JP2010528021A - 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 - Google Patents

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 Download PDF

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Publication number
JP2010528021A
JP2010528021A JP2010509424A JP2010509424A JP2010528021A JP 2010528021 A JP2010528021 A JP 2010528021A JP 2010509424 A JP2010509424 A JP 2010509424A JP 2010509424 A JP2010509424 A JP 2010509424A JP 2010528021 A JP2010528021 A JP 2010528021A
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Japan
Prior art keywords
ring
compound
compound according
aliphatic
cancer
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Pending
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JP2010509424A
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Japanese (ja)
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JP2010528021A5 (enExample
Inventor
マイケル モーティモア,
ジュリアン ゴレック,
ダニエル ロビンソン,
クリストファー デービス,
ジョン スタッドレイ,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2010528021A publication Critical patent/JP2010528021A/ja
Publication of JP2010528021A5 publication Critical patent/JP2010528021A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2010509424A 2007-05-24 2008-05-02 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 Pending JP2010528021A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US93987607P 2007-05-24 2007-05-24
PCT/US2008/062331 WO2008147626A2 (en) 2007-05-24 2008-05-02 Thiazoles and pyrazoles useful as kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2014097421A Division JP2014141529A (ja) 2007-05-24 2014-05-09 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

Publications (2)

Publication Number Publication Date
JP2010528021A true JP2010528021A (ja) 2010-08-19
JP2010528021A5 JP2010528021A5 (enExample) 2012-06-21

Family

ID=39926662

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2010509424A Pending JP2010528021A (ja) 2007-05-24 2008-05-02 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
JP2014097421A Pending JP2014141529A (ja) 2007-05-24 2014-05-09 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

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2014097421A Pending JP2014141529A (ja) 2007-05-24 2014-05-09 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

Country Status (8)

Country Link
US (1) US20110060013A1 (enExample)
EP (1) EP2164842A2 (enExample)
JP (2) JP2010528021A (enExample)
CN (1) CN101687852A (enExample)
AU (1) AU2008257044A1 (enExample)
CA (1) CA2687966A1 (enExample)
MX (1) MX2009012719A (enExample)
WO (1) WO2008147626A2 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2422367C (en) 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7601718B2 (en) 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
CA2627808A1 (en) 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
NZ576750A (en) 2006-11-02 2012-01-12 Vertex Pharma Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
CA2673353A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
JP5520057B2 (ja) 2007-03-09 2014-06-11 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 蛋白キナーゼの阻害剤として有用なアミノピリミジン
NZ579485A (en) 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
JP2010523700A (ja) 2007-04-13 2010-07-15 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 キナーゼインヒビターとして有用なアミノピリミジン
AU2008247592A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
CN101801959A (zh) 2007-05-02 2010-08-11 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶类化合物
NZ582879A (en) 2007-07-31 2012-03-30 Vertex Pharma Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
US8748626B2 (en) * 2010-04-15 2014-06-10 Novartis Ag Oxazole and thiazole compounds as KSP inhibitors
CN104024248A (zh) 2011-08-25 2014-09-03 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸pak1抑制剂
BR112014015549A8 (pt) 2011-12-22 2017-07-04 Hoffmann La Roche composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção
SI3459942T1 (sl) 2012-04-24 2021-05-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
HRP20211855T1 (hr) 2013-03-12 2022-03-04 Vertex Pharmaceuticals Incorporated Inhibitori dnk-pk
SI3424920T1 (sl) 2013-10-17 2020-08-31 Vertex Pharmaceuticals Incorporated Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk
HK1252425A1 (zh) 2015-06-05 2019-05-24 Vertex Pharmaceuticals Incorporated 用於治疗脱髓鞘疾病的三唑类药物
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
JOP20180113B1 (ar) 2016-06-16 2022-03-14 Denali Therapeutics Inc مركبات بيريميدين -2-يل امينو -h1- بيرازول كمثبطات lrrk2 للاستخدام في علاج اضطرابات تنكسية عصبية
MX394860B (es) 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
TWI885039B (zh) 2020-01-13 2025-06-01 美商邊際分析公司 經取代吡唑并嘧啶及其用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003077921A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
WO2003078423A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Compositions useful as inhibitors of protein kinases
JP2004516292A (ja) * 2000-12-21 2004-06-03 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2006501176A (ja) * 2002-06-20 2006-01-12 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 タンパク質キナーゼの阻害剤としての置換ピリミジンおよびピリミジン誘導体を調製する方法
WO2006046734A2 (ja) * 2004-10-29 2006-05-04 Banyu Pharma Co Ltd オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) * 1964-05-12 J-aminoindazole derivatives
US3935183A (en) * 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) * 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3998951A (en) * 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) * 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
DOP1981004033A (es) * 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102194L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
SE8102193L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
JPS58124773A (ja) * 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc 5−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
ATE262902T1 (de) * 1994-11-10 2004-04-15 Millennium Pharm Inc Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose
IL117659A (en) * 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6267952B1 (en) * 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
ATE245641T1 (de) * 1998-02-17 2003-08-15 Tularik Inc Antivirale pyrimidinderivate
AU5777299A (en) * 1998-08-21 2000-03-14 Du Pont Pharmaceuticals Company Isoxazolo(4,5-d)pyrimidines as CRF antagonists
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
KR20010111298A (ko) * 2000-02-05 2001-12-17 버텍스 파마슈티칼스 인코포레이티드 Erk의 억제제로서 유용한 피라졸 조성물
AU2001237041B9 (en) * 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
CA2412592A1 (en) * 2000-06-28 2002-01-03 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
US6613776B2 (en) * 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ZA200301696B (en) * 2000-09-15 2004-04-28 Vertex Pharma Isoxazoles and their use as inhibitors of erk.
US6610677B2 (en) * 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2422367C (en) * 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6716851B2 (en) * 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
DE10061863A1 (de) * 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US6949544B2 (en) * 2001-03-29 2005-09-27 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
DE60214701T2 (de) * 2001-04-13 2007-09-13 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren von c-jun-n-terminalen-kinasen (jnk) und anderen proteinkinasen
US20030096813A1 (en) * 2001-04-20 2003-05-22 Jingrong Cao Compositions useful as inhibitors of GSK-3
EP1404669A2 (en) * 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
US6689778B2 (en) * 2001-07-03 2004-02-10 Vertex Pharmaceuticals Incorporated Inhibitors of Src and Lck protein kinases
US6698980B2 (en) * 2001-07-30 2004-03-02 Stewart Mining Products Inc. Rock stabilizing apparatus and method
US20030199526A1 (en) * 2001-12-07 2003-10-23 Deborah Choquette Pyrimidine-based compounds useful as GSK-3 inhibitors
DE60327999D1 (de) * 2002-03-15 2009-07-30 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
EP1485380B1 (en) * 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2003237121A1 (en) * 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
US7361665B2 (en) * 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
EP1605946B1 (en) * 2003-03-25 2008-05-28 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
US7169781B2 (en) * 2003-10-17 2007-01-30 Hoffmann-La Roche Inc. Imidazole derivatives and their use as pharmaceutical agents
CA2627808A1 (en) * 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004516292A (ja) * 2000-12-21 2004-06-03 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2004518743A (ja) * 2000-12-21 2004-06-24 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
WO2003077921A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
WO2003078423A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Compositions useful as inhibitors of protein kinases
JP2006501176A (ja) * 2002-06-20 2006-01-12 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 タンパク質キナーゼの阻害剤としての置換ピリミジンおよびピリミジン誘導体を調製する方法
WO2006046734A2 (ja) * 2004-10-29 2006-05-04 Banyu Pharma Co Ltd オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors

Also Published As

Publication number Publication date
US20110060013A1 (en) 2011-03-10
WO2008147626A2 (en) 2008-12-04
MX2009012719A (es) 2010-02-04
AU2008257044A1 (en) 2008-12-04
JP2014141529A (ja) 2014-08-07
EP2164842A2 (en) 2010-03-24
WO2008147626A3 (en) 2009-03-19
CA2687966A1 (en) 2008-12-04
CN101687852A (zh) 2010-03-31

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