DE60308387T2 - Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren - Google Patents

Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren Download PDF

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Publication number
DE60308387T2
DE60308387T2 DE60308387T DE60308387T DE60308387T2 DE 60308387 T2 DE60308387 T2 DE 60308387T2 DE 60308387 T DE60308387 T DE 60308387T DE 60308387 T DE60308387 T DE 60308387T DE 60308387 T2 DE60308387 T2 DE 60308387T2
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Prior art keywords
disease
disorder
compound
gsk
composition according
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DE60308387T
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DE60308387D1 (de
Inventor
J. Cornelia Pelham FORSTER
C. Larry Waltham PARK
W. Marion Stow WANNAMAKER
Yung-Mae Newton YAO
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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DE60308387T 2002-08-02 2003-07-31 Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren Expired - Lifetime DE60308387T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40096702P 2002-08-02 2002-08-02
US400967P 2002-08-02
PCT/US2003/023950 WO2004013140A1 (en) 2002-08-02 2003-07-31 Pyrazole compositions useful as inhibitors of gsk-3

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DE60308387D1 DE60308387D1 (de) 2006-10-26
DE60308387T2 true DE60308387T2 (de) 2007-09-20

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US (2) US7491730B2 (enExample)
EP (1) EP1532145B1 (enExample)
JP (3) JP4733388B2 (enExample)
KR (1) KR20050032105A (enExample)
CN (2) CN101037438A (enExample)
AR (1) AR040773A1 (enExample)
AT (1) ATE339419T1 (enExample)
AU (2) AU2003257078B2 (enExample)
BR (1) BR0313176A (enExample)
CA (1) CA2494100C (enExample)
CO (1) CO5700772A2 (enExample)
DE (1) DE60308387T2 (enExample)
DK (1) DK1532145T3 (enExample)
EA (1) EA200500299A1 (enExample)
EC (1) ECSP055640A (enExample)
ES (1) ES2273043T3 (enExample)
IL (1) IL166620A (enExample)
MX (1) MXPA05001367A (enExample)
NO (1) NO20051100L (enExample)
NZ (2) NZ538426A (enExample)
PL (1) PL374967A1 (enExample)
PT (1) PT1532145E (enExample)
TW (1) TWI324157B (enExample)
WO (1) WO2004013140A1 (enExample)
ZA (1) ZA200501124B (enExample)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001296871A1 (en) 2000-09-15 2002-03-26 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
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
PL374967A1 (en) 2002-08-02 2005-11-14 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
WO2004072029A2 (en) 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
WO2006007864A1 (en) * 2004-07-17 2006-01-26 Max Planck Geselllschaft Zur Förderung Der Wissenschaft Treating neurodegenerative conditions
US7335672B2 (en) 2004-09-13 2008-02-26 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US8771754B2 (en) * 2004-09-17 2014-07-08 Vanderbilt University Use of GSK3 inhibitors in combination with radiation therapies
EP1917259B1 (en) 2005-08-18 2012-01-25 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス,インコーポレイティド Pde阻害による神経新生の調節
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
CN101316597B (zh) 2005-11-03 2013-04-17 顶点医药品公司 用作激酶抑制剂的氨基嘧啶
NZ601687A (en) 2006-01-17 2014-03-28 Vertex Pharma Azaindoles useful as inhibitors of janus kinases
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2382975A3 (en) 2006-05-09 2012-02-29 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
HRP20120078T1 (hr) 2006-10-31 2012-02-29 Pfizer Products Inc. Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora
EP2086965B1 (en) * 2006-11-02 2010-02-10 Vertex Pharmaceuticals, Inc. Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
AU2007333650A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CN101678022A (zh) 2006-12-21 2010-03-24 弗特克斯药品有限公司 可用作蛋白激酶抑制剂的5-氰基-4-(吡咯并[2,3b]吡啶-3-基)嘧啶衍生物
US8802638B1 (en) 2007-01-25 2014-08-12 University Of South Florida Flavonoid treatment of glycogen synthase kinase-based disease
