CA2322162A1 - Inhibiteurs d'enzymes phospholipases - Google Patents

Inhibiteurs d'enzymes phospholipases Download PDF

Info

Publication number
CA2322162A1
CA2322162A1 CA002322162A CA2322162A CA2322162A1 CA 2322162 A1 CA2322162 A1 CA 2322162A1 CA 002322162 A CA002322162 A CA 002322162A CA 2322162 A CA2322162 A CA 2322162A CA 2322162 A1 CA2322162 A1 CA 2322162A1
Authority
CA
Canada
Prior art keywords
alkyl
cooh
indol
phenyl
benzyl
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
CA002322162A
Other languages
English (en)
Inventor
Lihren Chen
John L. Knopf
Jasbir S. Seehra
Frank Lovering
John C. Mckew
Yibin Xiang
Jean E. Bemis
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.)
Genetics Institute LLC
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
Application filed by Individual filed Critical Individual
Publication of CA2322162A1 publication Critical patent/CA2322162A1/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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—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
    • 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
    • C07D401/10—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 aromatic rings
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne des composés et des compositions pharmaceutiques qui conviennent pour le traitement ou la prévention d'affections inflammatoires chez un mammifère. Elle concerne des procédés qui consistent à administrer de nouveaux composés pharmaceutiquement efficaces de la formule (I) ou (II), ou des sels pharmaceutiquement acceptables desdits composés. Dans ladite formule, R¿1?-R¿5? sont tels que définis dans le mémorandum descriptif.
CA002322162A 1998-02-25 1999-02-24 Inhibiteurs d'enzymes phospholipases Abandoned CA2322162A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3059298A 1998-02-25 1998-02-25
US09/030,592 1998-02-25
PCT/US1999/003898 WO1999043654A2 (fr) 1998-02-25 1999-02-24 Inhibiteurs d'enzymes phospholipases

Publications (1)

Publication Number Publication Date
CA2322162A1 true CA2322162A1 (fr) 1999-09-02

Family

ID=21854952

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002322162A Abandoned CA2322162A1 (fr) 1998-02-25 1999-02-24 Inhibiteurs d'enzymes phospholipases

Country Status (21)

