JP2001517652A - プロテインチロシンキナーゼとしての、またプロテインセリン／トレオニンキナーゼ阻害剤としての置換オキシインドール誘導体 - Google Patents

プロテインチロシンキナーゼとしての、またプロテインセリン／トレオニンキナーゼ阻害剤としての置換オキシインドール誘導体

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Publication number
JP2001517652A
JP2001517652A JP2000512809A JP2000512809A JP2001517652A JP 2001517652 A JP2001517652 A JP 2001517652A JP 2000512809 A JP2000512809 A JP 2000512809A JP 2000512809 A JP2000512809 A JP 2000512809A JP 2001517652 A JP2001517652 A JP 2001517652A
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JP
Japan
Prior art keywords
aliphatic
het
aryl
alkoxy
hydroxy
Prior art date
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Pending
Application number
JP2000512809A
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English (en)
Japanese (ja)
Other versions
JP2001517652A5 (OSRAM
Inventor
スティーブン、トーマス、デイビス
スコット、ハワード、ディッカーソン
スティーブン、バーノン、フライ
フィリップ、アンソニ−、ハリス
ロバート、ニール、ハンター、ザ、サード
リー、フレデリック、カイパー
カーレイ、エリザベス、ラッケイ
マイケル、ジョセフ、ルッツィオ
ジェイムズ、マービン、ビール
ダンカン、ヘリック、ウォーカー
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.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of JP2001517652A publication Critical patent/JP2001517652A/ja
Publication of JP2001517652A5 publication Critical patent/JP2001517652A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • A61P17/06—Antipsoriatics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
    • A61P39/00—General protective or antinoxious agents
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    • 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
    • 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
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    • 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
    • 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
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • 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
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    • 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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    • C07D401/00—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
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    • 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
    • C07D403/04—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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    • 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
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    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
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    • 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
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    • 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
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    • 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
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
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  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2000512809A 1997-09-05 1998-09-03 プロテインチロシンキナーゼとしての、またプロテインセリン／トレオニンキナーゼ阻害剤としての置換オキシインドール誘導体 Pending JP2001517652A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9718913.8A GB9718913D0 (en) 1997-09-05 1997-09-05 Substituted oxindole derivatives
GB9718913.8 1997-09-05
PCT/EP1998/005559 WO1999015500A1 (en) 1997-09-05 1998-09-03 Substituted oxindole derivatives as protein tyrosine kinase and as protein serine/threonine kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2001517652A true JP2001517652A (ja) 2001-10-09
JP2001517652A5 JP2001517652A5 (OSRAM) 2006-01-05

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JP2000512809A Pending JP2001517652A (ja) 1997-09-05 1998-09-03 プロテインチロシンキナーゼとしての、またプロテインセリン／トレオニンキナーゼ阻害剤としての置換オキシインドール誘導体

Country Status (23)

Country Link
US (4) US6387919B1 (OSRAM)
EP (1) EP1009738B1 (OSRAM)
JP (1) JP2001517652A (OSRAM)
KR (1) KR20010023695A (OSRAM)
CN (1) CN1278794A (OSRAM)
AR (1) AR015432A1 (OSRAM)
AT (1) ATE267170T1 (OSRAM)
AU (1) AU747506B2 (OSRAM)
BR (1) BR9812048A (OSRAM)
CA (1) CA2302572A1 (OSRAM)
CO (1) CO4960633A1 (OSRAM)
DE (1) DE69824014T2 (OSRAM)
EE (1) EE200000117A (OSRAM)
ES (1) ES2221211T3 (OSRAM)
GB (1) GB9718913D0 (OSRAM)
HU (1) HUP0004490A3 (OSRAM)
MA (1) MA26542A1 (OSRAM)
PE (1) PE107699A1 (OSRAM)
PL (1) PL338991A1 (OSRAM)
TR (1) TR200001174T2 (OSRAM)
TW (1) TW520358B (OSRAM)
WO (1) WO1999015500A1 (OSRAM)
ZA (1) ZA988078B (OSRAM)

