CHs), (M-8935, Cl, CHs, F, c-Hex, H), (M-8936, Cl, CHs, F, c-Hex, Cl), (M-8937, Cl, CHs, F, c-Hex, F), (M-8938, Cl, CHs, F, c-Hex, CF3), (M-8939, Cl, CH3, F， c-Hex, Br), (M-8940, Cl, CHs, F, c- Hex, CHs), (M-8941, Cl, CHs, F, OH, H)， (M-8942, Cl, CHs, F， OH, Cl), (M-8943, Cl, CHs, F, OH, F), (M-8944, Cl, CHa., F, OH, CF3), (M-8945, Cl, CHs, F, OH, Br), (M-8946, Cl, CHs, F, OH, CH3), (M-8947, Cl, CHs, F, EtO, H), (M-8948, Cl, CH3) F, EtO, Cl), (M-8949, Cl, CHs, F, EtO, F), (M-8950, Cl, CH3) F, EtO, CF3), (M- 8951, Cl, CHs, F, EtO, Br), (M-8952, Cl, CH3) F， EtO, CHs), (M-8953, Cl, CH3) F, n-PrO, H), (M-8954, Cl, CHs, F, n-PrO, Cl), (M-8955, Cl, CH3; F, n-PrO, F), (M-8956, Cl, CHs, F, n-PrO, CF3), (M-8957, Cl, CHs, F, n-PrO, Br), (M-8958, Cl, CH3) F, n-PrO, CHs), (M-8959, Cl, CHs, F, PhO, H), (M-8960, Cl, CHs, F， PhO, Cl), (M-8961, Cl, CH3) F, PhO, F), (M-8962, Cl, CHs, F, PhO, CFs), (M-8963, Cl, CHs, F, PhO, Br), (M-8964, Cl, CH3, F, PhO, CHs), (M-8965, Cl, CHs, F, BnO, H), (M-8966, Cl, CHs, F, BnO, Cl), (M-8967, Cl, CH3, F, BnO, F), (M-8968, Cl, CH3) F， BnO, CPs), (M-8969, Cl, CH3, F, BnO, Br), (M-8970, Cl, CHs, F; BnO, CHs), (M-8971, Cl, CHs, F, PhC^CHaO, H), (M-8972, Cl, CH3) F, PI1CH2CH2O, Cl), (M-8973, Cl, CHs, F， PhCHaCHaO, F), (M-8974, Cl' CH3, F， PhCH2CH20, CPs), (M-8975, Cl, CHs, F, PhCH2CH20， Br), (M-8976, Cl, CHs, F, PhCHsCHaO, CHs), (M-8977, Cl, CH3, F, CFsO, H), (M-8978, Cl, CH3， F, CF30, Cl), (M-8979, Cl, CH3; F, CFsO, F); (M-8980, Cl, CH3) F, CFsO, CF3)，（M-8981, Cl, CH3, F, CF30, Br), (M-8982, Cl, CHs, F, CFsO, CHs), (M-8983, Cl, CH3, F, Ph, H), (M-8984, Cl, CHs, F, Ph, CI), (M-8985, CI, CHs, F, Ph, F), (M-8986, CI, CH3, F, Ph, CF3), (M-8987, CI, CH3) F, Ph, Br), (M-8988, CI, CHs, F, Ph, CHs), (M-8989, CI, CHs, F; 4-F-Ph, H), (M-8990, CI, CH3; F, 4-F-Ph, CI), (M-8991, CI, CH3) F, 4-F-Ph, P), (M-8992, CI, CHs, F, 4-F-Ph, CFs), (M-8993, CI, CHs, F, 4-F-Ph, Br), (M-8994, CI, CH3; F, 4-F-Ph, CHs), (M-8995, CI, CH3, F， 4-CFs-Pli, H), (M-8996, CI, CHs, F， 4-CFs-Ph, CI), (M-8997, CI, CH3, F, 4-CFs-Pli, F), (M-8998, Cl; CHs, F, 4- CFs-Ph, CFs), (M-8999, CI, CHs, F, 4-CF3-Ph; Br), (M-9000, CI, CH3) F, 4-CPs- Ph, CH3)， (M-9001, CI, CH3, F, 4-(Me)2N-Ph) H)， (M-9002, CI, CHs, F, 4- (Me)2N-Ph, CI), (M-9003, CI, CHs, F, 4-(Me)2N-Ph, F), (M-9004, CI, CHs, F， 4- (Me)2N-Ph; CF3), (M-9005, CI, CH3, F， 4-(Me)2N-Ph; Br), (M-9006, CI, CH3, F, 4-(Me)2N-Ph) CHs), (M-9007, CI, CHs, F, 4-OH-Ph, H)， (M-9008, CI, CHs, F, 4- OH-Pli, CI), (M-9009, CI, CHs, F, 4-OH-Ph, F), (M-9010, CI, CH3) F, 4-OH-Ph, CFs), (M-9011, CI, CHs, F, 4-OH-Ph, Br), (M-9012, CI, CHs, F, 4-OH-Ph, CHs), (M-9013, CI, CHs, F, 3, 4-di-F-Ph, H), (M-9014, CI, CH3, F, 3,4-di-F-Ph, CI), (M-9015, CI, CHs, F, 3,4-di-F-Ph, F), (M-9016, CI, CHs, F, 3,4-di-F-Pli, CFs), (M-9017, CI, CHs, F, 3,4-di-F-Ph, Br), (M-9018, CI, CH3, F, 3,4-di-F-Ph, CH3), (M-9019, CI, CHs, F， 4-COOH-Ph, H), (M-9020, CI, CH3， F, 4-COOH-Ph, CI), (M-9021, CI, CH3; F， 4-COOH-Ph, F), (M-9022, CI, CH3, F, 4-COOH-Ph, CF3), (M-9023, CI, CHs, F' 4-COOH-Ph, Br), (M-9024, CI, CHs, F, 4-COOH-Ph, CH3); (M-9025, CI, CHs, F, Bn, H), (M-9026, CI, CH3) F, Bn, CI), (M-9027, CI, CHs, F, Bn, F), (M-9028, CI, CHs, F, Bn, CFs), (M-9029, CI, CHs, F, Bn, Br), (M-9030, CI, CHs, F, Bn, CH3), (M-9031,. C1, CHs, F, 4-F-Bn, H)， (M-9032, CI, CH3, F, 4-P- Bn, CI), (M-9033, CI, CH3> F， 4-F-Bn, F), (M-9034, CI, CHs, F, 4-F-Bn, CFs), (M-9035, CI, CHs, F, 4-F-Bn, Br), (M-9036, CI, CHs, F, 4-F-Bn, CHs), (M-9037, CI, CH3) F, 2-Py, H), (M-9038, CI, CHs, F, 2-Py, CI), (M-9039, CI, CHs, F, 2-Py, F), (M-9040, CI, CH3) F, 2-Py, CF3), (M-9041, CI, CHs, F, 2-Py, Br), (M-9042, CI, CHs, F, 2-Py, CH3), (M-9043, CI, CHs, F, 3-Py; H), (M-9044, CI, CH3, F, 3-Py, CI), (M-9045, CI, CH3) F， 3-Py, P), (M-9046, CI, CHs, F, 3-Py, CF3), (M-9047, CI, CHs, F, 3-Py, Br), (M-9048, CI, CHs, F, 3-Py, CHs), (M-9049, CI, CHs, F, 4-Py, H), (M-9050, CI, C F, 4-Py, CI), (M-9051, CI, CH3, F, 4-Py, F), (M-9052, CI, CHs, F, 4-Py, CF3), (M-9053, CI, CH3 ) F， 4-Py, Br), (M-9054, CI, CH3; F, 4-Py, CH3), (M-9055, CI, CH3, F, 2-Th, H), (M-9056, CI, CH3; F, 2-Th, CI), (M-9057, CI, CHs, F, 2-Th, F), (M-9058, CI, CH3; F, 2-Th, CFs), (M-9059, CI, CH3, F, 2-Th, Br), (M-9060, CI, CHs, P, 2-Th, CHs), (M-9061, CI, CH3, F， 3-Th, H), (M-9062, CI, CH3) F, 3-Th, CI), (M-9063, CI, CHs, F, 3-Th, F), (M-9064, CI, CHs, F， 3-Th, CFs), (M-9065, CI, CH3) F, 3-Th, Br), (M-9066, CI, CH3, F, 3-Th, CHs), (M-9067, CI, CB.3, F, pyrazol-2-yl, H), (M-9068, CI, CHs, F, pyrazol-2-yl, CI), (M-9069, CI, CHs, F, pyrazoレ 2-yl, F), (M-9070, CI, CHs, F, pyrazoレ 2-yl, CF3), (M-9071, CI, CH3) F， pyrazol-2-yl, Br), (M-9072, CI, CHs, F, pyrazol-2-yl, CHs), (M-9073, CI, CHs, F, pyrazol-3-yl, H), (M-9074, CI, CHs, F, pyrazol-3-yl, CI), (M-9075, CI, CHs, F, pyrazol-3-yl, F)， (M-9076, CI, CH3, F, pyrazol-3-yl, CF3), (M-9077, CI, CH3) F, pyrazol-3-yl, Br), (M-9078, CI, CH3, P, pyrazol-3-yl, CH3), (M-9079, CI, CHs, F, pyrimidin-2-yl, H), (M-9080, CI, CHs, F, pyrimidin-2-yl, CI), (M- 9081, CI, CHs, P, pyrimidin-2-yl, F), (M-9082, CI, CHs, F, pyrimidin-2-yl, CFs), (M- 9083, CI, CHs, F, pyrimidin-2-yl; Br), (M-9084, CI, CHs, F, pyrimidin-2-yl, CHs), (M-9085, CI, CHs, F, pyrimidin-4-yl, H), (M-9086, CI, CHs, P, pyrimidin-4-yl, CI), (M-9087, CI, CHs, F, pyrimidin-4-yl, ), (M-9088, CI, CH3, F, pyrimidin- 4-yl, CFs), (M-9089, CI, CHs, F, pyrimidin-4-yl, Br), (M-9090, CI, CHs, F, pyrimidm-4-.yl, CHs), (M-9091, CI, CHs, F; pyrimidin-5-yl, H), (M-9092, CI, CHs, F, pyrimidin- 5-yl, CI), (M-9093, CI, CH3 ; F, pyrimidin-5-yl, F), (M-9094, CI, CHs, F, pyrimidin-5-yl, CFs), (M-9095, CI, CHs, F, pyrimidin-5-yl, Br), (M-9096, CI, CHs, F, pyrimidin-5-yl, CHs), (M-9097, CI, CHs, F, HOOCCH2CH2CH2, H), (M-9098, CI, CHs, F, HOOCCE CHsCEb, CI), (M-9099, CI, CH3, F, HOOCCH2CH2CH2, F), (M-9100, CI, CH3, F, HOOCCH2CH2CH2) CFs), (M-9101, CI, CHs, F, HOOCCH2CH2CH2, Br), (M-9102, CI, CHs, F， HOOCCH2CH2CH2, CHs), (M-9103, CI, CH3) F, HOOCCH2CH2CH2CH2, H), (M-9104, CI, CHs, F, HOOCCU2CU2CH2CII2, CI), (M-9105, CI, CHs, F，
HOOCCH2CH2CH2CH2, F); (M-9106, CI, CHs, F, HOOCCH2CH2CH2CH2, CF3), (M-9107, CI, CHs, F， HOOCCH2CH2CH2CH2> Br), (M-9108, CI, CH3; F,
HOOCCH2CH2CH2CH2, CHs), (M-9109, CI, CH3; F, (Me)2NGOCH2CH2CH2CH2, H), (M-9110, CI, CHs, F, (Me)2NCOCH2CH2CH2CH2, CI), (M-9111, CI, CH3, F, (Me)2NCOCH2CH2CH2CH2, F)' (M-9112, CI, CH3) F, (Me)2NCOCH2CH2CH2CH2, CF3), (M-9113, CI, CHs, F, (Me)2NCOCH2CH2CH2CH2, Br), (M-9114, CI, CHs, F, (Me)2NCOCH2CH2CH2CH2, CH3)，（M-9115, CI, CH3, F，
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-9116, CI, CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-9117, CI, CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-9118, CI, CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-9119, CI, CH3, F,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-9120, CI, CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2) CHs), (M-9121, CI, CHs' F, MeOCH2， H), (M- 9122， CI, CH3> F, MeOCH2; CI), (M-9123, CI, CH3, F, MeOCH2; F), (M-9124, CI, CH3, F， MeOCHs, CFs), (M-9125, CI, CH3) P, MeOCHs, Br), (M-9126, CI, CH3; F, MeOCH2) CHs), (M-9127, CI, CHs, F， EtOCHa, H)，（M-9128, CI, CH3, F; EtOCH2, CI), (M-9129, CI, CHs, F, EtOCH2) F)， (M-9130, CI, CHs, P, EtOC , CFs), (M-9131, CI, CHs, P, EtOCH2, Br), (M-9132, CI, CHs, F, EtOCH2, CHs), (M-9133, CI, CHs, F, EtOCH2CH2, H), (M-9134, CI, CH3， F, EtOCH2CH2, CI), (M-9135, CI, CHs, F, EtOCH2CH2, F), (M-9136, CI, CH3, F, EtOCHsCHs, CFs), (M-9137, CI, CHs, F, EtOCH2CH2; Br), (M-9138, CI, CH3; F, EtOCH2CH2; CHs), (M-9139, CI, CH3) F, MeOCH2CH2OCH2CH2， H)，（M-9140, CI, CHs, F, MeOCH2CH20CH2CH2, CI), (M-9141, CI, CHs, F， MeOCH2CH20CH2CH2) F), (M-9142, CI, CHs, F， MeOCH2CH2OCH2CH2, CF3), (M-9143, CI, CH3, F, MeOCH2CH2OCH2CH2, Br), (M-9144, CI, CH3, F, MeOCHsCHsOCHsCHs, CHs), (M-9145, CI, CHs, F, MeOCH2CH2; H); (M-9146, CI, CHs, F, MeOCH2CH2) CI), (M-9147, CI, CHs, F, MeOCH2CH2; F), (M-9148, CI, CHs, F, MeOCH2CH2, CF3), (M-9149, CI, CH3> F' MeOCH2CH2, Br), (M-9150, CI, CH3, F， MeOCH2CH2> CHs), (M-9151, CI, CHs, F, HOCH2, H), (M-9152, CI, CHs, F, HOCHs, CI), (M-9153, CI, CH3, F, HOCH2, F), (M-9154, CI, CHs, F， HOCH2, CF3), (M-9155, CI, CHs, F, HOCH2, Br), (M-9156, CI, CHs, F， HOCH2; CH3), (M-9157, CI, CH3; F, HOCH2CH2) H), (M-9158, CI, CH3, F, HOCH2CH2, CI), (M-9159, CI, CH3, F, HOCH2CH2, F), (M-9160, CI, CHs, F, HOCH2CH2) CFs), (M-9161, CI, CH3, F, HOCH2CH2, Br), (M-9162, CI, CHs, F, HOCH2CH2) CH3)，（M-9163, CI, CHs, F, HOCH2CH2CH2; H), (M-9164, CI, CHs, F; HOCH2CH2CH2, CI), (M-9165, CI, CHs, F， HOCH2CH2CH2, F), (M-9166, CI, CHs, F, HOCH2CH2CH2; CFs), (M-9167, CI, CH3, F， HOGHsCB CB , Br), (M- 9168， CI, CHs, F, HOCH2CH2CH2, CHs), (M-9169, CI, CHs, F,
HOCH2CH2CH2CH2; H), (M-9170, CI, CH3) F, HOCH2CH2CH2CH2, CI), (M-9171, CI, CHs, F, HOCH2CH2CH2CH2) F), (M-9172, CI, CHs, F, HOCH2CH2CH2CH2, CFs), (M-9173, CI, CHs, F, HOCH2CH2CH2CH2, Br), (M-9174, CI, CH3; F, HOCH2CH2CH2CH2, CHs), (M-9175, CI, CHs, F, HOCH2CH2CH2CH2CH2, H), (M-9176, CI, CHs, F, HOCH2CH2CH2CH2CH2, CI), (M-9177, CI, CHs, F,
- HOCH2CH2CH2CH2CH2, F), (M-9178, CI, CHs, F， HOCH2CH2CH2CH2CH2, CFs), (M-9179, CI, CHs, F, HOCH2CH2CH2CH2CH2> Br), (M-9180, CI, CH3) F，
HOCH2CH2CH2CH2CH2, CHs), (M-9181, CI, CHs, F, HOCH2CH2OCH2CH2, H), (M-9182, CI, CH3> F, HOCH2CH2OCH2CH2, CI), (M-9183, CI, CHs, F,
HOCH2CH2OCH2CH2， F), (M-9184, CI, CHs, F, HOCH2CH2OCH2CH2) CFs), (M-9185, CI, CH3) F, HOCH2CH2OCH2CH2, Br), (M-9186, CI, CH3; F，
HOCH2CH2O CH2CH2, CHs), (M-9187, CI, CH3) F, (Me)2N, H), (M-9188, CI, CH3, F, (Me)2N, CI), (M-9189, CI, CHs, F, (Me)2N， F), (M-9190, CI, CHs, F, (Me)2N; CFs), (M-9191, CI, CHs, F, (Me)2N, Br), (M-9192, CI, CH3, F, (Me)2N, CHs), (M-9193, CI, CH3) F, piperidin-4-yl-metliyl, H)， (M-9194, CI, CHs, F， piperidin-4-yl-methyl, CI), (M-9195, CI, CHs, F, piperidin-4-yl-methyl, F), (M-9196, CI, CHs, F, piperidin-4-yレ methyl, CFs), (M-9197, CI, CHs, P, piperidin-4-yl-metliyl, Br), (M-9198, CI, CHs, F, piperidin-4-yl-metliyl, CH3), (M-9199, CI, CHs, F， cyclohexylmethyl, H), (M-9200, CI, CHs, F，
cyclohexylmethyl, CI), (M-9201, CI, CH3, F， cyclohexylmethyl, F), (M-9202, CI, CHs, F, cyclohexylmethyl, CF3), (M-9203, CI, CHs, F, cyclohexylmethyl, Br), (M-9204, CI, CHs, F, cyclohexylmethyl, CHs), (M-9205, CI, CH3, CI, H， H), (M-9206, CI, CHs, CI, H, CI), (M-9207, CI, CHs, CI, H, F), (M-9208, CI, CH3, CI, H, CFs), (M-9209, CI, CHs, CI, H, Br), (M-9210, CI, CH3; CI, H, CH3), (M-9211, CI, CHs, CI, F, H), (M-9212, CI, CHs, CI, F, CI), (M-9213, CI, CHs, CI, F, F),
(M-9214, CI, CH3, CI, F, CF3)， (M-9215, CI, CHs, CI, F, Br), (M-9216, CI, CHs, CI, F, CHs), (M-9217, CI, CHs, CI, CI, H), (M-9218, CI, CHs, CI, CI, Cl)， (M-9219, CI, CHs, CI, CI, F), (M-9220, CI, CH3; CI, CI, CFs), (M-9221, CI, CH3, CI, CI, Br), (M-9222, CI, CH3, CI, CI, CHs), (M-9223, CI, CHs, CI, CHs, H), (M-9224, CI, CHs, CI, CH3, CI), (M-9225, CI, CH3, CI, CHs, F), (M-9226, CI, CHs, CI, CH3) CFs), (M-9227, CI, CH3) CI, CH3) Br), (M-9228, CI, CH3) CI, CHs, CHs), (M-9229, CI, CHs, CI, Et, H), (M-9230, CI, CHs, CI, Et, CI), (M-9231, CI, CHs, CI, Et, F), (M-9232, CI, CH3, CI, Et, CFs), (M-9233, CI, CHs, CI, Et, Br), (M-9234, CI, CH3, CI, Et, CH3), (M-9235, CI, CHs, CI, n-Pr, H), (M-9236, CI, CH3, CI, n-Pr, CI), (M-9237, CI, CHs, CI, n-Pr, F), (M-9238, CI, CH3, CI, n-Pr, CFs), (M-9239, CI, CHs, CI, n-Pr, Br), (M-9240, CI, CHs, CI, n-Pr, CHs), (M-9241, CI, CHs, CI, c- Pr, H), (M-9242, CI, CH3, CI, c-Pr, CI), (M-9243, CI, CHs, CI, c-Pr, F), (M-9244, CI, CHs, CI, c-Pr, CFs), (M-9245, CI, CHs, CI, c-Pr, Br), (M-9246, CI, CHs, CI, c-Pr, CH3), (M-9247, CI, CHs, CI, i-Pr, H)， (M-9248, CI, CH3) CI, i-Pr, CI), (M- 9249, CI, CH3， CI, i-Pr, F), (M-9250, CI, CHs, CI, i-Pr, CFs), (M-9251, CI, CHs, CI, i-Pr, Br), (M-9252, CI, CHs, CI, i-Pr, CH3), (M-9253, CI, CHs, CI, n-Bu, H), (M-9254, CI, CHs, CI, n-Bu, CI), (M-9255, CI, CHs, CI, n-Bu, F), (M-9256, CI, CHs, CI, n-Bu, CFs), (M-9257, CI, CHs, CI, n-Bu, Br), (M-9258, CI, CH3) CI, n- Bu, CHs), (M-9259, CI, CH3, CI, i-Bu, H), (M-9260, CI, CH3) CI, i-Bu, CI), (M- 9261, CI, CHs, CI, i-Bu, F), (M-9262, CI, CHs, CI, i-Bu, CFs), (M-9263, CI, CH3, CI, i-Bu, Br), (M-9264, CI, CH3, CI, i-Bu, CH3), (M-9265, CI, CHs, CI, sec-Bu, H)， (M-9266, CI, CHs, CI, sec-Bu, CI), (M-9267, CI, CHa, CI, sec-Bu, F), (M-9268, CI, CHs, CI, sec-Bu, CFs), (M-9269, CI, CHs, CI, sec-Bu, Br), (M-9270, CI, CHs, CI, sec-Bu, CHs), (M-9271, CI, CH3， CI, n-Pen, H)， (M-9272, CI, CHs, CI, n-Pen, CI), (M-9273, CI, CHa, CI, n-Pen, F), (M-9274, CI, CH3, CI, n-Pen, CFs), (M-9275, CI, CHa, CI, n-Pen, Br), (M-9276, CI, CHa, CI, n-Pen, CH3), (M-9277, CI, CHs, CI, c-Pen, H), (M-9278, CI, CHa, CI, c-Pen, CI), (M-9279, CI, CH3) CI, c-Pen, F), (M-9280, CI, CHs, CI, c-Pen, CFs), (M-9281, CI, CH3; CI, c-Pen, Br), (M-9282, CI, CHs, CI, c-Pen, CHa), (M-9283, CI, CH3j CI, n-Hex, H), (M-9284, CI, CH3) CI, n-Hex, CI), (M-9285, CI, CH3) CI, n-Hex, F), (M-9286, CI, CH3, CI, n-Hex, CF3), (M-9287, CI, CH3) CI, n-Hex, Br), (M-9288, CI, CHs, CI, n-Hex, CHs), (M-9289, CI, CHs, CI, c-Hex, H), (M-9290, CI, CH3; CI, c-Hex, CI), (M-9291, CI, CHs, CI, c-Hex, F), (M-9292, CI, CHa, CI, c-Hex, CFs), (M-9293, CI, CHs, CI, c-Hex, Br), (M-9294, CI, CHs, CI, c-Hex, CHs), (M-9295, CI, CHs, CI, OH, H), (M-9296, CI, CHs' CI, OH, CI), (M-9297, CI, CHs, CI, OH, F), (M-9298, CI, CHs, CI, OH, CFs), (M-9299, CI, CH3, CI, OH, Br), (M-9300, CI, CH3, CI, OH, CH3), (M-9301, CI, CH3， CI, EtO, H), (M-9302, CI, CH3, CI, EtO, Cl)， (M-9303, CI, CH3) CI, EtO, F), (M-9304, CI, CHs, CI, EtO, CFs), (M-9305, CI, CH3, CI, EtO, Br), (M-9306, CI, CHs, CI, EtO, CHs), (M-9307, CI, CHs, CI, n-PrO, H), (M-9308, CI, CH3, CI, n- PrO, CI), (M-9309, Cl， CH3; CI, n-PrO, F), (M-9310, CI, CHs, CI, n-PrO, CF3), (M-9311, CI, CHs, CI, n-PrO; Br), (M-9312, CI, CH3) CI, n-PrO, CHs), (M-9313, CI, CHs, CI, PhO, H), (M-9314, CI, CHs, CI, PhO, CI), (M-9315, CI, CHs, CI, PhO, F), (M-9316, CI, CHs, Cl' PhO, CFs), (M-9317, CI, CHs, CI, PhO, Br), (M-9318, CI, CHs, Cl, PhO, CHs), (M-9319, Cl, CH3, Cl, BnO, H), (M-9320, Cl, CHs, Cl, BnO, Cl), (M-9321, Cl, CH3) Cl, BnO, F), (M-9322, Cl, CHs, Cl, BnO, CFs), (M-9323, Cl, CH3) Cl, BnO, Br), (M-9324, Cl, CH3, Cl, BnO, CHs), (M-9325, Cl, CH3, Cl, PhCH2CH20; H)， (M^9326, Cl, CHs, Cl, PhCH2CH20; Cl), (M-9327, Cl, CH3; Cl, PhCH2CH20, F), (M-9328, Cl, CH3, Cl, PhCH2CH20; CFs), (M-9329, Cl, CHs, Cl, PhCH2CH20, Br), (M-9330, Cl, CH3; Cl, PhCH2CH20; CHs), (M-9331, Cl, CHs, Cl, CFsO, H), (M-9332, Cl, CH3, Cl, CFsO, Cl), (M-9333, Cl, CH3, Cl, CF30, F), (M-9334, Cl, CH3, Cl, CFsO, CF3), (M-9335, Cl, CHs, Cl, CFsO, Br), (M-9336, Cl, CHs, Cl, CFsO, CHs), (M-9337, Cl, CHs, Cl, Ph, H), (M-9338, Cl, CH3) Cl, Ph, Cl), (M-9339, Cl, CHs, Cl, Ph, F), (M-9340, Cl, CHs, Cl, Ph, CF3), (M-9341, Cl, CHs, Cl, Ph, Br), (M-9342, Cl, CHs, Cl, Ph, CHs), (M-9343, Cl, CHs, Cl, 4-F-Ph, H), (M-9344, Cl, CH3, Cl, 4-F-Pli, Cl), (M-9345, Cl, CHs, Cl, 4-F-Ph, F), (M-9346, Cl, CH3) Cl, 4-F-Ph, CF3), (M-9347, Cl, CH3) Cl, 4-F-Ph, Br), (M- 9348, Cl, CHs, Cl, 4-F-Ph, CHs), (M-9349, Cl, CH3; Cl, 4-CF3-Ph, H), (M-9350, Cl, CH3, Cl, 4-CF3-Ph, Cl), (M-9351, Cl, CHs, Cl, 4-CF3-Ph; F), (M-9352, Cl, CHs, Cl, 4-CF3-PI1, CFs), (M-9353, Cl, CHs, Cl, 4-CF3-Ph, Br), (M-9354, Cl, CH3, Cl, 4-CF3-Ph, CHs), (M-9355, Cl, CHs, Cl, 4-(Me)2N-Ph, H), (M-9356, Cl, CH3, Cl, 4-(Me)2N-Ph, Cl), (M-9357, Cl, CH3, Cl, 4-(Me)2N-Ph， F), (M-9358, Cl, CHs, Cl, 4-(Me)2N-Ph, CFs), (M-9359, Cl, CHs, Cl, 4-(Me)2N-Ph, Br), (M-9360, Cl, CH3, Cl, 4-(Me)2N-Ph) CH3), (M-9361, Cl, CH3, Cl, 4-OH-Ph, H), (M-9362, Cl, CH3， Cl, 4-OH-Ph, CI), (M-9363, CI, CHs, CI, 4-OH-Ph, F), (M-9364, CI, CH3; CI, 4-OH- Ph, CF3), (M-9365, CI, CH3, CI, 4-OH-Ph, Br), (M-9366, CI, CH3, CI, 4-OH-Ph, CHs), (M-9367, CI, CHs, CI, 3,4-di-F-Ph, H), (M-9368, CI, CHs, CI, 3,4-di-F-Ph, CI), (M-9369, CI, CH3) CI, 3,4-di-F-Ph, F), (M-9370, CI, CHs, CI, 3, 4-di-F-Ph, CFs), (M-9371, CI, CHs, CI, 3, 4-di-F-Ph, Br), (M-9372, CI, CH3, CI, 3,4-di-F-Ph, CH3), (M-9373, CI, CHs, CI, 4-COOH-Ph, H)， (M-9374, CI, CHs, CI, 4-COOH-Ph, CI), (M-9375, CI, CHs, CI, 4-COOH-Ph, F), (M-9376, CI, CH3) CI, 4-COOH-Ph, CFs), (M-9377, CI, CHs, CI, 4-COOH-Ph, Br), (M-9378, Cl; CH3, CI, 4-COOH- Ph, CH3)， (M-9379, CI, CHs, CI, Bn, H), (M-9380, CI, CH3, CI, Bn, CI), (M-9381, CI, CHs, CI, Bn, F), (M-9382, CI, CHs, CI, Bn, CFs), (M-9383, CI, CH3; CI, Bn, Br), (M-9384, CI, CHs, CI, Bn, CHs), (M-9385, CI, CHs, CI, 4-F-Bn, H), (M-9386, CI, CH3) CI, 4-F-Bn, CI), (M-9387, CI, CH3, CI, 4-F-Bn, F), (M-9388, CI, CH3) CI, 4-F-Bn, CFs), (M-9389, CI, CHs, CI, 4-F-Bn, Br), (M-9390, CI, CHs, CI, 4-F-Bn, CH3), (M-9391, CI, CHs, CI, 2-Py, H), (M-9392, CI, CHs, CI, 2-Py, CI), (M-9393, CI, CH3> CI, 2-Py, F); (M-9394, CI, CHs, CI, 2-Py, CFs), (M-9395, CI, CH3, CI, 2-Py, Br), (M-9396, CI, CH3, CI, 2-Py, CH3), (M-9397, CI, CH3, CI, 3-Py, H), (M-9398, CI, CHs, CI, 3-Py, CI), (M-9399, CI, CHs, CI, 3-Py, F), (M-9400, CI, CH3; CI, 3-Py, CFs), (M-9401, CI, CH3; CI, 3-Py, Br), (M-9402, CI, CHs, CI, 3- Py, CH3); (M-9403, CI, CH3, CI, 4-Py, H), (M-9404, CI, CH3, CI, 4-Py, CI), (M- 9405, CI, CHs, CI, 4-Py, F), (M-9406, CI, CHs, CI, 4-Py, CFs), (M-9407, CI, CH3) CI, 4-Py, Br), (M-9408, CI, CHs, CI, 4-Py, CHs), (M-9409, CI, CH3, CI, 2-T , H), (M-9410, CI, CH3, CI,- 2-Th, CI), (M-9411, CI, CH3, CI, 2-Th, F), (M-9412, CI, CHs, CI, 2-Th, CFs), (M-9413, CI, CH3, CI, 2-Th, Br), (M-9414, CI, CH3, CI, 2- Th; CHs), (M-9415, Cl; CHs, CI, 3-Th, H), (M-9416, CI, CHs, CI, 3-Th, CI), (M- 9417, CI, CHs, CI, 3-Th, F), (M-9418, CI, CHs, CI, 3-Th, GF3), (M-9419, CI, CHs, CI, 3-Th, Br), (M-9420, CI, CH3; CI, 3-Th, CHs), (M-9421, CI, CHs, CI,
Figure imgf000252_0001
Ο ο
(Me)2NCOCH2CH2CH2CH2, CF3); (M-9467, CI, CH3, CI,
(Me)2NCOCH2CH2CH2CH2, Br), (M-9468, CI, CHs, CI,
(Me)2NCOCH2CH2CH2CH2, CH3), (M-9469, CI, CH3> CI,
(Me)2NCOCH2CH2CH2CH2CH2; H), (M-9470, CI, CH3) CI,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-9471, CI, CHs, CI,
(Me)2NCOCH2CH2CH2CH2CH2) F), (M-9472, CI, CH3; CI,
(Me)2NCOCH2CH2CH2CH2CH2; CF3)， (M-9473, CI, CH3) CI,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-9474, CI, CH3) CI,
(Me)2NCOCH2CH2CH2CH2CH2， CH3), (M-9475, CI, CH3) CI, MeOCH2> H)， (M- 9476, CI, CHs, CI, MeOCH2, CI), (M-9477, CI, CHs, CI, MeOCH2, F), (M-9478, CI, CHs, CI, MeOCH2, CF3), (M-9479, CI, CHs, CI, MeOCHa, Br), (M-9480, CI, CH3, CI, MeOCH2, CHs), (M-9481, CI, CH3, CI, EtOCH2) H), (M-9482, CI, CH3, CI, EtOCHa, CI), (M-9483, CI, CHs, CI, EtOCH2) F), (M-9484, CI, CH3, CI, EtOCH2) CF3), (M-9485, CI, CH3) CI, EtOCH2j Br), (M-9486, CI, CH3; CI, EtOCH2, CHs), (M-9487, CI, CH3, CI, EtOCHaCHa, H), (M-9488, CI, CH3, CI, EtOCH2CH2, CI), (M-9489, CI, CHs, CI, EtOCH2CH2; F), (M-9490, CI, CH3, CI, EtOCH2CH2, CF3), (M-9491, CI, CH3, CI, EtOCH2CH2) Br), (M-9492, CI, CH3, CI, EtOCH2CH2, CHs), (M-9493, CI, CHs, CI, MeOCHsCHsOCBbCHs, H), (M-9494, CI, CH3， CI, MeOCH2CH2OCH2CH2j CI), (M-9495, CI, CHs, CI, MeOCH2CH2OCH2CH2, F), (M-9496, CI, CH3) CI, MeOCH2CH2OCU2CU2, CFs), (M-9497, CI, CH3) CI,
MeOCH2CH2OCH2CH2, Br), (M-9498, CI, CH3， CI, MeOCH2CH2OCH2CH2, CH3), (M-9499, CI, CH3> CI, MeOCH2CH2) H), (M-9500, CI, CH3, CI, MeOCH2CH2) CI), (M-9501, CI, CH3; CI, MeOCH2CH2; F)， (M-9502, CI, CH3; CI, MeOCH2CH2) CFs), (M-9503, CI, CHs, CI, MeOCH2CH2) Br), (M-9504, CI, CHs, CI,
MeOCHaCHa, CHs), (M-9505, CI, CH3) CI, HOCH2; H), (M-9506, CI, CHs, CI, HOCH2, CI), (M-9507, CI, CH3) CI, HOCH2, F), (M-9508, CI, CHs, Cl， HOCH2) CF3); (M-9509, CI, CHs, CI, HOCH2) Br), (M-9510, CI, CH3， CI, HOCH2; CHs), (M-9511, CI, CH3, CI, HOCH2CH2, H), (M-9512, CI, CH3， CI, HOCH2CH2, Gl), (M-9513, CI, CHs, CI, HOCH2CH2) F), (M-9514, CI, CH3; CI, HOCH2CH2; CFs), (M-9515, CI, CH3， CI, HOCH2CH2, Br), (M-9516, CI, CHs, CI, HOCH2CH2) CH3), (M-9517, CI, CH3) CI, HOCH2CH2CH2; H); (M-9518, CI, CH3) CI,
HOCH2CH2CH2; CI), (M-9519, CI, CHs, CI, HOCH2CH2CH2, F), (M-9520, CI, CH3) CI, HOCH2CH2CH2， CFs), (M-9521, CI, CH3) CI, HOCH2CH2CH2) Br), (M-9522, CI, CHs, CI, HOCH2CH2CH2) CH3), (M-9523, CI, CH3) CI,
HOCH2CH2CH2CH2, H), (M-9524, CI, CH3， CI, HOCH2CH2CH2CH2, CI), (M- 9525， CI, CHs, CI, HOCH2CH2CH2CH2) F), (M-9526, CI, CHs, CI,
HOCH2CH2CH2CH2, CFs), (M-9527, CI, CH3, CI, HOCH2CH2CH2CH2, Br), (M- 9528, CI, CH3; CI, HOCE CH2CH2CH2， CHs), (M-9529, CI, CHs, CI,
HOCHaCHsCHsCHaCHa, H), (M-9530, CI, CH3, CI, HOCE CHsCE CK CEb, CI), (M-9531, CI, CHs, CI, HOCH2CH2CH2CH2CH2) F), (M-9532, CI, CH3, CI, HOCHaCHaCHsCHaCHa, CFs), (M-9533, CI, CHs, CI, HOCHaCHsCHaCHaCHs, Br), (M-9534, CI, CHs, CI, HOCH2CH2CH2CH2CH2; CH3)， (M-9535, CI, CH3, CI, HOCH2CH2OCH2CH2) H), (M-9536, CI, CHs, CI, HOCH2CH20CH2CH2; CI), (M-9537, CI, CHs, CI, HOCH2CH2OCH2CH2, F), (M-9538, CI, CHs, CI,
HOCH2CH2OCH2CH2! CF3); (M-9539, CI, CHs, CI, HOCH2CH2OCH2CH2) Br), (M-9540, CI, CHs, CI, HOCH2CH2OCH2CH2, CHs), (M-9541, CI, CHs, CI, (Me)2N, H), (M-9542, CI, CHs, CI, (Me)2N, CI), (M-9543, CI, CHs, CI, (Me)2N, F), (M- 9544， CI, CH3, CI, (Me)2N, CFs), (M-9545, C1, CHs, CI, (Me)2N, Br), (M-9546, CI, CH3, CI, (Me)2N, CHs), (M-9547, CI, CHs, CI, piperidin-4-yl-metliyl, H), (M- 9548, CI, CHs, CI, piperidin-4-yレ： methyl, CI), (M-9549, CI, CHs, CI, piperidin- 4-yl-methyl, F), (M-9550, CI, CHs, CI, piperidin-4-yl-methyl, CFs), (M-9551, CI, CHs, CI, piperidm-4-yl-met yl, Br), (M-9552, CI, CH3, CI, piperidin-4-yl- methyl, CHs), (M-9553, CI, CHs, CI, cyclohexylmethyl, H), (M-9554, CI, CHs, CI, cyclohexylmethyl, CI), (M-9555, CI, CHs, CI, cyclohexylmethyl, F), (M-9556, CI, CHs, CI, cyclohexylmethyl, CFs), (M-9557, CI, CHs, CI, cyclohexylmethyl, Br), (M-9558, CI, CH3) CI, cyclohexylmethyl, CHs), (M-9559, CHs, H, H, H, H), (M-9560, CHs, H, H， H, CI), (M-9561, MeO, H， H, H, F), (M-9562, MeO, H, H, H, CF3), (M-9563, CHs, H, H, H, Br), (M-9564, CHs, H, H， H, CHs), (M-9565, MeO, H, H, F, H), (M-9566, CH3> H, H, F, CI), (M-9567, MeO, F' H, F, F), (M-9568, CH3, H, H, F, CFs), (M-9569, CH3) H, H, F, Br), (M-9570, CH3, H, H, F, CH3), (M-9571, CH3, H, H， CI, H), (M-9572, MeO, F, H， H, i-Pr), (M-9573, CH3, H, H, CI, F), (M-9574, CH3; H, H, CI, CFs), (M-9575, CH8; H, H， CI, Br), (M-9576, CHs, H, CI, CHs), (M-9577, CHs, H, H, CHs, H); (M-9578, CH3; H, H, CH3, CI), (M-9579, CHs, H' H, CHs, F), (M-9580, CHs, H, H, CH3, CFs), (M-9581, CHs, H, H, CH3, Br), (M-9582, CH3, H' H, CH3) CH3), (M-9583, CH3, H， H， Et, H), (M- 9584, CHs, H, H, Et, CI), (M-9585, CHs, H, H; Et, F), (M-9586, CHs, H; H, Et, CFs), (M-9587, CH3, H, H, Et, Br), (M-9588, CHs, H, H, Et, CHs), (M-9589, CHs, H, H, n-Pr, H), (M-9590, CH3, H, H, n-Pr, CI), (M-9591, CHs, H, H, n-Pr, F), (M-9592, CHs, H, H, n-Pr, CF3), (M-9593, CH3， H, H, n-Pr, Br), (M-9594, CHs, H, H, n-Pr, CHs), (M-9595, CHs, H, H, c-Pr, H), (M-9596, CH3, H， H， c-Pr, CI), (M-9597, CHs, H, H, c-Pr, F), (M-9598, CH3, H， H, c-Pr, CFs), (M-9599, CH3) H, H， c-Pr, Br), (M-9600, CH3, H， H, c-Pr, CHs), (M-9601, CH3, H, H, i-Pr, H),
(M-9602, CHs, H, H' i-Pr, CI), (M-9603, CHs, H, H, i-Pr, F), (M-9604, CH3; H， H, i-Pr, CFs), (M-9605, CHs, H, H， i-Pr, Br), (M-9606, CHs, H, H, i-Pr, CH3), (M- 9607, CH3) H, H, n-Bu, H), (M-9608, CH3, H, H, n-Bu, CI), (M-9609, CH3, H, H, n-Bu, F), (M-9610, CHs, H, H, n-Bu, CFs), (M-9611, CHs, H, H, n-Bu, Br), (M- 9612, CHs, H, H, n-Bu, CHs), (M-9613, CH3, H, H, i-Bu, H), (M-9614, CH3, H, H, i-Bu, CI), (M-9615, CHs, H, H, i-Bu, F), (M-9616, CHs, H, H, i-Bu, CFs), (M- 9617, CE.3, H, H, i-Bu, Br), (M-9618, C H, H, i-Bu, CHs), (M-9619, CHs, H, H' sec-Bu, H), (M-9620, CH3; H, H, sec-Bu, CI), (M-9621, CHs, H, H, sec-Bu, F), (M-9622, CHs, H, H, sec-Bu, CFs), (M-9623, CHs, H, H, sec-Bu, Br), (M-9624, CHs, H, H, sec-Bu, CHs), (M-9625, CHs, H' H' n-Pen, H), (M-9626, CHa, H, H, n-Pen, CI), (M-9627, CHs, H, H, n-Pen, F), (M-9628, CHs, H, H, n-Pen, CFs), (M-9629, CHs, H, H, n-Pen, Br), (M-9630, CHs, H, H, n-Pen, CHs), (M-9631, CH3) H, H, c-Pen, H), (M-9632, CH3, H, H, c-Pen, CI), (M-9633, CH3, H， H， c- Pen, F)，（M-9634, CHs, H, H, c-Pen, CF3); (M-9635, CH3' H, H， c-Pen, Br), (M- 9636， CH3, H, H, c-Pen, CHs), (M-9637, CHs, H， H, n-Hex, H), (M-9638, CH3, H, H, n-Hex, CI), (M-9639, CH3> H, H, n-Hex, F)， (M-9640, CHs, H, H， n-Hex, CFs), (M-9641, CHs, H, H, n-Hex, Br), (M-9642, CH3, H, H, n-Hex, CHs), (M-9643, CHs, H, H， c-Hex, H), (M-9644, CH3, H, H, c-Hex, CI), (M-9645, CH3， H, H, c- Hex, F), (M-9646, CH3; H, H, c-Hex, CFs), (M-9647, CHs, H, H, c-Hex, Br), (M-9648, CHs, H, H, c-Hex, CHs), (M-9649, CH3; H, H, OH, H), (M-9650, CHs, H, H, OH, CI), (M-9651, CHs, H, H, OH, F), (M-9652, CHs, H, H, OH, CFs), (M-9653, CH3) H, H， OH, Br), (M-9654, CHs, H， H, OH, CHs), (M-9655, CHs, H, H， EtO, H), (M-9656, CHs, H, H， EtO, CI), (M-9657, CH3, H， H, EtO, F), (M-9658, CHs, H, H， EtO, CFs), (M-9659, CHs, H, H, EtO, Br), (M-9660, CHs, H, H, EtO, CHs), (M-9661, CH3) H, H, n-PrO, H), (M-9662, CHs, H, H, n-PrO, CI), (M-9663, CHs, H, H, n-PrO, F), (M-9664, CHs, H, H, n-PrO; CF3), (M-9665, CHs, H, H, n-PrO, Br), (M-9666, CHs, H， H, n-PrO, CHs), (M-9667, CHs, H, H, PhO, H), (M-9668, CHa, H, H, PhO, CI), (M-9669, CH3, H, H, PhO, F), (M-9670, CHa, H, H, PhO, CFs), (M-9671, CH3, H, H, PhO, Br), (M-9672, CH3, H, H, PhO, CH3), (M-9673, CHs, H, H, BnO, H)， (M-9674, CHs, H, H, BnO, CI), (M-9675, CHs, H, H, BnO, F), (M-9676, CHs, H, H, BnO, CFs), (M-9677, CH3, H， H， BnO, Br), (M-9678, CHs, H, H, BnO, CHs), (M-9679, CH3, H, H, PhCH2CH20, H), (M-9680, CH3, H, H, PliCHsCHaO, CI), (M-9681, CHs, H, H, PhCH2CH20, F), (M-9682, CHs, H, H, PhCHaCHsO, CFs), (M-9683, CH3) H, H, PI1CH2CH2O, Br), (M-9684, CH3， H, H， PI1GH2CH2O, CH3), (M-9685, MeO, H， H, CFsO, H), (M-9686, CH3) H, H， CFsO, CI), (M-9687, CHs, H, H, CFsO, F), (M-9688, CHa, H, H, CFsO, CFs), (M-9689, CHa, H, H, CFsO, Br), (M-9690, CH3, H, H, CF30, CHs), (M-9691, CH3, H, H, Ph, H), (M-9692, CHs, H, H, Ph, CI), (M-9693, CHs, H, H, Ph, F)， (M-9694, CHs, H, H, Ph, CFs), (M-9695, CHs, H, H, Ph; Br), (M-9696, CHs, H, H, Ph, CHs), (M- 9697, CH3; H, H, 4-F-Ph, H), (M-9698, CH3, H, H, 4-F-Ph, CI), (M-9699, CH3， H, H, 4-F-Ph, F); (M-9700, CH3> H, H, 4-F-Ph, CF3), (M-9701, CH3; H, H, 4-F-Ph, Br), (M-9702, CHs, H, H, 4-F-Ph, CHs), (M-9703, CH3) H, H; 4-CF3-Ph, H),
(M-9704, CHs, H, H, 4-CFa-Pli, CI), (M-9705, CH3, H, H, 4-CF3-Ph, F), (M-9706, CH3, H, H, 4-CFs-Pli, CFs), (M-9707, CHs, H, H, 4-CF3-Ph, Br), (M-9708, CHs, H, H, 4-CF3-Ph, CHa), (M-9709, CHa, H, H, 4-(Me)2N-Ph, H), (M-9710, CH3, H, H, 4-(Me)2N-Ph, CI), (M-9711, CH3, H, H, 4-(Me)2N-Ph, F), (M-9712, CH3) H, H, 4-(Me)2N-Ph; CFs), (M-9713, CHs, H, H， 4-(Me)2N-Ph, Br), (M-9714, CHs, H， H, 4-(Me)2N-Ph, CH3), (M-9715, CH3， H, H, 4-OH-Ph, H), (M-9716, CHs, H, H, 4- OH-Pli, CI), (M-9717, CHs, H, H, 4-OH-Ph, F), (M-9718, CHs, H, H, 4-OH-Ph, CFs), (M-9719, CHs, H, H, 4-OH-Ph, Br), (M-9720, CHs, H, H, 4-OH-Ph, CHs), (M-9721, CHs, H, H, 3,4-di-F-Ph, H), (M-9722, CHs, H, H, 3,4-di-F-Ph, CI), (M-9723, CHs, H, H, 3,4-di-F-Ph, F), (M-9724, CH3) H, H, 3'4-di-F-Ph, CFs), (M-9725, CHs, H, H, 3,4-di-F-Ph, Br), (M-9726, CHs, H, H, 3,4-di-F-Ph, CHa), (M'9727, CHs, H, H, 4-COOH-Ph, H), (M-9728, CHa, H, H, 4-COOH-Ph, CI), (M-9729, CHs, H, H, 4-COOH-Ph, F), (M-9730, CHs, H, H, 4-COOH-Ph, CFs), (M-9731, CHs, H, H, 4-COOH-Ph, Br), (M-9732, CHs, H, H, 4-COOH-Ph, CHs), (M-9733, CHs, H, H, Bn, H), (M-9734, CHs, H, H, Bn, CI), (M-9735, CH3, H, H, Bn, F), (M-9736, CHs, H, H, Bn, CFs), (M-9737, CH3, H， H, Bn, Br), (M-9738, CH3, H, H, Bn, CHs), (M-9739, CHs, H, H, 4-F-Bn, H)， (M-9740, CH3; H, H' 4- F-Bn, CI), (M-9741, CHs, H, H, 4-F-Bn, F), (M-9742, CHs, H, H, 4-F-Bn, CPs), (M-9743, CHs, H, H, 4-F-Bn, Br), (M-9744, CHs, H, H, 4-F-Bn, CHs), (M-9745, CHs, H, H, 2-Py, H), (M-9746, CH3, H， H, 2-Py, CI), (M-9747, CHs, H, H, 2-Py, F), (M-9748, CHs, H, H, 2-Py, CFs), (M-9749, CH3) H, H, 2-Py, Br), (M-9750, CH3) H, H; 2-Py, CH3); (M-9751, CHs, H, H, 3-Py, H), (M-9752, CHs, H, H, 3- Py, CI), (M-9753, CHs, H, H, 3-Py, F), (M-9754, CHs, H, H， 3-Py, CFs), (M-9755, CHa, H, H, 3-Py, Br), (M-9756, CH3) H, H, 3-Py, CHs), (M-9757, CHs, H, H, 4- Py, H), (M-9758, CHs, H, H, 4-Py, CI), (M-9759, CH3, H, H; 4-Py, F)， (M-9760, CHa, H， H, 4-Py, CFs), (M-9761, CHs, H' H, 4-Py, Br), (M-9762, CH8) H, H, 4- Py, CHs), (M-9763, CHs, H， H, 2-Th, H), (M-9764, CH3, H， H, 2-Th, Cl)， (M-9765, CHs, H， H, 2-Th, F), (M-9766, CHs, H， H, 2-Th, CFs), (M-9767, CHs, H, H, 2-Th, Br), (M-9768, CH3) H, H, 2-Th, CHs), (M-9769, CH3, H, H, 3-Th, H), (M-9770, CHs, H, H, 3-Th, CI), (M-9771, CH3) H, H, 3-Th, F), (M-9772, CH3> H, H, 3-Th, CFs), (M-9773, CH3; H, H, 3-Th, Br), (M-9774, CH3, H, H, 3-Th, CH3); (M-9775, CHs, H, H, pyrazol-2-yl, H), (M-9776, CHs, H, H, pyrazol-2-yl, CI), (M-9777, CHs, H, H, pyrazol-2-yl, F), (M-9778, CHs, H, H, pyrazol-2-yl, CFs), (M-9779, CHs, H, H， pyrazoレ 2-yl, Br), (M-9780, CH3, H, H, pyrazol-2-yl, CHs), (M-9781, CHs, H, H, pyrazol-3-yl, H), (M-9782, CHs, H, H, pyrazol-3-yl, CI), (M-9783, CHs, H, H, pyrazoレ 3-yl' F), (M-9784, CHs, H, H, pyrazoレ 3-yl, CFs), (M-9785, CHs, H, H, pyrazol-3-yl, Br), (M-9786, CH3, H, H, pyrazol-3-yl, CHs), (M-9787, CHs, H, H, pyrimidin-2-yl, H), (M-9788, CHs, H, H, pyrimidin-2-yl, CI), (M- 9789, CH3, H, H, pyrimidin-2-yl, F), (M-9790, CH3; H, H, pyrimidin-2-yl; CFs), (M-9791, CH3> H, H, pyrimidin-2-yl, Br), (M-9792, CH3, H, H, pyrimidin-2-yl, CHs), (M-9793, CHs, H, H, pyrimidin-4-yl, H), (M-9794, CHs, H; H;
pyrimidin-4-yl, CI), (M-9795, CH3; H, H, pyrimidin-4-yl, F); (M-9796, CHs, H, H, pyrimidin-4-yl, CFs), (M-9797, CHa, H, H, pyrimidin-4-yl, Br), (M-9798, CHs, H, H, pyrimidin-4-yl, CHa), (M-9799, CHs, H， H, pyrimidm-5-yl, H)' (M-9800, CH3, H, H, pyrimidin-5-yl, CI), (M-9801, CH3, H, H, pyrimidin-5-yl, F), (M- 9802, C H, H, pyrimidin-5-yl, CF3), (M-9803, CH3) H, H, pyrimidin-5-yl, Br), (M-9804, CH3; H, H, pyrimidin-5-yl; CHs), (M-9805, CH3， H, H,
HOOCCH2CH2CH2, H), (M-9806, CH3, H, H， HOOCCH2CH2CH2， CI), (M-9807, CH3， H, H, HOOCCH2CH2CH2, F), (M-9808, CH3, H, H, HOOCCH2CH2CH2, CFs), (M-9809, CHs, H, H, HOOCCH2CH2CH2) Br), (M-9810, CH3; H, H, HOOCCH2CH2CH2, CHs), (M-9811, CHs, H, H, HOOCCH2CH2CH2CH2; H), (M-9812, CHs, H, H, HOOCCH2CH2CH2CH2, CI), (M-9813, CHs, H, H，
HOOCCH2CH2CH2CH2; F), (M-9814, CH3, H, H， HOOCCH2CH2CH2CH2, CFs), (M-9815, CHs, H， H, HOOCCH2CH2CH2CH2, Br), (M-9816, CH3, H, H,
HOOCCH2CH2CH2CH2, CHs), (M-9817, CH3, H, H, (Me)2NCOCH2CH2CH2CH2, H)， (M-9818, CHs, H, H, (Me)2NC0CH2CH2CH2CH2, CI), (M-9819, CHs, H, H, (Me)2NCOCH2CH2CH2CH2， F), (M-9820, CHs, H, H, (Me)2NCOGH2CH2CH2CH2, CF3), (M-9821, CH3， H, H, (Me)2NCOCH2CH2CH2CH2, Br), (M-9822, CH3， H, H, (Me)2NC0CH2CH2CH2CH2; CHs), (M-9823, CHs, H, H,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-9824, CH3, H, H,
(Me)2NC0CH2CH2CH2CH2CH2, CI), (M-9825, CHs, H, H,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-9826, CHs, H, H,
(Me)2NCOCH2CH2CH2CH2CH2, CF3), (M-9827, CH3, H, H,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-9828, CH3, H, H,
(Me)2NC0CH2CH2CH2CH2CH2) CHs), (M-9829, CH3, H, H, MeOCH2> H), (M- 9830, CHs, H, H, MeOCB , CI), (M-9831, CHs, H, H, MeOC F)， (M-9832, CHs, H, H, MeOCH , CF3), (M-9833, CHa, H, H, MeOCHa, Br), (M-9834, CHs, H, H， MeOCH2; CHs), (M-9835, CHs, H, H, EtOCH2, H), (M-9836, CH3; H, H, EtOCH2, CI), (M-9837, CH3, H, H, EtOCH2, F), (M-9838, CH3, H, H, EtOCHa, CF3), (M- 9839, CH3, H, H, EtOCH2, Br), (M-9840, CH3, H' H, EtOCHs, CHs), (M-9841, CHs, H, H, EtOCH2CH2, H)， (M-9842, CHs, H, H, EtOCH2CH2) CI), (M-9843, CHs, H， H, EtOCHaCHa, F), (M-9844, CHs, H, H， EtOCH2CH2) CFs), (M-9845, CH3, H, H, EtOCH2CH2; Br), (M-9846, CH3) H, H, EtOCH2CH2) CH3), (M-9847, CH3, H, H, MeOCH2CH2OCH2CH2, H), (M-9848, CH3, H, H,
MeOCH2CH20CH2CH2, CI), (M-9849, CH3) H, H, MeOCH2CH2OCH2CH2, F), (M-9850, CH3， H, H, MeOCH2CH2OCH2CH2, CFs), (M-9851, CHs, H, H, MeOCH2CH2OGH2CH2， Br), (M-9852, CH3, H, H, MeOCH2CH2OCH2CH2, CH3)， (M-9853, CHs, H, H, MeOCH2CH2> H), (M-9854, CHs, H, H, MeOCH2CH2, CI), (M-9855, CH3, H, H, MeOCH2CH2, F), (M-9856, CH3) H, H, MeOCH2CH2, CFs), (M-9857, CHs, H, H, MeOCH2CH2; Br), (M-9858, CH3, H, H, MeOCH2CH2, CH3), (M-9859, CHs, H, H; HOCH2, H), (M-9860, CHs, H, H, HOCH2> CI), (M-9861, CH3, H, H, HOCH2, F), (M-9862, CHs, H, H, HOCH2, CFs), (M-9863, CHs, H, H, HOCH2, Br), (M-9864, CHs, H， H, HOCH2) CH3), (M-9865, CHs, H, H,
HOCH2CH2; H), (M-9866, CHs, H， H, HOCH2CH2, CI), (M-9867, CH3, H, H， HOCH2CH2, F), (M-9868, CH3, H, H, HOCH2CH2, CFs), (M-9869, CHs, H, H, HOCH2CH2, Br), (M-9870, CHs, H, H, HOCH2CH2) CHs), (M-9871, CH3) H, H, HOCH2CH2CH2, H)， (M-9872, CH3, H, H, HOCH2CH2CH2, CI), (M-9873, CH3; H, H, HOCH2CH2CH2, F), (M-9874, CHs, H, H, HOCH2CH2CH2, CFs), (M-9875, . CH3) H, H， HOCH2CH2CH2, Br), (M-9876, CH3, H, H, HOCH2CH2CH2, CH3), (M-9877, CHs, H, H, HOCH2CH2CH2CH2， H), (M-9878, CHs, H, H,
HOCH2CH2CH2CH2, CI), (M-9879, CHs, H, H, HOCH2CH2CH2CH2, F), (M-9880, CH3, H, H, HOCH2CH2CH2CH2, CFs), (M-9881, CH3, H, H, HOCH2CH2CH2CH2, Br), (M-9882, CHs, H, H, HOCH2CH2CH2CH2, CHs), (M-9883, CH3, H, H,
HOCH2CH2CH2CH2CH2, H), (M-9884, CHs, H, H, HOCH CHsCHsCHsCHb, CI), (M-9885, CH3， H, H, HO CH2CH2CH2CH2CH2, F), (M-9886, CH3, H, H，
HO CH2CH2CH2CH2CH2, CF3), (M-9887, CH3, H, H, HO CH2CH2CH2CH2CH2, Br), (M-9888, CHs, H, H， HOCH2CH2CH2CH2CH2, CHs), (M-9889, CHs, H, H, HOCH2CH20CH2CH2, H), (M-9890, CHs, H, H; HOCH2CH2OCH2CH2, CI), (M- 9891, CH3, H, H, HOCH2CH2OCH2CH2, F), (M-9892, CH3, H, H,
HOCH2CH2OCH2CH2, CFs), (M-9893, CHs, H, H, HOCH2CH2OCH2CH2, Br), (M-9894, CH3, H, H, HOCH2CH2OCH2CH2, CH3), (M-9895, CHs, H' H, (Me)2N, H), (M-9896, CH3， H, H, (Me)2N, CI), (M-9897, CHs, H' H, (Me)2N, F)， (M-9898, CH3, H, H, (Me)2N, CF3), (M-9899, CH3, H, H, (Me)2N, Br), (M-9900, CHs, H， H， (Me)2N, CHs), (M-9901, CH3, H, H, piperidin-4-yレ methyl, H), (M-9902, CH3, H, H, piperidin-4-yl-metliyl, CI), (M-9903, CHs, H, H, piperidm-4-yl-methyl, F), (M-9904, CHs, H, H, piperidin-4-yレ methyl, CF3), (M-9905, CH3> H, H;
piperidin-4-yレ methyl' Br), (M-9906, CHs, H, H, piperidin-4-yl-metliyl, CHs), (M-9907, CHs, H, H, cyclohexylmethyl, H), (M-9908, CH3, H, H,
cyclohexylmethyl, CI), (M-9909, CH3, H, H， cyclohexylmetliyl, F), (M-9910,
CHs, H, H, cyclohexylmethyl, CFs), (M-9911, CHs, H, H, cyclohexylmethyl, Br), (M-9912, CHs, H, H, cyclohexylmethyl, CHs), (M-9913, CHs, H, F, H, H), (M- 9914, CHs, H， F, H, CI), (M-9915, CHs, H, F, H, F)， (M-9916, CH3， H, F, H， CF3), (M-9917, CH3, H, F, H， Br), (M-9918, CHs, H, F， H, CH3), (M-9919, CH3) H， F, P, H), (M-9920, CHs, H, F, F, CI), (M-9921, CH3) H, F, F, F), (M-9922, CH3> H; F, F, CFs), (M-9923, CHs, H， F, F， Br), (M-9924, CH3 ) H, F， F, CHs), (M-9925, CHs, H, F, CI, H), (M-9926, CHs, H, F, CI, CI), .(M-9927, CHs, H' F, CI, F), (M-9928, CHs, H, F, CI, CFs), (M-9929, CH3, H, JF, CI, Br), (M-9930, CHs, H, P, CI, CH3), (M-9931, CH3) H, F, CHs, H), (M-9932, CHs, H, P, CHs, CI), (M-9933, CHs, H, F, CHs, F), (M-9934, CHs, H, F, CHs, CFs), (M-9935, CH3) H, P; CHs, Br), (M-9936, CHs, H， F， CHs, CHs), (M-9937, CHs, H, F， Et, H), (M-9938, CHs, H, F, Et, CI), (M-9939, CHs, H, F, Et, F), (M-9940, CHs, H， F, Et, CFs), (M-9941, CH3' H, F, Et, Br), (M-9942, CHs, H, F, Et, CH3), (M-9943, CHs, H, F, n-Pr, H), (M-9944, CH3, H, F' n-Pr, CI), (M-9945, CHs, H; F, n-Pr, F), (M-9946, CH3) H, F, n-Pr, CPs), (M-9947, CHs, H, F, n-Pr, Br), (M-9948, CH3, H, F, n-Pr, CHs), (M-9949, CHs, H， F, c-Pr, H)， (M-9950, CHs, H, F, c-Pr, CI), (M-9951, CHs, H, F, c-Pr, F), (M-9952, CHs, H, F, c-Pr, CFs), (M-9953, CHs, H, F, c-Pr, Br), (M-9954, CH3; H, F, c-Pr, CH3), (M-9955, CHs, H, F, i-Pr, H), (M-9956, CHs, H, F, i-Pr, CI), (M-9957, CHs, H, F, i-Pr, F)， (M-9958, CH3, H, F, i-Pr, CF3)， (M-9959, CHs, H, F, i-Pr, Br), (M-9960, CHs, H, F， i-Pr, CHs), (M-9961, CH3; H, F, n-Bu, H), (M-9962, CH3, H, F, n-Bu, CI), (M-9963, CH3; H, F, n-Bu, F), (M-9964, CH3, H, F， n-Bu, CFs),
