JP2002514228A - 受容体チロシンキナーゼ阻害剤、特にｒａｆキナーゼ阻害剤としてのベンジリン−１，３−ジヒドロ−インドール−２−オン誘導体 - Google Patents

受容体チロシンキナーゼ阻害剤、特にｒａｆキナーゼ阻害剤としてのベンジリン−１，３−ジヒドロ−インドール−２−オン誘導体

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Publication number
JP2002514228A
JP2002514228A JP51383999A JP51383999A JP2002514228A JP 2002514228 A JP2002514228 A JP 2002514228A JP 51383999 A JP51383999 A JP 51383999A JP 51383999 A JP51383999 A JP 51383999A JP 2002514228 A JP2002514228 A JP 2002514228A
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Japan
Prior art keywords
aliphatic
het
optionally
aryl
substituted
Prior art date
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Ceased
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JP51383999A
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English (en)
Japanese (ja)
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JP2002514228A5 (US06268391-20010731-C00042.png
Inventor
ジュニア ロバート、ウォルトン、マックナット
デイビッド、ケンダル、ユング
フィリップ、アンソニー、ハリス
ロバート、ニール、ハンター、ザ、サード
ジェイムズ、マービン、ビール
スコット、ディッカーソン
カレン、エリザベス、ラッキー
マイケル、ロバート、ピール
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Glaxo Group Ltd
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Glaxo Group Ltd
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Publication of JP2002514228A publication Critical patent/JP2002514228A/ja
Publication of JP2002514228A5 publication Critical patent/JP2002514228A5/ja
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
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    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/56—Heterocyclic 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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D405/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
JP51383999A 1997-08-06 1998-08-04 受容体チロシンキナーゼ阻害剤、特にｒａｆキナーゼ阻害剤としてのベンジリン−１，３−ジヒドロ−インドール−２−オン誘導体 Ceased JP2002514228A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9716557.5A GB9716557D0 (en) 1997-08-06 1997-08-06 Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
GB9716557.5 1997-08-06
PCT/EP1998/004844 WO1999010325A1 (en) 1997-08-06 1998-08-04 Benzylidene-1,3-dihydro-indol-2-one derivatives as receptor tyrosine kinase inhibitors, particularly of raf kinases

Publications (2)

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JP2002514228A true JP2002514228A (ja) 2002-05-14
JP2002514228A5 JP2002514228A5 (US06268391-20010731-C00042.png) 2006-01-05

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EP (1) EP1003721B1 (US06268391-20010731-C00042.png)
JP (1) JP2002514228A (US06268391-20010731-C00042.png)
AR (1) AR016789A1 (US06268391-20010731-C00042.png)
AT (1) ATE344241T1 (US06268391-20010731-C00042.png)
AU (1) AU9158498A (US06268391-20010731-C00042.png)
DE (1) DE69836332T2 (US06268391-20010731-C00042.png)
ES (1) ES2272008T3 (US06268391-20010731-C00042.png)
GB (1) GB9716557D0 (US06268391-20010731-C00042.png)
MA (1) MA26529A1 (US06268391-20010731-C00042.png)
PE (1) PE112699A1 (US06268391-20010731-C00042.png)
WO (1) WO1999010325A1 (US06268391-20010731-C00042.png)
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Cited By (5)

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WO2005080392A1 (ja) * 2004-02-19 2005-09-01 Takeda Pharmaceutical Company Limited ピラゾロキノロン誘導体およびその用途
JP2005532284A (ja) * 2002-04-03 2005-10-27 アラーガン、インコーポレイテッド キナーゼ阻害物質としての（３ｚ）−３−（３−ヒドロ−イソベンゾフラン−１−イリデン）−１，３−ジヒドロ−２ｈ−インドール−２−オン類
JP2007528884A (ja) * 2004-03-12 2007-10-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規なシクロアルキル含有５−アシルインドリノン、その製法及びその医薬品としての使用
JP2010538091A (ja) * 2007-09-06 2010-12-09 ボストン バイオメディカル， インコーポレイテッド キナーゼ阻害剤の組成物ならびに癌およびキナーゼに関連する他の疾患の治療のためのそれらの使用
JP2016513656A (ja) * 2013-03-13 2016-05-16 ボストン バイオメディカル， インコーポレイテッド がんの処置のための、がん幹細胞経路キナーゼの阻害剤としての３−（アリールまたはヘテロアリール）メチレンインドリン−２−オン誘導体

