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
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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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    • 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
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)

Cited By (8)

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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

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CN101413143B (zh) 2002-12-19 2013-09-18 斯克里普斯研究学院 稳定甲状腺素运载蛋白和抑制甲状腺素运载蛋白错折叠的组合物和方法
CA2526594C (fr) 2003-05-27 2011-11-08 Robert Per Haegerkvist Utilisation d'un inhibiteur de tyrosine kinase c-abl-, pdgf-r- ou c-kit- dans le traitement du diabete
US7442709B2 (en) 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
EP1658289B1 (fr) * 2003-08-21 2009-03-18 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
AU2004308299B2 (en) * 2003-12-19 2011-11-24 Plexxikon, Inc. Compounds and methods for development of Ret modulators
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
US7728026B2 (en) 2005-04-11 2010-06-01 Abbott Laboratories, Inc. 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors
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
CA2607901C (fr) 2005-06-13 2016-08-16 Rigel Pharmaceuticals, Inc. Methodes et compositions pour le traitement de maladies osseuses degeneratives comprenant un compose inhibiteur syk 2,4-pyrimidinediamine
WO2007070173A2 (fr) 2005-10-31 2007-06-21 Merck & Co., Inc. Inhibiteurs de la cetp
EP1966157B1 (fr) 2005-11-15 2010-03-24 Abbott Laboratories 1h-benzimidazole-4-carboxamides substitues efficaces en tant qu inhibiteurs de parp
CA2642229C (fr) 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions et methodes destinees a l'inhibition de la voie jak
MX2008014004A (es) 2006-05-02 2008-11-12 Abbott Lab 1h-benzimidazol-4-carboxamidas sustituidas son inhibidores de parp potentes.
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
CN101616587A (zh) * 2006-12-05 2009-12-30 孙仲铭 吲唑化合物
PT2265607T (pt) 2008-02-15 2017-03-08 Rigel Pharmaceuticals Inc Compostos de pirimidina-2-amina e sua utilização como inibidores de jak cinases
ES2546502T3 (es) 2008-04-16 2015-09-24 Portola Pharmaceuticals, 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
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
WO2010083199A1 (fr) 2009-01-19 2010-07-22 Abbott Laboratories Inhibiteurs benzthiazole de la poly(adp-ribose)polymérase
EP3205654B1 (fr) 2010-05-20 2019-01-02 Array Biopharma, Inc. Composés macrocycliques comme inhibiteurs de la kinase 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
MX2013008833A (es) 2011-02-02 2013-12-06 Amgen Inc Metodos y composiciones relacionadas con la inhibicion de receptor del factor de crecimiento similar a la insulina 1 (igf-1r).
TR201816421T4 (tr) 2011-02-07 2018-11-21 Plexxikon Inc Kinaz modülasyonu için bileşikler ve metotlar ve bunların endikasyonları.
MX2014003043A (es) 2011-09-16 2015-02-05 Pfizer Formas solidas de un inhibidor de disociacion transtiretina.
US9359308B2 (en) 2011-11-23 2016-06-07 Portola Pharmaceuticals, 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***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
PL3322706T4 (pl) 2015-07-16 2021-07-19 Array Biopharma, Inc. Podstawione związki pirazolo[1,5-a]pirydynowe jako inhibitory kinazy ret
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
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
TW202410896A (zh) 2017-10-10 2024-03-16 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
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
TW201938169A (zh) 2018-01-18 2019-10-01 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[3,4-d]嘧啶化合物
CA3087972C (fr) 2018-01-18 2023-01-10 Array Biopharma Inc. Composes de pyrazolyl[4,3-c]pyridine substitues utilises en tant qu'inhibiteurs de la kinase ret
US11964988B2 (en) 2018-09-10 2024-04-23 Array Biopharma Inc. Fused heterocyclic compounds as RET kinase inhibitors

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

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
DENNY ET AL.: "Potential antitumor agents. 59. Structure-activity relationships for 2-phenylbenzimidazole-4-carboxamides, a new class of "minimal" DNA-intercalating agents which may not act via topoisomerase II", JOURNAL OF MEDICINAL CHEMISTRY, vol. 33, no. 2, February 1990 (1990-02-01), pages 814 - 819, XP002007402 *

Cited By (9)

* 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

Also Published As

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

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