WO2000008202A3 - Modulateurs 3-methylidenyl-2-indolinone de proteine kinase - Google Patents

Modulateurs 3-methylidenyl-2-indolinone de proteine kinase Download PDF

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Publication number
WO2000008202A3
WO2000008202A3 PCT/US1999/017845 US9917845W WO0008202A3 WO 2000008202 A3 WO2000008202 A3 WO 2000008202A3 US 9917845 W US9917845 W US 9917845W WO 0008202 A3 WO0008202 A3 WO 0008202A3
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WO
WIPO (PCT)
Prior art keywords
methylidenyl
protein kinase
indolinone
modulators
prodrugs
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US1999/017845
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English (en)
Other versions
WO2000008202A2 (fr
WO2000008202A9 (fr
Inventor
Peng Cho Tang
Li Sun
Todd Anthony Miller
Congxin Liang
Ngoc My Tran
Anh Thi Nguyen
Asaad Nematalla
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Sugen LLC
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Sugen LLC
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Publication date
Application filed by Sugen LLC filed Critical Sugen LLC
Priority to JP2000563824A priority Critical patent/JP2002522452A/ja
Priority to AU54684/99A priority patent/AU5468499A/en
Priority to CA002383623A priority patent/CA2383623A1/fr
Priority to US09/762,198 priority patent/US6531502B1/en
Publication of WO2000008202A2 publication Critical patent/WO2000008202A2/fr
Publication of WO2000008202A3 publication Critical patent/WO2000008202A3/fr
Publication of WO2000008202A9 publication Critical patent/WO2000008202A9/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • C07D401/02—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
    • C07D401/10—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 aromatic rings
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne de nouveaux composés 3-méthylidényl-2-indolinone ainsi que leurs sels physiologiquement acceptables et leurs promédicaments. Ces composés modulent l'activité des protéines kinases et par conséquent sont supposés convenir à la prévention et au traitement des troubles cellulaires liés à la protéine kinase, comme par exemple le cancer.
PCT/US1999/017845 1998-01-21 1999-08-04 Modulateurs 3-methylidenyl-2-indolinone de proteine kinase Ceased WO2000008202A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2000563824A JP2002522452A (ja) 1998-08-04 1999-08-04 蛋白質キナーゼの調節剤３−メチリデニル−２−インドリノン
AU54684/99A AU5468499A (en) 1998-08-04 1999-08-04 3-methylidenyl-2-indolinone modulators of protein kinase
CA002383623A CA2383623A1 (fr) 1998-08-04 1999-08-04 Modulateurs 3-methylidenyl-2-indolinone de proteine kinase
US09/762,198 US6531502B1 (en) 1998-01-21 1999-08-04 3-Methylidenyl-2-indolinone modulators of protein kinase

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US12925698A 1998-08-04 1998-08-04
US09/129,256 1998-08-04
US9547098P 1998-08-05 1998-08-05
US60/095,470 1998-08-05
US10217898P 1998-09-28 1998-09-28
US60/102,178 1998-09-28
US11610799P 1999-01-15 1999-01-15
US60/116,107 1999-01-15

Related Child Applications (3)

Application Number Title Priority Date Filing Date
US09/762,198 A-371-Of-International US6531502B1 (en) 1998-01-21 1999-08-04 3-Methylidenyl-2-indolinone modulators of protein kinase
US09762198 A-371-Of-International 1999-08-04
US10/383,690 Division US6855730B2 (en) 1998-08-05 2003-03-10 3-methylidenyl-2-indolinone modulators of protein kinase

Publications (3)

Publication Number Publication Date
WO2000008202A2 WO2000008202A2 (fr) 2000-02-17
WO2000008202A3 true WO2000008202A3 (fr) 2000-05-18
WO2000008202A9 WO2000008202A9 (fr) 2000-07-27

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/017845 Ceased WO2000008202A2 (fr) 1998-01-21 1999-08-04 Modulateurs 3-methylidenyl-2-indolinone de proteine kinase

Country Status (4)

Country Link
JP (1) JP2002522452A (fr)
AU (1) AU5468499A (fr)
CA (1) CA2383623A1 (fr)
WO (1) WO2000008202A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777417B2 (en) 2001-09-10 2004-08-17 Sugen, Inc. 3-(4,5,6,7-tetrahydroindol-2-ylmethylidiene-2-indolinone derivatives as kinase inhibitors

Families Citing this family (41)

