DE60120193D1 - Pyrazolverbindungen als protein-kinasehemmer - Google Patents

Pyrazolverbindungen als protein-kinasehemmer

Info

Publication number
DE60120193D1
DE60120193D1 DE60120193T DE60120193T DE60120193D1 DE 60120193 D1 DE60120193 D1 DE 60120193D1 DE 60120193 T DE60120193 T DE 60120193T DE 60120193 T DE60120193 T DE 60120193T DE 60120193 D1 DE60120193 D1 DE 60120193D1
Authority
DE
Germany
Prior art keywords
protein kinase
hemmer
pyrazol compounds
pyrazol
compounds
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
DE60120193T
Other languages
English (en)
Other versions
DE60120193T2 (de
Inventor
Ronald Knegtel
David Bebbington
Hayley Binch
Julian Golec
Sanjay Patel
Jean-Damien Charrier
David Kay
Robert Davies
Pan Li
Marion Wannamaker
Cornelia Forster
Albert C Pierce
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27398347&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DE60120193(D1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of DE60120193D1 publication Critical patent/DE60120193D1/de
Publication of DE60120193T2 publication Critical patent/DE60120193T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • 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
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    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D491/02Heterocyclic 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
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    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
DE60120193T 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer Expired - Lifetime DE60120193T2 (de)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US23279500P 2000-09-15 2000-09-15
US232795P 2000-09-15
US25788700P 2000-12-21 2000-12-21
US257887P 2000-12-21
US28694901P 2001-04-27 2001-04-27
US286949P 2001-04-27
PCT/US2001/028740 WO2002022601A1 (en) 2000-09-15 2001-09-14 Pyrazole compounds useful as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
DE60120193D1 true DE60120193D1 (de) 2006-07-06
DE60120193T2 DE60120193T2 (de) 2007-03-29

Family

ID=27398347

Family Applications (8)

Application Number Title Priority Date Filing Date
DE60128709T Expired - Lifetime DE60128709T2 (de) 2000-09-15 2001-09-14 Triazol-verbindungen als protein-kinase-inhibitoren
DE60119749T Expired - Lifetime DE60119749T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60110616T Expired - Lifetime DE60110616T3 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60120193T Expired - Lifetime DE60120193T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60124744T Expired - Lifetime DE60124744T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60120198T Expired - Lifetime DE60120198T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60119748T Expired - Lifetime DE60119748T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60120194T Expired - Lifetime DE60120194T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer

Family Applications Before (3)

Application Number Title Priority Date Filing Date
DE60128709T Expired - Lifetime DE60128709T2 (de) 2000-09-15 2001-09-14 Triazol-verbindungen als protein-kinase-inhibitoren
DE60119749T Expired - Lifetime DE60119749T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60110616T Expired - Lifetime DE60110616T3 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer

Family Applications After (4)

Application Number Title Priority Date Filing Date
DE60124744T Expired - Lifetime DE60124744T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60120198T Expired - Lifetime DE60120198T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60119748T Expired - Lifetime DE60119748T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
DE60120194T Expired - Lifetime DE60120194T2 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer

Country Status (24)

Country Link
US (7) US6696452B2 (de)
EP (8) EP1318997B1 (de)
JP (9) JP4105947B2 (de)
KR (4) KR20030032035A (de)
CN (3) CN100355750C (de)
AP (1) AP2003002762A0 (de)
AT (8) ATE327991T1 (de)
AU (9) AU2001290914A1 (de)
BR (1) BR0114088A (de)
CA (8) CA2422378C (de)
DE (8) DE60128709T2 (de)
DK (1) DK1318997T3 (de)
ES (3) ES2242771T5 (de)
HK (8) HK1057543A1 (de)
HU (4) HUP0401819A3 (de)
IL (6) IL154784A0 (de)
MX (8) MXPA03002299A (de)
NO (4) NO327708B1 (de)
NZ (4) NZ525014A (de)
PE (1) PE20020451A1 (de)
PL (1) PL361676A1 (de)
PT (2) PT1317448E (de)
TW (1) TWI303636B (de)
WO (8) WO2002022607A1 (de)

