EA200000873A1 - Phospholipase A Inhibitors - Google Patents

Phospholipase A Inhibitors

Info

Publication number
EA200000873A1
EA200000873A1 EA200000873A EA200000873A EA200000873A1 EA 200000873 A1 EA200000873 A1 EA 200000873A1 EA 200000873 A EA200000873 A EA 200000873A EA 200000873 A EA200000873 A EA 200000873A EA 200000873 A1 EA200000873 A1 EA 200000873A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
phospholipase
cpla
formulas
iii
Prior art date
Application number
EA200000873A
Other languages
Russian (ru)
Inventor
Джасбир С. Сихра
ЙиБин Ксианг
Джин Бемис
Джон МакКью
Неелу Кайла
Лихрен Чен
Original Assignee
Дженетикс Инститьют, Инк.
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 Дженетикс Инститьют, Инк. filed Critical Дженетикс Инститьют, Инк.
Publication of EA200000873A1 publication Critical patent/EA200000873A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/32Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/22Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an aralkyl radical attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/86Oxygen and sulfur atoms, e.g. thiohydantoin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/34Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/06Heterocyclic 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/10Heterocyclic 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 aromatic rings

Abstract

Описываются ингибиторы активности cPLA, имеющие химическую формулу, выбранную из группы, состоящей из формул (I), (II) и (III), (IV), (V) или (VI)Международная заявка была опубликована вместе с отчетом о международном поиске.Inhibitors of cPLA activity are described, having a chemical formula selected from the group consisting of formulas (I), (II) and (III), (IV), (V) or (VI). The international application was published together with an international search report.

EA200000873A 1998-02-25 1999-02-17 Phospholipase A Inhibitors EA200000873A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3010298A 1998-02-25 1998-02-25
PCT/US1999/003388 WO1999043672A1 (en) 1998-02-25 1999-02-17 Inhibitors of phospholipase a2

Publications (1)

Publication Number Publication Date
EA200000873A1 true EA200000873A1 (en) 2001-04-23

Family

ID=21852517

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000873A EA200000873A1 (en) 1998-02-25 1999-02-17 Phospholipase A Inhibitors

Country Status (19)

Country Link
EP (1) EP1062216A1 (en)
JP (1) JP2002504551A (en)
KR (1) KR20010041346A (en)
CN (1) CN1298404A (en)
AU (1) AU3297099A (en)
BG (1) BG104781A (en)
BR (1) BR9909242A (en)
CA (1) CA2322163A1 (en)
EA (1) EA200000873A1 (en)
EE (1) EE200000522A (en)
HR (1) HRP20000513A2 (en)
HU (1) HUP0100156A3 (en)
ID (1) ID26123A (en)
IL (1) IL137540A0 (en)
NO (1) NO20004217L (en)
PL (1) PL342516A1 (en)
SK (1) SK12782000A3 (en)
TR (1) TR200002445T2 (en)
WO (1) WO1999043672A1 (en)