(M-9965, CHs, H, F, n-Bu, Br), (M-9966, CH3, H, F, n-Bu, CHs), (M-9967, CHs, H, F, i-Bu; H), (M-9968, CH3, H, F, i-Bu, CI), (M-9969, CHs, H; F, i-Bu, F)， (M-9970, CHs, H, F, i-Bu, CF3), (M-9971, CHs, H, F, i-Bu; Br), (M-9972, CHs, H, F, i-Bu, CHs), (M-9973, CHs, H, F, sec-Bu, H), (M-9974, CHs, H' F, sec-Bu, CI), (M-9975, CHs, H, F, sec-Bu, F), (M-9976, CHs, H, F, sec-Bu, CFs), (M-9977, CHs, H, F, sec-Bu, Br), (M-9978, CH3, H, F, sec-Bu, CH3), (M-9979, CHs, H, F, n-Pen, H), (M-9980, CHs, H, F， n-Pen, CI), (M-9981, CH3) H, F, n-Pen, F), (M-9982, CHs, H, F, n-Pen, CF3), (M-9983, CH3) H, F, n-Pen, Br), (M-9984, CH3, H, F, n-Pen, CHs), (M-9985, CHs, H, F, c-Pen, H)， (M-9986, CH3, H， F; c-Pen, CI), (M-9987, CHs, H, F, c-Pen, F)，（M-9988, CH3, H, F; c-Pen, CFs), (M-9989, CH3; H, F, c-Pen, Br), (M-9990, CH3) H, F， c-Pen, CHs), (M-9991, CHs, H, F, n-Hex, H); (M-99.92, CHs, H, F, n-Hex, CI), (M-9993, CHs, H, F, n-Hex, F), (M-9994, CH3> H, F， n-.Hex, CPs), (M-9995, CH3) H, F， n-Hex, Br), (M-9996, CH3) H, F, n-Hex; CHs), (M-9997, CHs, H, F, c-Hex, H), (M-9998, CHs, H, F, c-Hex, CI), (M-9999, CHs, H, F, c-Hex, F), (M-10000, CHs, H, F, c-Hex, CFs), (M-10001, CHs, H, F, c-Hex, Br), (M-10002, CHs, H, F, c-Hex, CHs), (M-10003, CHs, H, F, OH, H), (M-10004, CH3, H, F; OH, CI), (M-10005, CHs, H, F, OH, F); (M-10006, CHs, H' F, OH, CFs), (M-10007, CH3, H, F, OH, Br), (M-10008, CHs, H, F, OH, CHs), (M-10009, CHs, H, F, EtO, H), (M-10010, CHs, H， F, EtO, CI), (M-10011, CH3， H' F, EtO, F), (M-10012, CHs, H, F, EtO, CF3), (M-10013, CHs, H, F EtO, Br), (M-10014, CHs, H, F, EtO, CHs), (M-10015, CHs, H, F， n-PrO, H), (M-10016, CHs, H, F, n-PrO, CI), (M-10017, CHs, H, F, n-PrO, F), (M-10018, CH3, H, F' n-PrO, CPs), (M-10019, CHs, H, F, n-PrO, Br), (M-10020, CHs, H， F， n-PrO, CHs), (M-10021, CHs, H, F, PhO, H), (M-10022, CHs, H, F, PhO, CI), (M-10023, CH3) H， F, PhO, F), (M-10024, CHs, H, F, PhO, CFs), (M-10025, CH3) H, F, PhO, Br), (M-10026, CH3, H, F, PhO, CHs), (M- 10027, CH3, H， F, BnO, H), (M-10028, CHs, H, F, BnO, CI), (M-10029, CH3， H, F, BnO, F), (M-10030, CHs, H, F, BnO, CFs), (M-10031, CHs, H, F, BnO, Br), (M-10032, CH3, H, F, BnO, CH3), (M- 10033, CH3) H, F, PhCH2CH20, H), (M-10034, CHs, H, F, PI1CH2CH2O, CI), (M-10035, CHs, H, F, PhCH2CH20; F), (M-10036, CH3， H, F, PhCH2CH20; CFs), (M-10037, CHs, H, F, PhCHsCB O, Br), (M- 10038, CHs, H, F, PhCH2CH20， CHs), (M-10039, CHs, H, F, CF30, H), (M-10040, CH3; H, F, CF3O, CI), (M- 10041, CH3, H, F, CFsO, F), (M- 10042, CH3, H' F, CF30, CFs), (M-10043, CHs, H, F, CFsO, Br), (M-10044, CHs, H, F, CF30, CHs), (M-10045, CHs, H, F, Ph, H), (M-10046, CHs, H, F, Ph, CI), (M-10047, CH3; H， F, Ph, F), (M-10048, CHs, H, F， Ph, CPs), (M-10049, CH3> H, F, Ph, Br), (M-10050, CHs, H, F, Ph, CHs), (M- 10051, CH3) H， F, 4-F-Ph, H), (M-10052, CHs, H, F, 4-F-P , CI), (M-10053, CH3) H, F, 4-F-Ph, F), (M-10054, CH3, U, F， 4-F-Ph, CFs), (M-10055, CHs, H, F, 4- F-Ph, Br), (M-10056, CH3) H, F， 4-F-Ph, CH3), (M-10057, CH3) H; F, 4-CFs-Pli, H), (M-10058, CHs, H; F, 4-CFs-Ph, CI), (M-10059, CHs, H, F, 4-CFs-Ph, F), (M-10060, CHs, H, F, 4-CF3-Ph, CF3), (M-10061, CHs, H, F, 4-CF3-Ph, Br),
(M-10062, CHs, H, F, 4-CFs-Ph, CHs), (M-10063, CH3, H, F, 4-(Me)2N-P , H), (M-10064, CHs, H， F, 4-(Me)2N-Ph, CI), (M-10065, CHs, H, F, 4-(Me)2N-Ph, F)， (M-10066, CH3; H, F, 4-(Me)2N-Pli) CF3), (M-10067, CH3， H, F, 4-(Me)2N-Ph; Br), (M-10068, CHs, H, F, 4-(Me)2N-Pli> CHs), (M-10069, CH3) H' F, 4-OH-Ph, H), (M-10070, CH3, H, F, 4-OH-Ph, CI), (M-10071, C H, F, 4-OH-Ph, F), (M-10072, CHs, H, F, 4-OH-Ph, CFs), (M-10073, CH3> H， F, 4-OH-Ph, Br), (M- 10074, CHs, H, F, 4-OH-Ph, CHs), (M-10075, CHs, H, F, 3,4-di-P-Pli, H), (M- 10076, CHs, H, F, 3,4-di-F-Ph, CI), (M-10077, CHs, H, F, 3,4-di-F-Ph, F), (M- 10078， CHs, H, F, 3,4-di-F-Ph; CFs), (M-10079, CHs, H, F, 3,4-di-F-Ph, Br), (M-10080, CHs, H, F, 3,4-di-F-Ph, CHs), (M-10081, CHs, H, F, 4-COOH-Ph, H), (M-10082, CHs, H, F, 4-COOH-Ph, CI), (M-10083, CHs, H, F, 4-COOH-Ph, F), (M-10084, CHs, H, F, 4-COOH-Ph, CFs), (M-10085, CH3, H, F, 4-COOH-Ph, Br), (M-10086, CH3, H， F, 4-COOH-Ph, CH3)，（M-10087, CH3; H, F， Bn, H), (M- 10088, CHs, H, F, Bn, CI), (M-10089, CHs, H, F, Bn, F), (M-10090, CHs, H, F, Bn, CFs), (M-10091, CHs, H, F, Bn, Br), (M-10092, CHs, H， F, Bn, CHs), (M-10093, CHs, H, F, 4-P-Bn, H), (M- 10094, CHs, H; F, 4-F-Bn, CI), (M-10096, CHs, H, F, 4-F-Bn, F), (M-10096, GHs, H， F, 4-F-Bn, CFs), (M-10097, CHs, H, F, 4-F-Bn, Br), (M-10098, CHs, H, F, 4-F-Bn, CHs), (M-10099, CH3) H, F, 2-Py; H), (M- 10100， CHs, H, F, 2-Py, CI), (M-10101, CHs, H, F, 2-Py, F), (M-10102, CH3, H, F, 2-Py, CFs), (M-10103, CHs, H, F, 2-Py, Br), (M-10104, CHs, H, F, 2-Py, CH3), (M-10105, CHs, H, F， 3-Py, H), (M-10106, CHs, H, F, 3-Py, CI), (M-10107, CHs, H, F, 3-Py, F), (M-10108, CHs, H' F, 3-Py, CFs), (M-10109, CHs, H, F, 3-Py, Br), (M-.lOllO, CHs, H, F, 3-Py, CHs), (M-10111, CH3, H, F， 4-Py, H), (M-10112, CH3) H， F, 4-Py, CI), (M-10113, CHs, H, F, 4-Py, F), (M-10114, CH3) H, F, 4-Py, CFa), (M-10115, CHs, H, F, 4-Py, Br), (M-10116, CH3， H, F, 4-Py, CH3), (M-10117, CHs, H, F, 2-Th, H), (M-10118, CHs, H, F, 2-Th, CI), (M-10119, CHs, H, F, 2-Th, F), (M-10120, CHs, H, F, 2-Th, CF3), (M-10121, CHs, H, F， 2-Th, Br), (M-10122, o o
Figure imgf000265_0001
y y (y y) (,,, p,¾,,33 Co3l CFM 01H H Fazll FM 012 C Hr F---- y yy (,y ( p,,,,,3 Caos CM 0H uzl ffi HraolI1 FrlM CH Fzl----- ),„,),,,,,33 0 Cs 3 CH 019 017 CH K ¾ Ίι B18H FΊΊι2r- ,:)，,,¾,s 3Tii CI C T 01 C FH ¾ F26 H- ,,,.3s Q1HΪ K 04 CJH ffi ¾ Ϊ (M-10170, CH3, H, F, HOOCCH2CH2CH2CH2, CH3), (M-10171, CH3, H, F, (Me)2NCOCH2CH2CH2CH2, H), (M- 10172, CH3, H, F,
(Me)2NCOCH2CH2CH2CH2; CI), (M-10173, CH3) H, F,
(Me)2NCOCH2CH2CH2CH2, F), (M-10174, CHs, H, F,
(Me)2NCOCH2CH2CH2CH2, CFs), (M-10175, CHs, H, F,
(Me)2NCOCH2CH2CH2CH2, Br), (M-10176, CHs, H, F,
(Me)2NCOCH2CH2CH2CH2) CH3), (M-10177, CH3, H, F,
(Me)2NCOCH2CH2CH2CH2CH2) H), (M-10178, CH3, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-10179, CHs, H, F,
(Me)2NCOCH2CH2CH2CH2CH2j F), (M-10180, CHs, H, F,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-10181, CH3, H, F,
(Me)2NCOCH2CH2CH2CH2CH2) Br), (M-10182, CHs, H F,
(Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-10183, CH3> H, F, MeOCH2, H), (M- 10184, CHs, H, F, MeOCH2) CI), (M-10185, CHs, H, F, MeOCHs, F), (M-10186, CH3, H, F, MeOCH2, CF3), (M-10187, CHs, H, F, MeOCH2, Br), (M-10188, CH3, H, F, MeOCH2) CHs), (M-10189, CHs, H, F, EtOCH2, H), (M-10190, CHs, H, F, EtOCHa, CI), (M-10191, CHs, H F, EtOCH2; F), (M-10192, CH3, H, F, EtOCH2, CF3), (M-10193, CHs, H, F, EtOCHa, Br), (M-10194, CHs, H, F EtOCH2) CHs), (M-10195, CHs, H, F, EtOCH2CH2, H), (M-10196, CHs, H, F, EtOCH2CH2, CI), (M-10197, CHs, H F, EtOCH2CH2) F), (M-10198, CH3) H, F, EtOCH2CH2; CF3), (M-10199, CHs, H, F, EtOCH2CH2) Br), (M-10200, CH3; H, F, EtOCHsCHs, CHs), (M-10201, CHa, H F, MeOCH2CH2OCH2CH2, H), (M-10202, CH3> H, F,
MeOCH2CH2OCH2CH2; CI), (M-10203, CH3, H, F, MeOCH2CH2OCH2CH2, F), (M-10204, CHs, H, F, MeOCH2CH2OCH2CH2, CF3), (M-10205, CH3, H, F, MeOCH2CH2OCH2CH2, Br), (M-10206, CHs, H, F, MeOCH CHsOCHsCHs, CHs), (M-10207, CHs, H, F, MeOCH2CH2; H), (M-10208, CHs, H, F, MeOCH2CH2) CI), (M-10209, CHs, H' F, MeOCHaCHa, F), (M-10210, CHs, H, F, MeOCH2CH2) CPs), (M-10211, CH3, H, F, MeOCH2CH2j Br), (M-10212, CH3, H, F, MeOCH2CH2) CH3), (M-10213, CH3) H, F, HOCH2) H), (M-10214, CH3, H, F, HOCH2, CI), (M-10215, CHs, H, F, HOCH2, F), (M-10216, CH3; H, F, HOCH2, CF3), (M-10217, CH3, H, F， HOCH2, Br), (M-10218, CHs, H, F, HOCH2, CHs), (M-10219, CHs, H, P, HOCH2C¾ H), (M-10220, CH3, H, F, HOCHaCHs, CI), (M-10221, CHs, H， F, HOCH2CH2, F), (M-10222, CH3, H, F, HOCH2CH2) CF3), (M-10223, CH3, H, F, HOCH2CH2, Br), (M-10224, CHs, H, F, HOCH2CH2, CHs), (M-10225, CHs, H, F， HOCH2CH2CH2， H), (M-10226, CHs, H, F, HOCH2CH2CH2, CI), (M-10227, CHs, H， F, HOCH2CH2CH2, F), (M-10228, CH3) H, F, HOCHaCHaCHs, CFs), (M-
10229, CH3, H, F, HOCH2CH2CH2, Br), (M-10230, CHs, H, F, HOCH2CH2CH2, CHs), (M-10231, CHs, H, F, HOCH2CH2CH2CH2, H), (M-10232, CHs, H, F, HOCH2CH2CH2CH2, CI), (M-10233, CHs, H, F, HOCH2CH2CH2CH2, P), (M- 10234， CHs, H, F， HOCH2CH2CH2CH2; CF3), (M-10235, CHs, H, F,
HOCH2CH2CH2CH2, Br), (M-10236, CHs, H, F, HOCH2CH2CH2CH2， CHs), (M- 10237, CHs; H, F, HOCH2CH2CH2CH2CH2) H), (M-10238, CH3) H; F,
HOCH2CH2CH2CH2CH2> CI), (M-10239, CHs, H, P, HOCH2CH2CH2CH2CH2, F), (M-10240, CH3; H, F, HOCH2CH2CH2CH2CH2, CFs), (M-10241, CH3, H, F， HOCH2CH2CH2CH2CH2, Br), (M-10242, CH3， H, F, HOCH2CH2CH2CH2CH2, CHs), (M-10243, CHs, H， F， HOCH2CH2OCH2CH2, H), (M-10244, CH3; H, F, HOCH2CH2OCH2CH2, CI), (M-10245, CHs, H, F, HOCH2CH2OCH2CH2, F)， (M-10246, CHs, H, F,; HOCH2CH2OCH2CH2, CF3), (M-10247, CH3, H, F， HOCH2CH2QCH2CH2, Br), (M-10248, CH3, H, F, HOCH2CH2OCH2CH2， CHs), (M-10249, CHs, H, F, (Me)2N, H), (M-10250, CH3, H, F, (Me)2N, CI), (M-10251, CHs, H, F, (Me)2N, F), (M-10252, CH3, H, F, (Me)2N, CF3), (M-10253, CHs, H, F, (Me)2N, Br), (M-10254, CH3, H, F, (Me)2N, CHs), (M-10255, CHs, H, F, piperidm-4-yl-methyl, H), (M-10256, CHs, H, F, piperidin-4-yl-methyl, CI), (M-10257, CHs, H' F, piperidin-4-yl-methyl, F), (M-10258, CH3, H, F, piperidm-4-yl-met yl, CFs), (M-10259, CH3, H, F, piperidin-4-yレ methyl, Br), (M-10260, CHs, H, F, piperidm-4-yl-methyl, CH3), (M-10261, CHs, H, F, cyclohexylmethyl, H), (M-10262, CHs, H, F, cyclohexylmethyl, CI), (M-10263, CHs, H, F, cyclohexylmethyl, F), (M-10264, CHs, H, F, cyclohexylmethyl, CFs), (M-10265, CHs, H, F, cyclohexylmethyl, Br), (M-10266, CH3; H, F，
cyclohexylmethyl, CHs), (M-10267, CH3) H' CI, H, H), (M-10268, CHs, H， CI, H, CI), (M-10269, CHs, H， CI, H, F), (M-10270, CHs, H, CI, H, CFs), (M-10271, CHs, H, CI, H, Br), (M-10272, CH3) H, CI, H, CHs), (M-10273, CH3; H, CI, P, H)，
(M-10274, CHs, H, CI, F, CI), (M-10275, CH3, H, CI, F， F), (M-10276, CHs, H， CI, F, CFs), (M-10277, CHs, H， CI, F, Br), (M-10278, CH3， H, CI, F' CH3), (M-10279, CHs, H, C CI H), (M-10280, CH3) H, CI, CI, CI), (M-10281, CHs, H; CI, CI, F), (M-10282, CHs, H, CI, CI, CF3), (M-10283, CHs, H; CI, CI, Br), (M-10284, CHs, H, CI, CI, CHs), (M- 10285, CHs, H, CI, CH3, H), (M-10286, CHs, H, CI, CHs, CI), (M-10287, CHs, H, CI, CH3, F), (M-10288, CH3) H, CI, CHs, CFs), (M-10289, CHs, H, CI, CHs, Br), (M-10290, CH3, H, CI, CH3, CHs), (M-10291, CH3, H' CI, Et, H), (M-10292, CHs, H, CI, Et, CI), (M-10293, CHs, H' CI, Et, F), (M-10294, CHs, H, CI, Et, CFs), (M-10295, CHs, H, CI, Et, Br), (M-10296, CHs, H， CI, Et, CHs), (M-10297, CHs, H, CI, n-Pr, H), (M-10298, CHs, H, CI, n-Pr, CI), (M-10299, CHs, H, CI, n-Pr, F)， (M-10300, CHs, H, CI, n-Pr, CFs), (M-10301, CHs, H， CI, n-Pr, Br), (M-10302, CHs, H, CI, n-Pr, CH3), (M-10303, CHs, H, CI, c-Pr, H), (M- 10304, CHs, H, CI, c-Pr, CI), (M-10305, CH3; H, CI, c-Pr, F), (M-10306, CHs, H, CI, c-Pr, CFs), (M-10307, CH3j H, CI, c-Pr, Br), (M-10308, CHs, H, CI, c-Pr, CH3), (M-10309, CHs' H, CI, i-Pr, H), (M-10310, CH3, H, CI, i-Pr, CI), (M-10311, CHs, H, CI, i-Pr, F), (M-10312, CHs, H, CI, i-Pr, CFs), (M-10313, CHa' H, CI, i-Pr, Br), (M-10314, CHs, H, CI, i-Pr, CH3), (M-10315, CHs, H, CI, n-Bu, H), (M-10316, CH3) H, CI, n-Bu, CI), (M-10317, CH3) H, Cl' n-Bu, F), (M-10318, CH3) H, CI, n-Bu, CFs), (M-10319, CHs, H, Cl, n-Bu, Br), (M-10320, CH3, H, Cl, n-Bu, CH3), (M-10321, CHs, H, Cl, i-Bu, H), (M-10322, CH3, H， Cl, i-Bu, Cl), (M-10323, CHs, H, Cl, i-Bu, F), (M-10324, CHs, H, Cl, i-Bu, CFs), (M-10325, CHs, H, Cl, i-Bu; Br), (M-10326, CH3, H, Cl, i-Bu, CHs), (M-10327, CHs, H, Cl, sec-Bu, H), (M- 10328, CH3, H, Cl, sec-Bu, Cl), (M-10329, CHs, H， Cl, sec-Bu, F), (M-10330, CH3， H, Cl, sec-Bu, CFs), (M-10331, CHs, H, Cl, sec-Bu, Br), (M-10332, CH3, H, Cl, sec-Bu, CHs), (M-10333, CHs, H, Cl, n-Pen; H), (M-10334,. CH3) H, Cl, n-Pen, Cl), (M-10335, CH3, H, Cl, n-Pen, F), (M-10336, CHs, H, Cl, n-Pen, CFs), (M- 10337, CHs, H, Cl, n-Pen, Br), (M-10338, CH3, H; Cl, n-Pen, CH3), (M-10339, CHs, H, Cl, c-Pen, H), (M-10340, CH3) H, Cl, c-Pen, Cl), (M-10341, CHs, H， Cl, c-Pen, F), (M-10342, CHs, H, Cl, c-Pen, CF3), (M-10343, CHs, H, Cl, c-Pen, Br), (M-10344, CH3, H, Cl, c-Pen, CH3), (M-10345, CHs, H, Cl, n-Hex, H), (M-10346, CH3, H, Cl, n-Hex, Cl), (M-10347, CHs, H, Cl, n-Hex, F)， (M-10348, CH3) H, Cl, n-Hex, CFs), (M-10349, CH8; H, Cl, n-Hex, Br), (M-10350, CHs, H, Cl, n-Hex, CHs), (M-10351, CHs, H, Cl, c-Hex, H)，（M-10352, CH3, H, Cl, c-Hex, Cl), (M- 10353, CHs, H, Cl, c-Hex, F), (M-10354, CHs, H, Cl, c-Hex, CFs), (M-10355, CHs, H, Cl, c-Hex, Br), (M-10356, CHs, H, Cl, c-Hex, CH3), (M-10357, CHs, H, Cl, OH, H), (M-10358, CHs, H, Cl, OH, Cl), (M-10359, CH3; H, Cl, OH, F), (M-10360, CH3, H' Cl, OH, CF3), (M-10361, CH3; H, Cl, OH, Br), (M-10362, CH3, H, Cl, OH, CHs), (M-10363, CHs, H, Cl, EtO, H), (M-10364, CHs, H, Cl, EtO, Cl), (M-10365, CH3; H， Cl, EtO, F), (M-10366, CH3, H, Cl, EtO, CFs), (M-10367, CHs, Cl, EtO, Br), (M-10368, CHs, H, Cl, EtO, CHs), (M-10369, CH3, H, Cl, n-PrO, H), (M-10370, CHs, H, Cl, n-PrO, Cl), (M-10371, CH3; H, Cl, n-PrO, F), (M-10372, CH3, H, Cl, n-PrO; CF3), (M-10373, CH3, H, Cl, n-PrO, Br), (M-10374, CH3, H, CI, n-PrO, CHs), (M- 10375, CHs, H, CI, PhO, H), (M-10376, CHs, H, CI, PhO, CI), (M-10377, CH3， H, CI, PhO, F), (M- 10378, CH3, H, CI, PhO, CF3), (M-10379, CHs, H, CI, PhO, Br), (M- 10380, CH3， H, CI, PhO, CHs), (M- 10381, CHs, H, CI, BnO, H), (M- 10382, CHs, H, CI, BnO, CI), (M-10383, CHs, H， CI, BnO, F), (M- 10384, CH3) H, CI, BnO, CF3), (M-10385, CHs, H, CI, BnO, Br), (M-10386, CHs, H, CI, BnO, CHa), (M-10387, CHs, H, CI, PhCHsCHsO, H), (M-10388, CHs, H, CI, PhCH2CH20; CI), (M-10389, CH3, H, CI, PI1CH2CH2O, F); (M-10390, CH3, H, Cl' PhCH2CH20, CFs), (M-10391, CH3) H, Cl, PhCH2CH20, Br), (M-10392, CHs, H, Cl, PhCH2CH20; CHs), (M-10393, CHs, H, Cl, CP3O, H), (M-10394, CHs, H, Cl, CFsO, Cl), (M-10395, CH3, H, Cl, CFsO, F), (M-10396, CHa, H， Cl, CF3O, CFs), (M-10397, CH3, H, Cl, CFsO, Br), (M- 10398, CH3, H, Cl, CFsO, CH3), (M- 10399, CHs, H, Cl, Ph, H), (M-10400, CHs, H, Cl, Ph, Cl), (M-10401, CHs, H, Cl, Ph, F)， (M-10402, CH3, H, Cl, Ph, CFs), (M-10403, CHs, H, Cl, Ph, Br), (M-10404, CH3; H; Cl, Ph, CH3), (M- 10405, CH3; H, Cl, 4-F-Ph, H), (M-10406, CHs, H, Cl, 4-F- Ph, Cl), (M- 10407, CH3; H, Cl, 4-F-Ph, F), (M-10408, CH3) H, Cl, 4-F-Ph, CF3); (M-10409, CHs, H, Cl, 4-F-Ph, Br), (M-10410, CHa, H, Cl, 4-F-Ph, CHs), (M- 10411, CHs, H, Cl, 4-CFa-Ph, H), (M-10412, CHs, H, Cl, 4-CF3-Pli; Cl), (M- 10413， CHs, H, Cl, 4-CFs-Pli, F), (M-10414, CHs, H, Cl, 4-CF3-Ph, CFs), (M- 10415, CHs, U, Cl, 4-CF3-Ph; Br), (M-10416, CHs, H, Cl, 4-CF3-Ph, CHs), (M- 10417, CHs, H; Cl, 4-(Me)2N-Ph, H), (M- 10418, CHa, H, Cl, 4-(Me)2N-Ph, Cl), (M-10419, CH3, H, Cl, 4-(Me)2N-Ph, F), (M-10420, CHs, H, Cl, 4-(Me)2N-Ph, CF3), (M-10421, CH3, H, Cl, 4-(Me)2N-Pli) τ), (M-10422, CHs, H, Cl, 4- (Me)2N-Ph, CH3), (M-10423, CHs, H, Cl, 4-OH-Ph, H), (M-10424, CHs, H, Cl, 4-OH-Ph, Cl), (M- 10425, CHa, H, Cl, 4-OH-Ph, F), (M-10426, CH3, H, Cl, - OH-Ph, CF3), (M-10427, CHs, H, Cl, 4-OH-Pli, Br), (M-10428, CHs, H; Cl, 4- OH-Ph, CHs), (M-10429, CHs, H, Cl, 3,4-di-F-Ph, H), (M-10430, CHs, H, Cl, 3,4-di-F-Ph, CI), (M-10431, CHs, H， CI, 3,4-di-F-Ph, F)， (M-10432, CHs, H, CI, 3,4-di-F-Ph, CFs), (M-10433, CHs, H, CI, 3,4-di-F-Ph, Br), (M-10434, CHs, H， CI, 3,4-di-F-P ; CHs), (M-10435, CH3) H, CI, 4-COOH-Ph, H), (M-10436, CH3) H, CI, 4-COOH-Ph, CI), (M-10437, CH3, H, CI, 4-COOH-Ph, F), (M-10438, CHs, H, CI, 4-COOH-Pli, CF3), (M-10439, CHs, H, CI, 4-COOH-Ph, Br), (M-10440, CHa, H, CI, 4-COOH-Ph, CHs), (M-10441, CHs, H, CI, Bn, H), (M-10442, CHs, H, CI, Bn, CI), (M-10443, CHs, H, CI, Bn, F), (M-10444, CHs, H, CI, Bn, CF3), (M-10445, CH3) H, CI, Bn, Br), (M-10446, CHs, H, CI, Bn, CHa), (M-10447, CH3) H, CI, 4-F-Bn, H), (M-10448, CH3, H, CI, 4-F-Bn, CI), (M-10449, CHs, H, CI, 4-F-Bn, F), (M-10450, CH3, H, CI, 4-F-Bn, CF3), (M-10451, CH3, H, CI, 4-F-Bn, Br), (M- 10452, CH3) H， CI, 4-F-Bn, CH3), (M-10453, CH3, H， CI, 2-Py, H), (M-10454, CHs, H; CI, 2-Py, CI), (M-10455, CHs, H, CI, 2-Py, F), (M-10456, CH3, H, CI,
2- Py, CFs), (M-10457, CHs, H, CI, 2-Py, Br), (M-10458, CHs, H, CI, 2-Py, CH3), (M-10459, CHs, H, CI, 3-Py, H), (M-10460, CH3, H, CI, 3-Py, CI), (M-10461, CHs, H, CI, 3-Py, F), (M-10462, CHs, H, CI, 3-Py, CF3), (M-10463, CHs, H, CI, 3-Py, Br), (M-10464, CH3) H, CI, 3-Py, CHs), (M-10465, CH3j H, CI, 4-Py, H), (M- 10466， CH3, H, CI, 4-Py, CI), (M-10467, CH3, H, CI, 4-Py, F), (M-10468, CHs, H, CI, 4-Py, CFs), (M-10469, CH3) H, CI, 4-Py, Br), (M-10470, CHs, H, CI, 4-Py, CHs), (M-10471, CHs, H; CI, 2-Th, H), (M-10472, CH3, H, CI, 2-Th, CI), (M- 10473, CHs, H, CI, 2-Th, F), (M-10474, CH3j H, CI, 2-Th, CF3)， (M-10475, CHs, H, CI, 2-Th, Br), (M-10476, CH3) H, CI, 2-Th, CHs), (M-10477, CH3, H, CI, 3-Th, H), (M- 10478, CHs, H, Cl， 3-Th, CI), (M-10479, CHs, H, CI, 3-Th, F)，（M-10480, CH3) H, CI, 3-Th, CF3), (M.10481, CH3) H, CI, 3-Th, Br), (M- 10482, CHs, H, CI,
3- Th, CHs), (M-10483, CH3, H' CI, pyrazol-2-yl, H), (M-10484, CH3, H, CI, pyrazol-2-yl, CI), (M-10485, CHs, H, CI, pyrazol-2-yl, F)， (M-10486, CHs, H, CI, pyrazol-2-yl, CF3)， (M-10487, CH3; H, CI, pyrazol-2-yl, Br), (M-10488, C H, CI, pyrazol-2-yl; CH3), (M-10489, CHs, H, CI, pyrazol-3-yl, H), (M-10490, CH3, H, CI, pyrazol-3-yl, CI), (M-10491, CHs, H, CI, pyrazol-3-yl, F), (M-10492, CH3, H' CI, pyrazol-3-yl, CFs), (M-10493, CH3) H, CI, pyrazol-3-yl, Br), (M-10494, CHs, H, CI, pyrazoレ 3-yl, CH3), (M-10495, CH3) H, CI, pyrimidin-2-yl, H), (M- 10496， CH3, H， CI, pyrimidin-2-yl, CI), (M-10497, CHs, H, CI, pyrimidin-2-yl, F), (M-10498, CH3, H, CI, pyrimidin-2-yl, CFs), (M-10499, CH3, H, CI, pyrimidin-2-yl, Br), (M-10500, CH3, H, CI, pyrimidin-2-yl, CHs), (M-10501, CHs, H, CI, pyrimidm-4-yl, H), (M-10502, CHs, H, CI, pyrimidin-4-yl, CI), (M- 10503, CHs, H, CI, pyrimidin-4-yl, F), (M-10504, CHs, H, CI, pyrimidin-4-yl, CFs), (M-10505, CHs, H, CI, pyrimidin-4-yl, Br), (M-10506, CH3, H, CI, pyrimidin-4-yl, CHs), (M-10507, CHs, H, CI, pyrimidin-5-yl, H), (M-10508, CH3, H, CI, pyrimidm-5-yl, CI), (M-10509, CHs, H, CI, pyrimidin-5-yl, F)， (M-10510, CHs, H, CI, pyrimidin-5-yl, CFs), (M-10511, CHs, H, CI, pyrimidin-5-yl, Br), (M-10512, CHs, H, CI, pyrimidin-5-yl, CH3), (M-10513, CHs, H, CI,
HOOCCH2CH2CH2) H)，（M-10514, CH3， H, CI, HOOCCH2CH2CH2, CI), (M- 10515, CHs, H, CI, HOOCCH2CH2CH2, F), (M-10516, CHs, H, CI,
HOOCCH2CH2CH2, CF3), (M-10517, CHs, H, CI, HOOCCH2CH2CH2, Br), (M- 10518, CHs, H, CI, HOOCCH2CH2CH2, CH3), (M-10519, CH3, H, CI,
HOOCCH2CH2CH2CH2, H), (M-10520, CH3， H, CI, HOOCCH2CH2CH2CH2, CI), (M-10521, CHs, H, CI, HOOCCH2CH2CH2CH2, F), (M-10522, CHs, H, CI,
HOOCCH2CH2CH2CH2) CF3), (M-10523, CH3, H, CI, HOOCCH2CH2CH2CH2, Br), (M-10524, CHs, H, Cl' HOOCCH2CH2CH2CH2, CH3), (M-10525, CHs, H, CI, (Me)2NCOCH2CH2CH2CH2, H), (M-10526, CH3; H, Cl,
(Me)2NCOCH2CH2CH2CH2) Cl), (M-10527, CH3, H, Cl,
(Me)2NCOCH2CH2CH2CH2, F), (M-10528, CHs, H, Cl,
(Me)2NCOCH2CH2CH2CH2, CFs), (M-10529, CH3, H, Cl, (Me)2NCOCH2CH2CH2CH2> Br), (M-10530, CH3, H, CI,
