WO2002055517A2 - 4-(hetero)aryl substituted indolinones - Google Patents

4-(hetero)aryl substituted indolinones Download PDF

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Publication number
WO2002055517A2
WO2002055517A2 PCT/US2001/048564 US0148564W WO02055517A2 WO 2002055517 A2 WO2002055517 A2 WO 2002055517A2 US 0148564 W US0148564 W US 0148564W WO 02055517 A2 WO02055517 A2 WO 02055517A2
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WO
WIPO (PCT)
Prior art keywords
sep
indol
phenyl
dihydro
methyl
Prior art date
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Ceased
Application number
PCT/US2001/048564
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English (en)
French (fr)
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WO2002055517A3 (en
Inventor
Jingrong Cui
Ruofei Zhang
Hong Shen
Ji Yu Chu
Fang-Jie Zhang
Marcel Koenig
Steven Huy Do
Xiaoyuan Li
Chung Chen Wei
Peng Cho Tang
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Priority to JP2002556186A priority Critical patent/JP2004518669A/ja
Priority to EP01997065A priority patent/EP1349852A2/en
Priority to CA002432114A priority patent/CA2432114A1/en
Publication of WO2002055517A2 publication Critical patent/WO2002055517A2/en
Publication of WO2002055517A3 publication Critical patent/WO2002055517A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • 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
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PCT/US2001/048564 2000-12-20 2001-12-20 4-(hetero)aryl substituted indolinones Ceased WO2002055517A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2002556186A JP2004518669A (ja) 2000-12-20 2001-12-20 ４−アリール置換インドリノン
EP01997065A EP1349852A2 (en) 2000-12-20 2001-12-20 4-(hetero)aryl substituted indolinones
CA002432114A CA2432114A1 (en) 2000-12-20 2001-12-20 4-(hetero)aryl substituted indolinones

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25647900P 2000-12-20 2000-12-20
US60/256,479 2000-12-20

Publications (2)

Publication Number Publication Date
WO2002055517A2 true WO2002055517A2 (en) 2002-07-18
WO2002055517A3 WO2002055517A3 (en) 2002-09-26

Family

ID=22972383

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/048564 Ceased WO2002055517A2 (en) 2000-12-20 2001-12-20 4-(hetero)aryl substituted indolinones

Country Status (7)

Country Link
US (2) US6677368B2 (enExample)
EP (1) EP1349852A2 (enExample)
JP (1) JP2004518669A (enExample)
AR (1) AR035721A1 (enExample)
CA (1) CA2432114A1 (enExample)
PE (1) PE20020776A1 (enExample)
WO (1) WO2002055517A2 (enExample)

Cited By (26)

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WO2003031438A1 (en) * 2001-10-10 2003-04-17 Sugen, Inc. 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors
WO2003004006A3 (en) * 2001-06-29 2003-05-30 Ab Science Use of potent, selective and non toxic c-kit inhibitors for treating tumor angiogenesis
WO2003074047A1 (en) * 2002-03-04 2003-09-12 4Sc Ag Indole derivatives as modulators of potassium channels
WO2003051838A3 (en) * 2001-12-13 2003-09-18 Abbott Lab Protein kinase inhibitors
US6686362B2 (en) 2001-12-27 2004-02-03 Theravance, Inc. Indolinone derivatives
WO2004113304A1 (en) * 2003-05-22 2004-12-29 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
WO2004105763A3 (en) * 2003-05-27 2005-06-02 Robert Per Haegerkvist Use of tyrosine kinase inhibitor to treat diabetes
JP2005538100A (ja) * 2002-07-31 2005-12-15 スミスクライン ビーチャム コーポレーション Ｉ．Ａ．慢性関節リウマチの治療においてｐ３８キナーゼ阻害剤として使用される縮合ヘテロアリール誘導体
JP2007519692A (ja) * 2004-01-30 2007-07-19 スミスクライン ビーチャム コーポレーション ｐ３８キナーゼ阻害剤として使用するための縮合ヘテロアリール誘導体
EP1829862A1 (en) * 2006-03-02 2007-09-05 Laboratorios Del Dr. Esteve, S.A. Sigma receptor compounds
US7297709B2 (en) 2003-05-22 2007-11-20 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
WO2008138184A1 (fr) * 2007-05-14 2008-11-20 Shanghai Hengrui Pharmaceutical Co.Ltd. Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
EP1893194A4 (en) * 2005-05-26 2009-07-01 Scripps Research Inst IMPROVED PROTEIN KINASE HEMMER ON INDOLINON BASE
US7678805B2 (en) 2001-06-29 2010-03-16 Ab Science Use of tyrosine kinase inhibitors for treating inflammatory bowel diseases (IBD)
US7683057B2 (en) 2006-09-15 2010-03-23 Tyrogenex, Inc. Kinase inhibitor compounds
US7700610B2 (en) 2001-06-29 2010-04-20 Ab Science Use of tyrosine kinase inhibitors for treating allergic diseases
US7727731B2 (en) 2001-06-29 2010-06-01 Ab Science Potent, selective and non toxic c-kit inhibitors
US7741335B2 (en) 2001-06-29 2010-06-22 Ab Science Use of tyrosine kinase inhibitors for treating inflammatory diseases
US7855225B2 (en) 2006-03-02 2010-12-21 Astellas Pharma Inc. 17βHSD type 5 inhibitor
EP2076128A4 (en) * 2006-10-06 2011-01-05 PROTEIN CHINESE INHIBITOR AND ITS USE METHOD
EP2308875A1 (en) 2003-12-22 2011-04-13 Abbott Laboratories Fused bicycloheterocycle substituted quinuclidine derivatives as .alpha.7 nAChR modulators
US8012966B2 (en) 2006-01-27 2011-09-06 Shanghai Hengrui Pharmaceutical Co., Ltd. Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors
US8273785B2 (en) 2006-09-11 2012-09-25 Curis, Inc. Substituted 2-indolinone as PTK inhibitors containing a zinc binding moiety
CN105408320A (zh) * 2013-03-13 2016-03-16 北京强新生物科技有限公司 用于治疗癌症的作为癌症干细胞途径激酶抑制剂的3-(芳基或杂芳基)甲基吲哚-2-酮衍生物
RU2650682C2 (ru) * 2014-02-10 2018-04-17 Шицзячжуан Илин Фармасьютикал Ко., Лтд. Пирролзамещенное производное индолона, способ его получения, включающая его композиция и применение

