CA2298813A1 - Modulateurs de pyrrolidine et de piperidine de l'activite du recepteur de chemokine - Google Patents

Modulateurs de pyrrolidine et de piperidine de l'activite du recepteur de chemokine Download PDF

Info

Publication number
CA2298813A1
CA2298813A1 CA002298813A CA2298813A CA2298813A1 CA 2298813 A1 CA2298813 A1 CA 2298813A1 CA 002298813 A CA002298813 A CA 002298813A CA 2298813 A CA2298813 A CA 2298813A CA 2298813 A1 CA2298813 A1 CA 2298813A1
Authority
CA
Canada
Prior art keywords
phenyl
alkyl
substituted
3alkyl
trifluoromethyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002298813A
Other languages
English (en)
Inventor
Richard J. Budhu
Jeffrey J. Hale
Edward Holson
Christopher Lynch
Malcolm Maccoss
Sander G. Mills
Scott C. Berk
Christopher A. Willoughby
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Individual
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
Priority claimed from GBGB9801009.3A external-priority patent/GB9801009D0/en
Application filed by Individual filed Critical Individual
Publication of CA2298813A1 publication Critical patent/CA2298813A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés de pyrrolidine et de pipéridine représentés par la formule (I) (dans laquelle R?1¿, R?2¿, R?3¿, R?4a¿, R?4b¿, R?4c¿, R?4d¿, R?4e¿, R?4f¿, R?4g¿, R?4h¿, m, n, x et y sont tels qu'ils sont définis dans le descriptif) et présentant une utilité en tant que modulateurs de l'activité du récepteur de chemokine. En particulier, ces composés sont utiles en tant que modulateurs des récepteurs de chemokine CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, soit CXCR-3, soit CXCR-4.
CA002298813A 1997-08-28 1998-08-27 Modulateurs de pyrrolidine et de piperidine de l'activite du recepteur de chemokine Abandoned CA2298813A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US5774397P 1997-08-28 1997-08-28
US60/057,743 1997-08-28
GB9801009.3 1998-01-16
GBGB9801009.3A GB9801009D0 (en) 1998-01-16 1998-01-16 Pyrrolidine and piperidine modulators of chemokine receptor activity
PCT/US1998/017755 WO1999009984A1 (fr) 1997-08-28 1998-08-27 Modulateurs de pyrrolidine et de piperidine de l'activite du recepteur de chemokine

Publications (1)

Publication Number Publication Date
CA2298813A1 true CA2298813A1 (fr) 1999-03-04

Family

ID=26312970

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002298813A Abandoned CA2298813A1 (fr) 1997-08-28 1998-08-27 Modulateurs de pyrrolidine et de piperidine de l'activite du recepteur de chemokine

Country Status (5)