(Me)2NCOCH2CH2CH2CH2' CH3), (M-10531, CH3, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2) H), (M-10532, CHs, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2， CI), (M-10533, CHs, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-10534, CH3) H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-10535, CH3) H; CI,
(Me)2NCOCH2CH2CH2CH2CH2， Br), (M- 10536, CH3, H, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-10537, CHs, H, CI, MeOCH2) H)， (M- 10538, CHs, H, CI, MeOCHs, CI), (M-10539, CH3, H, CI, MeOCH2) F), (M- 10540, Oils, H, CI, MeOCH2, CFs), (M-10541, CHs, H, CI, MeOCHs, Br), (M-10542, CHs, H, CI, MeOCH2; CH3), (M-10543, CH3, H, Gl, EtOCHa, H), (M-10544, CHs, H， CI, EtOCHs, CI), (M- 10545, CHs, H, CI, EtOCHs, F), (M-10546, CHs, H, CI, EtOCH2, CFs), (M-10547, CHs, H, CI, EtOCH2, Br), (M-10548, CH3, H, CI, EtOCH2, CH3), (M-10549, CHs, H, CI, BtOCH2CH2, H), (M-10550, CHs, H， CI, EtOCH2CH2; CI), (M-10551, CHs, H; CI, EtOCH2CH2; F), (M- 10552, CH3> H, CI, EtOCH2CH2) CFs), (M-10553, CHs, H, CI, EtOCHsCHs, Br), (M-10554, CHs, H， CI,
EtOCH2CH2, CHs), (M-10555, CHs, H' CI, MeOCBbCHsOCHsCH , H)，（M-10556, CH3) H, CI, MeOCH2CH2OCH2CH2; CI), (M- 10557, CH3; H, CI,
MeOCH2CH2OCH2CH2, F), (M-10558, CH3, H, CI, MeOCH2CH2OCH2CH2， CFs), (M-10559, CHs, H, CI, MeOCH2CH20CH2CH2) Br), (M-10560, CHs, H, CI, MeOCH2CH2OCH2CH2, CHs), (M-10561, CH3, H, CI, MeOCH2CH2, H), (M- 10562,. CHs, H, CI, MeOCHsCHs, CI), (M-10563, CHs, H, CI, MeOCH2CH2, F), (M-10564, CHs, H, CI, MeOCH2CH2, CFs), (M- 10565, CHs, H, CI, MeOCH2CH2) Br), (M-10566, CHs, H, CI, MeOCH2CH2, CH3), (M-10567, CHs, H, CI, HOCH2, H), (M-10568, CHs, H, CI, HOCH2> CI), (M- 10569, CHs, H, CI, HOCH2, F), (M- 10570, CH3, H' CI, HOCH2, CF3), (M-10571, CHs, H, CI, HOGH2, Br), (M- 10572, CHs, H, CI, HOCHs, CHs), (M-10573, CHs, H, CI, HOC¾CH2) H), (M-10574, CH3, H, CI, HOCH2CH2, CI), (M-10575, CH3, H, CI, HOCH2CH2; F)， (M-10576, CHs, H, CI, HOCH2CH2) CFs), (M-10577, CHs, H, CI, HOCH2CH2) Br), (M-10578, CHs, H， CI, HOCH2CH2, CHs), (M-10579, CH3) H, CI, HOCH2CH2CH2, H), (M- 10580, CH3; H, CI, HOCH2CH2CH2, CI), (M-10581, CHs, H, CI, HOCH2CH2CH2; F), (M-10582, CHs, H; CI, HOCH2CH2CH2! CFs), (M-10583, CHs, H, CI,
HOCH2CH2CH2, Br), (M-10584, CH3, H, CI, HOCH2CH2CH2) CH3), (M-10585, CHs, H, CI, HOCH2CH2CH2CH2, H), (M-10586, CHs, H， CI, HOCH2CH2CH2CH2, CI), (M-10587, CHs, H， CI, HOCH2CH2CH2CH2, F), (M-10588, CHs, H， CI, HOCH2CH2CH2CH2; CFs), (M-10589, CH3, H, CI, HOCH2CH2CH2CH2， Br), (M-10590, CHs, H, CI, HOCH2CH2CH2CH2, CH3), (M-10591, CH3, H, CI, HOCH2CH2CH2CH2CH2; H), (M-10592, CHa, H, CI, HOCH2CH2CH2CH2CH2， CI), (M-10593, CHs, H, CI, HOCH2CH2CH2CH2CH2, F), (M-10594, CHs, H, CI, HOCH2CH2CH2CH2CH2, CF3), (M-10595, CH3， H, CI, HOCH2CH2CH2CH2CH2， Br), (M-10596, CHa, H, CI, HOCH2CH2CH2CH2CH2, CHs), (M-10597, CH3, H, CI, HOCH2CH2OCH2CH2) H), (M-10598, CHs, H, CI, HOCH2CH2OCH2CH2, CI), (M-10599, CHs, H' CI, HOCH2CH2OCH2CH2, F), (M-10600, CH3, H, CI,
HOCH2CH2OCH2CH2) CFs), (M-10601, CH3, H, CI, HOCH2CH2OCH2CH2' Br), (M-10602, CH3; H, CI, HOCH2CH2OCH2CH2, CHs), (M-10603, CHs, H， CI, (Me)2N, H), (M-10604, CH3, H, CI, (Me)2N, CI), (M-10605, CH3， H, CI, (Me)2N, F), (M-10606, CHs, H, CI, (Me)2N, CFs), (M-10607, CH3, H, CI, (Me)2N, Br), (M-10608' CHs, H, CI, (Me)2N, CH3), (M-10609, CHs, H， CI, piperidin-4-yl- methyl, H), (M-10610, CH3) H, CI, piperidm-4-yl-methyl, CI), (M-10611, CHs, H, CI, piperidin-4-yl-methyl, F), (M-10612, CH3) H, CI, piperidin-4-yl-methyl, CFs), (M-10613, CHs, H, CI, piperidin-4-yl-methyl, Br), (M-10614, CH3; H, CI, piperidin-4-yl-methyl, CHs), (M-10615, CH3, H, CI, cyclohexylmethyl, H), (M- 10616, CHs, H, CI, cyclohexylmethyl, CI), (M-10617, CHs, H, CI, cyclohexylmethyl, F), (M-10618, CHs, H, CI, cyclohexylmethyl, CFs), (M-10619, CHs, H, CI, cyclohexylmethyl, Br), (M- 10620， CHs, H， CI, cyclohexylmethyl, CHs), (M-10621, CHs, F, H， H, H), (M-10622, CHs, F' H, H, CI), (M-10623, CH3， F, H, H, F), (M-10624, CH3) F; H, H, CF3)， (M-10625, CHs, F, H, H, Br), (M- 10626, CHs, F, H, H, CH3), (M-10627, CHs, F, H' F, H), (M-10628, CH3, F, H, F, CI), (M-10629, CH3, F, H, F, F), (M-10630, CHs, F， H, F, CF3)， (M-10631, CHs, F, H, F, Br), (M-10632, CH3, F, H, F, CHs), (M-10633, CHs, F, H, CI, H), (M-10634, CH3, F, H, CI, Cl); (M-10635, CH3, F, H, CI, F), (M-10636, CH3) F, H, CI, CFs), (M-10637, CH3) F, H, CI, Br), (M-10638, CH3, F, H, CI, CH3), (M-10639, CH3, F, H; CHs, H), (M-10640, CHs, F, H, CH3, CI), (M-10641, CHs, F, H, CH3; F), (M- 10642, CHs, F, H, CH3, CFs), (M-10643, CH3> F, H, CHs, Br), (M-10644, CHs, F, H, CHs, CHs), (M-10645, CHs, F， H, Et, H), (M-10646, CHs, F, H, Et, CI), (M- 10647, CHs, F， H, Et, F), (M-10648, CHs, F, H' Et, CF3), (M-10649, CHs, F, H, Et, Br), (M-10650, CH3, F, H， Et, CH3)，（M-10651, CHs, F, H, n-Pr, H), (M-10652, CHs, P, H, n-Pr, CI), (M-10653, CHs, F, H, n-Pr, F), (M-10654, CH3, F, H, n-Pr, CFs), (M-10655, CHs, F, H, n-Pr, Br), (M-10656, CHs, F, H, n-Pr, CHs), (M- 10657, CHs, F, H, c-Pr, H), (M-10658, CH3, F, H, c-Pr, CI), (M-10659, CH3, F, H, c-Pr, F)， (M-10660, CHs, F, H， c-Pr, CF3), (M-10661, CH3, F, H, c-Pr, Br), (M- 10662, CHs, F' H, c-Pr, CH3), (M-10663, CH3> F, H, i-Pr, H), (M-10664, CHs, F' H, i-Pr, CI), (M-10665, CH3, F, H, i-Pr, F), (M-10666, CH3， F, H, i-Pr, CF3), (M-10667, CHs, F, H, i-Pr, Br), (M-10668, CHa, F, H, i-Pr, CHs), (M-10669, CH3, F, H, n-Bu, H)， (M- 10670, CHs, F, H, n-Bu, CI), (M-10671, CHs, F, H, n-Bu, F)， (M-10672, CHs, F, H, n-Bu, CFs), (M-10673, CHs, F, H, n-Bu, Br), (M-10674, CHs, P, H, n-Bu, CHs), (M-10675, CHs, F, H, i-Bu, H), (M-10676, CHs, F, H, i- Bu, CI), (M-10677, CH3, F, H, i-Bu, F), (M-10678, CHs, F, H, i-Bu, CF3), (M- 10679, CH3) F, H， i-Bu, Br), (M-10680, CHs, F, H, i-B , CHs), (M-10681, CHs, F, H, sec-Bu, H)，（M-10682, CHs, F, H, sec-Bu, CI), (M-10683, CHs, F, H' sec-Bu, F)， (M-10684, CHs, F, H, sec-Bu, CFs), (M-10685, CHs, F, H， sec-Bu, Br), (M- 10686， CHs, F, H, sec-Bu, CHs), (M-10687, CHs, F, H， n-Pen, H), (M-10688, CH3， F, H, n-Pen, CI), (M-10689, CHs, F, H; n-Pen, F), (M-10690, CH3, F， H, n-Pen, CFs), (M-10691, CHs, F, H, n-Pen, Br), (M-10692, CH3) F, H, n-Pen, CHs), (M- 10693, CH3, F, H, c-Pen, H), (M-10694, CHs, F， H, c-Pen, CI), (M-10695, CH3, F, H, c-Pen, F), (M-10696, CHs, F， H, c-Pen, CF3), (M-10697, CHs, F, H, c-Pen, Br), (M-10698, CH3, F, H, c-Pen, CH3), (M-10699, CHs, F, H, n-Hex, H), (M-10700, CH3) F, H, n-Hex, CI), (M-10701, CH3) F, H, n-Hex, F), (M-10702, CH3; F, H, n-Hex, CFs), (M-10703, CHs, F， H, n-Hex, Br), (M-10704, CHs, F, H; n-Hex, CHs), (M-10705, CH3, F, H, c-Hex, H), (M-10706, CH3, F, H, c-Hex, CI), (M- 10707, CH3, F, H, c-Hex, F), (M-10708, CHs, F, H, c-Hex, CFs), (M-10709, CHs, P, H, c-Hex, Br), (M-10710, CHs, F, H, c-Hex, CHs), (M-10711, CH3, F, H, OH, H), (M-10712, CHs, F' H, OH, CI), (M-10713, CHs, F, H, OH, F), (M-10714, CH3, F, H' OH, CF3), (M-10715, CH3, F, H, OH, Br), (M-10716, CH3, F, H, OH, CH3)， (M-10717, CHs, F， H, EtO, H), (M-10718, CHs, F, H, EtO, CI), (M-10719, CH3, F, H， EtO, F), (M-10720, CHs, F, H, EtO, CFs), (M-10721, CHs, F, H, EtO, Br), (M-10722, CHs, F, H, EtO, CHs), (M-10723, CH3, F， H, n-PrO, H), (M-10724, CH3, F, H, n-PrO, CI), (M-10725, CHs, F, H, n-PrO, F), (M-10726, CHs, F, H, n-PrO, CFs), (M-10727, CHs, F, H; n-PrO, Br), (M-10728, CHs, F; H, n-PrO, CHs), (M-10729, CH3,.F, H, PhO, H), (M-10730, CH3, F, H, PhO, CI), (M-10731, . CH3, F, H， PhO, F), (M-10732, CHs, F, H, PhO, CF3), (M-10733, CHs, F, H, PhO, Br), (M-10734, CHs, F, H, PhO, CHs), (M-10735, CHs, P, H, BnO, H), (M-10736, CHs, F, H, BnO, CI), (M-10737, CH3) F, H, BnO, F), (M-10738, CHs, F, H, BnO, CFs), (M-10739, CH3) F, H, BnO, Br), (M-10740, CH3) F, H, BnO, CH3), (M- 10741, CHs, F, H, PhCH2CH20, H), (M-10742, CH3) F, H, PhCH2CH20, CI), (M-10743, CH3， F, H， PhCH2CH20> F), (M-10744, CHs, F, H, PI1CH2CH2O, CFs), (M-10745, CHs, F， H, PI1CH2CH2O, Br), (M-10746, CH3) F, H, PhCH2CH20; CHs), (M-10747, CHs, F, H, CFsO, H)， (M-10748, CHs, F， H, CF30, CI), (M- 10749, CH3, F, H, CFsO, F), (M-10750, CH3, F, H, CFsO, CFs), (M-10751, CHs, F, H, CFsO, Br), (M-10752, CHs, F, H, CFsO, CHs), (M-10753, CH3, F, H, Ph, H), (M-10754, CHs, F, H, Ph, CI), (M-10755, CHs, F, H, Ph, F); (M-10756, CHs, F, H, Ph; CFs), (M-10757, CHs, F, H， Ph, Br), (M-10758, CHs, F, H, Ph, CH3), (M- 10759, CHs, F, H, 4-F-Ph, H), (M-10760, CH3) F, H, 4-F-Ph, Cl)， (M-10761, CHs, F, H, 4-F-Ph, F), (M-10762, CH3; F, H, 4-F-Ph, CFs), (M-10763, CHs, F; H, 4- F-P , Br), (M-10764, CHs, F, U, 4-F-Ph, CH3), (M-10765, CH3, F, H, 4-CFs-Ph, H), (M-10766, CHs, F, H, 4-CF3-Ph, CI), (M-10767, CH3) F， H, 4-CFs-Ph, F), (M-10768, CHs, F， H, 4-CFs-Ph, CF3), (M-10769, CHs, F, H, 4-CF3-Ph, Br), (M-10770, CH3) F, H, 4-CFs-Ph, CHs), (M-10771, CHs, F, H, 4-(Me)2N-Ph, H), (M-10772, CHs, F, H, 4-(Me)2N-Ph, CI), (M-10773, CH3, F, H, 4-(Me)2N-Ph, F), (M-10774, CHs, F, H, 4-(Me)2N-Ph, CF3), (M-10775, CHs, F, H， 4-(Me)2N-Pli) Br), (M-10776, CHs, F, H, 4-(Me)2N-Ph, CH3)， (M-10777, CH3, F, H, 4-OH-Ph, H)' (M-10778, CHs, F, H, 4-OH-Ph, CI), (M-10779, CHs, F, H, 4-OH-Ph, F), (M-10780, CHs, F， H， 4-OH-Ph, CFs), (M-10781, CHs, F, H， 4-OH-Ph, Br), (M- 10782, CH3, F, H, 4-OH-Ph, CHs)， (M-10783, CHs, F, H, 3;4-di-F-Ph, H)，（M- 10784, CHs, F， H， 3,4-di-F-Ph, CI), (M-10785, CH3, F, H, 3,4-di-F-Ph, F), (M- 10786, CH3) F， H, 3,4-di-F-Ph, CFs), (M-10787, CH3, F, H, 3,4-di-F-Ph, Br), (M-10788, CHs, F, H, 3,4-di-F-Ph, CH3), (M-10789, CHs, F, H, 4-COOH-Ph, H), (M-10790, CHs, F, H, 4-COOH-Ph, CI), (M-10791, CH3, F, H, 4-COOH-Ph, F), (M-10792, CH3; F, H, 4-COOH-Ph, CF3), (M-10793, CHs, F, H, 4-COOH-Ph, Br), (M-10794, CHs, F, H, 4-COOH-Ph, CHs), (M-10795, CHs, F, H, Bn, H), (M- 10796, C F, H, Bn, CI), (M- 10797, CHs, P; H' Bn, F), (M-10798, CHs, F, H, Bn, CFs), (M-10799, CH3, F, H, Bn, Br), (M-10800, CH3) F, H, Bn, CHs), (M-10801, CH3, F, H, 4-F-Bn, H), (M- 10802, CHs, F, H, 4-F-Bn, CI), (M-10803, CHs, F， H, 4-F-Bn, F), (M-10804, CHs, F, H， 4-F-Bn, CFs), (M-10805, CH3, F, H, 4-F-Bn, Br), (M- 10806, CHs, F, H, 4-F-Bn, CH3), (M-10807, CH3; F, H, 2-Py, H), (M- 10808, CHs, F, H, 2-Py, CI), (M-10809, CHs, F, H, 2-Py, F), (M-10810, CHs, F, H;
2- Py, CFs), (M- 10811, CHs, F, H; 2-Py, Br), (M- 10812, CH3， F, H, 2-Py, CH3)， (M-10813, CHa, F, H, 3-Py, H), (M-10814, CHs, F， H, 3-Py, CI), (M- 10815, CHs, F, H, 3-Py, F), (M-10816, CHs, F, H, 3-Py, CFs), (M-10817, CHs, F, H, 3-Py, Br), (M-10818, CHs, F， H, 3-Py, CH3), (M-10819, CH3, F, H, 4-Py, H), (M-10820, CHs, P, H, 4-Py, CI), (M-10821, CHs, F, H, 4-Py, F), (M-10822, CHs, F, H, 4-Py, CF3), (M- 10823, CH3; F， H, 4-Py, Br), (M-10824, CH3, F, H， 4-Py, CHa), (M- 10825, CH3, F, H, 2-Th, H), (M- 10826, CH3， F, H, 2-Th, CI), (M- 10827, CHs, F, H, 2-Th, F), (M-10828, CHs, F, H, 2-Th, CFs), (M-10829, CHs, F, H, 2-Th, Br), (M-10830, CHs, F, H， 2-Th, CHs), (M-10831, CH3, F, H, 3-Th, H), (M-10832, CH3, F, H,
3- Th, CI), (M-10833, CH3, F， H, 3-Th, F), (M-10834, CHs, F, H, 3-Th, CFs), (M- 10835, CHa, F, H, 3-Th, Br), (M- 10836, CHs, F, H, 3-Th, CH3), (M- 10837, CHs, F' H, pyrazoレ 2-yl, H), (M-10838, CH3) F, H, pyrazoレ 2-yl, CI), (M-10839, CHs, F, H, pyrazol-2-yl, F), (M- 10840, CH3) F, H, pyrazol-2-yl, CFs), (M- 10841, CHs, F, H, pyrazol-2-yl, Br), (M-10842, CHs, F, H, pyrazol-2-yl, CHs), (M- 10843, CHa, F, H, pyrazol-3-yl, H), (M-10844, CHs, F, H, pyrazol-3-yl, CI), (M-10845, CHs, F, H, pyrazol-3-yl, F), (M- 10846, CH3, F, H, pyrazol-3-yl, CFs), (M-10847, CHs, F, H, pyrazol-3-yl, Br), (M-10848, CHa, F, H' pyrazol-3-yl, CHs), (M-10849, CHs, F, H, pyrimidin-2-yl, H), (M-10850, CHs, F, H, pyrimidin-2-yl, CI), (M- 10851, CH3, F, H, pyrimidin-2-yl, F), (M-10852, CH3， F, H, pyrimidin-2-yl, CF3), (M-10853, CHs, F, H, pyrimidin-2-yl, Br), (M-10854, CH3; F, H' pyrimidin-2-yl, CH3), (M-10855, CHs, F, H; pyrimidin-4-yl, H), (M-10856, CHs, F, H, pyrimidin-4-yl, CI), (M-10857, CHs, F, H, pyrimidin-4-yl, F), (M-10858, CHs, F, H, pyrimidin-4-yl, CF3), (M-10859, CHs, F, H, pyrimidin-4-yl, Br), (M-10860, CHs, F, H, pyrimidin-4-yl, CH3), (M-10861, CH3) F, H, pyrimidin-5-yl, H), (M-10862, CHs, F， H, pyrimidin-5-yl; CI), (M-10863, CHs, F, H, pyrimidin-5-yl, F), (M-10864, CHs, F, H, pyrimidin-5-yl, CFs), (M-10865, CH3, F, H,
pyrimidin-5-yl, Br), (M-10866, CHs, F, H, pyrimidin-5-yl, CHs), (M-10867, CHs, P, H， HOOCCH2CH2CH2> H), (M-10868, CH3, F, H, HOOCCH2CH2CH2j CI), (M-10869, CHs, F, H, HOOCCH2CH2CH2> F), (M-10870, CHs, F, H,
HOOCCH2CH2CH2; CF3), (M-10871, CHs, F， H, HOOCCH2CH2CH2， Br), (M- 10872, CHs, F, H, HOOCCH2CH2CH2) CH3); (M-10873; CHs, F, H,
HOOCCH2CH2CH2CH2, H), (M-10874, CHs, F， H; HOOCCH2CH2CH2CH2, CI), (M-10875, CH3; F, H, HOOCCH2CH2CH2CH2, F), (M-10876, CHs, F， H，
HOOCCH2CH2CH2CH2j CFs), (M-10877, CH3, F, H， HOOCCHsCHsCHsCHa, Br), (M-10878, CHs, F, H, HOOCCHsCHsCH CHb, CH3), (M-10879, CH3， F, H, (Me)2NCOCH2CH2CH2CH2; H), (M-10880, CHs, F, H,
(Me)2NCOCH2CH2CH2CH2, Cl)，（M-10881, CH3, F, H，
(Me)2NCOCH2CH2CH2CH2, F), (M- 10882, CH3) F' H,
(Me)2NCOCH2CH2CH2CH2, CF3), (M-10883, CH3; F, H,
(Me)2NCOCH2CH2CH2CH2, Br), (M-10884, CHs, F, H,
(Me)2NCOCH2CH2CH2CH2, CH3), (M-10885, CHs, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M.10886, CHs, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M- 10.887, CHs, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-10888, CH3, F, H,
(Me)2NCOCH2CH2CH2CH2CH2, CF3), (M-10889, CHs, F, H,
(Me)2NCOGH2CH2CH2CH2CH2, Br), (M-10890, CH3， F, H, (Me)2NCOCH2CH2CH2CH2CH2, CH3), (M-10891, CH3' F, H, MeOCH2, H), (M- 10892, CHs, F; H, MeOCH2) CI), (M-10893, CH3, F， H, MeOCH2, F), (M-10894, CHs, F, H, MeOCH2; CFs), (M-10895, CHs, F, H, MeOCH2, Br), (M-10896, CH3; F, H, MeOCH2， CH3), (M-10897, CHs, F, H, EtOCH2; H), (M-10898, CHs, F, H, EtOCH2) CI), (M-10899, CHs, P; H, EtOCH2; F), (M-10900, CHs, F, H, EtOCH2) CFs), (M-10901, CHs, F, H, EtOCH2) Br), (M-10902, CH3, F, H, EtOCH2, CHs), (M-10903, CH3, F, H, EtOCH2CH2, H), (M-10904, CHs, F， H, EtOCH2CH2) CI), (M-10905, CHs, F, H, EtOCH2CH2> F), (M-10906, CHs, F, H, EtOCH2CH2; CFs), (M-10907, CH3, F, H, EtOCH2CH2) Br), (M-10908, CHs, F， H, EtOCH2CH2) CHs), (M-10909, CHs, F, H, Me 0 CH2 CH20 CH2 CH2; H), (M- 10910, CHs, F, H,
MeOCH2CH2OCH2CH2' CI), (M-10911, CHs, F, H, MeOCH2CH2OCH2CH2, F), (M-10912, CH3) F, H, MeOCH2CH2OCH2CH2, CF3), (M-10913, CH3, F, H， MeOCH2CH20CH2CH2, Br), (M-10914, CHs, F， H, MeOCHsCB OCB CHs, CH3), (M-10915, CHs, F, H, MeOCH2CH2, H), (M-10916, CHs, F, H, MeOCHsCHs, CI), (M-10917, CH3， F， H, MeOCH2CH2) F)，（M-10918, CHs, F, H, MeOCH2CH2, CFs), (M-10919, CH3, F, H, MeOCH2CH2; Br), (M-10920, CHs, F, H, MeOCHaCHa, CH3), (M-10921, CHs, F, H, HOCH2, H)， (M-10922, CHs, F, H， HOCH2, CI), (M-10923, CHs, F, H, HOCH2, F), (M-10924, CH3, F, H， HOCH2, CFs), (M-10925, CHs, F, H, HOCH2, Br), (M-10926, CH3, F, H, HOCHa, CH3), (M-10927, CHs, F, H, HOCH2CH2, H), (M-10928, CHs, F, H， HOCH2CH2, CI), (M-10929, CH3, F, H, HOCH2CH2, F), (M-10930, CH3' F, H, HOCH2CH2, CFs), (M-10931, CH3, F, H, HOCH2CH2, Br), (M-10932, CH3, F, H, HOCH2CH2) CH3), (M-10933, CH3, F, H, HOCH2CH2CH2, H), (M-10934, CH3, F, H, HOCH2CH2CH2, CI), (M-10935, CH3, F， H, HOCH2CH2CH2, F), (M-10936, CH3, F, H， HOCH2CH2CH2, CFs), (M- 10937, CH3) F, H, HOCH2CH2CH2; Br), (M-10938, CH3) F, H, HOCH2CH2CH2, CH3), (M-10939, CH3) F, H, HOCH2CH2CH2CH2, H), (M-10940, CHs, F, H, HOCH2CH2CH2CH2; CI), (M-10941, CHs, F, H, HOCHaCHaCHaCHa, F), (M- 10942, CH3, F, H, HOCH2CH2CH2CH2, CF3), (M-10943, CHs, F, H,
HOCH2CH2CH2CH2) Br), (M-10944, CH3, F, H, HOCH2CH2CH2CH2， CHs), (M- 10945, CHs, F， H, HOCH2CH2CH2CH2CH2; H), (M-10946, CHs, F, H,
HOCH2CH2CH2CH2CH2, CI), (M-10947, CH3; F, H, HOCH2CH2CH2CH2CH2, F), (M-10948, CH3) F, H, HOCH2CH2CH2CH2CH2, CFs), (M- 10949, CHs, F, H, HOCH2CH2CH2CH2CH2, Br), (M-10950, CH3) F, H, HOCH2CH2CH2CH2CH2, CHs), (M-10951, CHs, F， H, HOCH2CH2OCH2CH2; H), (M-10952, CHs, F, H, HOCH2CH2OCH2CH2, CI), (M- 10953.. CH3, F, H, HOCH2CH2OCH2CH2， F), (M- 10954, CHs, F, H， HOCH2CH2OCH2CH2， CFs), (M- 10955, CH3) F, H，
HOCH2CH2OCH2CH2, Br), (M- 10956, CHs, F， H, HOCH2CH2OCH2CH2， CHs), (M-10957, CHs, F, H, (Me)2N, H), (M-10958, CH3, P; H, (Me)2N; CI), (M- 10959, CH3, P, H, (Me)2N, F), (M- 10960, CHs, F, H, (Me)2N, CFs), (M-10961, CH3, F, H, (Me)2N, Br), (M-10962, CH3, F， H, (Me)2N, CHs), (M- 10963, CH3， F' H， piperidin-4-yl-methyl, H), (M-10964, CHs, F, H, piperidin-4-yl-metliyl, CI), (M-10965, CHs, F, H, piperidin-4-yl-methyl, F), (M-10966, CH3, F, H, piperidin-4-yレ methyl, CF3), (M-10967, CHs, F, H, piperidin-4-yレ: methyl, Br), (M-10968, CHs, F， H, piperidin-4-yレ methyl, CH3), (M-10969, CH3, F, H， cyclohexylmetliyl, H), (M-10970, CH3> F, H, cyclohexylmethyl' CI), (M-10971, CHs, F, H, cyclohexylmetliyl, F), (M-10972, CHs, F, H, cyclohexylmethyl, CFs), (M-10973, CHs, F, H, cyclohexylmetliyl, Br), (M-10974, CH3, F, H,
cyclohexylmetliyl, CHs), (M-10975, CH3, F, F, H; H), (M-10976, CHs, F， F, H, CI), (M- 1097.7, CHs, F, F， H, F), (M-10978, CHs, P, F, H, CF3), (M-10979, CH3, F' F, H, Br), (M- 10980, CHs, F, F, H, CH3), (M-10981, CH3, F, F, F, H), (M- 10982, CH3, F, F, F, CI), (M- 10983, CHs, F， F, F, F), (M-10984, CH3, F, F， F, CF3),
(M-10985, CHs, F, F, F, Br), (M-10986, CHs, F, F, F, CHs), (M- 10987, CHs, F, F, CI, H), (M-10988, CHa, F, F, CI, CI), (M-10989, CHs, F, F, CI, F), (M-10990, CH3, F, F, CI, CFs), (M-10991, CHs, F， F, CI, Br), (M-10992, CHs, F, F, CI, CHs), (M-10993, CHs, F, F, CHs, H), (M-10994, CH3, F, F, CH3, CI), (M-10995, CHs, F, F， CH3> F), (M-10996, CH3) F, F, CHs, CF3), (M-10997, CHs, F, F， CH3; Br), (M-10998, CHa, F, F, CHs, CH3)，（M-10999, CHs, F, F， Et, H), (M-11000, CH3, F， F' Et, CI), (M-11001, CHs, F, F, Et, F), (M- 11002, CHa, F， F, Et, CFs), (M-11003, CHs, F, F, Et, Br), (M-11004, CH3, F, F, Et, CH3), (M-11005, CHs, F, F, n-Pr, H)， (M-11006, CHa, F, F, n-Pr, CI), (M-11007, CHs, F, F, n-Pr, F), (M-11008, CHs, F, F, n-Pr, CFs), (M-11009, CHs, F, F, n-Pr, Br), (M-11010, CHs, F, F, n-Pr, CHs), (M-11011, CHs, F, F' c-Pr, H), (M-11012, CHs, F, F, c-Pr, CI), (M-11013, CH3, F, F, c-Pr, F), (M-11014, CHs, F, F, c-Pr, CF3), (M-11015, CHs, F, F, c-Pr, Br), (M-11016, CHs, F, F, c-Pr, CHs), (M-11017, CHs, F, F, i-Pr, H), (M-11018, CHs, F, F, i-Pr, CI), (M-11019, CHs, F, F, i-Pr, F), (M-11020, CHs, P, F, i-Pr, CFs), (M-11021, CHa, F, F， i-Pr, Br), (M-11022, CHa, F, F, i-Pr, CHs), (M-11023, CHs, F, F， n-Bu, H), (M-11024, CHs, F, F, n-Bu, CI), (M-11025, CH3; F, F, n-Bu, F), (M-11026, CHs, F, F, n-Bu, CFs), (M- 11027, CHa, F, F, n-Bu, Br), (M-11028, CHs, F, F, n-Bu, CHs), (M-11029, CHs, F, F, i-Bu, H), (M-11030, CH3) F, F, i- Bu, CI), (M-11031, CH3> F, P, i-Bu, F), (M-11032, CHs, F, F, i-Bu, CFs), (M- 11033, CH3, F, F, i-Bu, Br), (M-11034, CH3; F, F, i-Bu, CHs), (M-11035, CH3, F， F, sec-Bu, H), (M-11036, CH3， F, F, sec-Bu, CI), (M-11037, CHs, F, F， sec-Bu, F)， (M-11038, CHs, F, F, sec-Bu, CFs), (M-11039, CHs, F, F, sec-Bu, Br), (M-11040,.CH3) F, F, sec-Bu, CH3), (M-11041, CH3, F, F, n-Pen, H);. (,M- 11042, CHs, F, F, n-Pen, CI), (M-11043, CHs, F, F, n-Pen, F), (M-11044, CH3) F, F, n-Pen, CF3), (M-11045, CH3, F, F, n-Pen, Br), (M-11046, CH3, F, F, n-Pen, CHs), (M-11047, CHs, F, F, c-Pen, H), (M-11048, CHs, F, F, c-Pen, CI), (M-11049, CHs, F, F， c- Pen, F), (M-11050, CHa, F, F， c-Pen, CF3); (M-11051, CHs, F， F, c-Pen, Br), (M-11052, CHs, F, F, c-Pen, CHs), (M-11053, CHs, F, F, n-Hex, H), (M-11054, CHs, F, F, n-Hex, CI), (M-11055, CHs, F, F, n-Hex, F), (M-11056, CH3) F, F, n-Hex, CFs), (M-11057, CHs, F， F, n-Hex, Br), (M-11058, CHs, F, F, n-Hex, CH3), (M-11059, CH3, F, F, c-Hex, H)， (M-11060, CHs, F' F, c-Hex, CI), (M-11061, CHs, F, F， c-Hex, F), (M-11062, CHs, F, F, c-Hex, CFs), (M-11063, CHs, F， F, c-Hex, Br), (M-11064, CHs, F, F, c-Hex, CHs), (M-11065, CHs, F, F, OH, H), (M-11066, CHs, F, F, OH, CI), (M-11067, CH3) F, F, OH, F), (M-11068, CH3, F, F, OH, CF3), (M-11069, CHs, F, F， OH, Br), (M-11070, CHs, F, F, OH, CH3), (M-11071, CH3, F, F, EtO, H), (M-11072, CHs, F, F, EtO, CI), (M-11073, CH3, F, P, EtO, F)， (M-11074, CHs, F, F, EtO, CFs), (M-11075, CHs, F， F, EtO, Br), (M-11076, CH3; F; F, EtO, CH3), (M-11077, CH3, F, F, n-PrO, H), (M-11078, CH3, F, F， n-PrO, CI), (M-11079, CHs, F, F， n-PrO, F), (M- 11080, CHs, F, F, n-PrO, CFs), (M- 11081, CHs, F, F, n-PrO, Br), (M-11082, CH3; F' F, n-PrO, CH3), (M-11083, CHs, F, F, PhO, H), (M-11084, CHs, F, F， PhO, CI), (M-11085, CHs, F, F, PhO, F), (M-11086, CHs, F, F, PhO, CFs), (M-11087, CHs, F, F, PhO, Br), (M-11088, CH3; F, F, PhO, CHs), (M-11089, CHs, F, F, BnO, H), (M-11090, CHs, F, F, BnO, CI), (M-11091, CHs, F, F, BnO, F), (M-11092, CHs, F， F, BnO, CFs), (M-11093, CH3) F, F, BnO, Br), (M-11094, CHs, F, F, BnO, CH3), (M-11095, CH3, F, F,
PhCH2CH20, H), (M-11096, CH3, F, F， PhCHaCHaO, CI), (M-11097, CH3, P; F, PhCHaCHaO, F), (M-11098, CH3, F, F, PhCH2CH20; CPs), (M-11099, CHs, F, F, P CH2CH20, Br), (M-11100, CH3, F, F, P CH2CH20, CHs), (M-11101, CHs, F， F, CFsO, H), (M-11102, CHs, E, F, CFsO, CI), (M-11103, CHs, F, F, CFsO, F), (M- 11104, CHs, F, F, CFsO, CF3)， (M-11105, CH3, F, F' CFsO, Br), (M-11106, CHa, F, F, CFsO, CHs), (M-11107, CH3, F, F, Ph, H), (M-11108, CHs, F, F, Ph, CI), (M-11109, CHs, F, F, Ph, F), (M-11110, CH3, F, F， Ph, CFs), (M-11111, CHs, F, F, Ph, Br), (M-11112, CHs, F, F, Ph, CH3), (M-11113, CHs, F, F, 4-F-Ph, H), b
〇
Ω
Figure imgf000284_0001
p,,,, C3o C 31H JP 4K 4jH?IHC C:： P： P:il---
((,),) p,),,,39 C;2s2 CHMeNph CH F 4MeNphH Br F--- ，237 C2 CHMeNpli F eNphF --- ，,,,,32 C CH F F 4MeplIPIN N--- 3s33 CH F ^C P CH FF Br- ps3S CC Fp CF 21H F 4 F F 4CFh F-.-
(,,, ：,,),,,M1114 C3 F1 F 4〕 5。 F 4FPli FFPh M F---- -- en
Figure imgf000285_0001
Figure imgf000286_0001
o o
MeOCHsCHsOCHsCHs, CI), (M-11265, CHs, F, F, MeOCH2CH2OCH2CH2> F), (M-11266, CHs, F, F, MeOCH2CH2OCH2CH2; CF3)， (M-11267, CH3, F, F， MeOCH2CH2OCH2CH2, Br), (M-11268, CHs, F, F， MeOCH2CH2OCH2CH2) CHs), (M-11269, CHs, F, F, MeOCH2CH2) H), (M-11270, CHs, F， F, MeOCH2CH2, CI), (M-11271, CHs, F, F, MeOCH2CH2, F), (M-11272, CH3, F, F, MeOCH2CH2; CF3), (M-11273, CHs, F, F, MeOCH2CH2) Br), (M-11274, CH3) F, F, MeOCHaCHa, CH3), (M-11275, CHs, F, F' HOCH2, H), (M-11276, CH3, F, F, HOCHa, CI), (M-11277, CHs, F, F, HOCH2, F), (M-11278, CHs, F, F, HOCH2, CP3), (M-11279, CHs, F, F' HOCHa, Br), (M-11280, CH3, F, F, HOCH2, CH3), (M-11281, CHs, F, F, HOCH2CH2> H), (M-11282, CH3, F, F, HOCH2CH2) CI), (M-11283, CH3, F' F, HOCH2CH2, F), (M-11284, CHs, F, F, HOCHaCHs, CF3), (M-11285, CH3， F, F, HOCH2CH2, Br), (M-11286, CHs, F, F, HOCH2CH2) CHs), (M-11287, CH3， F, F, HOCH2CH2CH2, H)， (M-11288, CH3, F, F, HOCH2CH2CH2， CI), (M-11289, CHs, F, F, HOCH2CH2CH2, F), (M-11290, CH3) F, F, HOCH2CH2CH2, CF3), (M-11291, CHs, F, F, HOCH2CH2CH2, Br), (M-11292, CH3, F, F, HOCH2CH2CH2) CH3), (M-11293, CH3, F， F, HOCH2CH2CH2CH2, H), (M-11294, CH3, F, F，
HOCH2CH2CH2CH2, CI), (M-11295, CHs, F, F, HOCH2CH2CH2CH2, F), (M- 11296, CHa, F, F, HOCH2CH2CH2CH2, CFs), (M-11297, CH3, F, F,
HOCH2CH2CH2CH2, Br), (M-11298, CHs, F, F， HOCH2CH2CH2CH2， CH3), (M- 11299, CHs, F, F, HOCHsCE CHsCHsCHs, H), (M-11300, CH3; F, F,
HOCH2CH2CH2CH2CH2, CI), (M-11301, CH3, F, F, HOCH2CH2CH2CH2CH2, F), (M-11302, CHs, E, F, HOCH2CH2CH2CH2CH2, CF3), (M-11303, CH3, F， F, HOCH2CH2OH2CH2CH2, Br), (M-11304, CH3, F, F, HOCH2CH2CH2CH2CH2, CHs), (M-11305, CH3; F, F, HOCH2CH2OCH2CH2) H), (M-11306, CH3) F, F, HOCH2CH2OCH2CH2, CI), (M-11307, CH3) P, F, HOCH2CH2OCH2CH2, F), (M- 11308, CHs, F' F, HOCH2CH2OCH2CH2, CF3), (M-11309, CHs, F, F, HOCH2CH2OCH2CH2, Br), (M-11310, CHs, F, F， HOCH2CH2OCH2CH2, CHs), (M-11311, CHs, F, F, (Me)2N, H), (M-11312, CH3, F， F, (Me)2N; Cl)， (M-11313, CHs, Έ, F, (Me)2N, F), (M-11314, CH3, F, F, (Me)2N, CFs), (M-11315, CH3) F, F, (Me)2N, Br), (M-11316, CH3, F, F, (Me)2N, CHs), (M-11317, CH3， F, F, piperidm-4-yl-methyl, H), (M-11318, CHs, F, F, piperidin-4-yl-metliyl, CI), (M-11319, CHs, F, F, piperidin-4-yl-metliyl, F), (M-11320, CHs, F, F, piperidin-4-yl-metliyl, CFs), (M-11321, CH3， F, F, piperidin-4-yレ methyl, Br), (M-11322, CHs, F, F, piperidin-4-yl-methyl, CHs), (M-11323, CH3, F, F, cyclohexylmetliyl, H), (M- 11324, CHs, F, F, cyclohexylmethyl, CI), (M-11325, CH3, F, F, cyclohexylmethyl, F), (M-11326, CH3, F, F, cyclohexylmethyl, CFs), (M-11327, CHs, F, F, cyclohexylmethyl, Br), (M-11328, CHs, F, F,
cyclohexylmethyl, CHs), (M-11329, CHs, F, CI, H, H); (M-11330, CH3; F, CI, H, CI), (M-11331, CH3, F, CI, H, F)' (M-11332, CHs, F, CI, H， CF3)， (M-11333, CH3, F, CI, H; Br), (M-11334, CHs, F, CI, H, CH3); (M-11335, CHs, F; CI, F, H), (M- 11336, CH3; F, CI, F, CI), (M-11337, CH3, P, CI, F, F), (M-11338, CH3, F, CI, F, CFs), (M-11339, CH3, F， CI, F， Br), (M-11340, CH3) F, CI, F, CHs), (M-11341, CHs, F, CI, CI, H), (M-11342, CHs, F, CI, CI, CI), (M-11343, CH3; F, CI, CI, F), (M-11344, CHs, F, CI, CI, CFs), (M-11345, CHs, F, CI, CI, Br), (M-11346, CHs, F, CI, CI, CHs), (M-11347, CHs, F, CI, CHs, H), (M-11348, CHs, F, CI, CHs, CI), (M-11349, CHs, F, CI, CHs, F), (M-11350, CH3, F, CI, CHs, CFs), (M-11351, CH3, F, CI, CHs, Br), (M-11352, CH3> F， CI, CHs, CHs), (M-11353, CH3> F, CI, Et, H), (M-11354, CHs, F, CI, Et, CI), (M-11355, CHs, F' CI, Et, F), (M-11356, CHs, F, CI, Et, CF3), (M-11357, CHs, F, CI, Et, Br), (M-11358, CHs, F， CI, Et, CHs), (M-11359, CHs, F, CI, n-Pr, H), (M-11360, CH3, F, CI, n-Pr, CI), (M-11361, CHs, F, CI, n-Pr, F), (M-11362, CH3> F, CI, n-Pr, CF3), (M-11363, CHs, F, CI, n-Pr, Br), (M-11364, CHs, F, CI, n-Pr, CH3), (M-11365, CHs, F, Cl; c-Pr, H), (M-11366, CHs, F, CI, c-Pr, CI), (M-11367, CHs, F, CI, c-Pr, F), (M-11368, CHs, F, CI, c- Pr, CFs), (M-11369, GH3, F, CI, c-Pr, Br), (M-11370, CHs, F, CI, c-Pr, CHs), (M-11371, CH3, P, CI, i-Pr, H), (M-11372, CH3, F, CI, i-Pr, CI), (M-11373, CHs, F, CI, i-Pr, F), (M-11374, CH3, F, CI, i-Pr, CFs), (M-11375, CHs, F, CI, i-Pr, Br), (M-11376, CH3) F, CI, i-Pr, CH3)， (M-11377, CH3, F， CI, n-Bu, H), (M-11378, CH3; F, CI, n-Bu, CI), (M-11379, CHs, F, CI, n-Bu, F), (M-11380, CHs; F, CI, n-Bu, CF3), (M-11381, CHs, F, CI, n-Bu, Br), (M-11382, CHs, F, CI, n-Bu, CH3)， (M-11383, CHs, P, CI, i-Bu, H), (M-11384, CHs, F, CI, i-Bu, CI), (M-11385, CH3， F, CI, i-Bu, F), (M-11386, CH3) F, CI, i-Bu, CFs), (M-H387, CHs, F, CI, i-Bu, Br), (M-11388, CH3) F, CI, i-Bu, CHs), (M-11389, CH3, F, CI, sec-Bu, H), (M-11390, CHs, F, CI, sec-Bu, CI), (M-11391, CH3; F, CI, sec-Bu, F); (M-11392, CHs, F, CI, sec-Bu, CFs), (M-11393, CH3, F, CI, sec-Bu, Br), (M-11394, CHs, F, CI, sec-Bu, CHs), (M-11395, CH3) F, CI, n-Pen, H), (M-11396, CHs, F, CI, n-Pen, CI), (M- 11397, CHs, F, CI, n-Pen, F), (M-11398, CHs, F, CI, n-Pen, CFs), (M-11399, CH3) F, CI, n-Pen, Br), (M-11400, CH3, F, CI, n-Pen, CHs), (M-11401, CH3, F, CI, c- Pen, H), (M-11402, CHs, F, CI, c-Pen, CI), (M-11403, CH3, F, CI, c-Pen, F), (M-11404, CHs, F, CI, c-Pen, CFs), (M-11405, CH3; F, CI, c-Pen, Br), (M-11406, CHs, F, CI, c-Pen, CHs), (M-11407, CH3， F, CI, n-Hex, H)， (M-11408, CH3, F, CI, n-Hex, CI), (M-11409, CHs, F, CI, n-Hex, F), (M-11410, CHs, F, CI, n-Hex, CFs), (M-11411, CHs, F, CI, n-Hex, Br), (M-11412, CHs, F, CI, n-Hex, CHs), (M-11413, CH3> F， CI, c-Hex, H), (M-11414, CHs, F, CI, c-Hex, CI), (M-11415, CH3, F, CI, c-Hex, F), (M-11416, CHs, F, CI, c-Hex, CFs), (M-11417, CHs, F, CI, c-Hex, Br), (M-11418, CHs, F, CI, c-Hex, CH3), (M-11419, CH3, F; CI, OH, H)， (M-11420, CHs, F, CI, OH, CI), (M-11421, CH3; F, CI, OH, F)， (M-11422, CHs, F, CI, OH, CF3), (M-11423, CHs, F, CI, OH, Br), (M-11424, CH3, F, CI, OH, CHs), (M-11425, CHs, F, CI, EtO, H), (M-11426, CH3， F, CI, EtO, CI), (M-11427, CHs, F, CI, EtO, F), (M-11428, CHs, F, Cl, EtO, CFs), (M-11429, CH3, F, Cl, EtO, Br), (M- 11430, CHs, F, Cl, EtO, CHs), (M-11431, CHs, F， Cl, n-PrO, H), (M-11432, CH3) F, Cl, n-PrO, Cl), (M- 11433, CHs, F, Cl, n-PrO; F),,(M-11434, CH3, F, Cl, n-PrO, CFs), (M-11435, CHs, F; Cl, n-PrO, Br), (M-11436, CHs, F, Cl, n-PrO, CH3), (M-11437, CHs, F, Cl, PhO, H), (M- 11438, CHs, F， Cl, PhO, Cl), (M- 11439, CHs, F, Cl, PhO, F), (M- 11440, CHs, F, Cl, PhO, CFs), (M-11441, CHs, F, Cl, PhO, Br), (M- 11442, CHs, F, Cl, PhO, CHs), (M- 11443, CH3, F, Cl, BnO, H), (M-11444, CHs, F， Cl, BnO, Cl), (M- 11445, CH3) F, Cl, BnO, F), (M-11446, CH3) F, Cl, BnO, CFs), (M-11447, CHs, F, Cl, BnO, Br), (M-11448, CHs, F; Cl, BnO, CHs), (M-11449, CH3; F， Cl, PhCH2CH20; H), (M-11450, CHs, F, Cl, P CH2CH20) Cl), (M-11451, CH3, F, Cl, PhCH2CH20, F), (M-11452, CHs, F， Cl, PhCH2CH20, CFs), (M- 11453, CHa, F' Cl, PhCH2CH20, Br), (M-11454, CH3, F, Cl, PhCH2CH20, CHs), (M- 11455, CHs, F， Cl, CFsO, H), (M- 11456, CH3, F， Cl, CFsO, Cl), (M-11457, CHs, F, Cl, CFsO, P), (M- 11458, CHs, F, Cl, CFsO, CFs), (M-11459, CH3, F, Cl, CFsO, Br), (M-11460, CHs, F， Cl, CFsO, CHs), (M-11461, CHs, P, Cl, Ph, H), (M-11462, CHs, F, Cl, Ph, Cl), (M-11463, CH3; F, Cl, Ph, F), (M-11464, CH3; F, Cl, Ph, CFs), (M-11465, CH3; F, Cl, Ph， Br), (M-11466, CH3, F, Cl, Ph, CHs), (M- 11467, CHs, F, Cl, 4-F-Ph, H), (M-11468, CHs, F, Cl, 4-F-Ph; Cl), (M- 11469, CH3, F, Cl, 4-F-Ph, F), (M-11470, CHs, F, Cl, 4-F-Ph, CFs), (M-11471, CHs, F, Cl, 4-F-Ph, Br), (M-11472, CH3; F, Cl, 4-F-Ph, CHs), (M- 11473, CH3) F, Cl, 4-CF3- Ph, H), (M-11474, CHs, F, Cl, 4-CF3-Ph; Cl), (M-11475, CHs, F, Cl, 4-CF3-Pli， F), (M-11476, CHs, F, Cl, 4-CFs-Pli, CFs), (M- 11477, CH3) F, Cl, 4-CF3-Ph, Br), (M- 11478, CHa, F, Cl, 4-CF3-Ph, CHs), (M-11479, CH3) F， Cl, 4-(Me)2N-Ph) H), (M- 11480, CHs, F, Cl, 4-(Me)2N-Ph, Cl), (M-11481, CHs, F, Cl, 4-(Me)2N-Ph) F), (M-11482, CH3, F, Cl, 4-(Me)2N-Ph, CFs), (M-11483, CHs, F, Cl, 4-(Me)2N-Pli, Br), (M-11484, CH3; F, Cl, 4-(Me)2N-Ph; CHs), (M-11485, CHs, F, Cl, 4-OH-Ph, H), (M-11486, CHs, F, CI, 4-OH-Ph, CI), (M-11487, CH3, F, CI, 4-OH-Pli, F), (M-11488, CH3) F, CI, 4-OH-Ph, CFs), (M-11489, CHs, F, CI, 4-OH-Ph, Br), (M-11490, CHs, F, CI, 4-OH-Ph, CH3), (M-11491, CH3， F, CI, 3,4-di-F-Ph, H), (M-11492, CHs, F, CI, 3,4-di-F-Ph, CI), (M-11493, CHs, F, CI, 3,4-di-F-Ph, F); (M-11494, CH3, F, CI, 3,4-di-F-Ph, CFs), (M-11495, CH3, F， CI, 3,4-di-F-Ph, Br), (M-11496, CH3, F, CI, 3,4-di-F-Ph, CHs), (M-11497, CHs, F, CI, 4-COOH-Ph, H), (M-11498, CHs, F, CI, 4-COOH-Ph, CI), (M-11499, CH3; F, CI, 4-COOH-Ph, F), (M-11500, CHs, F, CI, 4-COOH-Ph, CF3), (M-11501, CH3, F, CI, 4-COOH-Ph, Br), (M-11502, CH8) F, CI, 4-COOH-Ph, CH3), (M-11503, CH3, F, CI, Bn, H), (M-11504, CHa, F, CI, Bn, CI), (M-11505, CH3, F, CI, Bn, F), (M-11506, CH3; F, CI, Bn, CFs), (M-11507, CHs, F, CI, Bn, Br), (M-11508, CHs, F, CI, Bn, CHs), (M-11509, CHs, F, CI, 4-F-Bn, H), (M-11510, CHa, F, CI, 4-F-Bn, CI), (M-11511, CH3) F， CI, 4-F-Bn, F), (M-11512, CH3) F, CI, 4-F-Bn, CF3), (M-11513, CHs, F， CI, 4-F-Bn, Br), (M-11514, CHs, F, CI, 4-F-Bn, CHs), (M-11515, CHs, F， CI, 2- Py, H), (M-11516, CHs, F, CI, 2-Py, CI), (M-11517, CH3, F, CI, 2-Py, F), (M-
11518， CHs, F, CI, 2-Py, CFs), (M-11519, CH3, F, CI, 2-Py, Br), (M-11520, CH3, F， CI, 2-Py, CHs), (M-11521, CH3, F, CI, 3-Py, H), (M-11522, CHs, F， CI, 3-Py, CI), (M-11523, CHs, F, CI, 3-Py, F)， (M-11524, CH3, F， CI, 3-Py, CFs), (M-11525, CHs, F, CI, 3-Py, Br), (M-11526, CH3， F, CI, 3-Py, CHs), (M-11527, CH3; F, CI, 4-Py, H); (M-11528, CHs, F, Cl， 4-Py, CI), (M-11529, CHs, F, CI, 4-Py, F), (M- 11530, CHs, F， CI, 4-Py, CFs), (M-11531, CHs, F, CI, 4-Py, Br), (M-11532, CH3; F, CI,— ,4-Py, CHs), (M-11533, CH3, F, CI, 2-Th, H), (M-11534, CHs, F, CI, 2-Th, CI), (M-11535, CHa, F, CI, 2-Th, F), (M-11536, CH3; F, CI, 2-Th, CF3), (M-11537, CHs, F, CI, 2-Th., Br), (M-11538, CHs, F, CI, 2-Th, CH3), (M-11539, CHs, F, CI, 3-Th, H), (M-11540, CH3) F， CI, 3-Th, CI), (M-11541, CHs, F, CI, 3-Th, F), (M- 11542, CHs, F, CI, 3-Th, CFs), (M-11543, CH3) F, CI, 3-Th, Br), (M-11544, CH3, t
o
Figure imgf000292_0001
(Me)2NCOCH2CH2CH2CH2, F); (M-11590, CHs, F, CI,
(Me)2NCOCH2CH2CH2CH2, CF3), (M-11591, CH3, F, CI,
(Me)2NCOCH2CH2CH2CH2, Br), (M-11592, CHs, F, CI,
(Me)2NCOCH2CH2CH2CH2, CHs), (M-11593, CH3) F, CI,
(Me)2NCOCH2GH2CH2CH2CH2, H)， (M-11594, CH3, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-11595, CHs, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2， F), (M-11596, CH3) P, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-11597, CH3, F, CI,
(Me)2NC0CH2CH2CH2CH2CH2) Br), (M-11598, CH3, F, CI,
(Me)2NCOCH2CH2CH2CH2CH2, CHs), (M-11599, CH3， F， CI, MeOCH2) H), (M- 11600, CHs, F, CI, MeOCE , CI), (M-11601, CHs, F, CI, MeOCHs, F), (M-11602, GH3, F, CI, MeOCH2, CPs), (M-11603, CHs' F, CI, MeOCH2， Br), (M-11604, CH3, F, CI, MeOCH , CH3), (M-11605, CHs, F, CI, EtOCH2) H), (M-11606, CH3) F, CI, EtOCH , CI), (M-11607, CHs, F, CI, EtOCHs, F), (M-11608, CH3, F, CI, EtOCHs, CP3); (M-11609, CH3, F, CI, EtOCH2> Br), (M-11610, CH3, F, CI, EtOCH2, CH3), (M-11611, CHs, F, CI, EtOCH2CH2, H), (M-11612, CHs, F, CI, EtOCH2CH2, CI), (M-11613, CHs, F， CI, EtOCH2CH2) F), (M-11614, CHs, F' CI, EtOCH2CH2, CFs), (M-11615, CHs, F, CI, EtOCH2CH2; Br), (M-11616, CHs, F' CI, EtOCH2CH2, CHs), (M-11617, CHs, F， CI, MeOCH2CH2OCH2CH2) H), (M-11618, CHs, F, CI, MeOCH2CH2OCH2CH2, CI), (M-11619, CHs, F, CI, MeOCHbCB OCHsCH , F), (M-11620, CHs, F, CI, MeOCHsCHsOCE CHs, CFs), (M-11621, CHs, F, CI, MeOCH2CH20CH2CH2) Br), (M-11622, CH3, F, CI, MeOGH2CH2OCH2CH2, CHs), (M-11623, CH3) F, CI, MeOCH2CH2; H), (M-11624, CHs, F, CI,
MeOCH2CH2) CI), (M-11625, CHs, F, CI, MeOCH2CH2; F), (M-11626, CHs, F, CI, MeOCH2CH2; CFs), (M-11627, CH3, F, CI, MeOCH2CH2, Br), (M-11628, CHs, F, CI, MeOCH2CH2) CHs), (M-11629, CHs, F, CI, HOCHa, H)， (M-11630, CH3) P, CI, HOCH2, CI), (M-11631, CH3, F' CI, HOCH2, F), (M-11632, CH3) F, CI, HOCH2, CFs), (M-11633, CHs, F, CI, HOCH2> Br), (M-11634, CHs, F, CI, HOCHa, CHs), (M-11635, CHs, F, CI, HOCH2CH2) H), (M-11636, CHs, F, CI, HOCH2CH2; CI), (M-11637, CHs, F, CI, HOCH2CH2, F), (M-11638, CHs, F, CI, HOCH2CH2, CFs), (M-11639, CHs, F, CI, HOCH2CH2， Br), (M-11640, CH3, F, Cl， HOCH2CH2; CH3), (M-11641, CH3, F, CI, HOCH2CH2CH2, H), (M-11642, CH3, F, CI,
HOCH2CH2CH2, CI), (M-11643, CHs, F, CI, HOCHsCHsCH , F), (M-11644, CH3, F， CI, HOCH2CH2CH2, CP3), (M-11645, CH3, F, CI, HOCH2CH2CH2) Br), (M- 11646, CH3, F, CI, HOCH2CH2CH2, CHs), (M-11647, CH3, F， CI,
HOCH2CH2CH2CH2, H), (M-11648, CH3, F， CI, HOCH2CH2GH2CH2, CI), (M- 11649, CHs, F, CI, HOCH2CH2CH2CH2, F)， (M-11650, CHs, F, CI,
HOCH2CH2CH2CH2, CF3), (M-11651, CH3, F, CI, HOCH2CH2CH2CH2, Br), (M-11652, CHs, F, CI, HOCH2CH2CH2CH2; CHs), (M-11653, CH3, F, CI, HOCHaCHsCHsCHsCHs, H), (M-11654, CHs, F, CI, HOCH2CH2CH2CH2CH2, CI), (M-11655, CHs, F, CI, HOCH2CH2CH2CH2CH2， F), (M-11656, CHs, F, CI,
HOCH2CH2CH2CH2CH2, CFs), (M-11657, CHs, F, CI, HOCH2CH2CH2CH2CH2.. Br), (M-11658, CHs, F, CI, HOCH2CH2CH2CH2CH2, CHs), (M-11659, CHs, F, CI, HOCH2CH2OCH2CH2, H), (M-11660, CHs, F, CI, HOCH2CH2OCH2CH2, CI), (M-11661, CHs, F, CI, HOCH2CH20CH2CH2) F), (M-11662, CH3) F, CI,
HOCH2CH2OCH2CH2, CF3), (M-11663, CHs, F, CI, HOCH2CH2OCH2CH2, Br), (M-11664, CHs, F, CI, HOCH2CH2OCH2CH2.. CHs), (M-11665, CHs, F; CI, (Me)2N, H), (M-11666, CH3) F, CI, (Me)2N, CI), (M-11667, CHs, F, Cl， (Me)2N, F), (M-11668, CH3) F, CI, (Me)2N, CF3), (M-11669, CHs, F, CI, (Me)2N, Br), (M- 11670, CH3; F, CI, (Me)2N, CHs), (M-11671, CHs, P, CI, piperidin-4-yl-methyl, H), (M-11672, CHs, F, CI, piperidin-4-yl-methyl, CI), (M-11673, CH3, F, CI, piperidin-4-yl-methyl, F), (M-11674, CHs, F, CI, piperidin-4-yl-metliyl, CFs), (M-11675, CH3, P, CI, piperidm-4-yl-methyl; Br), (M-11676, CHs, F; CI, piperidin-4-yl-methyl; CHs), (M-11677, CHs, F, CI, cyclohexylmethyl, H), (M- 11678, CHs, F, CI, cyclohexylmethyl, CI), (M-11679, CHs, F, CI,