Country Link
EP (1) EP1062205A2 (fr)
JP (1) JP2002504541A (fr)
KR (1) KR20010041344A (fr)
CN (1) CN1310706A (fr)
AU (1) AU765427B2 (fr)
BG (1) BG104779A (fr)
BR (1) BR9908275A (fr)
CA (1) CA2322162A1 (fr)
EA (1) EA003876B1 (fr)
EE (1) EE200000488A (fr)
GE (1) GEP20032920B (fr)
HR (1) HRP20000551A2 (fr)
HU (1) HUP0101146A3 (fr)
ID (1) ID26250A (fr)
IL (1) IL137719A0 (fr)
NO (1) NO20004219L (fr)
NZ (1) NZ506329A (fr)
PL (1) PL343007A1 (fr)
SK (1) SK12752000A3 (fr)
TR (1) TR200002447T2 (fr)
WO (1) WO1999043654A2 (fr)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19917504A1 (de) * 1999-04-17 2000-10-19 Dresden Arzneimittel Verwendung von Hydroxyindolen, die Inhibitoren der Phosphodiesterase 4 sind, zur Therapie chronisch obstruktiver Lungenerkrankungen
TR200003194T2 (tr) * 1998-05-01 2001-03-21 Eli Lilly And Company Hastalık tedavisine mahsus sPLA2 önleyici bileşikler
TWI269654B (en) * 1999-09-28 2007-01-01 Baxter Healthcare Sa N-substituted indole-3-glyoxylamide compounds having anti-tumor action
DE19951360A1 (de) 1999-10-26 2001-05-03 Aventis Pharma Gmbh Substituierte Indole
DE19962300A1 (de) * 1999-12-23 2001-06-28 Asta Medica Ag Substituierte N-Benzyl-Indol-3-yl-glyoxylsäure-Derivate mit Antitumorwirkung
DE19963178A1 (de) 1999-12-27 2001-07-05 Gruenenthal Gmbh Substituierte Indol-Mannichbasen
DE10006139A1 (de) * 2000-02-11 2001-08-16 Merck Patent Gmbh Indol-3-yl-Derivate
AUPQ876400A0 (en) * 2000-07-14 2000-08-03 University Of Queensland, The Compositions and method of using them
JP2004513076A (ja) 2000-07-25 2004-04-30 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病治療で有用なｎ−置換インドール類
DE10037310A1 (de) 2000-07-28 2002-02-07 Asta Medica Ag Neue Indolderivate und deren Verwendung als Arzneimittel
EP1415987B1 (fr) 2000-10-20 2007-02-28 Eisai R&D Management Co., Ltd. Composes heteroaromatiques azotes pour le traitement des maladies de cancer
EP1349858B1 (fr) 2000-11-02 2008-08-27 THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Agents permettant la reduction de la proteine precurseur amyloide et le traitement de la demence et procede d'utilisation de tels agents
TWI224101B (en) 2001-06-20 2004-11-21 Wyeth Corp Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
EP1844771A3 (fr) * 2001-06-20 2007-11-07 Wyeth Dérives d'acide indole substitue utilises en tant qu'inhibiteurs de l'inhibiteur-1 (PAI-1) de l'activateur plasminogene
DE60221391T2 (de) 2001-06-20 2008-04-17 Wyeth Substituierte indolsäurederivate als inhibitoren von plasminogen-aktivator-inhibitor-1 (pai-1)
EP1411925A1 (fr) 2001-08-03 2004-04-28 PHARMACIA & UPJOHN COMPANY 5-arylsulfonyl indoles presentant une affinite avec les recepteurs 5-ht6
AU2002323474B2 (en) 2001-09-13 2006-10-05 Synta Pharmaceuticals Corp 3-glyoxlylamideindoles for treating cancer
US7605156B2 (en) 2001-12-03 2009-10-20 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2
TWI334778B (en) * 2001-12-03 2010-12-21 Wyeth Corp Inhibitors of cytosolic phospholipase a2
US6635771B2 (en) 2001-12-03 2003-10-21 Wyeth N-benzhydryl indole compounds
US6797708B2 (en) 2001-12-03 2004-09-28 Wyeth Inhibitors of cytosolic phospholipase A2
US7101875B2 (en) 2001-12-03 2006-09-05 Wyeth Methods for treating arthritic disorders
US7713964B2 (en) 2001-12-03 2010-05-11 Wyeth Llc Methods for treating asthmatic conditions
US6984735B2 (en) 2001-12-03 2006-01-10 Wyeth Process for making an aldehyde
WO2003087087A2 (fr) * 2002-04-09 2003-10-23 Astex Technology Limited Composes pharmaceutiques
AUPS282602A0 (en) 2002-06-07 2002-06-27 Garvan Institute Of Medical Research Method of inhibiting cell proliferation
JP4340232B2 (ja) 2002-08-29 2009-10-07 メルク エンド カムパニー インコーポレーテッド 抗糖尿病活性を有するインドール類
NZ538031A (en) 2002-08-29 2007-10-26 Merck & Co Inc Indoles having anti-diabetic activity
UA80453C2 (en) 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
DK1569899T3 (da) 2002-12-10 2006-10-23 Wyeth Corp Substituerede 3-alkyl- og 3-arylalkyl-1H-indol-1-yl-eddikesyrederivater som inhibitorer af plasminogenaktivator-inhibitor-1 (PAI-1)
BR0316574A (pt) 2002-12-10 2005-10-04 Wyeth Corp Derivados de ácido acético 3-carbonil-1h-indol-1-il substituìdo como inibidores do inibidor-1 do ativador do plasminogênio (pai-1)
CA2509191A1 (fr) 2002-12-10 2004-06-24 Wyeth Derives d'acide 1h-indol-3-yl glyoxylique a substitution aryle, aryloxy et alkyloxy en tant qu'inhibiteurs de l'inhibiteur de l'activateur du plasminogene-1 (pai-1)
US7056943B2 (en) 2002-12-10 2006-06-06 Wyeth Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
US7129264B2 (en) * 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7582773B2 (en) 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7420083B2 (en) 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7265148B2 (en) 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7446201B2 (en) 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7534894B2 (en) 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
US7141592B2 (en) 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7351726B2 (en) 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7332521B2 (en) 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
CN101006053A (zh) 2004-06-18 2007-07-25 比奥里波克斯公司 用于治疗炎症的吲哚
JP2008510814A (ja) 2004-08-23 2008-04-10 ワイス Ｐａｉ−１阻害剤としてのピロロ−ナフチル酸
CA2577846A1 (fr) 2004-08-23 2006-03-02 Wyeth Acides thiazolo-naphthyliques
US7754747B2 (en) 2004-08-23 2010-07-13 Wyeth Llc Oxazolo-naphthyl acids
ATE428421T1 (de) 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
ATE501119T1 (de) 2005-01-19 2011-03-15 Biolipox Ab Entzündungshemmende indol-derivate
WO2007024294A2 (fr) 2005-05-03 2007-03-01 Cgi Pharmaceuticals, Inc. Certains urees substitues, modulateurs de l'activite des kinases
TW200718687A (en) 2005-05-27 2007-05-16 Wyeth Corp Inhibitors of cytosolic phospholipase A2
EP1925676A4 (fr) 2005-08-02 2010-11-10 Eisai R&D Man Co Ltd Procédé d'analyse de l' effet d 'un inhibiteur de vascularisation