Families Citing this family (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1509285A (en) * 2000-01-17 2004-06-30 Substituted aryl ketons
US6670388B1 (en) 2000-06-27 2003-12-30 Smithkline Beecham Corporation Fatty acid synthase inhibitors
AU2001272915A1 (en) * 2000-07-14 2002-01-30 Eli Lilly And Company Method for treating sepsis
AU2001277056B2 (en) 2000-07-25 2005-09-29 Merck & Co., Inc. N-substituted indoles useful in the treatment of diabetes
KR100884877B1 (en) 2000-12-28 2009-02-23 다이이찌 세이야꾸 가부시기가이샤 VLA-4 inhibitors
AU2002302248B2 (en) * 2001-05-23 2008-03-06 Merck Frosst Canada Ltd. Dihydropyrrolo[1,2-A]indole and tetrahydropyrido[1,2-A]-indole derivatives as prostaglandin D2 receptor antagonists
DK1397130T3 (en) 2001-06-20 2007-11-12 Wyeth Corp Substituted Indole Acid Derivatives as Inhibitors of Plasminogen Activator Inhibitor-1 (PAI-1)
TWI224101B (en) 2001-06-20 2004-11-21 Wyeth Corp Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
US7291639B2 (en) 2001-06-20 2007-11-06 Wyeth Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
JP4141954B2 (en) 2001-09-27 2008-08-27 エフ.ホフマン−ラ ロシュ アーゲー Indole derivatives as COXII inhibitors
US6984735B2 (en) 2001-12-03 2006-01-10 Wyeth Process for making an aldehyde
US6635771B2 (en) 2001-12-03 2003-10-21 Wyeth N-benzhydryl indole compounds
US7713964B2 (en) 2001-12-03 2010-05-11 Wyeth Llc Methods for treating asthmatic conditions
US7101875B2 (en) 2001-12-03 2006-09-05 Wyeth Methods for treating arthritic disorders
US7605156B2 (en) 2001-12-03 2009-10-20 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2
US6797708B2 (en) 2001-12-03 2004-09-28 Wyeth Inhibitors of cytosolic phospholipase A2
AUPS282602A0 (en) 2002-06-07 2002-06-27 Garvan Institute Of Medical Research Method of inhibiting cell proliferation
US7247741B2 (en) * 2005-01-21 2007-07-24 Ptc Therapeutics, Inc. Acetylamino benzoic acid compounds and their use for nonsense suppression and the treatment of disease
BR0313352A (en) 2002-07-31 2005-07-12 Euro Celtique Sa Compound, pharmaceutical compositions, method for producing a compound, method for treating, preventing or ameliorating a disorder and method for treating a mammal
JP4340232B2 (en) 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 Indoles having anti-diabetic activity
WO2004020409A1 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
US7795280B2 (en) 2002-11-07 2010-09-14 N.V. Organon Indoles useful in the treatment of androgen-receptor related diseases
CN1726191A (en) 2002-12-10 2006-01-25 惠氏公司 Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
EP1569899B1 (en) 2002-12-10 2006-06-28 Wyeth Substituted 3-alkyl- and 3-arylalkyl-1h-indol-1-yl-acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
CN1723198A (en) 2002-12-10 2006-01-18 惠氏公司 Aryl, aryloxy, and alkyloxy substituted 1h-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
DK1569900T3 (en) 2002-12-10 2006-10-23 Wyeth Corp Substituted 3-carbonyl-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
UA80453C2 (en) 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
US7129264B2 (en) * 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7094790B2 (en) 2003-05-07 2006-08-22 Abbott Laboratories Fused bicyclic-substituted amines as histamine-3 receptor ligands
EP1643991B1 (en) * 2003-07-11 2014-03-12 Merck Patent GmbH Benzimidazole carboxamides as raf kinase inhibitors
CN1826336B (en) 2003-07-24 2010-06-02 第一制药株式会社 Cyclohexanecarboxylic acid compound
WO2005012297A1 (en) * 2003-07-28 2005-02-10 Janssen Pharmaceutica N.V. Benzimidazole, benzthiazole and benzoxazole derivatives and their use as lta4h modulators
US7265148B2 (en) 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7446201B2 (en) 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7332521B2 (en) 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7420083B2 (en) 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7582773B2 (en) 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7141592B2 (en) 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7351726B2 (en) 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7119214B2 (en) * 2004-04-13 2006-10-10 Cephalon France Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