cyclohexylmethyl, F), (M-11680, CHs, F, CI, cyclohexylmethyl, CFs), (M-11681, CH3, F, CI, cyclohexylmethyl, Br), (M-11682, CHs, F, CI, cyclohexylmethyl, CHs), (M-11683, CHs, CHs, H, H， H), (M-11684, CHs, CHs, H, H, CI), (M-11685, CHs, CHs, H, H, F), (M-11686, CHs, CHs, H, H, CFs), (M-11687, CHs, CH3) H, H, Br), (M-11688, CHs, CH3) H, H， CHs), (M-11689, CHs, CHs, H, F, H), (M-11690, CHs, CH3, H, F， CI), (M-11691, CH3) CHs, H, F, F), (M-11692, CH3; CH3) H, P, CF3), (M-11693, CH3, CH3, H, F, Br), (M-11694, CH3, CHs, H, F, CH3), (M-11695, CHs, CH3; H, CI, H), (M-11696, CHs, CHs, H, CI, CI), (M-11697, CHs, CHs, H, CI, F), (M-11698, CHs, CHs, H, CI, CFs), (M-11699, CHs, CHs, H, CI, Br), (M-11700, CHs, CHs, H, CI, CH3), (M-11701, CHs, CHs, H; CHs, H), (M-11702, CHs, CHs, H' CHs, CI), (M-11703, CHs, CH3) H, CH3) F), (M- 11704, CH3) CHs, H, CH3, CFs), (M-11705, CH3, CH3, H， CHs, Br), (M-11706, CHs, CHs, H, CHs, CHs), (M-11707, CHs, CH3; H, Et, H), (M-11708, CHs, CHs, H, Et, CI), (M-11709, CHs, CH3, H， Et, F), (M-11710, CH3, CHs, H, Et, CFs), (M-11711, CHs, CHs, H, Et, Br), (M-11712, CHs, CH3, H, Et, CH3), (M-11713, CH3, CHs, H, n-Pr, H), (M-11714, CH3, CH3) H, n-Pr, CI), (M-11715, CH3, CH3) H, n-Pr, F), (M-11716, CH3, CH3, H, n-Pr, CFs), (M-11717, CHs, CHs, H, n-Pr, Br), (M-11718, CHs, CHs, H, n-Pr, CHs), (M-11719, CHs, CHs, H, c-Pr, H), (M-11720, CH3, CHs, H, c-Pr, CI), (M-11721, CHs, CHs, H, c-Pr, F), (M-11722, CHs, CH3, H, c-P.r, CFs), (M-11723, CH3, CHs, H, c-Pr, Br), (M-11724, CHs, CH3) H, c-Pr, CHs), (M-11725, CH3, CH3, H， i-Pr, H), (M-11726, CHs, CHs, H, i-Pr, CI), (M-11727, CH3, CH3, H, i-Pr, F), (M-11728, CHs, CHs, H, i-Pr, CFs), (M-11729, CHs, CHs, H, i-Pr, Br), (M-11730, CH3, CH3) H, i-Pr, CHs), (M-11731, CHs, CH3; H, n-Bu, H), (M-11732, CH3， CHs, H, n-Bu, CI), (M-11733, CH3， CH3, H, n-Bu, F), (M-11734, CHs, CHs, H, n-Bu, CFs), (M-11735, CHs, CH3> H, n-Bu, Br), (M-11736, CHs, CHa, H, n-Bu, CHs), (M- 11737, CHs, CHs, H, i-Bu, H), (M-11738, CHs, CHs, H, i-Bu, CI), (M-11739, CH3, CH3, H, i-Bu, F)， (M-11740, CHs, CH3; H, i-Bu, CF3), (M-11741, CHs, CH3; H, i-Bu, Br), (M-11742, CHs, CHs, H, i-Bu, CHs), (M-11743, CH3, CHs, H, sec-Bu, H), (M-11744, CHs, CH3) H, sec-Bu, CI), (M-11745, CHs, CHs, H, sec-Bu, F), (M-11746, CHs, CHs, H, sec-Bu, CFs), (M-11747, CH3, CH3, H, sec-Bu, Br), (M- 11748, CHs, CHs, H, sec-Bu, CHs), (M-11749, CHs, CH3, H, n-Pen, H), (M- 11750, CH3) CH3; H, n-Pen, CI), (M-11751, CHs, CHa, H, n-Pen, F)， (M-11752, CH3, CHs, H, n-Pen, CFs), (M-11753, CH3; CH3) H, n-Pen, Br), (M-11754, CH3; CHs, H, n-Pen, CHa), (M-11755, CHs, CH3, H, c-Pen, H), (M-11756, CHs, CHs, H, c-Pen, CI), (M-11757, CHs, CH3, H; c-Pen, F), (M-11758, CHs, CH3, H, c-Pen, CFs), (M-11759, CHs, CH3; H， c-Pen, Br), (M-11760, CHs, CHs, H, c-Pen, CHs), (M-11761, CHs, CHs, H, n-Hex, H), (M-11762, CHs, CH3, H, n-Hex, CI), CM- 11763, CHs, CHs, H, n-Hex, F), (M-11764, CH3， CH3; H, n-Hex, CFs), (M-11765, CHs, CHs, H， n-Hex, Br), (M-11766, CHs, CHs, H, n-Hex, CHs), (M-11767, CHs, CHs, H, c-Hex, H), (M-11768, CHs, CHs, H, c-Hex, CI), (M-11769, CHs, CH3, H, c-Hex, F), (M-11770, CH3, CHs, H, c-Hex, CFs), (M-11771, CHs, CHs, H, c-Hex, Br), (M-11772, CH3, CHa, H, c-Hex, CHs), (M-11773, CHs, CH3, H, OH, H)， (M-11774, CHs, CHs, H, OH, CI), (M-11775, CH3, CHs, H, OH, F), (M-11776, CHs, CH3， H, OH, CF3); (M-11777, CH3, CHs, H, OH, Br), (M-11778, CHs, CHs, H， OH, CH3), (M-.11779, CHs, CH3, H， EtO, H), (M-11780, CH3, CH3; H, EtO, .CI), (M-11781, CH3, CH3) H, EtO, F), (M-11782, CHs, CHs, H, EtO, CPs), (M-11783, CH3, CH3) H, EtO, Br), (M-11784, CHs, CHs, H, EtO, CH3); (M-11785, CH3, CH3, H, n-PrO, H), (M-11786, CH3; CH3; H, n-PrO; CI), (M-11787, CHs, CH3, H, n- PrO; F), (M-11788, CH3, CH3, H, n-PrO, CFs), (M-11789, CH3, CH3, H, n-PrO, Br), (M-11790, CHs, CHs, H, n-PrO, CHa), (M-11791, CHs, CHs, H, PhO, H), (M-11792, CHs, CHs, H, PhO, CI), (M-11793, CH3, CH3, H, PhO, F), (M-11794, CHs, CHs, H, PhO, CFs), (M-11795, CHs, CH3) H, PhO, Br), (M-11796, CHs, CHa, H, PhO, CHs), (M-11797, CHs, CH3) H, BnO, H), (M-11798, CH3, CHs, H， BnO, CI), (M-11799, CHs, CHs, H; BnO, F), (M-11800, CHs, CH8) H, BnO, CF3), (M- 11801, CHa, GH3， H, BnO, Br), (M-11802, CHs, CH3, H， BnO, CHs), (M-11803, CHs, CH3, H, PI1CH2CH2O, H), (M-11804, CHs, CH3) H, PI1CH2CH2O, CI), (M- 11805, CHs, CHs, H' PhCH2CH20; F), (M-11806, CHs, CHs, H, P CH2CH20; CFs), (M-11807, CH3, GH3) H, PhCH2CH20; Br), (M-11808, CHs, CH3) H, P CH2CH20; CHs), (M-11809, CHs, CH3, H, CF3O, H), (M-11810, CH3, CH3， H, CFsO, CI), (M-11811, CH3, CHs, H, CFsO, F), (M-11812, CHs, CHs, H; CFsO, CFs), (M-11813, CHs, CH3, H, CFsO, Br), (M-11814, CH3) CH3, H, CFsO, CHs), (M-11815, CH3, CHs, H, Ph， H), (M-11816, CHs, CH3, H, Ph, CI), (M-11817, CH3) CHs, H, Ph, F), (M-11818, CHs, CH3, H, Ph, CF3); (M-11819, CHs, CHs, H, Ph, Br), (M-11820, CHs, CHs, H, Ph, CHs), (M-11821, CHs, CH3， H, 4-F-Ph, H), (M-11822, CHs, CHa, H, 4-F-Ph, CI), (M-11823, CHs, CHs, H, 4-F-Ph, F), (M- 11824, CHs, CHs, H, 4-F-Ph, CFs), (M-11825, CH3， CH3, H, 4-F-Ph, Br), (M- 11826, CHs, CH3, H, 4-F-Ph, CHa), (M-11827, CHs, CH3; H, 4-CFs-Ph, H), (M- 11828, CHs, CHa, H; 4-CFa-Pli, CI), (M-11829, CHs, CH3) H, 4-CFs-Ph, F), (M- 11830, CHs, CH3) H, 4-CP3-Ph, CFs), (M-11831, CHs, CHs, H, 4-CF3-Ph, Br), (M-11832, CHs, CHa, H, 4-CF3-Ph; CHs), (M-11833, CHs, CH3, H, 4-(Me)2N-Ph, H), (M-11834, CHs, CHs, H, 4-(Me)2N-P ) CI), (M-11835, CH3, CHs, H, 4- (Me)2N-Ph; F)，（M-11836, CH3; CH3, H, 4-(Me)2N-Ph, CF3), (M-11837, CHa, CH3) H， 4-(Me)2N-Ph, Br), (M-11838, CH3) CH3, H, 4-(Me)2N-Ph, CH3), (M-11839, CH3) CHs, H, 4-OH-Ph, H), (M-11840, CHs, CH3) H, 4-OH-Ph; CI), (M-11841, CHs, CH3) H, 4-OH-Ph, F), (M-11842, CHs, CHs, H, 4-OH-Ph, CFs), (M-11843, 〇 )),,,SF 898 C C 3Tli7 CHH C 89 BrH-
Figure imgf000298_0001
,,),),F, CsH C 8s0345H 4Hh44 C CHP 8p BrHH H 4 CH---- CHs), (M-11899, CHs, CHa, H, pyrazol-2-yl, H), (M-11900, CH3; CHs, H, pyrazol-2-yl, CI), (M-11901, CHs, CHs, H, pyrazol-2-yl, F), (M-11902, CH3; CHs, H, pyrazol-2-yl, CFs), (M-11903, GH3, CH3; H, pyrazol-2-yl, Br), (M-11904, CHs, CHs, H, pyrazol-2-yl, CH3), (M-11905, CHs, CH3, H, pyrazol-3-yl, H), (M-11906, CHs, CHs, H, pyrazol-3-yl, CI), (M-11907, CHs, CHs, H, pyrazol-3-yl, F), (M- 11908, CHs, CHs, H, pyrazol-3-yl, CFs), (M-11909, CHs, CHs, H; pyrazol-3-yl, Br), (M-11910, CH3, CH3, H, pyrazol-3-yl, CHa), (M-11911, CHs, CHs, H, pyrimidin-2-yl, H), (M-11912, CHs, CHs, H, pyrimidin-2-yl, CI), (M-11913, CHs, CHs, H, pyrimidin-2-yl, F)，（M-11914, CH3, CH3, H, pyrimidin-2-yl, CFs), (M- 11915, CH3, CHs, H, pyrimidm-2-yl, Br), (M-11916, CHa, CHa, H, pyrimidin- 2-yl, CH3), (M-11917, CHs, CHa, H， pyrimidin-4-yl, H)， (M-11918, CH3, CHs, H, pyrimidin-4-yl, CI), (M-11919, CHs, CHs, H, pyrimidin-4-yl, F), (M-11920, CH3, CHs, H, pyrimidin-4-yl, CF3), (M-11921, CHa, CH3) H, pyrimidin-4-yl, Br), (M- 11922, CHs, CH3> H, pyrimidin-4-yl, CHs), (M-11923, CHs, CHs, H, pyrimidin-5-yl, H), (M-11924, CHa, CHs, H, pyrimidin-5-yl, CI), (M-11925, CHs, CHs, H, pyriraidin-5-yl, F), (M-11926, CHs, CHs, H， pyrimidin-5-yl, CFs), (M- 11927, CHs, CHs, H, pyrimidin-5-yl, Br), (M-11928, CHs, CHs, H, pyrimidin- 5-yl, CHs), (M-11929, CHs, CHs, H, HOOCCH2CH2CH2, H), (M-11930, CHs, CHs, H, HOOCCH2CH2CH2; CI), (M-11931, CHa, CH3) H, HOOCCH2CH2CH2, F), (M-11932, CHs, CHs, H, HOOCCH2CH2CH2, CFs), (M-11933, CHs, CHs, H, HOOCCH2CH2CH2, Br), (M-11934, CHs, CH3) H, HOOCCH2CH2CH2, CHs), (M-11935, CH3， CH3, H， HOOCCH2CH2CH2CH2, H), (M-11936, CHa, CHs, H, HOOCCH2CH2CH2CH2j CI), (M-11937, CH3, CH3; H, HOOCCH2CH2CH2CH2, F), (M-11938, CHs, CHa, H, HOOCCH2CH2CH2CH2, CF3), (M-11939, CHs, CHa, H, HOOCCH2CH2CH2CH2, Br), (M-11940, CHs, CHs, H, HOOCCH2CH2CH2CH2， CHs), (M-11941, CHs, CHs, H, (Me^NCOCHsCHsCHsCB , H), (M-11942, CHs, CH3) H, (Me)2NCOCH2CH2CH2CH2, CI), (M-11943, CH3; CHs, H,
(Me)2NCOCH2CH2CH2CH2, F), (M-11944, CHs, CH3, H,
(Me)2NCOCH2CH2CH2CH2; CFs), (M-11945, CHs, CHs, H,
(Me)2NCOCH2CH2CH2CH2) Br), (M-11946, CH3, CHs, H,
(Me)2NCOCH2CH2CH2CH2, CHs), (M-11947, CH3' CH3, H,
(Me)2NC0CH2CH2CH2CH2CH2) H), (M-11948, CH3; CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2, CI), (M-11949, CHs, CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2， F)， (M-11950, CH3, CH3, H,
(Me)2NC0CH2CH2CH2CH2CH2, CPs), (M-11951, CH3, CHs, H,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-11952, CHs, CH3, H,
(Me)2NCOCH2CH2CH2CH2CH2, CH3)， (M-11953, CH3, CHs, H, MeOCH2, H), (M-11954, CH3, CHs, H， MeOCH2, CI), (M-11955, CHs, CH3, H, MeOCH2, F), (M-11956, CH3, CHs, H, MeOCH2, CFs), (M-11957, CH3, CH3; H, MeOCH2) Br), (M-11958, CHs, CH3, H, MeOCH2, CHs), (M-11959, CHg, CHs, H' EtOCH2， H), (M-11960, CH3， CHs, H, EtOCHa, CI), (M-11961, CHs, CHs, H, EtOCHs, F),
(M-11962, CH3, CHs, H, EtOCH2, CFs), (M-11963, CHs, CH3, H, EtOCH2, Br), (M-11964, CHs, CHs, H, EtOCH2， CHs), (M-11965, CH3j CHs, H; EtOCH2CH2, H), (M-11966, CHs, CHs, H, EtOCH2CH2j CI), (M-11967, CHs, CHs, H,
EtOCH2CH2, F)， (M-11968, CH3; CH3, H, EtOCH2CH2) CFs), (M-11969, CHa, CH3, H, EtOCH2CH2) Br), (M-11970, CHs, CHs, H, EtOCH2CH2, CHa), (M- 11971, CH3) CHs, H, MeOCU2CH2OCH2CH2, H), (M-11972, CH3, CH3; H, MeOCH2CH2OCH2CH2, CI), (M-11973, CH3， CH3) H, MeOCH2CH2OCH2CH2, F), (M-11974, CH3; CHs, H, MeOCH2CH20CH2CH2， CFa), (M-11975, CH3, CH3, H, MeOCH2CH2OCH2CH2, Br), (M-11976, CHs, CH3, H, MeOCH2CH2OCH2CH2, CHs), (M-11977, CHs, CH3, H, MeOCH2CH2, H), (M-11978, CH8; CH3, H,
MeOCH2CH2, CI), (M-11979, CH3) CH3, H， MeOCH2CH2, F), (M-11980, CHs, CHs, H, MeOCH2CH2; CPs), (M-11981, CHs, CH3, H, MeOCH2CH2, Br), (M- 11982, CHs, CHs, H, MeOCH2CH2) CHs), (M-11983, CHs, CHs, H， HOCH2, H), (M-11984, CH3, CH3; H, HOCH2) CI), (M-11985, CH3) CH3> H; HOCH2; F), (M- 11986, CHs, CH3; H, HO CH2, CFs), (M-11987, CHs, CHs, H, HOCH2, Br), (M- 11988, CHs, CHs, H, HOCH2; CHs), (M-11989, CH3; CH3; H, HOCH2CH2, H)， (M-11990, CH3, CH3, H, HOCH2CH2, CI), (M-11991, CH3, CHs, H, HOCH2CH2, F), (M-11992, CH3, CHs, H, HOCH2CH2) CFs), (M-11993, CH3; CH3) H,
HOCH2CH2! Br), (M-11994, CH3, CHs, H, HOCH2CH2, CHs), (M-11995, CH3, CHs, H, H0CH2CH2CH2) H), (M-11996, CHs, CHs, H, HOCH2CH2CU2, CI), (M-11997, CH3, CHs, H, HOCH2CH2CH2, F), (M-11998, CHs, CHs, H,
HOCH2CH2CH2, CFs), (M-11999, CH3, CHs, H, HOCH2CH2GH2, Br), (M-12000, CHs, CH3, H, HO CH2CH2CH2) CHs), (M-12001, CH3, CH3, H,
HOCH2CH2CH2CH2, H), (M-12002, CHs, CH3, H, HOCH2CH2CH2CH2， CI), (M- 12003, CI-I3, CHs, H, HO CH2CH2CH2CH2, F), (M- 12004, CH3, CHs, H,
HOCH2CH2CH2CH2， CFs), (M-12005, CH3， CHs, H, HOCH2CH2CH2CH2, Br), (M-12006, CH3, CH3, H, HOCH2CH2CH2CH2; CHs), (M-12007, CHs, CH3; H, HOCHaCHsCHaCHsCHs, H), (M-12008, CHs, CHs, H, HOCH2CH2CH2CH2CH2, CI), (M-12009, CHs, CHs, H, HOCH2CH2CH2CH2CH2, F), (M-12010, CH3, CHs, H, HO CH2CH2CH2CH2CH2, CFs), (M-12011, CHs, CH3) H，
HO CH2CH2CH2CH2CH2, Br), (M-12012, CHs, CH3, H, HOCB CHsCHsCHsCHs, CH3), (M-12013, CHs, CHs, H， HO CH2CH2O CH2CH2, H), (M-12014, CHs, CHs, H, HO CH2GH2OCH2CH2, CI), (M-12015, CHs, CH3, H, HO CH2CH2O CH2CH2, F), (M-12016, CHs, CHs, H, HOCH2CH2O.CH2CH2; CF3), (M-12017, CHs, CH3, H, HOCH2CH2OCH2CH2, Br), (M-12018, CHs, CH3, H, HOCH2CH2OCH2CH2, CH3), (M-12019, CHs, CHs, H, (Me)2N, H), (M-12020, G C H, (Me)2N, CI), (M- 12021, CH3) CHs, H, (Me)2N, F), (M-12022, CH3; CH3) H, (Me)2N, CFs), (M- 12023, CH3, CHs, H, (Me)2N; Br), (M-12024, CH3; CHs, H, (Me)2N, CHs), (M- 12025, CHs, CHs, H, piperidin-4-yl-methyl, H), (M-12026, CHs, CHs, H, piperidin-4-yl-metliyl, CI), (M-12027, CH3) CH3) H, piperidin-4-yl-metliyl, F)， (M-12028, CHs, CHs, H, piperidin-4-yl-methyl, CF3), (M-12029, CHs, CHs, H, piperidm-4-yl-methyl, Br), (M-12030, CHs, CHs, H， piperidin-4-yレ methyl, CHs), (M-12031, CHs, CHs, H, cyclohexylmethyl, H), (M-12032, CHs, CHs, H, cyclohexylmethyl, CI), (M-12033, CH3, CHs, H, cyclohexylmethyl, F), (M-12034, CHs, CHs, H, cyclohexylmethyl, CF3), (M-12035, CH3, CHs, H,
cyclohexylmethyl, Br), (M-12036, CHs, CHs, H, cyclohexylmethyl, CHs), (M- 12037, CHs, CHs, F, H， H), (M-12038, CH3) CH3, F, H， CI), (M-12039, CH3; CHs, F, H, F), (M-12040, CH3, CHs, F, H, CFs), (M-12041, CH3; CH3, F, H, Br), (M- 12042, CH3, CH3) F， H， CH3), (M-12043, CHs, CHs, F, F, H), (M-12044, CH3, CHs, F, F， CI), (M-12045, CHs, CHs, F, F, F), (M-12046, CHs, CHs, F, F, CF3), (M-12047, CHs, CH3) F, F, Br), (M-12048, CH3> CH3, F, F, CHs), (M-12049, CH3; CH3; F, CI, H), (M-12050, CH3, CHs, F, CI, CI), (M-12051, CHs, CHs, F， CI, F)， (M-12052, CHs, CH3j F, CI, CF3), (M-12053, CH3, CHs, F, CI, Br), (M-12054, CHs, CH3, F, CI, CHs), (M- 12055, CHs, CHs, F, CH3, H), (M-12056, CH3, CHs, F, CHs, CI), (M-12057, CH3, CHs, F, CHs, F), (M-12058, CH3; CHs, F, CHs, CFs), (M-12059, CH3, CHs, F， CHs, Br), (M-12060, CHs, CH3) F, CHs, CH3), (M-12061, CH3, CHs, F, Et, H), (M-12062, CH3, CHs, F, Et, CI), (M-12063, CHs, CHs, F, Et, F), (M-12064, CHs, CHs, F' Et, CFs), (M-12065, CH3, CH3, F, Et, Br), (M-12066, CHs, CH3) F， Et, CH3), (M-12067, CHs, CH3, F， n-Pr, H), (M-12068, CHs, CH3, F, n-Pr, CI), (M-12069, CH3) CH3) F, n-Pr, F), (M-12070, CH3, CH3) F, n-Pr, CFs), (M-12071, CH3) CHs, F, n-Pr, Br), (M- 12072, CHs, CHs, F, n-Pr, CHs), (M-12073, CHs, CH3, F, c-Pr, H), (M- 12074, CH3， CH3， F, c-Pr, CI), (M-12075, CHs, CH3, F, c-Pr, F), (M-12076, CHs, CH3, F, c-Pr, CFs), (M-12077, CHs, CHs, F, c-Pr, Br), (M-12078, CHs, CH3) F, c-Pr, CHs), (M-12079, CH3) CHs, F, i-Pr, H), (M-12080, CHs, CH3) F, i-Pr, CI), (M-12081, CH3, CHs, F, i-Pr, F), (M-12082, CHs, CH3, F, i-Pr, CFs), (M-12083, CH3; CHs, F, i-Pr, Br), (M-12084, CH3, CHs, F， i-Pr, CH3), (M-12085, CH3; CHa, F, n-Bu, H), (M-12086, CHs, CHs, F, n-Bu, CI), (M-12087, CHs, CHs, F, n-Bu, F), (M-12088, CH3, CH3; F, n-Bu, CFs), (M-12089, CH3> CHs, F, n-Bu, Br), (M-12090, CHs, CH3, F, n-Bu, CHs), (M-12091, CH3, CHs, F, i-Bu, H), (M-12092, CH3， CH3) F, i-Bu, CI), (M-12093, CH3, CH3, F, i-Bu, F)， (M- 12094, CHs, CHs, F, i-Bu, CFs), (M-12095, CHs, CHs, F, i-Bu, Br), (M-12096, CH3) CH3, F, i-Bu, CHs), (M-12097, CH3, CHs, F, sec-Bu, H), (M-12098, CHs, CHs, F, sec-Bu, CI), (M-12099, CHs, CHs, F, sec-Bu, F), (M-12100, CH3, CHs, F, sec-Bu, CFs), (M-12101, CHs, CH3, F, sec-Bu, Br), (M-12102, CHs, CHs, F, sec-Bu, CHs), (M-12103, CHs, CHs, F, n-Pen, H), (M-12104, CHs, CH3， F, n-Pen, CI), (M-12105, CHs, CH3; F, n-Pen, F), (M-12106, CHs, CH3) F, n-Pen, CFs), (M-12107, CHs, CHs, F, n-Pen, Br), (M-12108, CHs, CHs, F, n-Pen, CHa), (M- 12109, CHs, CHs, F, c-Pen, H), (M-12110, CH3, CHs, F, c-Pen, CI), (M-12111, CHs, CHa, F, c-Pen, F), (M-12112, CH3, CHs, F， c-Pen, CFs), (M-12113, CHs, CH3; F, c-Pen, Br), (M-12114, CHs, CHs, F, c-Pen, CH3), (M-12115, CHs, CH3, F, n-Hex, H)' (M-12116, CH3) CH3' F， n-Hex, CI), (M-12117, CHs, CHs, F, n-Hex, F), (M-12118, CHs, CHs, F, n-Hex, CFs), (M-12119, CH3; CH3) F, n-Hex, Br), (M-12120, CH3; CH3; F, n-Hex, CHs), (M-12121, CHs, CHa, P, c-Hex, H), (M- 12122, CHa, CHs, F, c-Hex, CI), (M-12123, CHs, CH3) F, c-Hex, F), (M-12124, CHs, CH3, F, c-Hex, CF3); ( . 2125, CHs, CHs, F, c-Hex, Br), (M-12126, CHa, CH3; F' c-Hex, CHs), (M-12127, CH3; CH3) F, OH, H), (M-12128, CH3) CHs, F, OH, CI), (M-12129, CH3> CHs, F, OH, F), (M-12130, CHs, CHs, F, OH, CFs), (M-12131, CHs, CHs, F, OH, Br), (M-12132, CH3, CH3, F, OH, CHs), (M-12133, CHs, CH3, F, EtO, H), (M-12134, CH3, CHs, P, EtO, CI), (M-12135, CHs, CH3; F， EtO, F), (M-12136, CHs, CHs, F, EtO, CFs), (M-12137, CH3, CHs, F, EtO, Br), (M-12138, CHs, CHs, F, EtO, CH3), (M-12139, CHs, CHs, P, n-PrO, H), (M- 12140, CHs, CHs, F, n-PrO, CI), (M-12141, CH3) CHs, F, n-PrO, F), (M-12142, CHs, CHs, F, n-PrO, CFs), (M-12143, CHs, CHs, F， n-PrO, Br), (M-12144, CHs, CHs, F, n-PrO, CHs), (M-12145, CHs, CHs, F, PhO, H), (M-12146, CHs, CH3; P, PhO, CI), (M-12147, CH3, CH3) F, PhO, F), (M-12148, CHs, CHs, P; PhO, CF3), (M-12149, CHs, CHs, F, PhO, Br), (M-12150, CHs, CHs, F, PhO, CH3), (M-12151, CHs, CHs, F， BnO, H)' (M-12152, CHs, CHs, F, BnO, CI), (M-12153, CHs, CHs, F, BnO, F), (M- 12154, CH3, CH3, F, BnO, CFs), (M-12155, CH3, CH3, F, BnO, Br), (M-12156, CHs, CHs, F, BnO, CHs), (M-12157, CHs, CHs, F， PhCBbCHsO, H), (M-12158, CHs, CHs, F, PhCH CE O, CI), (M-12159, CHs, CH3, F, PI1CH2CH2O, F), (M-12160, CH3, CH3, F, PhCH2CH20, CFs), (M- 12161, CHs, CHs, F,
PhCHaCHaO, Br), (M-12162, CHs, CHs, F, PhCHsCHsO, CH3), (M-12163, CH3, CH3) F, CF30, H), (M-12164, CHs, CHs, P, CFsO, CI), (M-12165, CH3; CHs, F， CFsO, F), (M-12166, CHs, CHs, F, CFsO, CFs), (M-12167, CHs, CHs, F, CFsO, Br), (M-12168, CHs, CH3) F, CFsO, CHs), (M- 12169, CHs, CHs, F, Ph, H), (M- 12170, CH3; CHs, F， Ph, CI), (M-12171, CHs, CHs, F, Ph, F), (M-12172, CHs, CHs, F, Ph, CFs), (M- 12173, CHs, CHs, F， Ph, Br), (M-12174, CH3, CHs, P, Ph, CHs), (M-12175, CHs, CHs, F， 4-F-Ph, H), (M-12176, CH3, CH3, F, 4-F-Ph, CI), (M-12177, CHs, CHs, F， 4-F-Ph, F), (M- 12178, CHs, CHs, F, 4-F-Ph, CFs), (M- 12179, CH3, CHs, F, 4-F-Ph, Br), (M- 12180, CH3, CH3, F, 4-F-Ph, CH3), (M- 12181, CH3, CHs, F, 4-CF3-Pli, H), (M-12182, CH3) CH3) F， 4-CF3-Ph, CI), (M- 12183, CH3; CHs, F, 4-CFs-Ph, F)， (M-12184, CHs, CH3) F， 4-CF3-Ph, CPs), (M-12185, CHs, CHs, F, 4-CF3-Ph, Br), (M-12186, CHs, CHs, F, 4-CFa-Ph, CHs), (M-12187, CHs, CHs, F, 4-(Me)2N-Ph, H), (M-12188, CHs, CHs, F, 4-(Me)2N-Ph, CI), (M-12189, GHs, CH3, F, 4-(ΜΘ)2Ν-Ρ1Ι, F), (M-12190, CH3; CHS, F, 4- (Me)2N-Ph, CFs), (M-12191, CHs, CH3, F, 4-(Me)2N-P , Br), (M-12192, CHs, CH3, F， 4-(Me)2N-Pli> CHs), (M-12193, CH3; CHs, F; 4-0H-Ph; H), (M-12194, CHs, CHs, F, 4-OH-Pli, CI), (M-12195, CHs, CH3; F, 4-OH-Ph, F), (M-12196, CH3) CH3, F, 4-OH-Ph, CFs), (M-12197, CH3; CH3) F, 4-OH-Ph, Br), (M-12198, CHs, CH3, F, 4-OH-Ph, CHs), (M-12199, CHs, CH3, F, 3,4-di-F-Ph, H), (M- 12200, CHs, CHs, F, 3,4-di-F-Ph, CI), (M-12201, CHs, CHs, F， 3,4-di-F-Ph, F), (M- 12202, CHs, CHs, F, 3,4-di-F-Ph, CF3), (M-12203, CHs, CH3, F, 3,4-di-F-Ph, Br), (M-12204, CHs, CH3, F, 3,4-di-F-Ph, CHs), (M-12205, CH3) CHs, F, 4-COOH-Ph, H), (M-12206, CHs, CH3) F， 4-COOH-Ph, CI), (M-12207, CHs, CHs, P, 4- COOH-Ph, F), (M-12208, CHs, CH3, F, 4-COOH-Ph, CFs), (M-12209, CH3, CH3> F， 4-COOH-Ph, Br), (M-12210, CHs, CH3, F, 4-COOH-Ph, CHs), (M-12211, CHs, CHs, F, Bn, H), (M-12212, CHs, CHs, F, Bn, CI), (M-12213, CHs, CHs, F, Bn, F), (M-12214, CHs, CH3) F， Bn, CFa), (M-12215, CHs, CHs, F, Bn, Br), (M-12216, CHs, CHs, F, Bn, CH3), (M-12217, CHs, CHs, F, 4-F-Bn, H), (M-12218, CHs, CHs, F' 4-F-Bn, CI), (M-12219, CH3， CHs, F, 4-F-Bn, F), (M-12220, CH3) CHs, F, 4- F-Bii, CFs), (M-12221, CHs, CHs, F, 4-F-Bn, Br), (M-12222, CHs, CH3j F, 4-F- Bn, CHs), (M-12223, CHs, CH3) F, 2-Py, H), (M-12224, CHs, CH3, F, 2-Py, CI), (M-12225, CHs, CH3， F, 2-Py, F), (M-12226, CH3, CH3， F, 2-Py, CFs), (M-12227, CHs, CHs, F, 2-Py, Br), (M-12228, CHs, CHs, F, 2-Py, CHs), (M-12229, CHs, CHs, F, 3-Py, H), (M-12230, CH3) CH3; F, 3-Py, CI), (M-12231, CHs, CH3, F, 3-Py, F), (M-12232, CH3, CH3, F, 3-Py, CFs), (M-12233, CHs, CHs, F, 3-Py; Br), (M-12234, CHs, CH3, F, 3-Py, CHs), (M-12235, CHs, CH3) F, 4-Py, H), (M-12236, CHs, CH3， F, 4-Py, CI), (M-12237, CH3> CH3) F， 4-Py, F); (M-12238, CH3; CHs, F, 4-Py, CFs), (M-12239, CHs, CHs, F, 4-Py, Br), (M-12240, CH3, CHs, F, 4-Py, CHs), (M-12241, CH3, CHs, F, 2-Th, H), (M-12242, CH3) CHs, F, 2-Th, CI), (M-12243, CH3, CHs, F, 2-Th, F), (M-12244, CHs, CHs, F, 2-Th, CFs), (M-12245, CH3, CHs, (NO t
〇
K lN2
Figure imgf000306_0001
p,yy) (¾,,, 3335i CH C Ca H 22TlM 25M Fzol2l4r--- ,,),,),p,, 1a CS50 CHH F 3Ί¾ CS5 CH CH∞ Br22F 2 F-.
