[go: up one dir, main page]

PE20010904A1 - 2-SUBSTITUTED 4-CARBOXAMINE-1,2,3,4-TETRAHYDROQUINOLINE CRYSTAL - Google Patents

2-SUBSTITUTED 4-CARBOXAMINE-1,2,3,4-TETRAHYDROQUINOLINE CRYSTAL

Info

Publication number
PE20010904A1
PE20010904A1 PE2000001267A PE0012672000A PE20010904A1 PE 20010904 A1 PE20010904 A1 PE 20010904A1 PE 2000001267 A PE2000001267 A PE 2000001267A PE 0012672000 A PE0012672000 A PE 0012672000A PE 20010904 A1 PE20010904 A1 PE 20010904A1
Authority
PE
Peru
Prior art keywords
trifluoromethyl
ethyl
ethyl ester
quinoline
dihydro
Prior art date
Application number
PE2000001267A
Other languages
Spanish (es)
Inventor
Troy Anthony Appleton
Lyle Robinson Brostom
Douglas John Meldrum Allen
Derek Lawrence Tickner
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of PE20010904A1 publication Critical patent/PE20010904A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Cephalosporin Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

SE REFIERE A LA FORMA CRISTALINA DEL ESTER ETILICO O ETANOLATO DEL ESTER ETILICO DEL ACIDO [2R,4S]-4-[(3,5-BIS-TRIFLUOROMETIL-BENCIL)-METOXICARBONIL-AMINO]-2-ETIL-6-TRIFLUOROMETIL-3,4-DIHIDRO-2H-QUINOLINA-1-CARBOXILICO ANHIDRO QUE SE CARACTERIZA POR SU PATRON DE DIFRACCION DERAYOS X; UTILIZANDOSE DE 0,1 mg/Kg/DIA-10 mg/Kg/DIA. TAMBIEN SE REFIERE A PROCEDIMIENTOS PARA LA PREPARACION QUE COMPRENDE DISOLVER O MEZCLAR EL ESTER ETILICO DEL ACIDO [2R,4S]-4-[(3,5-BIS-TRIFLUOROMETIL-BENCIL)-METOXICARBONIL-AMINO]-2-ETIL-6-TRIFLUOROMETIL-3,4-DIHIDRO-2H-QUINOLINA-1-CARBOXILICO EN HEXANOS A TEMPERATURA AMBIENTE DE 2-24 HORAS. EL COMPUESTO I INHIBE A LA PROTEINA DE TRANSFERENCIA DEL ESTER DE COLESTERILO CETP Y PUEDE SER UTIL PARA EL TRATAMIENTO DE ATEROSCLEROSIS, ENFERMEDAD VASCULAR PERIFERICA, DISLIPIDEMIA, HIPERBETALIPOPROTEINEMIA, HIPOALFALIPOPROTEINEMIA, HIPERTRIGLICERIDEMIA, HIPERCOLESTEROLEMIAREFERS TO THE CRYSTALLINE FORM OF ETHYL ESTER OR ETHANOLATE OF ETHYL ESTER OF ACID [2R, 4S] -4 - [(3,5-BIS-TRIFLUORomethyl-BENZYL) -METOXICARBONIL-AMINO] -2-ETHYL-6-TRIFLUOROMETIL- 3,4-DIHYDRO-2H-QUINOLINE-1-CARBOXYL ANHYDRO WHICH IS CHARACTERIZED BY ITS X-RAY DIFFRACTION PATTERN; USING FROM 0.1 mg / Kg / DAY-10 mg / Kg / DAY. IT ALSO REFERS TO PROCEDURES FOR THE PREPARATION WHICH INCLUDES DISSOLVING OR MIXING THE ETHYL ESTER OF ACID [2R, 4S] -4 - [(3,5-BIS-TRIFLUOROMETHYL-BENZYL) -METOXYCARBONYL-AMINO] -2-ETHYL-6- TRIFLUORomethyl-3,4-DIHYDRO-2H-QUINOLINE-1-CARBOXYL IN HEXANS AT A ROOM TEMPERATURE OF 2-24 HOURS. COMPOUND I INHIBITS CHOLESTERYL ESTER TRANSFER PROTEIN CETP AND MAY BE USEFUL FOR THE TREATMENT OF ATHEROSCLEROSIS, PERIPHERAL VASCULAR DISEASE, DYSLIPIDEMIA, HYPERBETALIPOPROTEINEMIA, HYPOLIMETHALIPROTEINEMIA, HYPOLYPETHALIPROPHERICIA