Country Link
EP (1) EP1009405A4 (fr)
JP (1) JP2001526178A (fr)
AU (1) AU9206798A (fr)
CA (1) CA2298813A1 (fr)
WO (1) WO1999009984A1 (fr)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6025154A (en) 1995-06-06 2000-02-15 Human Genome Sciences, Inc. Polynucleotides encoding human G-protein chemokine receptor HDGNR10
US6743594B1 (en) 1995-06-06 2004-06-01 Human Genome Sciences, Inc. Methods of screening using human G-protein chemokine receptor HDGNR10 (CCR5)
AU2056800A (en) 1998-12-18 2000-07-03 Du Pont Pharmaceuticals Company Heterocyclic piperidines as modulators of chemokine receptor activity
US7217714B1 (en) 1998-12-23 2007-05-15 Agouron Pharmaceuticals, Inc. CCR5 modulators
EP1013276A1 (fr) 1998-12-23 2000-06-28 Pfizer Inc. Aminoazacycloalcanes comme modulateurs de CCR5
PE20001420A1 (es) 1998-12-23 2000-12-18 Pfizer Moduladores de ccr5
AU3389300A (en) * 1999-03-02 2000-09-21 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
WO2000051609A1 (fr) * 1999-03-02 2000-09-08 Merck & Co., Inc. Modulateurs de l'activite recepteur des chimiokines, a base de pyrrolidine a substitution 3-alkyle
US6303593B1 (en) * 1999-03-02 2001-10-16 Merck & Co., Inc. 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
US6248755B1 (en) * 1999-04-06 2001-06-19 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6265434B1 (en) * 1999-04-06 2001-07-24 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6399619B1 (en) * 1999-04-06 2002-06-04 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6498161B1 (en) 1999-04-06 2002-12-24 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
GB9912701D0 (en) * 1999-06-01 1999-08-04 Smithkline Beecham Plc Novel compounds
AU5328500A (en) 1999-06-11 2001-01-02 Merck & Co., Inc. N-cyclopentyl modulators of chemokine receptor activity
AU5469400A (en) 1999-06-11 2001-01-02 Merck & Co., Inc. Cyclopentyl modulators of chemokine receptor activity
WO2000076513A1 (fr) 1999-06-11 2000-12-21 Merck & Co., Inc. Modulateurs cyclopentyliques de l'activite du recepteur de la chimiokine
ATE344242T1 (de) * 1999-06-11 2006-11-15 Merck & Co Inc N-cyclopentylmodulatoren der chemokine rezeptoraktivität
WO2000076514A1 (fr) 1999-06-11 2000-12-21 Merck & Co., Inc. Modulateurs de cyclopentyle de l'activite du recepteur de chimiokine
US6358979B1 (en) 1999-06-11 2002-03-19 Merck & Co., Inc. N-cyclopentyl modulators of chemokine receptor activity
AU5473400A (en) 1999-06-11 2001-01-02 Merck & Co., Inc. Cyclopentyl modulators of chemokine receptor activity
WO2001064216A1 (fr) * 2000-02-28 2001-09-07 Merck & Co., Inc. Modulateurs 4-alkyl piperidinyl pyrrolidine d'activite de recepteur de chemokine
CA2413245A1 (fr) 2000-06-30 2002-01-10 Bristol-Myers Squibb Pharma Company N-ureidoheterocycloaklyl-piperidines utilises comme modulateurs de l'activite du recepteur de la chimiokine
US6531484B2 (en) 2000-10-11 2003-03-11 Merck & Co., Inc. Pyrrolidine modulators of CCR5 chemokine receptor activity
ATE341327T1 (de) 2001-02-28 2006-10-15 Merck & Co Inc Acylierte piperidin-derivate als melanocortin-4- rezeptor-agonisten
AU2002258414B2 (en) * 2001-02-28 2005-12-15 Merck Sharp & Dohme Corp. Acylated piperidine derivatives as melanocortin-4 receptor agonists
MXPA03008109A (es) * 2001-03-07 2003-12-12 Pfizer Prod Inc Moduladores de la actividad de receptores de quimiocinas.
GB0108099D0 (en) * 2001-03-30 2001-05-23 Hoffmann La Roche Aminopiperidine derivatives
PT1598340E (pt) * 2001-04-18 2009-04-13 Euro Celtique Sa Derivados de 1-(4-piperidinil)-1,3-di-hidro-2h-benzoxazole- 2-ona e compostos relacionados como análogos de nociceptina e ligandos orl1 para o tratamento da dor
JP4336196B2 (ja) 2001-07-18 2009-09-30 メルク エンド カムパニー インコーポレーテッド メラノコルチン受容体作動薬としての架橋ピペリジン誘導体
DK1531822T3 (da) 2002-06-12 2009-12-07 Chemocentryx Inc 1-aryl-4-substituerede piperazin derivater til anvendelse som CCR1 antagonister til behandlingen af inflammation og immunforstyrrelser
US7589199B2 (en) 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
US7842693B2 (en) 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
AU2003268493A1 (en) 2002-09-11 2004-04-30 Merck & Co., Inc. Piperazine urea derivatives as melanocortin-4 receptor agonists
EP1633343A1 (fr) 2003-05-30 2006-03-15 Neuromed Technologies, Inc. 3-aminomethyle-pyrrolidines comme inhibiteurs de canaux calciques de type n
EP1786815B1 (fr) 2003-09-10 2011-08-24 Virochem Pharma Inc. Composes spiro et procedes pour la modulation de l'activite de recepteur de chimiokine
GB0328906D0 (en) 2003-12-12 2004-01-14 Syngenta Participations Ag Chemical compounds
WO2005084667A1 (fr) 2004-03-03 2005-09-15 Chemocentryx, Inc. Hétérocycles d'azote bicycliques et pontés
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
EP2364705A3 (fr) * 2004-08-19 2012-04-04 Vertex Pharmaceuticals Incorporated Modulateurs des récepteurs muscariniques
NZ555770A (en) * 2004-12-24 2010-12-24 Astrazeneca Ab Heterocyclic piperazine-carboxamide compounds as CCR2B antagonists
US7635698B2 (en) 2004-12-29 2009-12-22 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
US7880002B2 (en) 2004-12-29 2011-02-01 Millennium Pharmaceuticals, Inc. Substituted piperazinyl-pyrrolidine compounds useful as chemokine receptor antagonists
JP2008526840A (ja) * 2005-01-06 2008-07-24 アストラゼネカ アクチボラグ 新規化合物
GB0505969D0 (en) 2005-03-23 2005-04-27 Novartis Ag Organic compounds
GB0514203D0 (en) 2005-07-11 2005-08-17 Novartis Ag Organic compounds
GB0525957D0 (en) 2005-12-21 2006-02-01 Astrazeneca Ab Methods
KR20080087841A (ko) * 2005-12-22 2008-10-01 버텍스 파마슈티칼스 인코포레이티드 무스카린 수용체의 조절제
US8129411B2 (en) 2005-12-30 2012-03-06 Novartis Ag Organic compounds
US7351706B2 (en) 2006-01-05 2008-04-01 Hoffmann-La Roche Inc. Indol-3-yl-carbonyl-spiro-piperidine derivatives
KR20080098070A (ko) * 2006-02-22 2008-11-06 버텍스 파마슈티칼스 인코포레이티드 무스카린성 수용체의 조절제로서의 스피로 축합된 피페리딘
ATE533744T1 (de) 2006-05-19 2011-12-15 Wyeth Llc N-benzoypyrrolidin-3-ylamine als histamin-3 antagonisten
US7727978B2 (en) 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
BRPI0813900A2 (pt) 2007-06-25 2014-12-30 Novartis Ag Derivados de n5-(2-etoxietil)-n3-(2-piridinil)-3,5-piperidinodicarboxa mida para uso como inibidores de renina
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
JP5580741B2 (ja) 2008-09-19 2014-08-27 武田薬品工業株式会社 含窒素複素環化合物およびその用途
WO2024020101A1 (fr) * 2022-07-21 2024-01-25 The Regents Of The University Of California Composés inhibiteurs de la prostaglandine e synthase 3 (ptges3)
CN115448864B (zh) * 2022-08-26 2023-12-22 上海方予健康医药科技有限公司 3-氟-3-（1-羟乙基）吡咯烷-1-羧酸叔丁酯的制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5635510A (en) * 1993-05-06 1997-06-03 Merrell Pharmaceuticals Inc. Substituted pyrrolidin-3-yl-alkyl-piperidines

Also Published As

Publication number Publication date
JP2001526178A (ja) 2001-12-18
EP1009405A4 (fr) 2001-05-09
EP1009405A1 (fr) 2000-06-21
WO1999009984A1 (fr) 1999-03-04
AU9206798A (en) 1999-03-16

Similar Documents

Publication Publication Date Title
US6166037A (en) Pyrrolidine and piperidine modulators of chemokine receptor activity
CA2298813A1 (fr) Modulateurs de pyrrolidine et de piperidine de l'activite du recepteur de chemokine
US6303593B1 (en) 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
US6136827A (en) Cyclic amine modulations of chemokine receptor activity
US6140349A (en) Cyclic amine modulators of chemokine receptor activity
US6362201B1 (en) 3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity
US5962462A (en) Spiro-substituted azacycles as modulators of chemokine receptor activity
US6489354B1 (en) 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
EP1003514A1 (fr) Amines cycliques modulant l'activite des recepteurs de chimiokines
AU770491B2 (en) Pyrrolidine modulators of chemokine receptor activity
CA2319781A1 (fr) Amines cycliques utilisees en tant que modulateurs de l'activite du recepteur de chemokine
US6372764B1 (en) Pyrrolidine modulators of chemokine receptor activity
WO1998025605A1 (fr) Azacycles spiro-substitues utilises comme modulateurs de l'activite des recepteurs de la chemokine
US6511994B2 (en) Modulators of CCR5 chemokine receptor activity
WO2000059498A1 (fr) Modulateurs de pyrrolidine de l'activite du recepteur des chimiokines
WO2000076514A1 (fr) Modulateurs de cyclopentyle de l'activite du recepteur de chimiokine
WO2000076512A1 (fr) Modulateurs cyclopentyliques de l'activite du recepteur de la chimiokine
US6538002B1 (en) Cyclopentyl modulators of chemokine receptor activity
US6593346B2 (en) N-cyclopentyl modulators of chemokine receptor activity
EP1192133B1 (fr) Modulateurs n-cyclopentyliques de l'activite du recepteur de la chimiokine
US6455548B2 (en) 4-alkyl piperidinyl pyrrolidine modulators of chemokine receptor activity
WO2004058702A2 (fr) 4-[(4-(carboxyethyl)piperidinyl)methyl]pyrrolidines servant de modulateurs de l'activite des recepteurs des chimiokines

Legal Events

Date Code Title Description
FZDE Dead