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WO2003020698A3 - Protein tyrosine kinase inhibitors - Google Patents

Protein tyrosine kinase inhibitors 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
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
PCT/IL2002/000740
Other languages
French (fr)
Other versions
WO2003020698A2 (en
Inventor
Doron Eren
Andrea Zaliani
Er David Pe
Oren Bogin
Avner Yayon
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Prochon Biotech Ltd
Original Assignee
Prochon Biotech Ltd
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/en
Application filed by Prochon Biotech Ltd filed Critical Prochon Biotech Ltd
Priority to AU2002334355A priority Critical patent/AU2002334355A1/en
Publication of WO2003020698A2 publication Critical patent/WO2003020698A2/en
Anticipated expiration legal-status Critical
Publication of WO2003020698A3 publication Critical patent/WO2003020698A3/en
Ceased legal-status Critical Current

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

Landscapes

  • 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

The present invention provides heterocyclic compounds which can act as protein tyrosine kinase inhibitors. Preferred embodiments include both novel and known substituted 2-aryl benzimidazole and benzofuro [3,2-c ] quinoline compounds. Methods of utilizing preferred compounds in preparation of medicaments for the treatment of proliferative, skeletal and metabolic diseases and disorders associated with abnormal protein tyrosine kinase activity, including cancer and skeletal dysplasia, are provided.
PCT/IL2002/000740 2001-09-06 2002-09-05 Protein tyrosine kinase inhibitors Ceased WO2003020698A2 (en)

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 (en) 2003-03-13
WO2003020698A3 true WO2003020698A3 (en) 2004-03-18

Family

ID=26324042

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IL2002/000740 Ceased WO2003020698A2 (en) 2001-09-06 2002-09-05 Protein tyrosine kinase inhibitors

Country Status (2)

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

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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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ATE405840T1 (en) 2002-12-19 2008-09-15 Scripps Research Inst COMPOSITIONS AND METHODS FOR STABILIZING TRANSTHYRETIN AND INHIBITING TRANSTHYRETIN MISFOLDING
NZ543709A (en) 2003-05-27 2009-04-30 Robert Per Hagerkvist Use of tyrosine kinase inhibitor to treat diabetes
US7442709B2 (en) 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
ATE425977T1 (en) * 2003-08-21 2009-04-15 Osi Pharm Inc 3-SUBSTITUTED IMIDAZOPYRIDINE DERIVATIVES AS C-KIT INHIBITORS
GB0325836D0 (en) * 2003-11-05 2003-12-10 Celltech R&D Ltd Biological products
JP5138938B2 (en) * 2003-12-19 2013-02-06 プレキシコン インコーポレーテッド Compounds and methods for the development of RET modulators
CA2566688A1 (en) 2004-05-20 2005-12-01 The Scripps Research Institute Transthyretin stabilization
MY146381A (en) 2004-12-22 2012-08-15 Amgen Inc Compositions and methods relating relating to anti-igf-1 receptor antibodies
WO2006110683A1 (en) 2005-04-11 2006-10-19 Abbott Laboratories 2-substituted-1h-benzimidazole-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 (en) * 2005-04-29 2011-02-16 Univ Ohio State Res Found SPECIFIC INHIBITORS AGAINST TYROSINE OF KERATINOCYTE GROWTH FACTOR RECEPTOR USEFUL IN PREVENTING CANCER METASTASES
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP2008543855A (en) 2005-06-13 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド Methods and compositions for treating degenerative bone disease
JP5301999B2 (en) 2005-10-31 2013-09-25 メルク・シャープ・アンド・ドーム・コーポレーション CETP inhibitor
US7462724B2 (en) 2005-11-15 2008-12-09 Abbott Laboratories Substituted 1H-benzimidazole-4-carboxamides are potent PARP inhibitors
JP2009528295A (en) 2006-02-24 2009-08-06 ライジェル ファーマシューティカルズ， インコーポレイテッド Compositions and methods for inhibition of the JAK pathway
US20070259937A1 (en) 2006-05-02 2007-11-08 Giranda Vincent L Substituted 1h-benzimidazole-4-carboxamides are potent parp inhibitors
EP1860104A1 (en) * 2006-05-22 2007-11-28 Aptanomics Anti-proliferative compounds deriving from a 3-aryl-coumarine or 3-aryl-quinolin-2-one and uses thereof
EP2091329A4 (en) * 2006-12-05 2011-02-23 Univ Nat Chiao Tung INDAZOLE COMPOUNDS
MX2010008926A (en) 2008-02-15 2011-02-23 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
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
CN102066338A (en) 2008-04-22 2011-05-18 波托拉医药品公司 protein kinase inhibitor
WO2010083199A1 (en) 2009-01-19 2010-07-22 Abbott Laboratories Benzthiazole inhibitors of poly(adp-ribose)polymerase
EP3521291A1 (en) 2010-05-20 2019-08-07 Array Biopharma, Inc. Macrocyclic compounds as trk kinase inhibitors
WO2012061428A2 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
MX2013008833A (en) 2011-02-02 2013-12-06 Amgen Inc Methods and compositons relating to inhibition of igf-1r.
JP5941069B2 (en) 2011-02-07 2016-06-29 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． Compounds and methods for kinase regulation and indications therefor
MX2014003043A (en) 2011-09-16 2015-02-05 Pfizer Solid forms of a transthyretin dissociation inhibitor.
AU2012340555B2 (en) 2011-11-23 2016-10-20 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
CN105646517A (en) * 2012-03-22 2016-06-08 巴塞利亚药业（中国）有限公司 Preparation methods of natural product Hirtellanine B and derivatives thereof and application of natural product Hirtellanine B and derivatives thereof in preparation of drug for treating tumor
US9676756B2 (en) 2012-10-08 2017-06-13 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
GB201223265D0 (en) * 2012-12-21 2013-02-06 Selvita Sa Novel benzimidazole derivatives as kinase inhibitors
KR20180041135A (en) 2015-07-16 2018-04-23 어레이 바이오파마 인크. A pyrazolo [1,5-a] pyridine compound substituted as a RET kinase inhibitor
JOP20190077A1 (en) 2016-10-10 2019-04-09 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TWI704148B (en) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (en) 2017-03-16 2019-09-16 Array Biopharma Inc Macrocyclic compounds as ros1 kinase inhibitors
TWI876442B (en) 2017-10-10 2025-03-11 美商絡速藥業公司 Formulations of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
TWI791053B (en) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 Crystalline forms of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile and pharmaceutical composition thereof
TW201932464A (en) 2018-01-18 2019-08-16 美商亞雷生物製藥股份有限公司 Substituted pyrazolyl[4,3-C]pyridine compounds as RET kinase inhibitors
US11603374B2 (en) 2018-01-18 2023-03-14 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
WO2020055672A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
CN119909072A (en) * 2025-01-24 2025-05-02 中国人民解放军空军军医大学 Application of benzofurano[3,2-c]quinolinone compounds in preventing and treating fatty liver disease associated with metabolic dysfunction

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Patent Citations (2)

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Non-Patent Citations (1)

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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 (en) 2003-03-13
AU2002334355A1 (en) 2003-03-18

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