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US6147106A (en) 1997-08-20 2000-11-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
WO1996040648A1 (en) * 1995-06-07 1996-12-19 Sugen, Inc. Quinazolines and pharmaceutical compositions
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
CO4940469A1 (es) 1997-03-05 2000-07-24 Sugen Inc Composicion oral de estabilidad mejorada que comprende un derivado de indolinona y una mezcla de gliceridos o esteres de polietilenglicol
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6316479B1 (en) 1997-05-19 2001-11-13 Sugen, Inc. Isoxazole-4-carboxamide compounds active against protein tryosine kinase related disorders
US6987113B2 (en) 1997-06-11 2006-01-17 Sugen, Inc. Tyrosine kinase inhibitors
US6051593A (en) * 1997-06-20 2000-04-18 Sugen, Inc. 3-(cycloalkanoheteroarylidenyl)-2- indolinone protein tyrosine kinase inhibitors
US6130238A (en) * 1997-06-20 2000-10-10 Sugen, Inc. 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
US6114371A (en) * 1997-06-20 2000-09-05 Sugen, Inc. 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
US6313158B1 (en) 1997-06-20 2001-11-06 Sugen, Inc. Bioavailability of 3-heteroarylidenyl-2-indolinones active as protein tyrosine kinase inhibitors
US6235769B1 (en) 1997-07-03 2001-05-22 Sugen, Inc. Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase
US6133305A (en) 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
US6531502B1 (en) 1998-01-21 2003-03-11 Sugen, Inc. 3-Methylidenyl-2-indolinone modulators of protein kinase
US6514981B1 (en) 1998-04-02 2003-02-04 Sugen, Inc. Methods of modulating tyrosine protein kinase function with indolinone compounds
US6569868B2 (en) 1998-04-16 2003-05-27 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
US6395734B1 (en) 1998-05-29 2002-05-28 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
AU760039B2 (en) 1998-12-17 2003-05-08 F. Hoffmann-La Roche Ag 4-aryloxindoles as inhibitors of JNK protein kinases
ES2301255T3 (es) * 1998-12-17 2008-06-16 F. Hoffmann-La Roche Ag 4,5-pirazinaxindoles como inhibidores de proteinoquinasas.
US6153634A (en) 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
AU770375B2 (en) 1998-12-17 2004-02-19 F. Hoffmann-La Roche Ag 4-alkenyl (and alkynyl) oxindoles as inhibitors of cyclin-dependent kinases, in particular CDK2
GB9904932D0 (en) * 1999-03-04 1999-04-28 Glaxo Group Ltd Composition and method for preventing/reducing the severity of side effects of chemotherapy and/or radiation therapy
US7064114B2 (en) 1999-03-19 2006-06-20 Parker Hughes Institute Gel-microemulsion formulations
US6689806B1 (en) 1999-03-24 2004-02-10 Sugen, Inc. Indolinone compounds as kinase inhibitors
JP2002540096A (ja) * 1999-03-24 2002-11-26 スージェン・インコーポレーテッド キナーゼ阻害剤としてのインドリノン化合物
JP2000281588A (ja) * 1999-03-30 2000-10-10 Sankyo Co Ltd ガンの予防又は治療薬及びそのスクリーニング方法
AU4556800A (en) * 1999-04-27 2000-11-10 Smithkline Beecham Plc Novel treatment
US6380178B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
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MA26529A1 (fr) 2004-12-20
US6268391B1 (en) 2001-07-31
ATE344241T1 (de) 2006-11-15
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ZA987037B (en) 2000-02-07
WO1999010325A1 (en) 1999-03-04

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