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
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
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 date
Application filed by Theravance Inc filed Critical Theravance Inc
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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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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

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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)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (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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US7195876B2 (en) * 2002-08-09 2007-03-27 Theravance, Inc. Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same
MXPA06004438A (es) * 2003-10-24 2006-06-20 Schering Ag Derivados de indolinona y su uso en el tratamiento de enfermedades como el cancer.
US20050171182A1 (en) * 2003-12-11 2005-08-04 Roger Briesewitz Methods and 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
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
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
AU2006304897B2 (en) 2005-10-18 2012-07-12 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
KR101367645B1 (ko) 2006-04-20 2014-02-27 얀센 파마슈티카 엔.브이. Ｃ-ｆｍｓ 키나제의 저해제로서의 복소환식 화합물
EP2016070B1 (en) 2006-04-20 2016-01-13 Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase
AU2007296740B2 (en) * 2006-09-11 2012-09-27 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
US9109227B2 (en) 2010-01-05 2015-08-18 Institut National De La Sante Et De La Recherche Medicale (Inserm) FLT3 receptor antagonists for the treatment or the prevention of pain disorders
CN102812022B (zh) 2010-01-12 2016-02-03 Ab科学有限公司 噻唑和噁唑激酶抑制剂
ES2607807T3 (es) 2012-08-07 2017-04-04 Janssen Pharmaceutica Nv Procedimiento para la preparación de los inibidores de las quinasas c-fms
AU2013299922B2 (en) 2012-08-07 2018-06-21 Janssen Pharmaceutica Nv Process for the preparation of heterocyclic ester derivatives
JP6407504B2 (ja) 2012-09-21 2018-10-17 アログ・ファーマシューティカルズ・インコーポレイテッドＡｒｏｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 恒常的に活性であるリン酸化型ｆｌｔ３キナーゼの阻害方法
BR112015016282A2 (en) 2013-01-07 2017-07-11 Arog Pharmaceuticals, Inc. crenolanib for treatment of mutated flt3 proliferative disorders
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
BR112017002001B1 (pt) 2014-07-31 2022-10-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Compostos e composição farmacêutica
EP3254698A1 (en) 2016-06-08 2017-12-13 Universite De Montpellier Flt3 receptor inhibitor at low dosage for the treatment of neuropathic pain
US12534764B2 (en) 2016-11-02 2026-01-27 Arog Pharmaceuticals, Inc. Crenolanib for treating FLT3 mutated proliferative disorders associated mutations
KR20180074792A (ko) 2016-11-02 2018-07-03 아로그 파마슈티칼스, 인코퍼레이티드 돌연변이 연관된 flt3 돌연변이된 증식성 장애를 치료하기 위한 크레노라닙
US12662706B2 (en) 2016-11-02 2026-06-23 Arog Pharmaceuticals, Inc. Crenolanib for treating FLT3 mutated proliferative disorders associated mutations
WO2018211018A1 (en) 2017-05-17 2018-11-22 INSERM (Institut National de la Santé et de 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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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
KR100743287B1 (ko) * 1998-05-29 2007-07-26 수젠, 인크. 피롤기로 치환된 2-인돌리논 단백질 인산화 효소 억제제
DE69906152T2 (de) * 1998-12-17 2004-02-12 F. Hoffmann-La Roche Ag 4-alkenyl (und alkinyl)oxoindole als inhibitoren cyclinabhängiger kinasen, insbesondere cdk2
IL143920A0 (en) 1998-12-31 2002-04-21 Sugen Inc 3-heteroarylidenyl-2-indolinone derivatives and pharmaceutical compositions containing the same
DE19924401A1 (de) 1999-05-27 2000-11-30 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
WO2001016130A1 (de) 1999-08-27 2001-03-08 Boehringer Ingelheim Pharma Kg Substituierte indolinone als tyrosinkinase inhibitoren
DE60014130T2 (de) 1999-10-06 2006-03-09 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Heterocyclische verbindungen verwendbar als tyrosinkinase inhibitoren
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
DE19949209A1 (de) 1999-10-13 2001-04-19 Boehringer Ingelheim Pharma In 5-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
AU2576501A (en) 1999-12-08 2001-06-18 Advanced Medicine, Inc. Protein kinase inhibitors
HRP20020751B1 (hr) * 2000-02-15 2011-01-31 Sugen Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze
WO2002002551A1 (en) 2000-06-30 2002-01-10 Sugen, Inc. 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
HU228668B1 (hu) 2000-08-18 2013-05-28 Millennium Pharmaceuticals Kináz inhibitor kinazolin-származékok és az ezeket tartalmazó gyógyszerkészítmények
PE20020776A1 (es) 2000-12-20 2002-08-22 Sugen Inc Indolinonas 4-aril sustituidas
US7195876B2 (en) 2002-08-09 2007-03-27 Theravance, Inc. Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same
US20050171182A1 (en) * 2003-12-11 2005-08-04 Roger Briesewitz Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases

Also Published As

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

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