AU2002360753B2 - Indolinone derivatives useful as protein kinase inhibitors - Google Patents

Indolinone derivatives useful as protein kinase inhibitors Download PDF

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Publication number
AU2002360753B2
AU2002360753B2 AU2002360753A AU2002360753A AU2002360753B2 AU 2002360753 B2 AU2002360753 B2 AU 2002360753B2 AU 2002360753 A AU2002360753 A AU 2002360753A AU 2002360753 A AU2002360753 A AU 2002360753A AU 2002360753 B2 AU2002360753 B2 AU 2002360753B2
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AU
Australia
Prior art keywords
compound
group
formula
pharmaceutically
hydrogen atom
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Ceased
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AU2002360753A
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English (en)
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AU2002360753A1 (en
Inventor
Roger Briesewitz
John H. Griffin
Jonathan W. Wray
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Innoviva Inc
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Theravance Inc
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Publication of AU2002360753A1 publication Critical patent/AU2002360753A1/en
Application granted granted Critical
Publication of AU2002360753B2 publication Critical patent/AU2002360753B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • C07D403/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • 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
    • C07D403/14Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
AU2002360753A 2001-12-27 2002-12-20 Indolinone derivatives useful as protein kinase inhibitors Ceased AU2002360753B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US34374601P 2001-12-27 2001-12-27
US34381301P 2001-12-27 2001-12-27
US60/343,813 2001-12-27
US60/343,746 2001-12-27
PCT/US2002/041252 WO2003057690A1 (en) 2001-12-27 2002-12-20 Indolinone derivatives useful as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
AU2002360753A1 AU2002360753A1 (en) 2003-07-24
AU2002360753B2 true AU2002360753B2 (en) 2008-08-21

Family

ID=26993599

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002360753A Ceased AU2002360753B2 (en) 2001-12-27 2002-12-20 Indolinone derivatives useful as protein kinase inhibitors

Country Status (21)

Country Link
US (3) US6686362B2 (enExample)
EP (1) EP1458713B1 (enExample)
JP (1) JP4363985B2 (enExample)
KR (1) KR100965519B1 (enExample)
CN (1) CN1290844C (enExample)
AT (1) ATE302771T1 (enExample)
AU (1) AU2002360753B2 (enExample)
BR (1) BR0215360A (enExample)
CA (1) CA2470480C (enExample)
CO (1) CO5611126A2 (enExample)
DE (1) DE60205776T2 (enExample)
DK (1) DK1458713T3 (enExample)
ES (1) ES2247411T3 (enExample)
HU (1) HUP0500111A3 (enExample)
IL (1) IL162203A0 (enExample)
MX (1) MXPA04006271A (enExample)
NO (1) NO327550B1 (enExample)
NZ (1) NZ533219A (enExample)
PL (1) PL208283B1 (enExample)
RU (1) RU2316554C2 (enExample)
WO (1) WO2003057690A1 (enExample)

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AU2003259713A1 (en) * 2002-08-09 2004-02-25 Theravance, Inc. Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same
EP1680401A2 (en) * 2003-10-24 2006-07-19 Schering Aktiengesellschaft Indolinone derivatives and their use in treating disease-states such as cancer
EP1699477A2 (en) * 2003-12-11 2006-09-13 Theravance, Inc. Compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases
SE0401790D0 (sv) * 2004-07-07 2004-07-07 Forskarpatent I Syd Ab Tamoxifen response in pre- and postmenopausal breast cancer patients
US7825244B2 (en) 2005-06-10 2010-11-02 Janssen Pharmaceutica Nv Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
US8071768B2 (en) 2005-06-10 2011-12-06 Janssen Pharmaceutica, N.V. Alkylquinoline and alkylquinazoline kinase modulators
US20060281788A1 (en) 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
EP1951234A2 (en) 2005-10-18 2008-08-06 Janssen Pharmaceutica N.V. Method of inhibiting flt3 kinase
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
KR101367646B1 (ko) 2006-04-20 2014-02-27 얀센 파마슈티카 엔.브이. C-fms 키나제의 저해제
KR101367645B1 (ko) 2006-04-20 2014-02-27 얀센 파마슈티카 엔.브이. C-fms 키나제의 저해제로서의 복소환식 화합물
US7928136B2 (en) 2006-09-11 2011-04-19 Curis, Inc. Substituted 2-indolinone as PTK inhibitors containing a zinc binding moiety
JO3240B1 (ar) 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
FR2948940B1 (fr) * 2009-08-04 2011-07-22 Servier Lab Nouveaux derives dihydroindolones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2521782B1 (en) 2010-01-05 2019-04-10 INSERM - Institut National de la Santé et de la Recherche Médicale Flt3 receptor antagonists for the treatment or the prevention of pain disorders
JP5734313B2 (ja) 2010-01-12 2015-06-17 アーべー・シオンス チアゾールおよびオキサゾールキナーゼ阻害剤
US9303046B2 (en) 2012-08-07 2016-04-05 Janssen Pharmaceutica Nv Process for the preparation of heterocyclic ester derivatives
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
KR101738063B1 (ko) 2012-09-21 2017-05-19 아로그 파마슈티칼스, 인코퍼레이티드 구조적으로 활성인 인산화된 flt3 키나제의 억제 방법
BR112015016282A2 (pt) 2013-01-07 2017-07-11 Arog Pharmaceuticals Inc crenolanibe para tratamento de distúrbios proliferativos de flt3 mutado
FR3008411B1 (fr) * 2013-07-12 2015-07-03 Servier Lab Nouveau sel de la 3-[(3-{[4-(4-morpholinylmethyl)-1h-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1h-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione, sa preparation, et les formulations qui le contiennent
US10463658B2 (en) 2013-10-25 2019-11-05 Videra Pharmaceuticals, Llc Method of inhibiting FLT3 kinase
WO2016016370A1 (en) 2014-07-31 2016-02-04 INSERM (Institut National de la Santé et de la Recherche Médicale) Flt3 receptor antagonists
EP3254698A1 (en) 2016-06-08 2017-12-13 Universite De Montpellier Flt3 receptor inhibitor at low dosage for the treatment of neuropathic pain
EA201991078A1 (ru) 2016-11-02 2019-11-29 Креноланиб для лечения пролиферативных расстройств, связанных с мутацией flt3
US20200171022A1 (en) 2017-05-17 2020-06-04 Inserm (Institut National De La Santé Et Da La Recherche Médicale) Flt3 inhibitors for improving pain treatments by opioids
WO2019057649A1 (en) 2017-09-19 2019-03-28 INSERM (Institut National de la Santé et de la Recherche Médicale) METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
WO2022019998A1 (en) 2020-07-20 2022-01-27 Arog Pharmaceuticals, Inc. Crystal forms of crenolanib and methods of use thereof
WO2022090547A1 (en) 2020-10-30 2022-05-05 Dsm Ip Assets B.V. Production of carotenoids by fermentation
US11969420B2 (en) 2020-10-30 2024-04-30 Arog Pharmaceuticals, Inc. Combination therapy of crenolanib and apoptosis pathway agents for the treatment of proliferative disorders

Family Cites Families (18)

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Publication number Priority date Publication date Assignee Title
MC2096A1 (fr) * 1989-02-23 1991-02-15 Hoffmann La Roche Pyrroles substitues
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
TR200003514T2 (tr) 1998-05-29 2002-05-21 Sugen Inc. Pirol ikame edilmiş 2-indolinon protein kinaz inhibitörleri
ES2192877T3 (es) * 1998-12-17 2003-10-16 Hoffmann La Roche 4-alquenil (y alquinil) oxindoles como inhibidores de kinasas ciclina-dependientes, en particular cdk2.
MXPA01006742A (es) 1998-12-31 2004-04-21 Sugen Inc Compuestos 3-heteroarilidenil-2-indolinona para modular la actividad de la quinasa de proteina y para utilizarse en la quimioterapia de cancer.
DE19924401A1 (de) 1999-05-27 2000-11-30 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
DE50012136D1 (en) 1999-08-27 2006-04-13 Boehringer Ingelheim Pharma Substituierte indolinone als tyrosinkinase inhibitoren
ES2225231T3 (es) 1999-10-06 2005-03-16 Boehringer Ingelheim Pharmaceuticals Inc. Compuestos heterociclicos, utiles como inhibidores de tirosina quinasas.
DE19949209A1 (de) 1999-10-13 2001-04-19 Boehringer Ingelheim Pharma In 5-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
UA75054C2 (uk) 1999-10-13 2006-03-15 Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу
WO2001042243A2 (en) 1999-12-08 2001-06-14 Advanced Medicine, Inc. Protein kinase inhibitors
BRPI0117360B8 (pt) 2000-02-15 2021-07-06 Upjohn Co inibidores de proteína de quinase de 2-indolinona de pirrol substituído, seus sais e composições farmacêuticas compreendendo os mesmos
WO2002002551A1 (en) 2000-06-30 2002-01-10 Sugen, Inc. 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
BR0113356A (pt) 2000-08-18 2004-04-20 Millennium Pharm Inc Derivados de quinazolina como inibidores de quinase
CA2432114A1 (en) 2000-12-20 2002-07-18 Sugen, Inc. 4-(hetero)aryl substituted indolinones
AU2003259713A1 (en) * 2002-08-09 2004-02-25 Theravance, Inc. Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same
EP1699477A2 (en) * 2003-12-11 2006-09-13 Theravance, Inc. Compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases

Also Published As

Publication number Publication date
AU2002360753A1 (en) 2003-07-24
US20030171378A1 (en) 2003-09-11
KR20040070283A (ko) 2004-08-06
WO2003057690A1 (en) 2003-07-17
ATE302771T1 (de) 2005-09-15
CA2470480A1 (en) 2003-07-17
KR100965519B1 (ko) 2010-06-23
US7223783B2 (en) 2007-05-29
EP1458713A1 (en) 2004-09-22
ES2247411T3 (es) 2006-03-01
CN1290844C (zh) 2006-12-20
US20060142281A1 (en) 2006-06-29
CO5611126A2 (es) 2006-02-28
PL369602A1 (en) 2005-05-02
HUP0500111A2 (hu) 2005-07-28
BR0215360A (pt) 2004-12-14
NZ533219A (en) 2005-10-28
RU2004122918A (ru) 2005-03-27
JP4363985B2 (ja) 2009-11-11
US6686362B2 (en) 2004-02-03
IL162203A0 (en) 2005-11-20
NO20042926L (no) 2004-07-08
JP2005514420A (ja) 2005-05-19
HK1068886A1 (en) 2005-05-06
CN1608063A (zh) 2005-04-20
DE60205776T2 (de) 2006-06-14
RU2316554C2 (ru) 2008-02-10
CA2470480C (en) 2010-12-14
HUP0500111A3 (en) 2009-10-28
EP1458713B1 (en) 2005-08-24
DE60205776D1 (en) 2005-09-29
MXPA04006271A (es) 2004-10-04
DK1458713T3 (da) 2005-10-31
US7060703B2 (en) 2006-06-13
PL208283B1 (pl) 2011-04-29
US20040198804A1 (en) 2004-10-07
NO327550B1 (no) 2009-08-10

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Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired