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

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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

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
IL14532901A IL145329A0 (en) 2001-09-09 2001-09-09 Protein tyrosine kinase inhibitors
IL145329 2001-09-09

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)

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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
US11964988B2 (en) 2019-09-06 2024-04-23 Array Biopharma Inc. Fused heterocyclic compounds as RET kinase inhibitors

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DK1587821T3 (da) 2002-12-19 2008-11-10 Scripps Research Inst Sammensætninger og fremgangsmåder til stabilisering af transthyretin og inhibering af transthyretin-fejlfolding
PL1631291T3 (pl) 2003-05-27 2010-04-30 Haegerkvist Robert P Zastosowanie inhibitorów kinazy tyrozynowej do leczenia cukrzycy
US7442709B2 (en) 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
WO2005021544A2 (fr) * 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. Inhibiteurs d'un ensemble d'imidazopyridine c n3 substitue
GB0325836D0 (en) * 2003-11-05 2003-12-10 Celltech R&D Ltd Biological products
EP1696920B8 (fr) * 2003-12-19 2015-05-06 Plexxikon Inc. Composes et methodes de developpement de modulateurs de ret
JP2007538103A (ja) 2004-05-20 2007-12-27 ザ スクリップス リサーチ インスティテュート トランスサイレチン安定化
MY146381A (en) 2004-12-22 2012-08-15 Amgen Inc Compositions and methods relating relating to anti-igf-1 receptor antibodies
WO2006110683A1 (fr) 2005-04-11 2006-10-19 Abbott Laboratories 1h-benzimidazole-4-carboxamides 2-substitues en tant qu'inhibiteurs de parp
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
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
US8334290B2 (en) 2005-10-31 2012-12-18 Merck Sharp & Dohme Corp. CETP inhibitors
CN101309908A (zh) 2005-11-15 2008-11-19 艾博特公司 作为有效parp抑制剂的取代的1h-苯并咪唑-4-甲酰胺化合物
CA2642229C (fr) 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions et methodes destinees a l'inhibition de la voie jak
US20070259937A1 (en) 2006-05-02 2007-11-08 Giranda Vincent L Substituted 1h-benzimidazole-4-carboxamides are potent parp inhibitors
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
KR20090127867A (ko) * 2006-12-05 2009-12-14 네이셔널 치아오 텅 유니버시티 인다졸 화합물
AU2009214440B2 (en) 2008-02-15 2014-09-25 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
AU2009244897B2 (en) 2008-04-16 2014-11-13 Alexion Pharmaceuticals, Inc. 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
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
PL3205654T3 (pl) 2010-05-20 2019-08-30 Array Biopharma, Inc. Związki makrocykliczne jako inhibitory kinazy TRK
TW201300360A (zh) 2010-11-01 2013-01-01 Portola Pharm Inc 做為ｊａｋ激酶調節劑之菸鹼醯胺
AU2012212075A1 (en) 2011-02-02 2013-07-18 Amgen Inc. Methods and compositons relating to inhibition of IGF-1R
MY162950A (en) 2011-02-07 2017-07-31 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2847293C (fr) 2011-09-16 2017-03-28 Richard Frederic Labaudiniere Formes solides d'un inhibiteur de la dissociation de derives de transthyretine
SG10201601352UA (en) 2011-11-23 2016-03-30 Portola Pharm Inc Pyrazine kinase inhibitors
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
EP2903970A4 (fr) 2012-10-08 2016-11-30 Portola Pharm Inc Inhibiteurs substitués de pyrimidinyl kinase
GB201223265D0 (en) * 2012-12-21 2013-02-06 Selvita Sa Novel benzimidazole derivatives as kinase inhibitors
KR20180041135A (ko) 2015-07-16 2018-04-23 어레이 바이오파마 인크. Ret 키나아제 억제제로서 치환된 피라졸로[1,5-a]피리딘 화합물
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز 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
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
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
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
JP7061195B2 (ja) 2018-01-18 2022-04-27 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ロ［３，４－ｄ］ピリミジン化合物
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
CA3087354C (fr) 2018-01-18 2023-01-03 Array Biopharma Inc. Composes de pyrrolo[2,3-d]pyrimidines substitues utilises en tant qu'inhibiteurs de la kinase ret
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US11964988B2 (en) 2019-09-06 2024-04-23 Array Biopharma Inc. Fused heterocyclic 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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