EP2121613A2 (en) * 2007-01-31 2009-11-25 Vertex Pharmaceuticals, Inc. 2-aminopyridine derivatives useful as kinase inhibitors
MX2009009590A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
JP2010520887A (ja) 2007-03-09 2010-06-17 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ジン
JP5393489B2 (ja) 2007-03-09 2014-01-22 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
CA2683785A1 (en) 2007-04-13 2008-10-23 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
JP5389785B2 (ja) 2007-05-02 2014-01-15 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 キナーゼ阻害剤として有用なチアゾールおよびピラゾール
CA2694381A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2008154241A1 (en) * 2007-06-08 2008-12-18 Abbott Laboratories 5-heteroaryl substituted indazoles as kinase inhibitors
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
CN101790532B (zh) 2007-07-31 2013-11-20 沃泰克斯药物股份有限公司 5-氟-1H-吡唑并[3,4-b]吡啶-3-胺及其衍生物的制备方法
KR20090031122A (ko) * 2007-09-21 2009-03-25 주식회사 중외제약 인다졸 골격을 함유하는 화합물, 이의 제조방법 및 상기화합물을 함유하는 약제학적 조성물
NZ586662A (en) 2007-12-19 2012-08-31 Vertex Pharma PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS JANUS KINASE 2 INHIBITORS
EP2262498A2 (en) * 2008-03-10 2010-12-22 Vertex Pharmceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
US8263547B2 (en) 2008-05-28 2012-09-11 Massachusetts Institute Of Technology DISC-1 pathway activators in the control of neurogenesis
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US9265764B2 (en) * 2009-02-27 2016-02-23 Massachusetts Institute Of Technology Uses of chemicals to modulate GSK-3 signaling for treatment of bipolar disorder and other brain disorders
WO2010104307A2 (ko) * 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 gsk3의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
AU2010262905B2 (en) 2009-06-17 2015-04-16 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2011059388A1 (en) * 2009-11-13 2011-05-19 Astrazeneca Ab Oxazolo[4,5-c]pyridine substituted pyrazine
US8592485B2 (en) 2010-06-17 2013-11-26 Healthpartners Research Foundation Methods and pharmaceutical compositions for treating the animal central nervous system for psychiatric disorders
KR20120063283A (ko) * 2010-12-07 2012-06-15 제일약품주식회사 신규한 피라졸로 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 약학적 조성물
KR20140014110A (ko) 2010-12-16 2014-02-05 버텍스 파마슈티칼스 인코포레이티드 인플루엔자 바이러스 복제의 억제제
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
EP2671885A1 (en) * 2012-06-05 2013-12-11 Ares Trading S.A. Imidazo-oxadiazole and Imidazo-thiadiazole derivatives
US8992951B2 (en) 2013-01-09 2015-03-31 Sapna Life Sciences Corporation Formulations, procedures, methods and combinations thereof for reducing or preventing the development, or the risk of development, of neuropathology as a result of trauma
CA3184040A1 (en) 2013-03-14 2014-10-02 The Brigham And Women's Hospital, Inc. Compositions and methods for epithelial stem cell expansion comprising a wnt agonist and a histone deacetylase inhibitor
EP3068782B1 (en) 2013-11-13 2018-05-23 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
ES2741444T3 (es) 2013-11-13 2020-02-11 Vertex Pharma Inhibidores de la replicación de virus de la gripe
WO2015155738A2 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
KR101731624B1 (ko) 2014-07-01 2017-05-04 광주과학기술원 세포 리프로그래밍 유도용 조성물
WO2016037016A1 (en) 2014-09-03 2016-03-10 The Brigham And Women's Hospital, Inc. Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss
WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
AU2017205194A1 (en) 2016-01-08 2018-07-19 Massachusetts Institute Of Technology Production of differentiated enteroendocrine cells and insulin producing cells
CN107151235B (zh) * 2016-03-04 2019-12-13 上海市计划生育科学研究所 噻二唑烷二酮基gsk3抑制剂在调节精子运动能力中的用途
WO2018217766A1 (en) 2017-05-22 2018-11-29 Whitehead Institute For Biomedical Research Kcc2 expression enhancing compounds and uses thereof
WO2020052648A1 (zh) * 2018-09-14 2020-03-19 江苏恒瑞医药股份有限公司 一种杂芳基并[4,3-c]嘧啶-5-胺类衍生物的晶型及制备方法
JP2022520671A (ja) 2019-02-08 2022-03-31 フリークエンシー・セラピューティクス・インコーポレイテッド 耳障害を治療するためのバルプロ酸化合物及びwnt作動薬

Family Cites Families (87)

* 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
MA18829A1 (fr) 1979-05-18 1980-12-31 Ciba Geigy Ag Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102193L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
SE8102194L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
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
JPS59173249U (ja) 1983-05-07 1984-11-19 日本碍子株式会社 避雷器素子を内蔵したオ−プンヒユ−ズカツトアウト
EP0136976A3 (de) 1983-08-23 1985-05-15 Ciba-Geigy Ag Verwendung von Phenylpyrimidinen als Pflanzenregulatoren
DE3725638A1 (de) 1987-08-03 1989-02-16 Bayer Ag Neue aryloxy (bzw. thio)aminopyrimidine
JPH0532662A (ja) 1990-11-09 1993-02-09 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
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
US5597920A (en) 1992-04-30 1997-01-28 Neurogen Corporation Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
JPH0665237A (ja) 1992-05-07 1994-03-08 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
ATE325113T1 (de) 1993-10-01 2006-06-15 Novartis Pharma Gmbh Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung
JPH10509708A (ja) 1994-11-10 1998-09-22 コア セラピューティクス,インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
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
WO1997009325A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6716575B2 (en) 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
EP0912559B1 (en) 1996-07-13 2002-11-06 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
JPH10130150A (ja) 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
JP4205168B2 (ja) 1996-10-02 2009-01-07 ノバルティス アクチエンゲゼルシヤフト ピリミジン誘導体およびその製造法
WO1998016502A1 (en) 1996-10-11 1998-04-23 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
EA200000409A1 (ru) 1997-10-10 2000-10-30 Сайтовиэ, Инк. Соединение, фармацевтическая композиция, способ ингибирования гибели клетки в одной клетке или ткани, способ лечения или снижения клеточной смерти, способ лечения или профилактики поликистозного заболевания почек или анемии/эритропоэза у животных, способ защиты органа или ткани млекопитающего от гибели клеток, способ снижения или профилактики гибели клеток в органе или ткани донора после их трансплантации, способ снижения или предотвращения гибели спермы или яйцеклеток
US6267952B1 (en) 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
JP2000026421A (ja) 1998-01-29 2000-01-25 Kumiai Chem Ind Co Ltd ジアリ―ルスルフィド誘導体及び有害生物防除剤
CA2321153A1 (en) 1998-02-17 1999-08-19 Timothy D. Cushing Anti-viral pyrimidine derivatives
KR20010041905A (ko) 1998-03-16 2001-05-25 시토비아 인크. 디펩티드 카스파제 억제제 및 이의 용도
JP4611524B2 (ja) 1998-06-02 2011-01-12 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド ピロロ[2,3d]ピリミジン組成物およびその使用
JP4533534B2 (ja) * 1998-06-19 2010-09-01 ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド グリコーゲンシンターゼキナーゼ3のインヒビター
WO2000011003A1 (en) 1998-08-21 2000-03-02 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
EP1119548B1 (en) * 1998-10-08 2004-12-08 SmithKline Beecham plc 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1h-pyrrole-2,5-dione as glycogen synthase kinase-3 inhibitor (gsk-3)
HK1039126B (en) 1998-10-08 2005-09-30 阿斯特拉曾尼卡有限公司 Quinazoline derivatives
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
AP2001002225A0 (en) 1999-01-13 2001-09-30 Warner Lambert Co 1-heterocycle substituted diarylamines.
EP1165085B1 (en) 1999-03-30 2006-06-14 Novartis AG Phthalazine derivatives for treating inflammatory diseases
WO2000078757A1 (en) 1999-06-17 2000-12-28 Shionogi Bioresearch Corp. Inhibitors of il-12 production
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
CZ2002534A3 (cs) 1999-08-13 2002-07-17 Vertex Pharmaceuticals Incorporated Inhibitory protein-kináz, farmaceutické prostředky, které je obsahují, a jejich pouľití
ES2306671T3 (es) 1999-10-07 2008-11-16 Amgen Inc. Inhibidores de triazina quinasa.
TR200201431T2 (tr) 1999-11-30 2002-09-23 Pfizer Products Inc. İmünosupresanlar olarak faydalı 2,4-diaminopirimidin bileşikleri
DK1246623T3 (da) 1999-12-02 2006-11-13 Osi Pharm Inc Forbindelser, som er specifikke for adenosin A1-, A2a- og A3-receptor og anvendelser deraf
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
CZ20013540A3 (cs) 2000-02-05 2002-03-13 Vertex Pharmaceuticals Incorporated Deriváty pyrazolu jako inhibitory ERK a farmaceutický prostředek, který je obsahuje
AU2001237041B9 (en) 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
CA2398446A1 (en) * 2000-04-18 2001-10-25 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinases
IL153246A0 (en) 2000-06-28 2003-07-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
CZ2003468A3 (cs) 2000-08-31 2004-05-12 Pfizeráproductsáinc Deriváty pyrazolu a jejich použití jako inhibitorů proteinkinázy
DE60122176T2 (de) 2000-09-15 2007-07-05 Vertex Pharmaceuticals Inc., Cambridge Isoxazole und ihre verwendung als erk-inhibitoren
US7473691B2 (en) 2000-09-15 2009-01-06 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
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2001296871A1 (en) 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2004509876A (ja) 2000-09-20 2004-04-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング 4−アミノ−キナゾリン
EP1351691A4 (en) 2000-12-12 2005-06-22 Cytovia Inc SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND ANALOGUES AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCERS, AND USE THEREOF
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)
WO2002050073A1 (en) * 2000-12-19 2002-06-27 Smithkline Beecham P.L.C. Pyrazolo[3,4-c]pyridines as gsk-3 inhibitors
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
CA2441733A1 (en) 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
JP2004535381A (ja) 2001-04-13 2004-11-25 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 c−JunN末端キナーゼ(JNK)および他のプロテインキナーゼのインヒビター
US20030096813A1 (en) 2001-04-20 2003-05-22 Jingrong Cao Compositions useful as inhibitors of GSK-3
AU2002308748A1 (en) 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
EP1399440B1 (en) 2001-06-15 2009-06-03 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors
DE60214198T2 (de) 2001-07-03 2007-08-09 Vertex Pharmaceuticals Inc., Cambridge Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen
MXPA04005510A (es) 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
EP1485100B1 (en) 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles as inhibitors of protein kinases
ATE365733T1 (de) 2002-03-15 2007-07-15 Vertex Pharma Zusammensetzungen brauchbar als protein-kinase- inhibitoren
WO2003078426A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azolylaminoazine as inhibitors of protein kinases
US20030207873A1 (en) 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
WO2003091246A1 (en) 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
PL374967A1 (en) * 2002-08-02 2005-11-14 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3

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