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US6316429B1 (en) * 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
DK1255752T3 (da) * 2000-02-15 2007-11-26 Sugen Inc Pyrrolsubstituerede 2-indolinonproteinkinaseinhibitorer
US6706709B2 (en) * 2000-06-02 2004-03-16 Sugen, Inc. Indolinone derivatives as protein kinase/phosphatase inhibitors
US20090197852A9 (en) * 2001-08-06 2009-08-06 Johnson Robert G Jr Method of treating breast cancer using 17-AAG or 17-AG or a prodrug of either in combination with a HER2 inhibitor
TWI259081B (en) * 2001-10-26 2006-08-01 Sugen Inc Treatment of acute myeloid leukemia with indolinone compounds
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US20050032871A1 (en) * 2002-09-03 2005-02-10 Sugen, Inc. Sulfonylated pyrrole-2-indolinone derivatives as kinase inhibitors
KR20120062863A (ko) * 2003-07-30 2012-06-14 리겔 파마슈티칼스, 인크. 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물
US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
ES2651349T3 (es) 2005-06-08 2018-01-25 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta JAK
ES2622493T3 (es) * 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
MX2008012482A (es) * 2006-03-31 2008-10-10 Abbott Lab Compuestos de indazol.
EP1918277B1 (en) * 2006-11-01 2015-06-10 Industrial Technology Research Institute Azulene compounds
JP5711537B2 (ja) 2008-02-15 2015-05-07 ライジェル ファーマシューティカルズ， インコーポレイテッド ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用
AU2009244897B2 (en) 2008-04-16 2014-11-13 Alexion Pharmaceuticals, Inc. 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
BRPI0910668A2 (pt) * 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
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US7897602B2 (en) * 2009-01-12 2011-03-01 Development Center For Biotechnology Indolinone compounds as kinase inhibitors
EP2459195A1 (en) * 2009-07-28 2012-06-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
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WO2014058921A2 (en) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
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Cited By (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7678805B2 (en) 2001-06-29 2010-03-16 Ab Science Use of tyrosine kinase inhibitors for treating inflammatory bowel diseases (IBD)
WO2003004006A3 (en) * 2001-06-29 2003-05-30 Ab Science Use of potent, selective and non toxic c-kit inhibitors for treating tumor angiogenesis
US7741335B2 (en) 2001-06-29 2010-06-22 Ab Science Use of tyrosine kinase inhibitors for treating inflammatory diseases
US7727731B2 (en) 2001-06-29 2010-06-01 Ab Science Potent, selective and non toxic c-kit inhibitors
US7700610B2 (en) 2001-06-29 2010-04-20 Ab Science Use of tyrosine kinase inhibitors for treating allergic diseases
WO2003031438A1 (en) * 2001-10-10 2003-04-17 Sugen, Inc. 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors
WO2003051838A3 (en) * 2001-12-13 2003-09-18 Abbott Lab Protein kinase inhibitors
US6686362B2 (en) 2001-12-27 2004-02-03 Theravance, Inc. Indolinone derivatives
US7060703B2 (en) 2001-12-27 2006-06-13 Theravance, Inc. Indolinone derivatives
US7223783B2 (en) 2001-12-27 2007-05-29 Theravance, Inc. Indolinone derivatives
WO2003074047A1 (en) * 2002-03-04 2003-09-12 4Sc Ag Indole derivatives as modulators of potassium channels
JP2005538100A (ja) * 2002-07-31 2005-12-15 スミスクライン ビーチャム コーポレーション Ｉ．Ａ．慢性関節リウマチの治療においてｐ３８キナーゼ阻害剤として使用される縮合ヘテロアリール誘導体
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US20040157909A1 (en) 2004-08-12
WO2002055517A3 (en) 2002-09-26
US20030069297A1 (en) 2003-04-10
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US6677368B2 (en) 2004-01-13
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