3 ,),,,,,, 3 22 CsS CK C FTh Br46 CM F 2Ί¾ 247HH2-- (M-12291, CHs, CHs, F, ΗΟΟΟΟΗ2ΟΗ2θΗ2ΟΗ2> F), (M-12292, CHs, CHs, F, HOOCCH2CH2CH2CH2, CFs), (M-12293, CH3, CH3, F, HOOCCH2CH2CH2CH2, Br), (M-12294, CH3, CHs, F, HOOCCH2CH2CH2CH2， CH3), (M-12295, CH3, CHs, F' (Me)2NCOCH2CH2CH2CH2, H)，（M-12296, CH3; CH3, F,
(Me)2NCOCH2CH2CH2CH2, CI), (M-12297, CH3, CH3) F,
(Me)2NCOCH2CH2CH2CH2) F), (M-12298, CHs, CH3) F，
(Me)2NCOCH2CH2CH2CH2， GF3), (M-12299, CH3， CH3) F，
(Me)2NCOCH2CH2CH2CH2, Br), (M-12300, CH3, CHs, F,
(Me)2NCOCH2CH2CH2CH2， CH3), (M-12301, CH3) CH3) F,
(Me)2NCOCH2CH2CH2CH2CH2, H), (M-12302, CH3， CHs, F,
(Me)2NCOCH2CH2CH2CH2CH2; CI), (M-12303, CH3, CH3> F，
(Me)2NCOCH2CH2CH2CH2CH2, F), (M-12304, CHs, CHs, F，
(Me)2NCOCH2CH2CH2CH2CH2, CFs), (M-12305, CHs, CHs, P,
(Me)2NCOCH2CH2CH2CH2CH2, Br), (M-12306, CH3, CH3, F,
(Me)2NCOGH2CH2CH2CH2CH2, CH3), (M-12307, CHs, CHs, F, MeOCH2, H), (M-12308, CHs, CHs, F, MeOCH2, CI), (M-12309, CHs, CHs, F, MeOCH2, F)， (M-12310, CHs, CHs, F, MeOCH2) CFs), (M-12311, CHs, CHs, F, MeOCHa, Br), (M-12312, CH3, CHa, F, MeOCH2) CH3), (M-12313, CH3, CHs, F, EtOCH2; H), (M-12314, CHs, CH3， F, EtOCHs, CI), (M-12315, CH3, CHs, F, EtOCH2> F), (M-12316, CHs, CHs, F, EtOCH2, CFs), (M-12317, CHs, CHs, F, EtOCHs, Br), (M-12318, CHs, CHa, F, EtOCH2, CHs), (M-12319, CHs, CHs, P, EtOCH2CH2, H), (M-12320, CHs, CHs, F, EtOCH2CH2) CI), (M-12321, CH3, CHs, F, EtOCH2C¾ F), (M-12322, CH3, CHs, F, EtOCH2CH2) CFs), (M-12323, CHs, CHs, F,
EtOCH2CH2j Br), (M-12324, CHs, CHs, F, EtOCH2CH2, CHs), (M-12325, CHs, CHs, F, MeOCHaCHaOCHsCHa, H), (M-12326, CH3) CH3, F,
MeOCH2CH2OCH2CH2, Cl)， (M-12327, CH3j CH3, F, MeOCH2CH2OGH2CH2, F), (M-12328, CHs, CHs, F, MeOCH2CH2OCH2CH2, CFs), (M-12329, CHs, CHs, F， MeOCH2CH2OCH2CH2, Br), (M-12330, CH3, CH3, F， MeOCHsCH OCHsCHs, CH3)， (M-12331, CHs, CHs, F, MeOCH2CH2) H), (M-12332, CHs, CHs, F, MeOCH2CH2, CI), (M-12333, CHs, CHs, F， MeOCH2CH2) F), (M-12334, CH3， CHs, F, MeOCH2CH2, CFs), (M-12335, CHs, CH3) F, MeOCHaCHs, Br), (M- 12336, CH3, CHs, F, MeOCH2CH2; CH3)， (M-12337, CH3, CHs, F， HOCH2, H), (M-12338, CHs, CHs, F, HOCH2; CI), (M-12339, CHs, CHs, F, HOCHa, F), (M- 12340, CHs, CH3, F, HOCH2, CF3), (M-12341, CHs, CHs, F, HOCH2, Br), (M- 12342, CH3> CH3) F， HOCH2) CHs), (M-12343, CH3, CH3, F, HOCH2CH2) H), (M- 12344, CHs, CHs, F， HOCH2CH2, CI), (M-12345, CHs, CH3) F, HOCH2CH2; F), (M-12346, CHs, CH3) F, HOCH2CH2, CPs), (M-12347, CH3) CHs, F,
HOCH2CH2, Br), (M-12348, CH3, CHs, F, HOCH2CH2, CHs), (M-12349, CH3, CHs, F, HOCH2CH2CH2) H), (M-12350, CH3, CH3, F, HOCH2CH2CH2, CI), (M- 12351, CHs, CHs, F， HOCH2CH2CH2, P), (M-12352, CHs, CHs, F,
HOCH2CH2CH2, CFs), (M-12353, CHs, CHs, F, HOCH2CH2CH2, Br), (M-12354, CHs, CHs, P, HOCH2CH2CH2, CHs), (M-12355, CH3, CHs, F,
HOCH2CH2CH2CH2, H), (M-12356, CH3, CHs, F, HOCH2CH2CH2CH2, CI), (M- 12357, CHs, CHs, F, HOCH CH CHsCHs, F), (M-12358, CHs, CH3, F,
HOCH2CH2CH2CH2; CFs), (M-12359, CHs, CH3; F, HOCH2CH2CH2CH2, Br), (M-12360, CHs, CHs, F, HOCH2GH2CH2GH2, CHs), (M-12361, CHs, CHs, F, HOCH2CH2CH2CH2CH2, H), (M-12362, CH3, CHs, F; HOCH2GH2GH2GH2GH2, CI), (M-12363, CHs, CHs, F, HOCH2CH2CH2.CH2CH2, F), (M-12364, CH3, CHs, F, HOCH2CH2CH2CH2CH2; CFs), (M-12365, CHs, CHs, F, HOCHsCHsCHsCB CHs, Br), (M-12366, CHs, CHs, P, HOCH2CH2CH2CH2CH2, CHs), (M-12367, CH3, CH3, F, HOCH2CH20CH2CH2, H), (M-12368, CH3) CH3) F,
HOCH2CH20CH2CH2) CI), (M-12369, CHs, CHs, F, HOCH2CH2OCH2CH2, F), b b
ο o
o
Figure imgf000309_0001
to t 〇
Figure imgf000310_0001
(M-12479, CHs, CH3, CI, c-Hex, Br), (M-12480, CHs, CH3) CI, c-Hex, CHs), (M-12481, CHs, CHs, CI, OH, H), (M-12482, CHs, CH3; CI, OH, CI), (M-12483, CHs, CHs, CI, OH, F), (M-12484, CHs, CH3; CI, OH, CFs), (M-12485, CH3; CH3) CI, OH, Br), (M-12486, CHs, CH3) CI, OH, CHs), (M-12487, CH3) CH3, CI, EtO, H), (M-12488, CHs, CHs, CI, EtO, Cl)，（M-12489, CH3, CH3, CI, EtO, F), (M- 12490, CHs, CHs, CI, EtO, CF3), (M-12491, CHs, CHs, CI, EtO, Br), (M-12492, CH3, CHs, CI, EtO, CHs), (M-12493, CH3， CH3, CI, n-PrO, H), (M-12494, CH3, CHs, CI, n-PrO; CI), (M-12495, CHs, CH3) CI, n-PrO, F), (M-12496, CHs, CH3, CI, n-PrO, CFs), (M-12497, CH3, CHs, CI, n-PrO, Br), (M-12498, CHs, CHs, CI, n- PrO, CHs), (M-12499, CHs, CHs, CI, PhO, H), (M-12500, CHs, CH3, CI, PhO, CI), (M-12501, CH3) CHs, CI, PhO, F), (M-12502, CHs, CHs, CI, PliO, CF3), (M-12503, CHs, CHs, CI, PhO, Br), (M-12504, CH3, CHs, CI, PhO, CH3), (M-12505, CHs, CH3, CI, BnO, H), (M-12506, CHs, CHs, CI, BnO, CI), (M-12507, CHs, CHs, CI, BnO, F)， (M- 12508, CHs, CHs, CI, BnO, CFs), (M-12509, CHs, CHs, CI, BnO, Br), (M-12510, CHs, CH3> CI, BnO, CHs), (M-12511, CHs, CHs, CI, PhCB CH O, H), (M-12512, CHs, CHs, CI, PhCH2CH20; CI), (M-12513, CHs, CHs, CI,
PhCH2CH20, F)， (M-12514, CH3; CH3, CI, PhCH2CH20; CFs), (M-12515, CH3, CHs, CI, PhCH2CH20, Br), (M-12516, CHs, CHs, CI, PhCHsCHsO, CH3), (M- 12517, CHs, CH3) CI, CFsO, H), (M-12518, CHs, CHs, CI, CFsO, CI), (M-12519, CHs, CH3, CI, CFsO, F)， (M-12520, CHs, CH3, CI, CFsO, CFs), (M-12521, CHs, CH3, CI, CFsO, Br), (M-12522, CHs, CH3; CI, CFsO, CHs), (M-12523, CHs, CHs, ■ CI, Ph, H), (M-12524, CH3, CHs, CI, Ph, CI), (M-12525, CHs, CHs, CI, Ph, F), (M-12526, CHs, CH3) CI, Ph, CF3), (M-12527, CHs, CHs, CI, Ph, Br), (M-12528, CHs, CHs, CI, Ph, CHs), (M-12529, CH3) CH3) CI, 4-P-Ph; H)， (M-12530, CHs, CH3; CI, 4-F-Ph, CI), (M-12531, CHs, CHs, CI, 4-F-Ph; F), (M-12532, CHs, CHs, CI, 4-P-Ph, CFs), (M-12533, CHs, CHs, CI, 4-F-Ph, Br), (M-12534, CH3, CHs, CI, 4-F-Ph, CHs), (M-12535, CH3; CHs, CI, 4-CFs-Ph, H), (M-12536, CH3) CHs, CI, 4-CFs-Pli, CI), (M-12537, CH3, CH3; CI, 4-GF3-Ph, F), (M-12538, CHs, CH3) CI, 4-CPVPli' CFs), (M-12539, CHs, CH3) CI, 4-CF3-Ph, Br), (M-12540, CH3, CH3) CI, 4-CF3-Ph, CHs), (M-12541, CH3, CHs, CI, 4-(Me)2N-Ph, H), (M-12542, CHs, CH3, CI, 4-(Me)2N-Ph, CI), (M-12543, CH3, CH3, CI, 4-(Me)2N-Ph, F)， (M-12544, CH3) CHs, CI, 4-(Me)2N-Ph; CFs), (M-12545, CHs, CHs, CI, 4-(Me)2N-Ph, Br), (M- 12546, CHs, CH3; CI, 4-(Me)2N-Ph; CHs), (M-12547, CHs, CH3, CI, 4-OH-Ph, H), (M-12548, CHs, CHa, CI, 4-OH-Ph, CI), (M-12549, CHs, CHs, CI, 4-OH-Ph, F), (M-12550, CHs, CH3; CI, 4-OH-Ph, CFs), (M-12551, CH3, CHs, CI, 4-OH-Ph, Br), (M-12552, CHs, CHs, CI, 4-OH-Ph, CHs), (M-12553, CH3; CHs, CI, 3,4-di-F-Ph, H), (M-12554, CH3) CHa, CI, 3,4-di-F-Ph, CI), (M-12555, CHs, CHs, CI, 3,4-di- F-Ph, F)， (M-12556, CHs, CHs, CI, 3,4-di-F-Ph, CF3), (M-12557, CHs, CHs, CI, 3,4-di-F-Ph, Br), (M-12558, CHs, CHs, CI, 3,4-di-F-Ph, CH3), (M-12559, CHs, CHs, CI, 4-COOH-Pli, H), (M-12560, CH3, CH3, CI, 4-COOH-Ph, CI), (M-12561, CHs, CH3, Cl， 4-COOH-Ph, F), (M-12562, CHs, CHs, CI, 4-COOH-Ph, CFs),
(M-12563, CH3, CH3, CI, 4-COOH-Ph, Br), (M-12564, CHs, CH3, CI, 4-COOH- Ph, CHs), (M-12565, CHs, CH3, CI, Bn, H), (M-12566, CH3, CHs, CI, Bn, CI), (M-12567, CHs, CHs, CI, Bn, F)， (M-12568, CH3; CH3) CI, Bn, CFs), (M-12569, CHs, CHs, CI, Bn, Br), (M- 12570, CHs, CH3) CI, Bn, CHs), (M-12571, CHs, CHs, CI, 4-F-Bn, H), (M-12572, CHs, CHs, CI, 4-F-Bn, CI), (M-12573, CH3) CHs, CI, 4-F-Bn, F), (M-12574, CH3, CH3, CI, 4-F-Bn, CFs), (M-12575, CH3, CHs, CI, 4- F-Bn, Br), (M-12576, CHs, CH3, CI, 4-F-Bn, CHs), (M-12577, CHs, CH3) CI, 2- Py, H), (M-12578, CH3, CH3, CI, 2-Py, CI), (M-12579, CH3) CHs, CI, 2-Py, F), (M-12580, CHs, CH3, CI, 2-Py, CFs), (M-12581, CHs, CH3, CI, 2-Py, Br), (M- 12582, CHs, CHs, CI, 2-Py, CH3), (M-12583, CHs, CHs, CI, 3-Py, H), (M-12584, CHs, CHs, CI, 3-Py; CI), (M-12585, CHs, CHs, CI, 3-Py, F), (M-12586, CH3, CHs, CI, 3-Py, CFs), (M-12587, CHa, CHs, CI, 3-Py, Br), (M-12588, CHs, CHs, CI, 3- Py, CH3); (M-12589, CH3) CHs, CI, 4-Py, H), (M-12590, CHs, CH3, CI, 4-Py, CI), (M-12591, CH3, CH3, CI, 4-Py, F), (M-12592, CHs, CH3, CI, 4-Py, CFs), (M- 12593, CH3> CH3) CI, 4-Py, Br), (M-12594, CH3> CH3) CI, 4-Py, CHs), (M-12595, CH3) CHs, CI, 2-Th, H); (M-12596, CHs, CHs, CI, 2-Th, CI), (M-12597, CHs, CH3; CI, 2-Th, F), (M-12598, CH3; CHs, CI, 2-Th, CF3); (M-12599, CHs, CHs, CI, 2-Th, Br), (M-12600, CHs, CH3) CI, 2-Th, CH3), (M-12601, CH3, CHs, CI, 3-Th, H), (M-12602, CH3, CH3, CI, 3-Th, CI), (M-12603, CHs, CHs, CI, 3-Th, F); (M-12604, CH3, CH3) CI, 3-Th, CF3); (M-12605, CHa, CH3) CI, 3-Th, Br), (M-12606, CHs, CHs, CI, 3-Th, CHs), (M-12607, CHs, CH3) CI, pyrazol-2-yl, H), (M-12608, CH3, CHs, CI, pyrazoレ 2-yl, CI), (M-12609, CHs, CHs, CI, pyrazol-2-yl, F), (M-12610, CHs, CHs, CI, pyrazol-2-yl; CFs), (M-12611, CHs, CHs, CI, pyrazol-2-yl, Br), (M-12612, CHs, CHa, CI, pyrazol-2-yl, CHs), (M-12613, CHs, CHs, CI, pyrazoレ 3-yl; H)， (M-12614, CHs, CHs, CI, pyrazol-3-yl, CI), (M-12615, CHs, CHs, CI, pyrazol-3-yl, F), (M-12616, CHs, CHs, CI, pyrazol-3-yl, CFs), (M-12617, CHs, CH3, CI, pyrazol-3-yl, Br), (M-12618, CHs, CHs, CI, pyrazol-3-yl; CHa), (M- 12619, CH3, CHs, CI, pyrimidin-2-yl, H), (M-12620, CH3; CHs, CI, pyrimidin- 2-yl, CI), (M-12621, CHs, CHs, CI, pyrimidm-2-yl, F), (M-12622, CHs, CHs, CI, pyrimidin-2-yl, CFs), (M-12623, CHs, CHs, Cl' pyrimidin-2-yl, Br), (M-12624, CHs' CHs, Cl, pyrimidin-2-yl, CHs), (M-12625, CHs, CHs, Cl, pyrimidin-4-yl, H), (M-12626, CHs, CHs, Cl, pyrimidin-4-yl, Cl), (M-12627, CHs, CHa, Cl, yrimidm-4-yl, F)， (M-12628, CHs, CHs, Cl, pyrimidin-4-yl, CFs), (M-12629, CHs, CH3, Cl, pyrimidin-4-yl, Br), (M-12630, CHs, CHs, Cl, pyrimidm-4-yl, CHs), (M-12631, CH3, CHs, Cl, pyrimidin-5-yl, H), (M-12632, CHs, CH3) Cl, pyrimidin-5-yl, Cl), (M-12633, CH3) CH3; Cl, pyrimidin- 5 -yl, F)， (M-12634, CHs, CHs, Cl, pyrimidin-5-yl, CFs), (M-12635, CHs, CH3, Cl, pyrimidin-5-yl, Br), b t
〇 en en
Figure imgf000314_0001
(M-12672, CHs, CH3, CI, EtOCH2) CH3), (M-12673, CH3, CH3, CI, EtOCH2CH2, H)， (M-12674, CHs, CHs, CI, EtOCH2CH2) CI), (M-12675, CH3; CH3, CI,
EtOCH2CH2, F); (M-12676, CHs, CH3, CI, EtOCH2CH2j CFs), (M-12677, CH3, CHs, CI, EtOCH2CH2; Br), (M-12678, CH3, CH3, CI, EtOCH2CH2) CH3), (M- 12679, CHs, CHs, CI, MeOCH2CH20CH2CH2) H), (M-12680, CH3) CHs, CI,
MeOCH2CH2OCH2CH2; CI), (M-12681, CH3, CHs, CI, MeOCH2GH20CH2CH2, F), (M-12682, CHs, CHs, CI, MeOCH2CH2OCH2CH2, CFa), (M-12683, CH3， CHa, CI, MeOCH2CH2OCH2CH2, Br), (M-12684, CHs, CH3, CI, MeOCH2CH2OGH2CH2, CHs), (M-12685, CH3) CHs, CI, MeOCH2CH2l H)， (M-12686, CHs, CH3, CI, MeOCHaCHs, CI), (M-12687, CH3; CHs, CI, MeOCH2CH2) F), (M-12688, CH3) CHs, CI, MeOCH2CH2, CFs), (M-12689, CH3, CH3) CI, MeOCH2CH2， Br), (M- 12690, CHs, CH3, CI, MeOCH2CH2, CHs), (M-12691, CH3, CHs, CI, HOCH2, H), (M-12692, CH3) CHs, CI, HO CHa, CI), (M-12693, CHa, CH3> CI, HO CHa, F), (M-12694, CHs, CHs, CI, HOCH2， CFs), (M-12695, CH3; CHs, CI, HOCHa, Br), (M-12696, CHs, CHs, CI, HOCHs, CHs), (M-12697, CHs, CH3; CI, HOCH2CH2, H), (M-12698, CHs, CH3> CI, HOCH2CH2, CI), (M-12699, CHs, CHs, CI,
HOCH2CH2> F), (M-12700, CH3) CHs, CI, HOCH2CH2; CFs), (M-12701, CHs, CHs, CI, HOCH2CH2, Br), (M-12702, CH3, CH3, CI, HOCH2CH2, CHs), (M-12703, CHs, CHs, CI, HOCH2CH2CH2' H), (M-12704, CHs, CHs, CI, HOCH2CH2CH2; CI), (M-12705, CHs, CH3; Cl， ΗΟΟΗ2ΟΗ2ΟΗ2; F), (M-12706, CH3, CHs, CI,
HOCH2CH2CH2) CFs), (M-12707, CH3, CHs, CI, HOCH2CH2CH2, Br), (M-12708, CHs, CH3) CI, HOCH2CH2CH2, CH3), (M- 12709, CH3, CH3) CI,
HOCH2CH2CH2CH2> H), (M-12710, CHs, CH3) CI, HOCH2CH2CH2CH2> CI), (M-12711, CH3; CHs, CI, HOCH2CIi2CU2CIi2, F); (M-12712, CH3; CHs, CI, HOCHaCHsCHsCHs, CF3); (M-12713, CHs, CHs, CI, HOCH2CH2CH2CH2; Br), (M-12714, CHs, CHa, CI, HOCH2CH2CH2CH2, CHs), (M-12715, CHs, CH3) CI, HOCH2CH2CH2CH2CH2, H), (M-12716, CHs, CH3; Gl, HOCH2CH2CH2CH2CH2, CI), (M-12717, CHs, CHs, CI, HOCH2CH2CH2CH2CH2; F), (M-12718, CH3, CHs, CI, HOCH2CH2CH2CH2CH2, CFs), (M-12719, CH3, CHs, CI,
HOCH2CH2CH2CH2CH2, Br), (M-12720, CH3, CH3， CI, HOCH2CH2CH2CH2CH2, CHs), (M-12721, CH3; CHs, CI, HOCH2CH2OCH2CH2, H), (M-12722, CH3， CH3, CI, HOCH2CH2OCH2CH2, CI), (M-12723, CH3) CHs, CI, HOCH2CH2OCH2CH2, F)， (M-12724, CHs, CHs, CI, HOCH2CH2OCH2CH2, CFs), (M-12725, CH3, CH3; CI, HOCH2CH20CH2CH2) Br), (M-12726, CH8> CHa, CI, HOCH2CH2OCH2CH2) CHs), (M-12727, CHs, CHa, CI, (Me)2N, H), (M-12728, CHs, CHs, CI, (Me)2N, CI), (M-12729, CH3， CHs, CI, (Me)2N, F), (M-12730, CHs, CH3) CI, (Me)2N, CF3), (M-12731, CHs, CHs, CI, (Me)2N, Br), (M-12732, CH3, CHs, CI, (Me)2N; CHa), (M-12733, CH3, CHs, CI, piperidin-4-yレ; methyl, H), (M-12734, CHs, CHs, Gl, piperidin-4-yl-methyl, CI), (M-12735, CHs, CHs, CI, piperidin-4-yl-metliyl, F), (M-12736, CHs, CHs, CI, piperidin-4-yl-metliyl, CFs), (M-12737, CHs, CHs, CI, piperidin-4-yl-metliyl, Br), (M-12738, CHs, CHs, CI, piperidin-4-yl-metliyl,
CHs), (M-12739, CH3, CH3, CI, cyclohexylmethyl, H); (M-12740, CH3) CHs, CI, cyclohexylmetiiyl, CI), (M-12741, CHs, CHs, CI, cyclohexylmethyl, F), (M- 12742, CHs, CHa, CI, cyclohexylmethyl, CFs), (M-12743, CH3, CH3, CI, cyclohexylmethyl, Br), (M-12744, CHs, CHs, CI, cyclohexylmetiiyl, CHs), (M- 12745, H, H, H, CF3j H), (M-12746, H, H, H, CF3, CI), (M-12747, H, H, H, CF3, F), (M-12748, H, H, H, CFs, CFs), (M-12749, H, H, H, CF3; Br), (M-12750, H, H, H， CPs, CHs), (M-12751, H， H, F, CF3) H), (M-12752, H, H， F, CF3) CI), (M.12753, H， H， F， CF3; F), (M-12754, H, H， F, CF3) CFs), (M-12755, H， H, F, CF3> Br), (M-12756, H, H, F, CFs, CHs), (M-12757, H, H, CI, CFs, H), (M-12758, H, H, CI, CFs, CI), (M-12759, H, H, CI, CF3, F), (M-12760, H, H, CI, CFs, CFs), (M-12761, H, H, CI, CF3, Br), (M-12762, H, H, CI, CFs, CH3); (M-12763, H, F, H, CFs, H), o Or
Figure imgf000317_0001
)),,,,,,,,,,„s F C0 F C3 C 7 c 77 FF H 277 H FFI7 JH ¾ F F
(,,),,,,,,,, C3ss9 HF7 F H C B 2768 C CH 76 267 HFr H F HF ,,,),,,,,,,,336 C Cs6 CF 274 HF76 F HF F 276 H F H H F CI 2 H 12833, F, F, CI, CFs, Br), (M-12834, F, F, CI, CF3, CHs), (M-12835, F, CHs, H， CF3; H), (M-12836, F, CH3, H, CF3) CI), (M-12837, F, CHs, H, CF3, F), (M-12838, F, CH3, H' CF3, CFs), (M-12839, P, CHs, H, CFs, Br), (M-12840, F, CHs, H, CF3) CHs), (M-12841, , C F, CPs, H), (M- 12842, F, CH3, F, CFs, CI), (M-12843, F, CH3, F, CF3, P), (M-12844, F, CH3, F, CF3， CFs), (M-12845, P, CHs, F, CF3) Br), (M-12846, F, CHs, F, CFs, CHs), (M-12847, F, CHs, CI, CFs, H), (M-12848, F， CHs, CI, CFs, CI), (M-12849, F, CH3) Cl， CFs, F), (M-12850, F, CHs, CI, CFs, CFs), (M-12851, F， CH3; CI, CFs, Br), (M-12852, F, CHs, CI, CFa, CHs), (M- 12853, CI, H, H， CFs, i-Pr), (M-12854, CI, H, H, CF3> CI), (M-12855, CI, H, H, CF3> F), (M-12856, CI, H， H, CFs, CFs), (M-12857, CI, H, H, CFs, Br), (M-12858, CI, H, H, CFs, CHs), (M-12859, CI, H' F, CF3, i-Pr), (M-12860, CI, H, F, CFs, CI), (M-12861, CI, H, F, CFs, F), (M-12862, CI, H; F, CFs, CF3), (M-12863, CI, H, F, CFs, Br), (M-12864, CI, H， F, CFs, CHs), (M-12865, CI, H， CI, CFs, H), (M-12866, CI, H; CI, CF3; CI), (M-12867, CI, H, CI, CFs, F), (M-12868, CI, H, CI, CF3; CFs), (M-12869, CI, H, CI, CFs, Br), (M-12870, CI, H, CI, CFs, CH3), (M-12871, CI, F, H， CFs, i-Pr), (M-12872, CI, F， H, CF3; CI), (M-12873, CI, F, H, CFa, F), (M- 12874, CI, F, H, CFs, CFs), (M-12875, CI, F, H, CFs, Br), (M-12876, CI, F, H, CFs, CHs), (M-12877, CI, F, F, CF3, H), (M-12878, CI, F， F, CF3) CI), (M-12879, CI, F, F, CFs, F), (M-12880, CI, F, P, CF3; CFs), (M-12881, CI, F' F, CFs, Br), (M-12882, CI, F, F, CFs, CH3), (M-12883, CI, F, CI, CFs, H), (M-12884, CI, F, CI, CF3) CI), (M-12885, CI, F, CI, CFs, F); (M-12886, CI, F, CI, CFs, CFs), (M-12887, CI, F, CI, CFs, Br), . (M-12888) CI, F, CI, CFa, CHs), (M-12889, CI, CH3) H, .CF-s, i-Pr), (M-12890, CI, CH3> H, CF3, CI), (M-12891, CI, CH3, H,, CFs, F), (M-12892, CI, CHs, H, CFs, CF3), (M-12893, CI, CHs, H, CFs, Br), (M-12894, CI, CHs, H, CFs, CHs), (M-12895, CI, CHs, F, CFs, i-Pr), (M-12896, CI, CH3, F, CFs, CI), (M-