Cited By (12)

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JP2008517932A (ja) * 2004-10-25 2008-05-29 リガンド・ファーマシューティカルズ・インコーポレイテッド トロンボポエチン活性を変調する化合物および変調方法
JP2008525370A (ja) * 2004-12-24 2008-07-17 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 線維症の治療又は予防のための薬物
JP2012504646A (ja) * 2008-10-01 2012-02-23 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 選択的サイクリン依存性キナーゼ４／６阻害剤を用いた化学療法化合物に対する造血系の防護
JP2012526850A (ja) * 2009-05-13 2012-11-01 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル サイクリン依存性キナーゼ阻害剤及びその用法
US9464092B2 (en) 2013-03-15 2016-10-11 G1 Therapeutics, Inc. Transient protection of normal cells during chemotherapy
US9717735B2 (en) 2014-04-17 2017-08-01 G1 Therapeutics, Inc. Tricyclic lactams for use in HSPC-sparing treatments for RB-positive abnormal cellular proliferation
US9808461B2 (en) 2010-11-17 2017-11-07 The University Of North Carolina At Chapel Hill Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6
US10231969B2 (en) 2014-09-12 2019-03-19 GI Therapeutics, Inc. Anti-neoplastic combinations and dosing regimens using CDK4/6 inhibitor compounds to treat RB-positive tumors
US10413547B2 (en) 2014-09-12 2019-09-17 G1 Therapeutics, Inc. Treatment of Rb-negative tumors using topoisomerase with cyclin dependent kinase 4/6 inhibitors
US10709711B2 (en) 2013-03-15 2020-07-14 G1 Therapeutics, Inc. Highly active anti-neoplastic and anti-proliferative agents
JP2022502455A (ja) * 2018-10-05 2022-01-11 イクノス サイエンシズ エスエー Ｍａｐ４ｋ１阻害剤として使用するためのインドリノン化合物
JP2022541610A (ja) * 2019-07-22 2022-09-26 ラジウス ファーマシューティカルズ，インコーポレイテッド エストロゲン受容体調節化合物

Families Citing this family (252)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6407132B1 (en) * 1997-07-25 2002-06-18 James Black Foundation Limited Substituted imidazole derivatives and their use as histamine H3 receptor ligands
GB9718913D0 (en) * 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
DE19816624A1 (de) * 1998-04-15 1999-10-21 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US6319918B1 (en) 1998-06-04 2001-11-20 Boehringer Ingelheim Pharma Kg Substituted indolinones with kinase inhibitory activity
DE19824922A1 (de) * 1998-06-04 1999-12-09 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
JP2002532503A (ja) * 1998-12-17 2002-10-02 エフ．ホフマン−ラ ロシュ アーゲー プロテインキナーゼ阻害剤としての４，５−ピラジノオキシンドール
WO2000035909A1 (en) 1998-12-17 2000-06-22 F. Hoffmann-La Roche Ag 4-aryloxindoles as inhibitors of jnk protein kinases
US6153634A (en) * 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
AU770060B2 (en) * 1998-12-17 2004-02-12 F. Hoffmann-La Roche Ag 4,5-azolo-oxindoles
WO2000035908A1 (en) * 1998-12-17 2000-06-22 F. Hoffmann-La Roche Ag 4-alkenyl (and alkynyl) oxindoles as inhibitors of cyclin-dependent kinases, in particular cdk2
WO2000042213A1 (en) 1999-01-13 2000-07-20 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
US6492398B1 (en) * 1999-03-04 2002-12-10 Smithkline Beechman Corporation Thiazoloindolinone compounds
GB9904933D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Compounds
GB9904930D0 (en) * 1999-03-04 1999-04-28 Glaxo Group Ltd Thiazoloindolinone compounds
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
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
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