PE2000001267A 1999-11-30 2000-11-28 2-SUBSTITUTED 4-CARBOXAMINE-1,2,3,4-TETRAHYDROQUINOLINE CRYSTAL PE20010904A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16805199P 1999-11-30 1999-11-30

Publications (1)

Publication Number Publication Date
PE20010904A1 true PE20010904A1 (en) 2001-09-10

Family

ID=22609901

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001267A PE20010904A1 (en) 1999-11-30 2000-11-28 2-SUBSTITUTED 4-CARBOXAMINE-1,2,3,4-TETRAHYDROQUINOLINE CRYSTAL

Country Status (28)

Country Link
EP (1) EP1246804A1 (en)
JP (1) JP2003515592A (en)
KR (1) KR20020058057A (en)
CN (1) CN1402711A (en)
AP (1) AP2002002531A0 (en)
AU (1) AU1048801A (en)
BG (1) BG106854A (en)
BR (1) BR0015836A (en)
CA (1) CA2392979A1 (en)
CO (1) CO5271716A1 (en)
EA (1) EA200200510A1 (en)
EC (1) ECSP003792A (en)
EE (1) EE200200277A (en)
GT (1) GT200000199A (en)
HU (1) HUP0203521A2 (en)
IL (1) IL149097A0 (en)
IS (1) IS6338A (en)
MA (1) MA26845A1 (en)
MX (1) MXPA02005354A (en)
NO (1) NO20022558D0 (en)
OA (1) OA12099A (en)
PA (1) PA8506301A1 (en)
PE (1) PE20010904A1 (en)
PL (1) PL355892A1 (en)
TN (1) TNSN00231A1 (en)
TR (1) TR200201446T2 (en)
UY (1) UY26454A1 (en)
WO (1) WO2001040190A1 (en)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7115279B2 (en) 2000-08-03 2006-10-03 Curatolo William J Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors
WO2003000295A2 (en) * 2001-06-21 2003-01-03 Pfizer Products Inc. Self-emulsifying formulations of cholesteryl ester transfer protein inhibitors
GT200200170A (en) * 2001-09-28 2003-05-23 PREPARATION OF INHIBITOR OF CETP ANHIDRO
WO2003063822A2 (en) * 2002-02-01 2003-08-07 Pfizer Products Inc. Method for making homogeneous spray-dried solid amorphous drug dispersions utilizing modified spray-drying apparatus
ATE395044T1 (en) 2002-02-01 2008-05-15 Pfizer Prod Inc PHARMACEUTICAL COMPOSITIONS OF AMORPHIC DISPERSIONS OF ACTIVE INGREDIENTS AND LIPOPHILIC MICROPHASE-FORMING MATERIALS
EP1920766B1 (en) * 2002-02-01 2017-08-23 Bend Research, Inc Pharmaceutical compositions of amorphous dispersions of drugs and lipophilic microphase-forming materials
RU2293078C2 (en) 2002-08-30 2007-02-10 Джапан Тобакко Инк. Dibenzylamine compounds, pharmaceutical composition and therapeutic or prophylactic agent based on thereof, method for treatment or prophylaxis of hyperlipidemia or arteriosclerosis
CA2500582A1 (en) 2002-10-04 2004-04-22 Millennium Pharmaceuticals, Inc. Pgd2 receptor antagonists for the treatment of inflammatory diseases
US7504508B2 (en) 2002-10-04 2009-03-17 Millennium Pharmaceuticals, Inc. PGD2 receptor antagonists for the treatment of inflammatory diseases
ATE461700T1 (en) 2002-12-20 2010-04-15 Pfizer Prod Inc DOSAGE FORM CONTAINING A CETP INHIBITOR AND A HMG-COA REDUCTASE INHIBITOR
US20040132771A1 (en) * 2002-12-20 2004-07-08 Pfizer Inc Compositions of choleseteryl ester transfer protein inhibitors and HMG-CoA reductase inhibitors