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US6569868B2 (en) 1998-04-16 2003-05-27 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
CN1136217C (zh) 1998-12-17 2004-01-28 霍夫曼-拉罗奇有限公司 作为jnk蛋白质激酶抑制剂的4-芳基羟吲哚
US6153634A (en) 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
BR9916327A (pt) 1998-12-17 2001-09-18 Hoffmann La Roche Oxindóis de 4-alquenila (e alquinila) como inibidores de cinases dependentes de ciclina, em particular, cdk2
WO2000035921A1 (fr) 1998-12-17 2000-06-22 F. Hoffmann-La Roche Ag 4,5-pyrazinoxindoles comme inhibiteurs de proteine kinase
US6878733B1 (en) 1999-11-24 2005-04-12 Sugen, Inc. Formulations for pharmaceutical agents ionizable as free acids or free bases
DK1233943T3 (da) * 1999-11-24 2011-08-15 Sugen Inc Ioniserbare indolinon derivater og anvendelse deraf som PTK ligander
US6313310B1 (en) 1999-12-15 2001-11-06 Hoffmann-La Roche Inc. 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
AR034118A1 (es) 2000-02-15 2004-02-04 Sugen Inc Compuestos de 2-indolinonas sustituidas con pirroles inhibidoras de proteinquinasas; sus composiciones farmaceuticas e intermediarios de sintesis
CA2407799A1 (fr) 2000-05-02 2001-11-08 Sugen, Inc. Derives d'acide acetique (2-oxindole-3-ylidenyl) et leur utilisation comme inhibiteurs de la proteine kinase
MY128449A (en) 2000-05-24 2007-02-28 Sugen Inc Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
AU2001268154A1 (en) 2000-06-02 2001-12-17 Sugen, Inc. Indolinone derivatives as protein kinase/phosphatase inhibitors
AR035721A1 (es) 2000-12-20 2004-07-07 Sugen Inc Indolinonas 4-aril sustituidas; sus composiciones farmaceuticas y metodo para modular la actividad catalitica de una proteina quinasa
AR042586A1 (es) 2001-02-15 2005-06-29 Sugen Inc 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa
WO2002070478A1 (fr) 2001-03-06 2002-09-12 Astrazeneca Ab Dérivés indolone capable de dégrader des vaisseaux
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
WO2002081466A1 (fr) 2001-04-09 2002-10-17 Sugen, Inc. Promedicaments a base de derives 3-(pyrrol-2-ylmethylidene)-2-indolinone
JPWO2002094809A1 (ja) * 2001-05-24 2004-09-09 山之内製薬株式会社 ３−キノリン−２（１ｈ）−イリデンインドリン−２−オン誘導体
WO2002096361A2 (fr) 2001-05-30 2002-12-05 Sugen, Inc. Derives de 5-aralkylsulfonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone utilises comme inhibiteurs de kinase
ES2275021T3 (es) 2001-09-27 2007-06-01 Smithkline Beecham Corporation Derivados de azoxoindol como inhibidores de trk proteina quinasa para el tratamiento de cancer y dolor cronico.
AU2003284572A1 (en) * 2002-11-22 2004-06-18 Yamanouchi Pharmaceutical Co., Ltd. 2-oxoindoline derivatives
JP4879492B2 (ja) * 2002-11-27 2012-02-22 アラーガン、インコーポレイテッド 疾患の治療のためのキナーゼ阻害剤
US7517697B2 (en) * 2003-02-05 2009-04-14 Applied Biosystems, Llc Compositions and methods for preserving RNA in biological samples
US7312215B2 (en) 2003-07-29 2007-12-25 Bristol-Myers Squibb Company Benzimidazole C-2 heterocycles as kinase inhibitors
GT200500321A (es) * 2004-11-09 2006-09-04 Compuestos y composiciones como inhibidores de proteina kinase.
EP1883403A4 (fr) * 2005-04-29 2011-02-16 Univ Ohio State Res Found Inhibiteurs specifiques contre la tyrosine du recepteur du facteur de croissance des keratinocytes utiles pour prevenir les metastases cancereuses
WO2009030270A1 (fr) * 2007-09-03 2009-03-12 Novartis Ag Dérivés dhydroindoles utilisés pour traiter la maladie de parkinson
JP2011506494A (ja) * 2007-12-21 2011-03-03 ユニバーシティ・ヘルス・ネットワーク 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体
EP2417127B1 (fr) * 2009-04-06 2014-02-26 University Health Network Inhibiteurs de kinases et procédé de traitement du cancer avec ceux-ci
FR2948940B1 (fr) * 2009-08-04 2011-07-22 Servier Lab Nouveaux derives dihydroindolones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
PT2556071T (pt) 2010-04-06 2016-11-22 Univ Health Network Inibidores de quinase e seus usos no tratamento de cancro
WO2012048411A1 (fr) * 2010-10-13 2012-04-19 University Health Network Inhibiteurs de plk4 et méthode de traitement du cancer à l'aide de ceux-ci
WO2012142029A2 (fr) * 2011-04-10 2012-10-18 Florida A&M University Modulateurs sélectifs des récepteurs des œstrogènes pour traitement de troubles à médiation par les récepteurs des œstrogènes
EP2895476B1 (fr) 2012-09-13 2016-06-22 F.Hoffmann-La Roche Ag 2-oxo-2,3-dihydro-indoles destinés au traitement de troubles du snc
WO2014066840A1 (fr) 2012-10-26 2014-05-01 Regents Of The University Of Minnesota Inhibiteurs d'aurora kinase
ES2908200T3 (es) 2013-10-18 2022-04-28 Univ Health Network Tratamiento para el cáncer de páncreas
JP6661766B2 (ja) * 2015-11-12 2020-03-11 エルジー・ケム・リミテッド ７−アザインドリン−２−オン誘導体又はその薬学的に許容される塩を有効成分として含有する医薬組成物
US10487054B2 (en) 2017-04-21 2019-11-26 Regents Of The University Of Minnesota Therapeutic compounds
SG11202103459WA (en) * 2018-10-05 2021-05-28 Ichnos Sciences S A Indolinone compounds for use as map4k1 inhibitors
GR1010103B (el) * 2020-07-02 2021-10-18 Uni-Pharma Κλεων Τσετης Φαρμακευτικα Εργαστηρια Αβεε, 3-ινδολ-2-υλομεθυλιδενο-ινδολιν-2-ονες με δραση αναστολης της αυτοταξινης
WO2022006412A2 (fr) * 2020-07-02 2022-01-06 The Regents Of The University Of Colorado, A Body Corporate Conjugués d'inhibiteurs d'ampk et d'agents de dégradation de protac et utilisations associées