12897, CI, CH3) F, CF3) F), (M-12898, CI, CHs, P, CF3) CFs), (M-12899, CI, CH3, F, CFs, Br), (M-12900, CI, CHs, F, CFs, CH3), (M-12901, CI, CH3; CI, CF3, H), (M-12902, CI, CH3) CI, CFs, CI), (M-12903, CI, CH3) CI, CF3, F)， (M-12904, CI, CHs, CI, CFs, CFs), (M-12905, CI, CH3) CI, CFs, Br), (M-12906, CI, CHs, CI, CFs, CHs), (M-12907, CHs, H, H, CF3, i-Pr), (M-12908, CHs, H, H, CF3, CI), (M-12909, CHs, H, H, CFs, F), (M-12910, CHs, H, H; CFs, CFs), (M-12911, CH3; H, H, CFs, Br), (M-12912, CHs, H， H, CFs, CHs), (M-12913, CHs, H, F, CFs, H), (M-12914, CHs, Ή, F, CFs, CI), (M-12915, CHs, H, F, CFs, F), (M-12916, CH3) H, F, CF3, CFs), (M-12917, CHs, H, F, CF3, Br), (M-12918, CH3, H, F, CF8> CH3), (M-12919, CHs, H, CI, CFs, H), (M-12920, CHs, H' CI, CFs, CI), (M-12921, CH3, H， CI, CFs, F), (M-12922, CH3, H, CI, CFs, CF3)， (M-12923, CH3, H, CI, CF3, Br), (M-12924, CHs, H， CI, CF3; CHs), (M-12925, CHs, F, H, CF3, H), (M-12926, CHs, F， H, CF3, CI), (M-12927, CHs, F, H, CFs, F)， (M- 12928. CHs, F, H, CFs, CFs), (M-12929, CHs, F, H， CF3, Br), (M-12930, CH3; F, H， CFs, CHs), (M-12931, CHs, F' P, CF3) H), (M-12932, CHs, P, F, CPs, CI), (M-12933, CH3, F, F, CFs, F); (M-12934, CH3, F, F, CFs, CFs), (M-12935, CH3) F, F, CF3> Br), (M-12936, CHs, F, F, CF3) CHs), (M-12937, CHs, F, CI, CF3, H); (M-12938, CHs, F, CI, CFs, CI), (M-12939, CHs, F， CI, CFs, F), (M-12940, CH3; F, CI, CF3, CF3), (M-12941, CHs, F， CI, CFs, Br), (M-12942, CHs, F， CI, CFs, CHs), (M-12943, CHs, CHs, H, CFs, H), (M-12944, CHs, CHs, H, CF3, CI), (M-12945, CHs, CHs, H, CPs, F), (M-12946, CH3, CH3, H, CFs, CF3), (M-12947, CHs, CH3) H, CFs, Br), (M-12948, CHs, CH3, H, CFs, CHs), (M-12949, CH3) CH3) F, CFs, H), (M-12950, CH3, CH3) F, CFs, CI), (M-12951, CHs, CHa, F, CFs, F), (M-12952, CHs, CHs, F, CFs, CPs), (M-12953, CHs, CHs, F, CFs, Br), (M-12954, CHs, CH3; F, CPs, CHs), (M-12955, CHs, CHs, CI, CFs, H), (M-12956, CHs, CH3) CI, CFs, CI), (M-12957, CH3) CHs, CI, CFs, F), (M-12958, CH3, CHs, CI, CFs, CFs), (M-12959, CHs, CHs, CI, CFs, Br), (M-12960, CH3, CH3, CI, CF3, CHs). 試験例
試験例 1 トロンボポェチン （TPO) の単離と精製
ヒ トおよびマウス ΊΤΟは、 R&D Systems社より購入した。 試験例 2 化合物（B-1)による in vitro巨核球コロニー增加作用
本化合物の巨核球系細胞の増殖 ·分化 · 成熟に対する作用を、 ヒ ト骨髄細胞を 用い、 メチルセルロースの半固形培養で巨核球コロニー形成法で調べた。 ヒ ト骨 髄細胞 2.2xl05個を 3 cmシャーレに播種し、 10%ェタノールに溶解した化合物を 1%添加して 37°C、 5% C02存在下で 7 日間培養し、 巨核球コロニー数を測定した。 その結果を図 1に示す。 試験例 3 化合物 (B-1)の TPO受容体応答性
本化合物の ΊΤΟ受容体応答性を、 コリンスらの J. Cell. Physiol., 137: 293-298 (1988)に記載されている方法に準じてヒ ト TP0受容体遺伝子を BaF-B03細胞に 導入して作成した、 TPO依存性細胞株 BaF/hTPORを用いて測定した。 トロンボ ポェチン受容体をコードする遺伝子の塩基配列は、 ビゴンらの Proc. Natl. Acad. Sci. 89:5640-5644 (1992)に記載されている。 なお親株である BaF-B03細胞には TP0は応答しない。 10%WEHI-3培養液を添加した RPMI培地にて増殖させた BAF/hTPOR細胞を PBSで 1回洗浄後、 WHEHI-3培養液を添加していない RPMI 培地に懸濁し、 96穴マイク口プレートに細胞を 5xl04/ゥエルになるように播種 して.、 本化合物あるいは TPOを添加した。 5%C02雰囲気下で, 37°C、 20時間培養 した後に、 細胞増殖判定試薬.である WST-1試薬 （宝酒造社製） を添加し、 4時間 後に 450nmの吸収を測定した。 その結果を図 2に示す。 また、 同様の手法を用い て作成したマウス ΊΤ0受容体を発現する BaF/mTPOR細胞の応答性を調べた結 果を図 3に示す。 E D 5。値をヒ ト T P Oの半最大応答性を示す化合物の濃度とし、 それぞれの化合物の E D 5。値を表 3 3に示した。
Figure imgf000322_0001
図 1に示したように、 本化合物添加により単独で巨核球コロニーが形成され、 コロニー数は濃度依存的に増加した。 以上の結果、 本化合物は単独で巨核球前駆 細胞の増殖 ·分化を促進し血小板産生能を有する巨核球を産生させることが明ら かとなった。
図 2に示したように、 本化合物は濃度依存的に ΊΤΟ依存性細胞株 BaF/hTPOR 細胞を増殖させた。 図 3に示したように、 本化合物は、 マウス TPO受容体を発現 させた： BaF/mTPOR細胞には応答しなかった。 以上の結果より、 本化合物がヒ ト TPO受容体に特異的に作用し、 TPOァゴニス トと して作用していることが明らか となった。 製剤例
製剤例 1
以下の成分を含有する顆粒剤を製造する。
成分 式 （ I ) で表わされる化合物 10 mg
乳糖 700 mg コーンスターチ 274 mg
HPC-L 16 mg
1000 mg
式 （ I ) で表わされる化合物と乳糖を 6 0メッシュのふるいに通す。 コーンス ターチを 1 2 0メ ッシュのふるいに通す。 これらを V型混合機にて混合する。 混 合末に H P C— L (低粘度ヒ ドロキシプロピルセルロース） 水溶液を添加し、 練 合、 造粒 （押し出し造粒 孔径 0. 5〜 l mm) したのち、 乾燥する。 得られた 乾燥顆粒を振動ふるい （ 1 2Z6 0メッシュ） で櫛過し顆粒剤を得る。
製剤例 2
以下の成分を含有するカプセル充填用散剤を製造する。
成分 式 （ I ) で表わされる化合物 10 mg 乳糠 79 mg
コーンスターチ 10 mg ステアリン酸マグネシゥム 1 mg
100 mg 式 （ I ) で表わされる化合物、 乳糖を 6 0メッシュのふるいに通す。 コーンス ターチは 1 2 0メッシュのふるいに通す。 これらとステアリン酸マグネシウムを V型混合機にて混合する。 1 0倍散 1 0 O m gを 5号硬- する。
製剤例 3
以下の成分を含有するカプセル充填用顆粒剤を製造する，
成分 式 （ I ) で表わされる化合物 丄 5 mg
乳糖 90 mg
コーンスターチ 42 mg
HPC-L 3 mg
150 mg 式 （ I ) で表わされる化合物、 乳糖を 6 0メッシュのふるいに通す。 コーンス ターチを 1 '2 0メッシュのふるいに通す。 これらを混合し、 混合末に H P C— L 溶液を添加して練合、 造粒、 乾燥する。 得られた乾燥顆粒を整粒後、 その 1 5 0 m gを 4号硬ゼラチンカプセルに充填する。
製剤例 4
以下の成分を含有する錠剤を製造する。
成分 式 （ I ) で表わされる化合物 10
乳糖 90 mg
微結晶セルロース 30 mg
CMC-Na 15 mg
ステアリン酸マグネシウム _ _ — 5 m 150 mg 式 （ I ) で表わされる化合物、 乳糖、 微結晶セルロース、 CMC— N a (カル ボキシメチルセルロース ナトリ ウム塩） を 6 0メッシュのふるいに通し、 混合 する。 混合末にステアリン酸マグネシウム混合し、 製錠用混合末を得る。 本混合 末を直打し、 1 5 0 mgの錠剤を得る。
製剤例 5
静脈用製剤は次のように製造する ：
式 （ I ) で表わされる化合物 1 0 0 m g 飽和脂肪酸グリセリ ド 1 0 0 0 m l 上記成分の溶液は通常、 1分間に 1 m 1 の速度で患者に静脈内投与される。 産業上の利用可能性
本発明化合物は、 トロンボポェチンァゴニス ト作用を有し、 血小板減少症等の 血小板数の異常を伴う血液疾患の治療または予防剤と して有効に機能し得ること を見出した。

Claims

請求の範囲
1. 一般式 （ I ) ：
X1— Y1— Z1— W1 (Γ)
[式中、 X 1は置換されていてもよいァリール、 置換されていてもよいァラルキ ル、 置換されていてもよいへテロアリール、 または置換されていてもよいへテロ ァリールアルキル ；
Y1は一 NRACO— （C RCRD) 0— 2—、 _NRACO— (CH2) 0— 2— V—、 一 N R A C O— C R c = C RD—、 —V— (CH2) 1_5-NRACO- (CH 2) 。-2 -、 - V- (CH2) 卜 5 - CONRA— (CH2) 0— 2 -、 — CONRA— (CH2) 。— 2—、 一 (CH2) 0— 2— NRA_ S 02 - (CH2) 0— 2 -、 一 （C H2) 0— 2 - S 02_NRA - (CH2) 0 — 2 -、 — NRA - (CH2) 0— 2 -、 一 NRA— CO— NRA—、 一 N R A— C S— N R A—、 - N = C (一 S RA) 一 N R A—、 一 NRAC S N RACO—、 - N = C (一 S RA) — NRACO—、 - N R A 一 （CH2) 丄— 2— NRA— CO—、 一 NRACONRANRBCO—、 または一N = C (一 NRARA) — N RACO— （式中、 RAはそれぞれ独立して水素原子ま たは低級アルキル； RBは水素原子またはフエニル； Rcおよび RDはそれぞれ独 立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されて いてもよい低級アルキルォキシ、 置換されていてもよい低級アルキルチオ、 置換 されていてもよい低級アルケニル、 置換されていてもよい低級アルキニル、 置換 されていてもよいァリール、 置換されていてもよいへテロアリール、 置換されて いてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていて もよいへテロァリールアルキル、 置換されていてもよい非芳香族複素環基、 また は置換されていてもよいアミノ ； Vは酸素原子または硫黄原子） ；
Z 1は置換されていてもよいフエ二レン、 置換されていてもよい単環へテロァリ レン、 置換されていてもよい単環非芳香族複素環ジィル、 または置換されていて もよい単環シクロアルカンジィル；
W1は式 ：
。
Figure imgf000327_0001
(式中、 R1 R2、 R3、 R4、 R7、 および R8はそれぞれ独立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されていてもよい低級アル キルォキシ、 置換されていてもよい低級アルキルチオ、 置換されていてもよい低 級ァルケニル、 置換されていてもよい低級アルキニル、 置換されていてもよいァ リール、 置換されていてもよいへテロアリール、 置換されていてもよいシクロア ルキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロアリー ルアルキル、 置換されていてもよい非芳香族複素環基、 または置換されていても よいアミノ ；
R 5、 R 6、 および R 9はそれぞれ独立して、 水素原子、 置換されていてもよい低 級アルキル、 置換されていてもよい低級アルケニル、 置換されていてもよい低級 アルキニル、 置換されていてもよいァリール、 置換されていてもよいへテロァリ ール、 置換されていてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロアリールアルキル、 または置換されていてもよい非 芳香族複素環基；
A 1は置換されていてもよいァリールまたは置換されていてもよいへテロアリ一 ル；
破線 （ ） は結合の存在または不存在を表わす） で表わされる基] で示され る化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそ れらの溶媒和物を有効成分と して含有する トロンボポェチン受容体ァゴニス ト作 用を有する医薬組成物。
2 . X 1が置換されていてもよいへテロアリールである請求項 1記載のトロンボ ポェチン受容体ァゴニス ト作用を有する医薬組成物。
3 . X 1が式 ：
Figure imgf000328_0001
(式中、 R 1。および R 1 1はそれぞれ独立して水素原子、 置換されていてもよい 低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 ハロゲン、 置換さ れていてもよいアミノカルボニル、 置換されていてもよいへテロアリール、 また は置換されていてもよいァリール； R 1 2は水素原子または低級アルキル） で示さ れる基である請求項 1記載のト口ンボポェチン受容体ァゴニス ト作用を有する医 薬組成物。
4. X 1が式：
Figure imgf000329_0001
(式中、 R 1。および R 1 1は請求項 3 と同意義） で示される基である請求項 1記 载の トロンポポェチン受容体ァゴニス ト作用を有する医薬組成物。
5. Y 1がー NH C O—、 一 C ONH—、 一 NH CH 2—、 一 NH CO— CH = C H—、 または一 NH S 02—である請求項 1〜 4のいずれかに記載のト口ンボポ ェチン受容体ァゴニス ト作用を有する医薬組成物。
6. Y 1がー NH C O—である請求項 1〜 4のいずれかに記載の ト口ンボポェチ ン受容体ァゴニス ト作用を有する医薬組成物。
7. Z 1がハロゲンまたは低級アルキルで置換されていてもよい 1 , 4—フエ二 レンである請求項 1〜 6のいずれかに記載の ト口ンボポェチン受容体ァゴニス ト 作用を有する医薬組成物。
8. R 1が水素原子または低級アルキルである請求項 1〜 7のいずれかに記載の ト口ンボポェチン受容体ァゴニス ト作用を有する医薬組成物。
9. R 2が水素原子、 低級アルキル、 ハロゲン、 低級アルキルォキシ、 低級アル キルチオ、 または置換されていてもよいアミノである請求項 1〜 8のいずれかに 記載の トロンボポェチ /受容体ァゴニス ト作用を有する医薬組成物。
1 0. W1が式 ：
Figure imgf000329_0002
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン ； R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそ れぞれ以下の置換基群 Aから選択される 1以上の置換基によって置換されていて もよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリ ール、 ァラルキル、 ヘテロァリール、 もしく はヘテロァリールアルキル ；破線は 請求項 1 と同意義 ；
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級ァルキルォキシ) で表わされる基である、 請求項 1〜 9のいずれかに記載の ト口ンボポェチン受容 体ァゴニス ト作用を有する医薬組成物。
1 1 . W 1が式 ：
Figure imgf000330_0001
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン ； R 2 6は水素原子または低級アルキル；破線は請求項 1 と同 意義） で表わされる基である、 請求項 1〜 9のいずれかに記載のトロンポポェチ ン受容体ァゴニス ト作用を有する医薬組成物。
1 2 . 血小板産生調節剤である請求項 1〜 1 1のいずれかに記載のトロンポポェ チン受容体ァゴニス ト作用を有する医薬組成物。
1 3 . 血小板産生を調節するための医薬を製造するための請求項 1〜 1 1 のいず れかに記載の化合物の使用。
1 4 . 請求項 1〜 1 1のいずれかに記載の化合物の治療上効果を示す量を人を含 む哺轧動物に投与することからなる、 哺乳動物の血小板産生を調節する方法。
1 5 . —般式 （ I I ) ：
X2— Y2-Z2— W2 (Π)
[式中、 X 2は置換されていてもよい 5員へテロァリールまたは置換されていて もよいピリジル ；
Y2は一 NRACO— （C RCRD) 。― 2—、 一 N RAC〇一 (C H 2) 0— 2— V—、 一 NRACO— CRC= CRD―、 —V— ( C H 2) 1_5-N RACO- (CH 2) 0 — 2—、 - V- (CH2) ト 5— CONRA— (CH2) 0— 2—、 一 CONRA— (CH2) 。― 2—、 一 (CH2) 。― 2— NRA - S 02 - (CH2) 0— 2—、 一 (C H2) 。_2 - S 02— NRA - (CH2) 。一 2 -、 ― NRA— (CH2) 。― 2 -、 一 NRA— CO— NRA―、 一 N RA— C S— N RA—、 一 N= C (― S RA) - N R 一 NRAC S NRACO—、 - N = C (- S RA) ― NRACO—、 - N R A 一 (CH2) 丄— 2— NRA— CO—、 一 NRACONRANRBCO—、 または一 N = C (— NRARA) — NRACO— (式中、 R Aはそれぞれ独立して水素原子ま たは低級アルキル ； RBは水素原子またはフエニル Rcおよび RDはそれぞれ独 立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されて いてもよい低級アルキルォキシ、 置換されていてもよい低級アルキルチオ、 置換 されていてもよい低級アルケニル、 置換されていてもよい低級アルキニル、 置換 されていてもよいァリール、 置換されていてもよいへテロアリール、 置換されて いてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていて もよいへテロァリールアルキル、 置換されていてもよい非芳香族複素環基、 また は置換されていてもよいアミノ ； Vは酸素原子または硫黄原子） ；
Z 2は置換されていてもよいフエ二レン、 置換されていてもよい 2 , 5—ピリジ ンジィル、 置換されていてもよい 2, 5—チォフェンジィル、 または置換されて いてもよい 2 , 5—フランジィル；
W2は式 ： b
Figure imgf000332_0001
(式中、 R 1 R2、 R3、 R4、 R7、 および R8はそれぞれ独立して、 水素原子、 ハロゲン、 置換されていてもよい低級アルキル、 置換されていてもよい低級アル キルォキシ、 置換されていてもよい低級アルキルチオ、 置換されていてもよい低 級ァルケニル、 置換されていてもよい低級アルキニル、 置換されていてもよいァ リール、 置換されていてもよいへテロアリール、 置換されていてもよいシクロア ノレキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロアリー ルアルキル、 置換されていてもよい非芳香族複素環基、 または置換されていても よいァミノ ；
R5、 R6、 および R9はそれぞれ独立して、 水素原子、 置換されていてもよい低 級アルキル、 置換されていてもよい低級アルケニル、 置換されていてもよい低級 アルキニル、 置換されていてもよいァリール、 置換されていてもよいへテロァリ ール、 置換されていてもよいシクロアルキル、 置換されていてもよいァラルキル、 置換されていてもよいへテロァリールアルキル、 または置換されていてもよい非 芳香族複素環基；
A 2は置換されていてもよいァリールまたは置換されていてもよいへテロアリ一 ル；
破線 （ ） は結合の存在または不存在を表わす） で表わされる基] で示され る化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそ れらの溶媒和物。
1 6 . X 2が式 ：
Figure imgf000333_0001
(式中、 R 1 °および R 1 1はそれぞれ独立して水素原子、 置換されていてもよい 低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 ハロゲン、 置換さ れていてもよいアミノカルボニル、 置換されていてもよいへテロアリール、 また は置換されていてもよいァリール） で示される基である請求項 1 5記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒 和物。
1 7 . X 2が式 ：
Figure imgf000333_0002
(式中、 R 1 6は水素原子、 置換されていてもよい低級アルキル、 カルボキシ、 低 級アルキルォキシカルボニル、 ハロゲン、 または置換されていてもよいアミノカ ノレホニル ；
R 1 7、 R 1 S、 R 1 9、 R2。、 R2 1、 R22、 および R 2 3はそれぞれ独立して水 素原子、 置換基群 Bから選択される 1以上の置換基によって置換されていてもよ いアルキル、 シクロアルキル、 置換基群 Bから選択される 1以上の置換基によつ て置換されていてもよいアルキルォキシ、 アルキルチオ、 ハロゲン、 置換基群 C から選択される 1以上の置換基によって置換されていてもよいフ-ニル、 置換基 群 Cから選択される 1以上の置換基によって置換されていてもよいへテロアリ一 ル、 または置換基群 Cから選択される 1以上の置換基によって置換されていても よい非芳香族複素環基、
置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカルポニル、 ァリールォキシカルボ二/レ、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエ二 ル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール ；
R 1 6および R 1 7は一緒になって一 C H 2—、 一 CH2 CH2—、 - C H 2 C H 2 C H2—、 一 O CH2—、 または一 S C H 2—を,形成してもよい） で示される墓であ る請求項 1 5または 1 6記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製 薬上許容される塩、 またはそれらの溶媒和物。
1 8. Y2がー NHCO—である請求項 1 5〜 1 7のいずれかに記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒 和物。
1 9. Z 2がハロゲンまたは低級アルキルで置換されていてもよい 1 , 4—フエ 二レンである請求項 1 5〜 1 8のいずれかに記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 0. R 1が水素原子または低級アルキルである請求項 1 5〜 1 9のいずれかに 記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 また はそれらの溶媒和物。
2 1. R 2が水素原子、 低級アルキル、 ハロゲン、 低級アルキルォキシ、 低級ァ ルキルチオ、 または置換されていてもよいアミノである請求項 1 5〜 2 0のいず れかに記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 2. W2が式 ：
Figure imgf000335_0001
(式中、 R R2、 R3、 R4、 R5、 R6、 R7、 R8、 および A2は請求項 1 5 と同意義、 ただし、 R 2はイミダゾリル、 トリァゾリル、 またはテトラゾリルで はない） である請求項 1 5〜 2 1のいずれかに記載の化合物、 そのプロ ドラッグ, もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 3. W2が式 ：
Figure imgf000335_0002
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン、 R1 4および R1 5はそれぞれ独立して水素原子、 またはそ れぞれ以下の置換基群 Aから選択される 1以上の置換基によって置換されていて もよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリ ール、 ァラルキル、 ヘテロァリール、 ヘテロァリールアルキル、 もしくは非芳香 族複素環基；
置換基群 A ： ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ） である請求項 1 5〜 2 2のいずれかに記載の化合物、 そのプロ ドラッグ、 もしく はそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 4. W 2が式 ：
Figure imgf000336_0001
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン； R 2 6は水素原子または低級アルキル；破線は請求項 1 5 と 同意義） で表わされる基である、 請求項 1 5〜 2 2のいずれかに記載の化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒 和物。
2 5 -般式 （ I I I ) ：
Figure imgf000336_0002
[式中、 R 1 6は水素原子、 置換されていてもよい低級アルキル、 カルボキシ、 低 級アルキルォキシ力ルポニル、 ハロゲン、 または置換されていてもよいアミノカ ノレホニノレ ；
R 1 7、 R 1 8、 R1 9、 R2 °、 および R 2 1はそれぞれ独立して水素原子、 置換基 群 Bから選択される 1以上の置換基によって置換されていてもよいアルキル、 シ ク口アルキル、 置換基群 Bから選択される 1以上の置換基によって置換されてい てもよいアルキルォキシ、 アルキルチオ、 ハロゲン、 置換基群 Cから選択される.
1以上の置換基によって置換されていてもよいフユニル、 置換基群 Cから選択さ れる 1以上の置換基によって置換されていてもよいへテロァリール、 または置換 基群 cから選択される 1以上の置換基によって置換'されていてもよい非芳香族複 素環基、
置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 力ルポキシ、 低級アルキ ルォキシカルボニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフユ二 ル、 非芳香族複素環基、 およびへテロアリール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カノレポキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール；
R 1 6およぴ R 1 7は一緒になつて一 C H 2—、 一 C H 2 C H 2—、 - C H 2 C H 2 C
H 2—、 一 O C H 2 —、 または一 S C H 2—を形成してもよい ；
R 3 1および R 3 2はそれぞれ独立して、 水素原子、 低級アルキル、 ハロゲン、 ノヽ 口低級アルキル、 低級アルキルォキシ、 ハロ低級アルキルォキシ、 またはヒ ドロ キシ ； '
W 3は式 ：
Figure imgf000337_0001
,または
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはハロゲン ； R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそれぞれ以下の置換基群 Aにより置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアノレキノレ、 ァリーノレ、 ァラルキル、 ヘテロァリーノレ、 ヘテロァリーノレァノレ キル、 もしくは非芳香族複素環基；
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ポキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ； R 2 4は水素原子または低級アルキル ；
R 2 5は低級アルキル、 置換されていてもよいァリール、 または置換されていても よい非芳香族複素環 ；
A 3はへテロァリール） で表わされる基] で示される化合物、 そのプロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。
2 6 . 一般式 （ I V— A ) ：
Figure imgf000338_0001
[式中、 R 2 7は水素原子、 C 1— 3アルキル、 トリフルォロメチル、 またはハロ ゲン ；
R 2 8、 R 2 9、 および R 3。はそれぞれ独立して水素原子、 置換基群 Bから選択さ れる 1以上の置換基によって置換されていてもよいアルキル、 シク口アルキル、 置換基群 Bから選択される 1以上の置換基によって置換されていてもよいアルキ ルォキシ、 アルキルチオ、 ハロゲン、 置換基群 Cから選択される 1以上の置換基 によって置換されていてもよいフ-ニル、 置換基群 Cから選択される 1以上の置 換基によって置換されていてもよいへテロアリ一ル、 または置換基群 Cから選択 される 1以上の置換基によって置換されていてもよい非芳香族複素環基、 置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカルボニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフユ二 ル、 非芳香族複素環基、 およびへテロア'リール、
置換基群 C ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミノ、 非芳香族複素環、 およびへテロアリール；
R 3 1および R 3 2はそれぞれ独立して、 水素原子、 低級アルキル、 ハロゲン、 ハ 口低級アルキル、 低級アルキルォキシ、 ハロ低級アルキルォキシ、 またはヒ ドロ キシ ；
W 4は式 ：
Figure imgf000339_0001
(式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはノヽロゲン ；
R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそれぞれ以下の置換基群 Aにより置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロアルキル、 ァリーノレ、 ァラルキル、 ヘテロァリール、 ヘテロァリールアル キル、 もしくは非芳香族複素環基；
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ； R 2 4は水素原子または低級アルキル） で表わされる基] で示される化合物、 その プロ ドラッグ、 もしくはそれらの製薬上許容される塩、 またはそれらの溶媒和物。 2 7 . 一般式 （ I V— B ) ：
Figure imgf000340_0001
[式中、 R 2 8、 R 2 S、 および R 3。はそれぞれ独立して水素原子、 置換基群 Bか ら選択される 1以上の置換基によって置換されていてもよいアルキル、 シクロア ルキル、 置換基群 Bから選択される 1以上の置換基によって置換されていてもよ いアルキルォキシ、 アルキルチオ、 ハロゲン、 置換基群 Cから選択される 1以上 の置換基によって置換されていてもよいフユニル、 置換基群 cから選択される 1 以上の置換基によって置換されていてもよいへテロアリール、 または置換基群 C から選択される 1以上の置換基によって置換されていてもよい非芳香族複素環基、 置換基群 B ： ヒ ドロキシ、 アルキルォキシ、 ハロゲン、 カルボキシ、 低級アルキ ルォキシカルボニル、 ァリールォキシカルボニル、 置換されていてもよいァミノ、 置換基群 Cから選択される 1以上の置換基によって置換されていてもよいフエ二 ル、 非芳香族褸素環基、 およびへテロアリール、
置換基群 c ： ヒ ドロキシ、 アルキル、 ハロゲン、 ハロ低級アルキル、 カルボキシ、 低級アルキルォキシカルボニル、 アルキルォキシ、 置換されていてもよいァミ ノ、 非芳香族複素環、 およびへテロアリール；
R 3 1および R 3 2はそれぞれ独立して、 水素原子、 低級アルキル、 ハロゲン、 ハ 口低級アルキル、 低級アルキルォキシ、 ハロ低級アルキルォキシ、 またはヒ ドロ キシ；
W 4は式 ：
Figure imgf000340_0002
または (式中、 R 1 3は水素原子、 低級アルキル、 低級アルキルォキシ、 低級アルキルチ ォ、 またはノヽロゲン ；
R 1 4および R 1 5はそれぞれ独立して水素原子、 またはそれぞれ以下の置換基群 Aにより置換されていてもよい低級アルキル、 低級アルケニル、 低級アルキニル、 シクロ アノレキル、 ァ リ ール、 ァラノレキル、 ヘテロァ リ ール、 ヘテロァ リ ーノレァノレ キル、 もしくは非芳香族複素環基； ·
置換基群 A ：ハロゲン、 ハロ低級アルキル、 置換されていてもよいァミノ、 カル ボキシ、 低級アルキルチオ、 低級アルキルシリル、 または低級アルキルォキシ ； R 24は水素原子または低級アルキル） で表わされる基 ；
Tは一 CH2—、 一 CH2 CH2—、 _ CH2 CH2 CH2—、 一 OCH2—、 また は一 S CH2— ] で示される化合物、 そのプロ ドラッグ、 もしくはそれらの製薬 上許容される塩、 またはそれらの溶媒和物。
2 8. 請求項 1 5〜 2 7のいずれかに記載の化合物を有効成分と して含有する医 薬組成物。 '
2 9. 請求項 1 5〜 2 7のいずれかに記載の化合物を有効成分として含有する ト 口ンボポェチン受容体ァゴニス ト作用を有する医薬組成物。
3 0 · 請求項 1 5〜 2 7のいずれかに記載の化合物を有効成分と して含有する血 小板産生調節剤。
3 1. 血小板産生を調節するための医薬を製造するための請求項 1 5〜 2 7のい ずれかに記載の化合物の使用。
3 2. 請求項 1 5〜 2 7のいずれかに記載の化合物の治療上効果を示す量を人を 含む哺乳動物に投与することからなる、 哺乳動物の血小板産生を調節する方法。
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AU2708901A (en) 2001-07-31
JP2008150386A (ja) 2008-07-03
US20100022542A1 (en) 2010-01-28
EP1253142A1 (en) 2002-10-30
US20030195231A1 (en) 2003-10-16
KR20050085991A (en) 2005-08-29
CN100491356C (zh) 2009-05-27
US7582665B2 (en) 2009-09-01
CA2397018C (en) 2012-01-03
EP1253142A4 (en) 2004-09-15
CA2397018A1 (en) 2001-07-26
CN1419547A (zh) 2003-05-21
AU777777B2 (en) 2004-10-28

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