AU2004222436A1 (en) 2003-03-17 2004-09-30 Japan Tobacco Inc. Method for increasing the oral bioavailability of S-(2-(((1- (2-ethylbutyl) cyclohexyl)carbonyl) amino) phenyl)-2-methylpropanethioate
EP1622872A1 (en) * 2003-03-28 2006-02-08 Pfizer Products Inc. 1,2,4-substituerte 1,2,3,4-tetrahydro-and 1,2 dihydro-quinoline and 1,2,3,4-tetrahydro-quinoxaline derivatives as cetp inhibitors for the treatment of atherosclerosis and obesity
ATE540671T1 (en) 2003-08-04 2012-01-15 Bend Res Inc PHARMACEUTICAL COMPOSITIONS OF AMORPHOUS DRUG ADSORBATES AND LIPOPHILIC MICROPHASE-FORMING MATERIALS
HRP20090581T1 (en) 2003-10-08 2009-12-31 Eli Lilly And Company COMPOUNDS AND PROCEDURES FOR THE TREATMENT OF DISLIPIDEMIA
CN1942428A (en) * 2004-04-13 2007-04-04 默克公司 CETP inhibitors
MXPA06014716A (en) * 2004-06-24 2007-03-12 Lilly Co Eli Compounds and methods for treating dyslipidemia.
WO2006033001A1 (en) * 2004-09-23 2006-03-30 Pfizer Products Inc. Quinoline compounds
WO2006033004A1 (en) * 2004-09-23 2006-03-30 Pfizer Products Inc. Quinoline compounds as cetp inhibitors
WO2006091674A1 (en) 2005-02-24 2006-08-31 Millennium Pharmaceuticals, Inc. Pgd2 receptor antagonists for the treatment of inflammatory diseases
WO2006098394A1 (en) * 2005-03-14 2006-09-21 Japan Tobacco Inc. Method for inhibiting lipid absorption and lipid absorption inhibitor
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
EP2134169A2 (en) 2007-03-09 2009-12-23 Indigene Pharmaceuticals Inc. Combination of metformin r-(+) lipoate and antihyperlipidemic agents for the treatment of diabetic hyperglycemia and diabetic complications
US20110243940A1 (en) 2008-12-16 2011-10-06 Schering Corporation Bicyclic pyranone derivatives and methods of use thereof
EP2379547A1 (en) 2008-12-16 2011-10-26 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
AR077208A1 (en) 2009-06-30 2011-08-10 Lilly Co Eli ACID DERIVATIVES TRANS-4 - [[(5S) -5 - [[[3,5-BIS (TRIFLUOROMETIL) PHENYLE] METHYL] (2-METHYL-2H-TETRAZOL-5-IL) AMINO) -2,3, 4,5-TETRAHIDRO-7,9-DIMETIL-1H-1-BENZAZEPIN-1-IL) METHYL) -CYCLHEXANCARBOXYL AND ITS CRYSTALLINE FORMS, PHARMACEUTICAL COMPOSITIONS THAT UNDERSTAND IT, ITS USE TO PREPARE A MEDICAM
PT3174995T (en) 2014-07-30 2020-10-15 Hoffmann La Roche Genetic markers for predicting responsiveness to therapy with hdl-raising or hdl mimicking agent

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5231102A (en) * 1989-03-08 1993-07-27 Merck Sharp & Dohme, Ltd. Tetrahydroquinoline derivatives useful for neurodegenerative disorders
WO1998033775A1 (en) * 1997-02-03 1998-08-06 American Home Products Corporation 2-substituted-1-acyl-1,2-dihydroquinoline derivatives to increase hdl-cholesterol level
US6197786B1 (en) * 1998-09-17 2001-03-06 Pfizer Inc 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines

Also Published As

Publication number Publication date
IL149097A0 (en) 2002-11-10
BR0015836A (en) 2002-08-06
HUP0203521A2 (en) 2003-02-28
JP2003515592A (en) 2003-05-07
CA2392979A1 (en) 2001-06-07
PA8506301A1 (en) 2002-08-26
BG106854A (en) 2002-12-29
ECSP003792A (en) 2002-04-23
WO2001040190A1 (en) 2001-06-07
KR20020058057A (en) 2002-07-12
CN1402711A (en) 2003-03-12
EP1246804A1 (en) 2002-10-09
UY26454A1 (en) 2001-07-31
MA26845A1 (en) 2004-12-20
EE200200277A (en) 2003-10-15
MXPA02005354A (en) 2002-12-11
OA12099A (en) 2006-05-04
GT200000199A (en) 2002-05-23
NO20022558L (en) 2002-05-29
PL355892A1 (en) 2004-05-31
TR200201446T2 (en) 2002-11-21
IS6338A (en) 2002-04-12
AU1048801A (en) 2001-06-12
EA200200510A1 (en) 2002-10-31
TNSN00231A1 (en) 2002-05-30
AP2002002531A0 (en) 2002-06-30
CO5271716A1 (en) 2003-04-30
NO20022558D0 (en) 2002-05-29

Similar Documents

Publication Publication Date Title
PE20010904A1 (en) 2-SUBSTITUTED 4-CARBOXAMINE-1,2,3,4-TETRAHYDROQUINOLINE CRYSTAL
AU2002303906B2 (en) Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
DE69232060T2 (en) Nitrogen-containing bicyclic compounds, processes for their preparation, their use as medicaments and compositions containing them
AP2004003059A0 (en) Salt forms of E-2-methoxy-N-(3-(4-(3-methyl-pyridin-3-yloxyl)-phenylamino)-quinazolin-6-yl)-allyl)-acetamide, its preparation and its use against cancer
US20040106616A1 (en) Substituted quinazolin-4-ylamine analogues
SK2722003A3 (en) Quinolinone derivatives as tyrosine kinase inhibitors
TR200200234T2 (en) Tyrosine Protein kinase SYK purine derivatives inhibitors
US8268846B2 (en) Amino heterocyclic linked pyrimidine derivatives
JPH05503530A (en) Angiotensin 2 antagonist containing substituted benzyl component
AU2002303906A1 (en) Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
TW200716648A (en) Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
EP1339706B1 (en) N-type calcium channel antagonists for the treatment of pain
WO2007022946A1 (en) Heterocyclic compounds and their use as binding partners for 5-ht5 receptors
JPS61282368A (en) Anticancer quinazoline derivative
DK0618906T3 (en) Substituted imidazole derivatives and their preparation and use
ES2038207T3 (en) PROCEDURE FOR THE OBTAINING OF 2-PIRIDIL-PENEM-COMPOUNDS.
CA2351644A1 (en) Pyrimidine derivatives and processes for the preparation thereof
Srivatava et al. Synthesis of substituted-4-oxo-1, 4-dihydro-3-[1-oxo-2-hydrazino-3-{p-toluenesulfon}] quinoline derivatives and their biological activity against bacterial infections
DE69717969D1 (en) SUBSTITUTED N-METHYL-N- (4- (PIPERIDIN-1-YL) -2-ARYLBUTYL) -BENZAMIDES FOR THE TREATMENT OF ALLERGIC DISEASES
US5447934A (en) Anti-allergic thiadiazolo [4,3-a]pyridine derivatives
PT99280A (en) PROCESS FOR THE PREPARATION OF INDOOR AND PHARMACEUTICAL COMPOUNDS DERIVATIVES
Gu et al. The Wittig–Horner reaction for the synthesis of neratinib
AR023709A1 (en) SEMIHYDROCLORIDE OF THE ACID 8-CIANO-1-CYCLOPROPIL-7- (1S, 6S-2,8-DIAZABICICLO [4.3.0] -NONAN-8-IL) -6-FLUOR-1,4-DIHIDRO-4-OXO- 3-CHINOLINCARBOXILICO, PROCEDURE FOR OBTAINING, MEDICATION, USE OF THE SAME FOR OBTAINING ANTIBACTERIAL DRUGS
JPH05112554A (en) New quinolonecarboxylic acid derivative
EP2432764A1 (en) Substituted quinolines for use as vegf inhibitors

Legal Events

Date Code Title Description
FD Application declared void or lapsed