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WO2003020698A3 - Inhibiteurs de la tyrosine kinase - Google Patents

Inhibiteurs de la tyrosine kinase Download PDF

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Publication number
WO2003020698A3
WO2003020698A3 PCT/IL2002/000740 IL0200740W WO03020698A3 WO 2003020698 A3 WO2003020698 A3 WO 2003020698A3 IL 0200740 W IL0200740 W IL 0200740W WO 03020698 A3 WO03020698 A3 WO 03020698A3
Authority
WO
WIPO (PCT)
Prior art keywords
tyrosine kinase
protein tyrosine
kinase inhibitors
compounds
skeletal
Prior art date
Application number
PCT/IL2002/000740
Other languages
English (en)
Other versions
WO2003020698A2 (fr
Inventor
Doron Eren
Andrea Zaliani
Er David Pe
Oren Bogin
Avner Yayon
Original Assignee
Prochon Biotech Ltd
Doron Eren
Andrea Zaliani
Er David Pe
Oren Bogin
Avner Yayon
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
Priority claimed from IL14532901A external-priority patent/IL145329A0/xx
Application filed by Prochon Biotech Ltd, Doron Eren, Andrea Zaliani, Er David Pe, Oren Bogin, Avner Yayon filed Critical Prochon Biotech Ltd
Priority to AU2002334355A priority Critical patent/AU2002334355A1/en
Publication of WO2003020698A2 publication Critical patent/WO2003020698A2/fr
Publication of WO2003020698A3 publication Critical patent/WO2003020698A3/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57—Aryl or substituted aryl radicals
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur des composés hétérocycliques inhibiteurs de la tyrosine kinase dont les préférés sont l'aryl benzimidazole substitué en 2 et la benzofuro [3,2-c ] quinoline, tous deux étant nouveaux et connus. L'invention porte également sur des procédés d'utilisation desdits composés préférés pour la préparation de médicaments traitant les maladies et troubles prolifératifs, du squelette et du métabolisme associés à une activité anormale de la tyrosine kinase, dont le cancer et la dysplasie du squelette.
PCT/IL2002/000740 2001-09-06 2002-09-05 Inhibiteurs de la tyrosine kinase WO2003020698A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002334355A AU2002334355A1 (en) 2001-09-06 2002-09-05 Protein tyrosine kinase inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US31718601P 2001-09-06 2001-09-06
US60/317,186 2001-09-06
IL145329 2001-09-09
IL14532901A IL145329A0 (en) 2001-09-09 2001-09-09 Protein tyrosine kinase inhibitors

Publications (2)

Publication Number Publication Date
WO2003020698A2 WO2003020698A2 (fr) 2003-03-13
WO2003020698A3 true WO2003020698A3 (fr) 2004-03-18

Family

ID=26324042

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IL2002/000740 WO2003020698A2 (fr) 2001-09-06 2002-09-05 Inhibiteurs de la tyrosine kinase

Country Status (2)

Country Link
AU (1) AU2002334355A1 (fr)
WO (1) WO2003020698A2 (fr)

Cited By (10)

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US7452879B2 (en) 2003-07-30 2008-11-18 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US7557210B2 (en) 2002-02-01 2009-07-07 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US8865735B2 (en) 2011-02-21 2014-10-21 Hoffman-La Roche Inc. Solid forms of a pharmaceutically active substance
US9096593B2 (en) 2009-11-06 2015-08-04 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
US9169250B2 (en) 2006-11-22 2015-10-27 Plexxikon Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US9248190B2 (en) 2005-06-08 2016-02-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US9447089B2 (en) 2009-04-03 2016-09-20 Plexxikon Inc. Compositions and uses thereof
US9469640B2 (en) 2007-07-17 2016-10-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US11851434B2 (en) 2017-01-18 2023-12-26 Array Biopharma Inc. Substituted pyrazolo[1,5-A]pyrazine compounds as ret kinase inhibitors