EP1919866A2 (fr) 2005-08-17 2008-05-14 Wyeth a Corporation of the State of Delaware Composes d'indole substitues et leur utilisation
GB0525141D0 (en) * 2005-12-09 2006-01-18 Novartis Ag Organic compounds
BRPI0706523A2 (pt) 2006-01-13 2011-01-04 Wyeth Corp composto de fórmula i; composição farmacêutica; método de tratamento de distúrbios que estão relacionados com ou são afetados pela inibição da recaptação de norepinefrina, o receptor de 5-ht6 ou o receptor de 5-ht2a; método de tratamento de um distúrbio de aprendizado, de um distúrbio cognitivo, de um distúrbio de memória, de um distúrbio de personalidade, de um distúrbio comportamental, de um distúrbio de movimento, de um distúrbio neurodegenerativo, de abstinência de droga, de distúrbio de sono, de um distúrbio alimentar, de uma toxicidade de droga aguda, de um distúrbio cardiovascular, de uma disfunção sexual, de um distúrbio gastrintestinal, de um distúrbio genitourinário, de um distúrbio de dor, de um distúrbio nervoso ou de um distúrbio de sintoma vasomotor; método de tratamento de doença de alzheimer, de um distúrbio de deficiência da atenção, de esquizofrenia, de doença de parkinson, de discinésia tardia, de ataxia, de bradicinésia, de discinésias paroxìsmicas, de sìndrome da perna irrequieta, de tremor, de tremor essencial, de epilepsia, de apoplexia ou de trauma na cabeça; método de tratamento de doença arterial coronariana, de enfarte do miocárdio, de ataque isquêmico transitório, de angina, de fibrilação atrial, de agregação plaquetária, de risco de formação de coágulo sanguìneo, de sìndrome do intestino irritável, de constipação crÈnica, de doença do refluxo gastrintestinal, de dispepsia, de incontinência urinária por estresse ou de incontinência urinária de urgência; método de tratamento de depressão, de distúrbio compulsivo obsessivo, de tendência ao suicìdio, de distúrbio de ansiedade, de distúrbio bipolar, de distúrbio de pánico, de abstinência de nicotina, de abstinência de álcool, de abstinência de cocaìna, de abstinência de heroìna, de abstinência de anfetamina, de abstinência de drogas narcóticas, de insÈnia, de apnéia do sono, de narcolepsia, de distúrbio afetivo sanzonal, de sìndrome da perna irrequieta, de distúrbio de sono de turno de trabalho, de sìndrome da fase do sono retardada, de anorexia nervosa, de bulimia nervosa, de sìndrome do comer noturno, de superalimentação compulsiva, de sìndrome da fadiga crÈnica, de fibromialgia, de neuropatia de dor, de dor antinociceptiva, de sìndrome da dor crÈnica, de neuropatia diabética, de fogacho ou de suor noturno; e uso de um composto
CN101374808B (zh) 2006-01-24 2011-05-25 伊莱利利公司 孕酮受体的吲哚磺酰胺调节剂
WO2007092207A1 (fr) * 2006-02-03 2007-08-16 Wyeth Composition destinée à l'administration de dérivés d'indole substitués par naphtyle, et méthodes d'utilisation associées
WO2007136103A1 (fr) 2006-05-18 2007-11-29 Eisai R & D Management Co., Ltd. Agent antitumoral destiné au cancer de la thyroïde
EP2049520A4 (fr) 2006-08-07 2011-01-05 Ironwood Pharmaceuticals Inc Composés d'indole
KR101472600B1 (ko) 2006-08-28 2014-12-15 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암에 대한 항종양제
UA97257C2 (en) * 2006-10-19 2012-01-25 Такеда Фармасьютикал Компани Лимитед Indole derivatives
EP2119707B1 (fr) 2007-01-29 2015-01-14 Eisai R&D Management Co., Ltd. Composition destinée au traitement d'un cancer de l'estomac de type indifférencié
CN101848895B (zh) 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
EP2247575B1 (fr) 2008-01-31 2016-03-23 Sanofi Indole-3-carboxamides cycliques, leur preparation et leur utilisation comme produits pharmaceutiques
JP5198560B2 (ja) 2008-04-28 2013-05-15 旭化成ファーマ株式会社 フェニルプロピオン酸誘導体及びその用途
BR112012003592B8 (pt) 2009-08-19 2021-05-25 Eisai R&D Man Co Ltd composição farmacêutica contendo derivado de quinolina
CA2802644C (fr) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Agent anticancereux utilisant des composes ayant un effet inhibiteur de kinase en combinaison
AR084433A1 (es) 2010-12-22 2013-05-15 Ironwood Pharmaceuticals Inc Inhibidores de la faah y composiciones farmaceuticas que los contienen
EP2700403B1 (fr) 2011-04-18 2015-11-25 Eisai R&D Management Co., Ltd. Agent thérapeutique pour les tumeurs
WO2012166899A2 (fr) 2011-06-03 2012-12-06 Eisai R&D Management Co., Ltd. Biomarqueurs pour la prédiction et l'estimation de la sensibilité de sujets atteints d'un cancer de la thyroïde et du rein vis-à-vis de composés lenvatinib
US8889730B2 (en) * 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
AU2013364953A1 (en) 2012-12-21 2015-04-30 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same
CN105264380B (zh) 2013-05-14 2017-09-05 卫材R&D管理有限公司 用于预测和评价子宫内膜癌受试者对乐伐替尼化合物响应性的生物标志
CA2957005C (fr) 2014-08-28 2021-10-12 Eisai R&D Management Co., Ltd. Derive de quinoline de purete elevee et son procede de fabrication
SG11201706630UA (en) 2015-02-25 2017-09-28 Eisai R&D Man Co Ltd Method for suppressing bitterness of quinoline derivative
WO2016140717A1 (fr) 2015-03-04 2016-09-09 Merck Sharp & Dohme Corp. Association d'un antagoniste de pd-1 et d'un inhibiteur des tyrosines kinases vegfr/fgfr/ret pour traiter le cancer
BR112017027227B1 (pt) 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
JP6553726B2 (ja) 2015-08-20 2019-07-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
JP6872195B2 (ja) * 2015-10-29 2021-05-19 国立大学法人東北大学 コラーゲン産生抑制剤
CN106810488B (zh) * 2015-11-27 2021-02-19 中国科学院上海药物研究所 一类用作GPR17和CysLT1双重拮抗剂的化合物、其制备方法和用途
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
BR112019023064A2 (pt) 2017-05-16 2020-06-09 Eisai R&D Man Co Ltd tratamento de carcinoma hepatocelular
CN108530354B (zh) * 2018-05-07 2019-12-10 青岛农业大学 一种含苯磺酰基喹啉类化合物的合成方法
PT3860998T (pt) 2018-10-05 2024-04-02 Annapurna Bio Inc Compostos e composições para o tratamento de condições associadas à atividade do recetor apj