TW200602317A (en) 2004-04-23 2006-01-16 Akzo Nobel Nv Novel androgens
US20050244367A1 (en) * 2004-05-03 2005-11-03 Ilypsa, Inc. Phospholipase inhibitors localized in the gastrointestinal lumen
AU2005254782A1 (en) 2004-06-18 2005-12-29 Biolipox Ab Indoles useful in the treatment of inflammation
MX2007002178A (en) 2004-08-23 2007-04-02 Wyeth Corp Oxazolo-naphthyl acids as plaminogen activator inhibtor type-1 (pai-1) modulators useful in the treatment of thrombosis and cardiovascular diseases.
CN101124207A (en) * 2004-09-21 2008-02-13 阿特西斯公司 Benzimidazole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof
ES2314739T3 (en) 2004-10-27 2009-03-16 Janssen Pharmaceutica Nv DERIVATIVES OF INDOL AS MODULATORS OF PROGESTERONE RECEPTORS.
ATE399156T1 (en) * 2004-10-27 2008-07-15 Hoffmann La Roche NEW INDOLE OR BENZIMIDAZOLE DERIVATIVES
US20090042949A1 (en) * 2005-01-19 2009-02-12 Benjamin Pelcman Indoles Useful in the Treatment of Inflammation
DE602005026867D1 (en) * 2005-01-19 2011-04-21 Biolipox Ab INFLAMMATORY INDOL DERIVATIVES
CA2594777A1 (en) * 2005-01-19 2006-07-27 Biolipox Ab Indoles useful in the treatment of inflamation
US20080249091A1 (en) * 2005-01-19 2008-10-09 Benjamin Pelcman Indoles Useful in the Treatment of Inflammation
WO2006109633A1 (en) * 2005-04-07 2006-10-19 Daiichi Sankyo Company, Limited Substituted indole compound
GT200600228A (en) 2005-05-27 2006-12-26 INHIBITORS OF PHOSPHOLIPASE A2 CITOSOLICA
AU2006279496A1 (en) 2005-08-17 2007-02-22 Wyeth Substituted indoles and use thereof
AR056690A1 (en) 2005-10-14 2007-10-17 Athersys Inc INDOL DERIVATIVES AS INDOL INHIBITORS AS INHIBITORS OF HISTAMINE RECEIVER 3 FOR THE PARKING OF SUENO DISORDERS AND COGNITIVES OBESITY AND OTHER SNC DISORDERS
EP1779848A1 (en) * 2005-10-28 2007-05-02 Nikem Research S.R.L. V-ATPase inhibitors for the treatment of inflammatory and autoimmune diseases
MX2008005666A (en) 2005-11-03 2009-03-02 Ilypsa Inc Multivalent indole compounds and use thereof as phospholipase-a2 inhibitors.
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
US8399666B2 (en) 2005-11-04 2013-03-19 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
GB2431927B (en) 2005-11-04 2010-03-17 Amira Pharmaceuticals Inc 5-Lipoxygenase-activating protein (FLAP) inhibitors
WO2008009924A2 (en) * 2006-07-18 2008-01-24 Biolipox Ab Indoles useful in the treatment of inflammation
JP5406716B2 (en) 2006-08-07 2014-02-05 アイアンウッド ファーマシューティカルズ インコーポレイテッド Indole compounds
BRPI0906433A2 (en) 2008-01-31 2019-09-24 Sanofi Aventis cyclic indole-3-carboxamides, their preparation and their use as a pharmaceutical
CN102137858B (en) 2008-05-23 2014-07-23 潘米拉制药有限责任公司 5-lipoxygenase-activating protein inhibitor
MX2011003239A (en) 2008-09-26 2011-04-28 Merck Sharp & Dohme Novel cyclic benzimidazole derivatives useful anti-diabetic agents.
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
EP2352374B1 (en) 2008-10-29 2014-09-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CA2741672A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
AR077280A1 (en) 2009-06-29 2011-08-17 Incyte Corp PYRIMIDINONES AS PI3K INHIBITORS, AND PHARMACEUTICAL COMPOSITIONS THAT UNDERSTAND THEM
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
AU2011210765A1 (en) 2010-01-28 2012-09-13 President And Fellows Of Harvard College Compositions and methods for enhancing proteasome activity
WO2011106273A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US8598156B2 (en) 2010-03-25 2013-12-03 Glaxosmithkline Llc Chemical compounds
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
US9617197B2 (en) * 2010-08-04 2017-04-11 University Of Virginia Patent Foundation Compositions and methods for treating inflammatory diseases
EP2606031B1 (en) 2010-08-20 2017-09-27 Amira Pharmaceuticals, Inc. Autotaxin inhibitors and uses thereof
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
AR084433A1 (en) 2010-12-22 2013-05-15 Ironwood Pharmaceuticals Inc FAAH INHIBITORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
CN103635230B (en) 2011-05-12 2017-10-31 普罗蒂斯特斯治疗公司 Albumen homeostasis conditioning agent
US9260416B2 (en) 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
SI2751109T1 (en) 2011-09-02 2017-03-31 Incyte Holdings Corporation Heterocyclylamines as pi3k inhibitors
ES2790358T3 (en) 2011-12-28 2020-10-27 Global Blood Therapeutics Inc Substituted Heteroaryl Aldehyde Compounds and Methods for Their Use in Increasing Tissue Oxygenation
PT3738434T (en) 2011-12-28 2023-11-13 Global Blood Therapeutics Inc Intermediates to obtain substituted benzaldehyde compounds and methods for their use in increasing tissue oxygenation
AR090548A1 (en) 2012-04-02 2014-11-19 Incyte Corp BICYCLIC AZAHETEROCICLOBENCILAMINS AS PI3K INHIBITORS
JP2015526520A (en) 2012-08-31 2015-09-10 プリンシピア バイオファーマ インコーポレイテッド Benzimidazole derivatives as ITK inhibitors
WO2014116228A1 (en) 2013-01-25 2014-07-31 President And Fellows Of Harvard College Usp14 inhibitors for treating or preventing viral infections
US20140274961A1 (en) 2013-03-15 2014-09-18 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
EA033555B1 (en) 2013-03-15 2019-10-31 Global Blood Therapeutics Inc Pharmaceutical compositions for treating sickle cell disorder
US9458139B2 (en) 2013-03-15 2016-10-04 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US8952171B2 (en) 2013-03-15 2015-02-10 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9802900B2 (en) 2013-03-15 2017-10-31 Global Blood Therapeutics, Inc. Bicyclic heteroaryl compounds and uses thereof for the modulation of hemoglobin
US10100043B2 (en) 2013-03-15 2018-10-16 Global Blood Therapeutics, Inc. Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
US10266551B2 (en) 2013-03-15 2019-04-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9422279B2 (en) 2013-03-15 2016-08-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
CN105073728A (en) 2013-03-15 2015-11-18 全球血液疗法股份有限公司 Compounds and uses thereof for the modulation of hemoglobin
PE20160078A1 (en) 2013-03-15 2016-03-02 Global Blood Therapeutics Inc COMPOUNDS AND THEIR USES TO MODULATE HEMOGLOBIN
US9604999B2 (en) 2013-03-15 2017-03-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
EP3049405A4 (en) 2013-09-26 2017-03-08 Pharmakea Inc. Autotaxin inhibitor compounds
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
EP3071205B1 (en) 2013-11-18 2020-02-05 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
MX370535B (en) 2013-11-18 2019-12-17 Forma Therapeutics Inc Tetrahydroquinoline compositions as bet bromodomain inhibitors.
EA201992707A1 (en) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. COMPOUNDS AND THEIR APPLICATIONS FOR HEMOGLOBIN MODULATION
MY189995A (en) 2014-02-07 2022-03-22 Global Blood Therapeutics Inc Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
CN117800973A (en) 2015-02-27 2024-04-02 因赛特控股公司 Salts of PI3K inhibitors and methods of making the same
MA41841A (en) 2015-03-30 2018-02-06 Global Blood Therapeutics Inc ALDEHYDE COMPOUNDS FOR THE TREATMENT OF PULMONARY FIBROSIS, HYPOXIA, AND AUTOIMMUNE AND CONNECTIVE TISSUE DISEASES
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US11020382B2 (en) 2015-12-04 2021-06-01 Global Blood Therapeutics, Inc. Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
EA034514B1 (en) 2015-12-15 2020-02-14 Астразенека Аб Isoindole compounds
AR108435A1 (en) 2016-05-12 2018-08-22 Global Blood Therapeutics Inc PROCESS TO SYNTHETIZE 2-HYDROXI-6 - ((2- (1-ISOPROPIL-1H-PIRAZOL-5-IL) -PIRIDIN-3-IL) METOXI) BENZALDEHYDE
TWI778983B (en) 2016-10-12 2022-10-01 美商全球血液治療公司 Tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
CN110730780A (en) 2017-06-14 2020-01-24 阿斯利康(瑞典)有限公司 2, 3-dihydroisoindole-1-carboxamides useful as ROR-gamma modulators
ES2966707T3 (en) 2018-10-01 2024-04-23 Global Blood Therapeutics Inc Hemoglobin modulators for the treatment of sickle cell disease
EP3860998B1 (en) 2018-10-05 2023-12-27 Annapurna Bio Inc. Compounds and compositions for treating conditions associated with apj receptor activity

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL109311A0 (en) * 1993-04-16 1994-07-31 Lilly Co Eli 1H-indole-3-acetamide sPla2 inhibitors
DE4338770A1 (en) * 1993-11-12 1995-05-18 Matthias Dr Lehr Indole-2-alkanoic acids and their derivatives as inhibitors of phospholipase A¶2¶
ES2196163T3 (en) * 1995-07-31 2003-12-16 Shionogi & Co PIRROLIDINE DERIVATIVES WITH AN INHIBITION ACTIVITY OF PHOSPHOLIPASE A2.
ATE255090T1 (en) * 1996-08-01 2003-12-15 Merckle Gmbh ACYLPYRROLDICARBONONIC ACIDS AND ACYLINDOLICARBONONIC ACIDS AND THEIR DERIVATIVES AS INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2
AU717430B2 (en) * 1996-08-26 2000-03-23 Genetics Institute, Llc Inhibitors of phospholipase enzymes

Also Published As

Publication number Publication date
HUP0100156A2 (en) 2001-07-30
AU3297099A (en) 1999-09-15
ID26123A (en) 2000-11-23
IL137540A0 (en) 2001-07-24
NO20004217L (en) 2000-10-23
NO20004217D0 (en) 2000-08-23
TR200002445T2 (en) 2000-12-21
PL342516A1 (en) 2001-06-18
WO1999043672A1 (en) 1999-09-02
WO1999043672A9 (en) 2000-05-04
KR20010041346A (en) 2001-05-15
SK12782000A3 (en) 2001-04-09
BR9909242A (en) 2000-11-14
CN1298404A (en) 2001-06-06
EP1062216A1 (en) 2000-12-27
BG104781A (en) 2001-10-31
JP2002504551A (en) 2002-02-12
HUP0100156A3 (en) 2002-12-28
HRP20000513A2 (en) 2001-12-31
CA2322163A1 (en) 1999-09-02
EE200000522A (en) 2002-02-15

Similar Documents

Publication Publication Date Title
EA200000873A1 (en) Phospholipase A Inhibitors
EA199900643A1 (en) SULFAMIDE METHOD PROTEASIS INHIBITORS
EA200000868A1 (en) PHOSPHOLIPAZ INHIBITORS
EA200000768A1 (en) SUBSTITUTED OXOAZAGETEROCYCLIC INHIBITORS OF THE FACTOR Xa
EA199800106A1 (en) COMPOUNDS AND CONTAINING THEIR PHARMACEUTICAL COMPOSITIONS
EA199900592A1 (en) Pesticidal 1-arylpyrazole
EA199901030A1 (en) METHOD AND SYSTEM OF DESIGNING AND MANUFACTURING LASER SCANNERS COMPATIBLE WITH THE GLOBAL INFORMATION NETWORK
DE69528528T2 (en) Thrombin Inhibitors
EA199900936A1 (en) FUNGICIDAL TRIFTOROMETHYLALKYLAMINOTRIAZOLOPYRIMIDINES
DE69620161T2 (en) thrombin inhibitors
EA199900758A1 (en) SMALL MOLECULES USEFUL AT TREATMENT OF INFLAMMATORY DISEASES
ATE37375T1 (en) PHOSPHONYL HYDROXYACYL AMINO ACID DERIVATIVES AND THEIR USE AS ANTIHYPERTENSIVES.
TR199800773T2 (en) Thrombin inhibitors.
AR062713A2 (en) ANTIMICROBIAL EMULSION
TR200100605T2 (en) Arylpiperazines and their use as metalloproteinase inhibitors (MMP)
EA200000098A1 (en) 4-AMINOPIRROL (3,2-d) Pyrimidine as antagonists of the neuropeptide Y neuropeptide
TR199801255T2 (en) Vitronectin receptor antagonists.
TR199800011T1 (en) Benzo$g] quinoline t�revleri
NO904208D0 (en) INHIBITORS WHICH INHIBIT RETROVIRAL PROTEAS.
CY1108567T1 (en) ANTI-THROUGH UNITS
DE69812634D1 (en) Metalloproteinase inhibitors
EA200000320A1 (en) IZOHINOLINY AS UROKINASE INHIBITORS
NO993626D0 (en) Mixture comprising an oil-soluble deposition inhibitor
TR200100885T2 (en) 2-Methyl-thieno-benzodiazepine formulation
EA200200005A1 (en) PIRASYNE INHIBITORS THROMBIN