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KR101089904B1 (ko) 2002-12-19 2011-12-05 더 스크립스 리서치 인스티튜트 트란스타이레틴 안정화 및 트란스타이레틴 미스폴딩 저해용조성물 및 방법
US7875616B2 (en) 2003-05-27 2011-01-25 Haegerkvist Robert Per Use of tyrosine kinase inhibitor to treat diabetes
CA2536174A1 (fr) * 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. Inhibiteurs d'un ensemble d'imidazopyridine c n3 substitue
US7442709B2 (en) 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
GB0325836D0 (en) * 2003-11-05 2003-12-10 Celltech R&D Ltd Biological products
AU2004308299B2 (en) * 2003-12-19 2011-11-24 Plexxikon, Inc. Compounds and methods for development of Ret modulators
AU2005245470A1 (en) 2004-05-20 2005-12-01 Foldrx Pharmaceuticals, Inc. 2-((hetero) aryl)-benzoxazole compounds and derivatives, compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
MY146381A (en) 2004-12-22 2012-08-15 Amgen Inc Compositions and methods relating relating to anti-igf-1 receptor antibodies
TWI375673B (en) 2005-04-11 2012-11-01 Abbott Lab 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors
US7728026B2 (en) 2005-04-11 2010-06-01 Abbott Laboratories, Inc. 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors
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
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006135915A2 (fr) 2005-06-13 2006-12-21 Rigel Pharmaceuticals, Inc. Methodes et compositions de traitement de maladies osseuses degeneratives
CA2627722A1 (fr) 2005-10-31 2007-06-21 Merck & Co., Inc. Inhibiteurs de la cetp
DE602006013191D1 (de) 2005-11-15 2010-05-06 Abbott Lab Substituierte 1h-benzimidazol-4-carbonsäureamide sind wirksame parp-inhibitoren
EP1991532B1 (fr) 2006-02-24 2017-01-11 Rigel Pharmaceuticals, Inc. Compositions et méthodes destinées à l'inhibition de la voie jak
CA2647373C (fr) 2006-05-02 2014-03-18 Abbott Laboratories 1h-benzimidazole-4-carboxamides substitues servant de puissants inhibiteurs de parp
EP1860104A1 (fr) * 2006-05-22 2007-11-28 Aptanomics Composés antiprolifératifs dérivés de la 3-aryl-coumarine ou de la 3-aryl-quinolin-2-one et leur utilisations
JP2010511721A (ja) * 2006-12-05 2010-04-15 ナショナル チャオ トン ユニバーシティ インダゾール化合物
AU2009214440B2 (en) 2008-02-15 2014-09-25 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases
MX2010011463A (es) 2008-04-16 2011-06-03 Portola Pharm Inc 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas.
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
CA2723185A1 (fr) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibiteurs de proteines kinases
WO2010083199A1 (fr) 2009-01-19 2010-07-22 Abbott Laboratories Inhibiteurs benzthiazole de la poly(adp-ribose)polymérase
DK3205654T3 (en) 2010-05-20 2019-04-15 Array Biopharma Inc MACROCYCLIC COMPOUNDS AS TRK-KINASE INHIBITORS
US9102625B2 (en) 2010-11-01 2015-08-11 Portola Pharmaceuticals, Inc. Nicotinamides as JAK kinase modulators
AU2012212075A1 (en) 2011-02-02 2013-07-18 Amgen Inc. Methods and compositons relating to inhibition of IGF-1R
CA2826123C (fr) 2011-02-07 2016-08-09 Plexxikon Inc. Composes et procedes de modulation de kinase, et leurs indications
CA2847293C (fr) 2011-09-16 2017-03-28 Richard Frederic Labaudiniere Formes solides d'un inhibiteur de la dissociation de derives de transthyretine
EP2782579B1 (fr) 2011-11-23 2019-01-02 Portola Pharmaceuticals, Inc. Inhibiteurs de de la pyrazine kinase
CN105646517A (zh) * 2012-03-22 2016-06-08 巴塞利亚药业（中国）有限公司 天然产物Hirtellanine B及其衍生物的制备方法与在制备治疗肿瘤药物中的应用
WO2014058921A2 (fr) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Inhibiteurs substitués de pyrimidinyl kinase
GB201223265D0 (en) * 2012-12-21 2013-02-06 Selvita Sa Novel benzimidazole derivatives as kinase inhibitors
WO2017011776A1 (fr) 2015-07-16 2017-01-19 Array Biopharma, Inc. Composés substitués de pyrazolo[1,5-a]pyridines comme inhibiteurs de la kinase ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
WO2018136663A1 (fr) 2017-01-18 2018-07-26 Array Biopharma, Inc. Inhibiteurs de ret
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
JP6997876B2 (ja) 2018-01-18 2022-02-04 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物
EP3740491A1 (fr) 2018-01-18 2020-11-25 Array Biopharma, Inc. Composés de pyrrolo[2,3-d]pyrimidines substitués utilisés en tant qu'inhibiteurs de la kinase ret
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
CA3111984A1 (fr) 2018-09-10 2020-03-19 Array Biopharma Inc. Composes heterocycliques condenses comme inhibiteurs de kinases ret

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO1997004771A1 (fr) * 1995-08-02 1997-02-13 Newcastle University Ventures Limited Composes benzimidazole
WO2000026192A1 (fr) * 1998-11-03 2000-05-11 Basf Aktiengesellschaft 2-phenylbenzimidazoles substitues, leur preparation et leur utilisation

Patent Citations (2)

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WO1997004771A1 (fr) * 1995-08-02 1997-02-13 Newcastle University Ventures Limited Composes benzimidazole
WO2000026192A1 (fr) * 1998-11-03 2000-05-11 Basf Aktiengesellschaft 2-phenylbenzimidazoles substitues, leur preparation et leur utilisation

Non-Patent Citations (1)

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Title
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Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7557210B2 (en) 2002-02-01 2009-07-07 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US7452879B2 (en) 2003-07-30 2008-11-18 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US7582648B2 (en) 2003-07-30 2009-09-01 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US9248190B2 (en) 2005-06-08 2016-02-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US9169250B2 (en) 2006-11-22 2015-10-27 Plexxikon Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US9487515B2 (en) 2006-11-22 2016-11-08 Plexxikon Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US9469640B2 (en) 2007-07-17 2016-10-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9447089B2 (en) 2009-04-03 2016-09-20 Plexxikon Inc. Compositions and uses thereof
US9096593B2 (en) 2009-11-06 2015-08-04 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US8865735B2 (en) 2011-02-21 2014-10-21 Hoffman-La Roche Inc. Solid forms of a pharmaceutically active substance
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
US11851434B2 (en) 2017-01-18 2023-12-26 Array Biopharma Inc. Substituted pyrazolo[1,5-A]pyrazine compounds as ret kinase inhibitors

Also Published As

Publication number Publication date
WO2003020698A2 (fr) 2003-03-13
AU2002334355A1 (en) 2003-03-18

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