Citations (5)

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US5339992A (en) * 1991-07-10 1994-08-23 Societe De Prospection Et D'inventions Techniques (S.P.I.T. Tubular cartridge for storing and applying a non-solid product, and a drive and thrust assembly for the cartridge
US5374652A (en) * 1990-02-28 1994-12-20 Farmitalia Carlo Erba S R L 2-oxindole compounds which are useful as tyrosine kinase inhibitors
US5382593A (en) * 1992-07-21 1995-01-17 Adir Et Compagnie New 3-(hydroxybenzylidenyl)-indolin-2-ones
US5409949A (en) * 1991-07-12 1995-04-25 Farmitalia Carlo Erba S.R.L. Methylen-oxindole derivatives compositions and tyrosine kinase inhibition therewith
US5650415A (en) * 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds

Patent Citations (5)

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US5374652A (en) * 1990-02-28 1994-12-20 Farmitalia Carlo Erba S R L 2-oxindole compounds which are useful as tyrosine kinase inhibitors
US5339992A (en) * 1991-07-10 1994-08-23 Societe De Prospection Et D'inventions Techniques (S.P.I.T. Tubular cartridge for storing and applying a non-solid product, and a drive and thrust assembly for the cartridge
US5409949A (en) * 1991-07-12 1995-04-25 Farmitalia Carlo Erba S.R.L. Methylen-oxindole derivatives compositions and tyrosine kinase inhibition therewith
US5382593A (en) * 1992-07-21 1995-01-17 Adir Et Compagnie New 3-(hydroxybenzylidenyl)-indolin-2-ones
US5650415A (en) * 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777417B2 (en) 2001-09-10 2004-08-17 Sugen, Inc. 3-(4,5,6,7-tetrahydroindol-2-ylmethylidiene-2-indolinone derivatives as kinase inhibitors

Also Published As

Publication number Publication date
WO2000008202A2 (fr) 2000-02-17
JP2002522452A (ja) 2002-07-23
WO2000008202A9 (fr) 2000-07-27
AU5468499A (en) 2000-02-28
CA2383623A1 (fr) 2000-02-17

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