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3271416A (en) * 1961-10-24 1966-09-06 Merck & Co Inc Indolyl aliphatic acids
GB1148909A (en) * 1965-04-19 1969-04-16 Sumitomo Chemical Co Process for production of novel phenylhydrazone and phenylhydrazine derivatives
SE314373B (fr) * 1966-04-12 1969-09-08 Sumitomo Chemical Co
FR1583552A (fr) * 1967-04-11 1969-11-14
FR2152377A1 (en) * 1971-09-09 1973-04-27 Sumitomo Chemical Co 1-phenyl-2-methyl-5-alkyl or alkoxy-3-indolylacetic acid - derivs - antiinflammatory, analgesic, antipyretic
BE790679A (fr) * 1971-11-03 1973-04-27 Ici Ltd Derives de l'indole
US4894386A (en) * 1987-04-15 1990-01-16 Ici Americas Inc. Aliphatic carboxamides
ES2045420T3 (es) * 1988-04-13 1994-01-16 Ici America Inc Amidas ciclicas.
GB8906032D0 (en) * 1988-04-14 1989-04-26 Ici America Inc Hetera-aliphatic carboxamides
US5420289A (en) * 1989-10-27 1995-05-30 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
US5095031A (en) * 1990-08-20 1992-03-10 Abbott Laboratories Indole derivatives which inhibit leukotriene biosynthesis
IL109311A0 (en) * 1993-04-16 1994-07-31 Lilly Co Eli 1H-indole-3-acetamide sPla2 inhibitors
IL109309A (en) * 1993-04-16 2000-06-29 Lilly Co Eli 1-H-indole-3-acetic acid hydrazide SPLA2 inhibitors and pharmaceutical compositions containing them
DE4338770A1 (de) * 1993-11-12 1995-05-18 Matthias Dr Lehr Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
JP3109974B2 (ja) * 1994-04-01 2000-11-20 イーライ・リリー・アンド・カンパニー １Ｈ−インドール−３−グリオキシルアミドｓＰＬＡ２阻害剤
US5639780A (en) * 1995-05-22 1997-06-17 Merck Frosst Canada, Inc. N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors
US5604253A (en) * 1995-05-22 1997-02-18 Merck Frosst Canada, Inc. N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors
ES2138366T3 (es) * 1995-10-10 2000-01-01 Pfizer Indol carbamatos como antagonistas de leucotrienos.
ES2208935T3 (es) * 1996-08-01 2004-06-16 Merckle Gmbh Acidos acil-pirrol-dicarboxilicos y acidos acil-indol-dicarboxilicos, asi como sus derivados como inhibidores de la fosfolipasa a2 citosolica.
EP0922028A1 (fr) * 1996-08-26 1999-06-16 Genetics Institute, Inc. Inhibiteurs des enzymes phospholipases

Also Published As

Publication number Publication date
EA003876B1 (ru) 2003-10-30
HRP20000551A2 (en) 2001-04-30
IL137719A0 (en) 2001-10-31
ID26250A (id) 2000-12-07
TR200002447T2 (tr) 2000-11-21
CN1310706A (zh) 2001-08-29
EP1062205A2 (fr) 2000-12-27
AU765427B2 (en) 2003-09-18
NO20004219L (no) 2000-10-23
WO1999043654A3 (fr) 1999-10-28
HUP0101146A2 (hu) 2001-08-28
EE200000488A (et) 2002-02-15
WO1999043654A2 (fr) 1999-09-02
JP2002504541A (ja) 2002-02-12
BR9908275A (pt) 2000-10-24
HUP0101146A3 (en) 2001-11-28
BG104779A (en) 2001-10-31
EA200000871A1 (ru) 2001-04-23
AU2782599A (en) 1999-09-15
PL343007A1 (en) 2001-07-30
NZ506329A (en) 2004-01-30
NO20004219D0 (no) 2000-08-23
SK12752000A3 (sk) 2001-03-12
KR20010041344A (ko) 2001-05-15
GEP20032920B (en) 2003-03-25

Similar Documents

Publication Publication Date Title
AU765427B2 (en) Inhibitors of phospholipase enzymes
US6500853B1 (en) Inhibitors of phospholipase enzymes
CA2322161A1 (fr) Inhibiteurs d'enzymes phospholipases
JP2002504551A (ja) ホスホリパーゼａ２の阻害剤
US6828344B1 (en) Inhibitors of phospholipase enzymes
PT1397130E (pt) Derivados ácidos de indole substituído como inibidores de inibidor 1 do activador de plasminogénio (pai-1)
WO2005030717A1 (fr) Derives d'acide indole substitues et leur utilisation en tant qu'inhibiteurs de pai-1
US20030153751A1 (en) Inhibitors of phospholipase enzymes
CA2509191A1 (fr) Derives d'acide 1h-indol-3-yl glyoxylique a substitution aryle, aryloxy et alkyloxy en tant qu'inhibiteurs de l'inhibiteur de l'activateur du plasminogene-1 (pai-1)
JP2007500253A (ja) ステロイドホルモン核内受容体のインドール誘導体モジュレーター
MX2007010112A (es) Compuesto indol y uso del mismo.
CA2330623A1 (fr) 11-aryl-benzo[b]naphto[2,3-d]furanes et 11-aryl-benzo[b]naphto[2,3-d]thiophenes utiles dans les traitements de la resistance insulinique et de l'hyperglycemie
AU2006251946A1 (en) Inhibitors of cytosolic phospholipase A2
WO2007140317A2 (fr) Méthodes d'utilisation d'inhibiteurs de la phospholipase a2 cytosolique dans le traitement de la thrombose
MXPA00008292A (en) Inhibitors of phospholipase enzymes
AU2010294018A1 (en) Use of indole derivatives as NURR-1 activators for the application thereof as a medicament for the treatment of Parkinson's disease
WO2007107385A2 (fr) Inhibiteurs de l'adénylate-cyclase soluble
CZ20003115A3 (cs) Inhibitory fosfolipázy
MXPA00008295A (en) Inhibitors of phospholipase enzymes
CZ20003117A3 (cs) Inhibitory fosfolipázy
MXPA00008294A (en) Inhibitors of phospholipase a2
EP1844771A2 (fr) Dérives d'acide indole substitue utilises en tant qu'inhibiteurs de l'inhibiteur-1 (PAI-1) de l'activateur plasminogene

Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued