WO1999043651A3 - Inhibitors of phospholipase enzymes - Google Patents

Inhibitors of phospholipase enzymes Download PDF

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Publication number
WO1999043651A3
WO1999043651A3 PCT/US1999/003899 US9903899W WO9943651A3 WO 1999043651 A3 WO1999043651 A3 WO 1999043651A3 US 9903899 W US9903899 W US 9903899W WO 9943651 A3 WO9943651 A3 WO 9943651A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
phospholipase enzymes
phospholipase
disclosed
enzymes
Prior art date
Application number
PCT/US1999/003899
Other languages
French (fr)
Other versions
WO1999043651A2 (en
Inventor
Jasbir S Seehra
Neelu Kaila
John C Mckew
Frank Lovering
Jean E Bemis
Yibin Xiang
Original Assignee
Genetics Inst
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 to SK1274-2000A priority Critical patent/SK12742000A3/en
Priority to IL13771899A priority patent/IL137718A0/en
Application filed by Genetics Inst filed Critical Genetics Inst
Priority to AU27826/99A priority patent/AU2782699A/en
Priority to EEP200000486A priority patent/EE200000486A/en
Priority to CA002322161A priority patent/CA2322161A1/en
Priority to KR1020007009456A priority patent/KR20010041343A/en
Priority to JP2000533409A priority patent/JP2002504539A/en
Priority to EP99908379A priority patent/EP1056719A2/en
Priority to BR9908280-2A priority patent/BR9908280A/en
Priority to HU0100757A priority patent/HUP0100757A3/en
Priority to EA200000868A priority patent/EA200000868A1/en
Publication of WO1999043651A2 publication Critical patent/WO1999043651A2/en
Publication of WO1999043651A3 publication Critical patent/WO1999043651A3/en
Priority to NO20004220A priority patent/NO20004220L/en
Priority to HR20000552A priority patent/HRP20000552A2/en
Priority to BG104780A priority patent/BG104780A/en

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Classifications

    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D209/30Indoles; 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
    • 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
    • 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
    • C07D403/12Heterocyclic 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
    • 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
    • C07D409/14Heterocyclic 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

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  • 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)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Novel compounds are disclosed which inhibit the activity of phospholipase enzymes, particularly cytosolic phospholipase A2. Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.
PCT/US1999/003899 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes WO1999043651A2 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
BR9908280-2A BR9908280A (en) 1998-02-25 1999-02-24 Phospholipase enzyme inhibitors
EP99908379A EP1056719A2 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
AU27826/99A AU2782699A (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
IL13771899A IL137718A0 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
CA002322161A CA2322161A1 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
KR1020007009456A KR20010041343A (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
HU0100757A HUP0100757A3 (en) 1998-02-25 1999-02-24 Indole derivatives as inhibitors of phospholipase enzymes and pharmaceutical compositions containing them
SK1274-2000A SK12742000A3 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
EEP200000486A EE200000486A (en) 1998-02-25 1999-02-24 Phospholipase enzyme inhibitors, a pharmaceutical composition containing them, and a method of treating an inflammatory response in a mammal.
JP2000533409A JP2002504539A (en) 1998-02-25 1999-02-24 Phospholipase enzyme inhibitors
EA200000868A EA200000868A1 (en) 1998-02-25 1999-02-24 PHOSPHOLIPAZ INHIBITORS
NO20004220A NO20004220L (en) 1998-02-25 2000-08-23 Inhibitors of phospholipase enzymes
HR20000552A HRP20000552A2 (en) 1998-02-25 2000-08-24 Inhibitors of phospholipase enzymes
BG104780A BG104780A (en) 1998-02-25 2000-09-19 Inhibitors of phospholipase enzymes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3006298A 1998-02-25 1998-02-25
US09/030,062 1998-02-25

Publications (2)

Publication Number Publication Date
WO1999043651A2 WO1999043651A2 (en) 1999-09-02
WO1999043651A3 true WO1999043651A3 (en) 1999-12-16

Family

ID=21852314

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/003899 WO1999043651A2 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes

Country Status (19)

Country Link
EP (1) EP1056719A2 (en)
JP (1) JP2002504539A (en)
KR (1) KR20010041343A (en)
CN (1) CN1299347A (en)
AU (1) AU2782699A (en)
BG (1) BG104780A (en)
BR (1) BR9908280A (en)
CA (1) CA2322161A1 (en)
EA (1) EA200000868A1 (en)
EE (1) EE200000486A (en)
HR (1) HRP20000552A2 (en)
HU (1) HUP0100757A3 (en)
ID (1) ID27280A (en)
IL (1) IL137718A0 (en)
NO (1) NO20004220L (en)
PL (1) PL342995A1 (en)
SK (1) SK12742000A3 (en)
TR (1) TR200002446T2 (en)
WO (1) WO1999043651A2 (en)

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US8841295B2 (en) 2005-11-04 2014-09-23 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
US8940752B2 (en) 2009-06-29 2015-01-27 Incyte Corporation Pyrimidinones as PI3K inhibitors
US9096600B2 (en) 2010-12-20 2015-08-04 Incyte Corporation N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
US9193721B2 (en) 2010-04-14 2015-11-24 Incyte Holdings Corporation Fused derivatives as PI3Kδ inhibitors
US9199982B2 (en) 2011-09-02 2015-12-01 Incyte Holdings Corporation Heterocyclylamines as PI3K inhibitors
US9309251B2 (en) 2012-04-02 2016-04-12 Incyte Holdings Corporation Bicyclic azaheterocyclobenzylamines as PI3K inhibitors
US9403847B2 (en) 2009-12-18 2016-08-02 Incyte Holdings Corporation Substituted heteroaryl fused derivatives as P13K inhibitors

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DE60128475T2 (en) 2000-07-25 2008-02-07 Merck & Co., Inc. N-SUBSTITUTED INDOLE USED IN THE TREATMENT OF DIABETES
NZ539682A (en) 2001-01-29 2006-03-31 Dimensional Pharm Inc Substituted indoles and their use as integrin antagonists
US6916850B2 (en) 2001-05-03 2005-07-12 Galileo Pharmaceuticals, Inc. Pyruvate derivatives
US6608196B2 (en) 2001-05-03 2003-08-19 Galileo Pharmaceuticals, Inc. Process for solid supported synthesis of pyruvate-derived compounds
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)
PT1397130E (en) 2001-06-20 2007-11-13 Wyeth Corp Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
WO2003000668A1 (en) * 2001-06-25 2003-01-03 Nippon Soda Co., Ltd. Oxa(thia)zolidine compounds, process for preparation thereof and anti-inflammatory agents
US7605156B2 (en) 2001-12-03 2009-10-20 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2
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
US6797708B2 (en) 2001-12-03 2004-09-28 Wyeth Inhibitors of cytosolic phospholipase A2
US6635771B2 (en) 2001-12-03 2003-10-21 Wyeth N-benzhydryl indole compounds
US7101875B2 (en) 2001-12-03 2006-09-05 Wyeth Methods for treating arthritic disorders
DK1892239T3 (en) * 2001-12-03 2013-03-25 Wyeth Llc Inhibitors of cytosol phospholipase A2
SI1451154T1 (en) * 2001-12-03 2008-06-30 Wyeth Corp Inhibitors of cytosolic phospholipase a2
AUPS282602A0 (en) 2002-06-07 2002-06-27 Garvan Institute Of Medical Research Method of inhibiting cell proliferation
US7186746B2 (en) 2002-08-29 2007-03-06 Merck & Co., Inc. Indoles having anti-diabetic activity
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
DE60332769D1 (en) 2002-11-07 2010-07-08 Organon Nv INDOLE FOR TREATING DISEASES RELATED TO THE ANDROGEN RECEPTOR
CN1726190A (en) 2002-12-10 2006-01-25 惠氏公司 Substituted 3-carbonyl-1h-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
MXPA05006282A (en) 2002-12-10 2005-08-19 Wyeth Corp Substituted 3-alkyl and 3-arylalkyl 1h.
AU2003296324A1 (en) 2002-12-10 2004-06-30 Wyeth Aryl, aryloxy, and alkyloxy substituted 1h-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
BR0316584A (en) 2002-12-10 2005-10-04 Wyeth Corp Substituted oxo-acetyl amino indole acetic acid derivatives as plasminogen activator inhibitor-1 inhibitors (parent-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)
TW200510305A (en) * 2003-07-25 2005-03-16 Wyeth Corp Process for the preparation of CPLA2 inhibitors
US7420083B2 (en) 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7582773B2 (en) 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7446201B2 (en) 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7141592B2 (en) 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7265148B2 (en) 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
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
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
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US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
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WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2016138363A1 (en) 2015-02-27 2016-09-01 Incyte Corporation Salts of pi3k inhibitor and processes for their preparation
US9732097B2 (en) 2015-05-11 2017-08-15 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
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Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8841295B2 (en) 2005-11-04 2014-09-23 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
US8940752B2 (en) 2009-06-29 2015-01-27 Incyte Corporation Pyrimidinones as PI3K inhibitors
US9434746B2 (en) 2009-06-29 2016-09-06 Incyte Corporation Pyrimidinones as PI3K inhibitors
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ID27280A (en) 2001-03-22
KR20010041343A (en) 2001-05-15
HUP0100757A3 (en) 2001-11-28
BR9908280A (en) 2000-10-31
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NO20004220L (en) 2000-10-05
IL137718A0 (en) 2001-10-31
AU2782699A (en) 1999-09-15
EE200000486A (en) 2002-02-15
SK12742000A3 (en) 2001-05-10
PL342995A1 (en) 2001-07-16
CN1299347A (en) 2001-06-13
EP1056719A2 (en) 2000-12-06
NO20004220D0 (en) 2000-08-23
CA2322161A1 (en) 1999-09-02
TR200002446T2 (en) 2000-12-21
JP2002504539A (en) 2002-02-12
HUP0100757A1 (en) 2001-08-28
BG104780A (en) 2001-10-31
HRP20000552A2 (en) 2001-04-30
WO1999043651A2 (en) 1999-09-02

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