DE60214198D1 - Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen - Google Patents

Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen

Info

Publication number
DE60214198D1
DE60214198D1 DE60214198T DE60214198T DE60214198D1 DE 60214198 D1 DE60214198 D1 DE 60214198D1 DE 60214198 T DE60214198 T DE 60214198T DE 60214198 T DE60214198 T DE 60214198T DE 60214198 D1 DE60214198 D1 DE 60214198D1
Authority
DE
Germany
Prior art keywords
inhibitors
src
pyrimidines
isoxazolyl
protein kinases
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.)
Expired - Lifetime
Application number
DE60214198T
Other languages
English (en)
Other versions
DE60214198T2 (de
Inventor
Guy Bemis
Huai Gao
Edmund Martin Harrington
Mark Ledeboer
Francesco Salituro
Jian Wang
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of DE60214198D1 publication Critical patent/DE60214198D1/de
Publication of DE60214198T2 publication Critical patent/DE60214198T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
DE60214198T 2001-07-03 2002-06-14 Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen Expired - Lifetime DE60214198T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30296901P 2001-07-03 2001-07-03
US302969P 2001-07-03
PCT/US2002/018956 WO2003004492A1 (en) 2001-07-03 2002-06-14 Isoxazolyl-pyrimidines as inhibitors of src and lck protein kinases

Publications (2)

Publication Number Publication Date
DE60214198D1 true DE60214198D1 (de) 2006-10-05
DE60214198T2 DE60214198T2 (de) 2007-08-09

Family

ID=23170022

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60214198T Expired - Lifetime DE60214198T2 (de) 2001-07-03 2002-06-14 Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen

Country Status (9)

Country Link
US (2) US6689778B2 (de)
EP (1) EP1417205B1 (de)
JP (1) JP4342937B2 (de)
AT (1) ATE337312T1 (de)
CA (1) CA2452603A1 (de)
DE (1) DE60214198T2 (de)
ES (1) ES2271283T3 (de)
HK (1) HK1065540A1 (de)
WO (1) WO2003004492A1 (de)

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US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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JP4342937B2 (ja) * 2001-07-03 2009-10-14 バーテックス ファーマシューティカルズ インコーポレイテッド ＳｒｃおよびＬｃｋタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
PL372198A1 (en) * 2002-02-06 2005-07-11 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
ATE468336T1 (de) * 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
DK1532145T3 (da) * 2002-08-02 2007-01-15 Vertex Pharma Pyrazolpræparater der er anvendelige som inhibitorer af GSK-3
AU2003270350A1 (en) * 2002-09-06 2004-03-29 Vertex Pharmaceuticals Incorporated Isoxazoles and their use in the treatment of ischemic diseases
KR20120032574A (ko) * 2002-10-03 2012-04-05 탈자진 인코포레이티드 혈관항상성 유지제 및 그의 사용 방법
US20050282814A1 (en) * 2002-10-03 2005-12-22 Targegen, Inc. Vasculostatic agents and methods of use thereof
WO2004072029A2 (en) * 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
AR045595A1 (es) * 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
US7592340B2 (en) * 2003-12-04 2009-09-22 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
JPWO2005080392A1 (ja) 2004-02-19 2007-08-02 武田薬品工業株式会社 ピラゾロキノロン誘導体およびその用途
EP1809614B1 (de) * 2004-04-08 2014-05-07 TargeGen, Inc. Benzotriazin-kinasehemmer
CA2578283A1 (en) 2004-08-25 2006-03-02 Targegen, Inc. Heterocyclic compounds and methods of use
JP5100126B2 (ja) * 2004-12-28 2012-12-19 あすか製薬株式会社 ピリミジニルイソオキサゾール誘導体
JP2008543775A (ja) * 2005-06-08 2008-12-04 ターゲジェン インコーポレーティッド 眼の障害を治療するための方法および組成物
US7737151B2 (en) * 2005-08-18 2010-06-15 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
NZ592990A (en) 2005-11-01 2013-01-25 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
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WO2007127366A2 (en) * 2006-04-25 2007-11-08 Targegen, Inc. Kinase inhibitors and methods of use thereof
CA2668429A1 (en) * 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
MX2009006690A (es) * 2006-12-19 2009-07-31 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
MX2009009592A (es) * 2007-03-09 2009-11-10 Vertex Pharma Aminopiridinas utiles como inhibidores de proteinas cinasas.
MX2009009591A (es) * 2007-03-09 2009-11-10 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
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CA2683785A1 (en) 2007-04-13 2008-10-23 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
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JP2010528021A (ja) * 2007-05-24 2010-08-19 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼのインヒビターとして有用なチアゾールおよびピラゾール
EP2176261B1 (de) * 2007-07-31 2012-12-19 Vertex Pharmaceuticals Incorporated Verfahren für die zubereitung von 5-fluor-1h-pyrazolo [3, 4-b] pyridin-3-amin und derivaten davon
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EP2265607B1 (de) 2008-02-15 2016-12-14 Rigel Pharmaceuticals, Inc. Pyrimidin-2-aminverbindungen und ihre verwendung als inhibitoren von jak-kinasen
JP2012501971A (ja) * 2008-09-03 2012-01-26 バーテックス ファーマシューティカルズ インコーポレイテッド 共結晶および共結晶を含む薬学的処方物
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PT2841428T (pt) 2012-04-24 2018-11-29 Vertex Pharma Inibidores de adn-pk
EP2922828B1 (de) 2012-11-21 2020-07-08 PTC Therapeutics, Inc. 4,6-diamino-pyrimidin-derivate als bmi-1 inhibitoren zur behandlung von krebs
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CN108064274A (zh) 2014-07-30 2018-05-22 耶达研究及发展有限公司 用于培养多能干细胞的培养基
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MX2019003317A (es) 2016-09-27 2019-08-05 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
CA3090063A1 (en) * 2018-02-08 2019-08-15 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
EP3914698A1 (de) 2019-01-23 2021-12-01 Yeda Research and Development Co. Ltd Kulturmedien für pluripotente stammzellen

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KR20020030791A (ko) 1999-08-12 2002-04-25 버텍스 파마슈티칼스 인코포레이티드 ｃ－ＪＵＮ Ｎ-말단 키나제(ＪＮＫ) 및 기타의 단백질키나제 억제제
WO2002083668A1 (en) * 2001-04-10 2002-10-24 Vertex Pharmaceuticals Incorporated Isoxaxole derivatives as inhibitors of src and other protein kinases
JP4342937B2 (ja) * 2001-07-03 2009-10-14 バーテックス ファーマシューティカルズ インコーポレイテッド ＳｒｃおよびＬｃｋタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン

Also Published As

Publication number Publication date
ATE337312T1 (de) 2006-09-15
HK1065540A1 (en) 2005-02-25
US6689778B2 (en) 2004-02-10
JP4342937B2 (ja) 2009-10-14
EP1417205A1 (de) 2004-05-12
WO2003004492A1 (en) 2003-01-16
US20050049246A1 (en) 2005-03-03
CA2452603A1 (en) 2003-01-16
DE60214198T2 (de) 2007-08-09
EP1417205B1 (de) 2006-08-23
JP2004536114A (ja) 2004-12-02
US20030171389A1 (en) 2003-09-11
ES2271283T3 (es) 2007-04-16

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