Families Citing this family (394)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69638073D1 (de) * 1996-09-04 2009-12-24 Intertrust Tech Corp Zuverlässige Infrastrukturhilfssysteme, Verfahren und Techniken für sicheren elektronischen Handel, elektronische Transaktionen, Handelsablaufsteuerung und Automatisierung, verteilte Verarbeitung und Rechteverwaltung
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6982260B1 (en) 1999-11-22 2006-01-03 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
CA2395593C (en) 1999-12-24 2011-08-02 Aventis Pharma Limited Azaindoles
US6660731B2 (en) * 2000-09-15 2003-12-09 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
ES2242771T5 (es) * 2000-09-15 2011-10-14 Vertex Pharmaceuticals Incorporated Compuestos de pirazol útiles como inhibidores de proteína quinasas.
AU2002222293A1 (en) * 2000-12-19 2002-07-01 Smithkline Beecham P.L.C. Pyrazolo(3,4-c)pyridines as gsk-3 inhibitors
ATE327989T1 (de) * 2000-12-21 2006-06-15 Vertex Pharma Pyrazolverbindungen als protein-kinase- inhibitoren
KR100847169B1 (ko) 2000-12-21 2008-07-17 글락소 그룹 리미티드 혈관형성 조절제로서의 피리미딘아민
WO2002079163A1 (en) * 2001-03-30 2002-10-10 Smithkline Beecham Corporation Aminopyridine derivatives as estrogen receptor modulators
EP1404669A2 (de) * 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclisch substituierte pyrazole als inhibitoren von src und anderen protein kinasen
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003018563A1 (en) 2001-08-31 2003-03-06 Northwestern University Anti-inflammatory and protein kinase inhibitor composition and method of use
WO2003030909A1 (en) * 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
CZ2004359A3 (cs) 2001-09-26 2004-09-15 Pharmacia Italia S.P.A. Aminoindazolové deriváty aktivní jako inhibitory kinázy, způsob jejich přípravy a farmaceutické prostředky obsahující tyto deriváty
TWI330183B (de) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
CA2469316A1 (en) 2001-12-07 2003-06-19 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as gsk-3 inhibitors
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
ATE323706T1 (de) 2001-12-17 2006-05-15 Smithkline Beecham Corp Pyrazolopyridazinderivate
AU2002361846A1 (en) * 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
KR20040085151A (ko) 2002-01-17 2004-10-07 뉴로젠 코포레이션 캡사이신 조절자로서의 치환된 퀴나졸린-4-일 아민 유사체
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
EP2322521B1 (de) * 2002-02-06 2013-09-04 Vertex Pharmaceuticals, Inc. Heteroaryl-Verbindungen und Ihre Anwendung als GSK-3-Hemmer
EP1485100B1 (de) * 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azolylaminoazine als proteinkinasehemmer
US7179826B2 (en) 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
DE60332604D1 (de) * 2002-03-15 2010-07-01 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
IL163737A0 (en) * 2002-04-05 2005-12-18 Boehringer Ingelheim Pharma Method of treating mucus hypersecretion
AU2003231232A1 (en) 2002-05-01 2003-11-17 Vertex Pharmaceuticals Incorporated Crystal structure of aurora-2 protein and binding pockets thereof
ATE493987T1 (de) 2002-05-22 2011-01-15 Amgen Inc Aminopyrimidin-derivate zur verwendung als vanilloid-rezeptor-liganden zur behandlung von schmerzen
WO2003104230A1 (ja) * 2002-06-07 2003-12-18 協和醱酵工業株式会社 二環性ピリミジン誘導体
WO2003106455A1 (en) 2002-06-14 2003-12-24 Applied Research Systems Ars Holding N.V. Azole methylidene cyanide derivatives and their use as protein kinase modulators
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
EP1534716B1 (de) * 2002-07-17 2008-04-23 Pfizer Italia S.r.l. Heterobicyclische pyrazolderivate als kinaseinhibitoren
EP1575506A4 (de) * 2002-07-25 2008-04-23 Scios Inc Verfahren zur verbesserung der lungenfunktion mit tgf-beta hemmern
BR0313059B8 (pt) 2002-07-29 2021-07-27 Rigel Pharmaceuticals composto, e, composição farmacêutica
EP1739087A1 (de) * 2002-08-02 2007-01-03 Vertex Pharmaceuticals Incorporated Pyrazolenthaltende Zusammensetzungen und ihre Verwendung als Gsk-3 Inhibitoren
KR20050032105A (ko) * 2002-08-02 2005-04-06 버텍스 파마슈티칼스 인코포레이티드 Gsk-3의 억제제로서 유용한 피라졸 조성물
DE60325865D1 (de) * 2002-08-13 2009-03-05 Merck Sharp & Dohme Phenylpyridazin derivative als liganden für gaba-rezeptoren
KR20050042478A (ko) 2002-08-14 2005-05-09 버텍스 파마슈티칼스 인코포레이티드 프로테인 키나아제 억제제 및 이의 용도
MXPA05001807A (es) 2002-09-05 2005-04-19 Aventis Pharma Sa Nuevos derivados de aminoindazol utilizados como medicamentos y composiciones farmaceuticas que los contienen.
FR2844267B1 (fr) * 2002-09-05 2008-02-15 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
UA80295C2 (en) 2002-09-06 2007-09-10 Biogen Inc Pyrazolopyridines and using the same
WO2004024159A1 (en) * 2002-09-10 2004-03-25 Scios Inc. INHIBITORS OF TFGβ
US7312227B2 (en) 2002-11-01 2007-12-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
JP2006508107A (ja) 2002-11-05 2006-03-09 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 Jakおよび他のプロテインキナーゼのインヒビターとして有用な化合物
ATE527250T1 (de) 2002-11-21 2011-10-15 Novartis Ag 2,4,6-trisubstituierten pyrimidinen als phosphotidylinositol (pi) 3-kinase inhibitoren und deren verwendung zur behandlung von krebs
CN1735607B (zh) * 2002-11-21 2010-06-09 诺华疫苗和诊断公司 2,4,6-三取代的嘧啶作为磷脂酰肌醇(pi)3-激酶抑制剂及其在治疗癌症中的应用
JP4666256B2 (ja) * 2002-12-10 2011-04-06 小野薬品工業株式会社 含窒素複素環化合物およびその医薬用途
FR2848554A1 (fr) * 2002-12-12 2004-06-18 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
CA2507948A1 (fr) 2002-12-12 2004-07-29 Aventis Pharma S.A. Derives d'aminoindazoles et leur utilisation comme inhibiteurs de kinases
CA2509239A1 (en) 2002-12-13 2004-07-01 Neurogen Corporation Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
US7601718B2 (en) 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US7157455B2 (en) * 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
WO2004087056A2 (en) * 2003-03-28 2004-10-14 Scios Inc. BI-CYCLIC PYRIMIDINE INHIBITORS OF TGFβ
US7763627B2 (en) * 2003-04-09 2010-07-27 Exelixis, Inc. Tie-2 modulators and methods of use
US7638530B2 (en) * 2003-04-24 2009-12-29 Merck & Co., Inc. Inhibitors of Akt activity
WO2004096808A1 (en) * 2003-04-28 2004-11-11 De Novo Pharmaceuticals Limited Triazine compounds and their use
CA2528834A1 (en) * 2003-06-13 2005-02-10 Arena Pharmaceuticals, Inc. 5-substituted 2h-pyrazole-3-carboxylic acid derivatives as agonists for the nicotinic acid receptor rup25 for the treatment of dyslipidemia and related diseases
JP2007524615A (ja) * 2003-06-20 2007-08-30 コーリー ファーマシューティカル ゲーエムベーハー 低分子トール様レセプター(tlr)アンタゴニスト
TW200510373A (en) 2003-07-14 2005-03-16 Neurogen Corp Substituted quinolin-4-ylamine analogues
US7329664B2 (en) 2003-07-16 2008-02-12 Neurogen Corporation Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
PT1656372E (pt) 2003-07-30 2013-06-27 Rigel Pharmaceuticals Inc Métodos para o tratamento ou prevenção de doenças autoimunes com compostos de 2,4-pirimidinadiamina
TW200521119A (en) * 2003-08-05 2005-07-01 Vertex Pharma Compositions useful as inhibitors of voltage-gated ion channels
AU2004263148B2 (en) * 2003-08-06 2008-08-21 Vertex Pharmaceuticals, Incorporated Aminotriazole compounds useful as inhibitors of protein kinases
AU2004276341B2 (en) * 2003-09-23 2011-04-14 Vertex Pharmaceuticals Incorporated Pyrazolopyrrole derivatives as protein kinase inhibitors
GB0323137D0 (en) 2003-10-03 2003-11-05 Chang Lisa C W 2,4,6- Trisubstituted pyrimidines and their different uses
US7579349B2 (en) * 2003-10-17 2009-08-25 Astrazeneca Ab 4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer
WO2005047268A2 (en) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
AU2004289304A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Pyridine compounds
CN102127056B (zh) * 2003-12-03 2013-08-21 Ym生物科学澳大利亚私人有限公司 微管蛋白抑制剂
AU2004297235A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
CA2548009A1 (en) * 2003-12-09 2005-06-23 Vertex Pharmaceuticals Incorporated Naphthyridine derivatives and their use as modulators of muscarinic receptors
JP2007514759A (ja) * 2003-12-19 2007-06-07 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
TW200530235A (en) 2003-12-24 2005-09-16 Renovis Inc Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
WO2005070891A2 (en) 2004-01-23 2005-08-04 Amgen Inc Compounds and methods of use
WO2005073224A2 (en) 2004-01-23 2005-08-11 Amgen Inc Quinoline quinazoline pyridine and pyrimidine counds and their use in the treatment of inflammation angiogenesis and cancer
US7534798B2 (en) 2004-02-11 2009-05-19 Amgen Inc. Vanilloid receptor ligands and their use in treatments
EP1742936A2 (de) 2004-04-13 2007-01-17 Icagen, Inc. Polycyclische pyridine als kaliumionenkanalmodulatoren
JP2007533753A (ja) * 2004-04-23 2007-11-22 タケダ サン ディエゴ インコーポレイテッド インドール誘導体及びキナーゼ阻害剤としてのその使用
US7793137B2 (en) 2004-10-07 2010-09-07 Cisco Technology, Inc. Redundant power and data in a wired data telecommunincations network
ES2391577T3 (es) 2004-05-14 2012-11-27 Millennium Pharmaceuticals, Inc. Los compuestos y métodos para inhibir la progresión mitótica mediante la inhibición de la aurora quinasa
EP1604988A1 (de) 2004-05-18 2005-12-14 Sanofi-Aventis Deutschland GmbH Pyridazinonderivate, Methoden, um selbige herzustellen, und ihre Verwendung als Pharmazeutika
EP1598348A1 (de) 2004-05-18 2005-11-23 Aventis Pharma Deutschland GmbH Pyridazinonderivate als CDK2-Inhibitoren
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
GB0415364D0 (en) * 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
US20080261821A1 (en) * 2004-07-21 2008-10-23 The Regents Of Te University Of California Mechanism-Based Crosslinkers
US7550598B2 (en) * 2004-08-18 2009-06-23 Takeda Pharmaceutical Company Limited Kinase inhibitors
US7858813B2 (en) 2004-08-19 2010-12-28 Dsm Ip Assets B.V. Process for the rectification of mixtures of high-boiling air-and/or temperature-sensitive useful products
GB0419416D0 (en) * 2004-09-01 2004-10-06 Inst Of Ex Botany Ascr 4-Arylazo-3,5-Diamino-Pyrazole compounds and use thereof
CA2579143A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
CA2581454A1 (en) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
TW200624431A (en) 2004-09-24 2006-07-16 Hoffmann La Roche Phthalazinone derivatives, their manufacture and use as pharmaceutical agents
US7285569B2 (en) 2004-09-24 2007-10-23 Hoff Hoffmann-La Roche Inc. Tricycles, their manufacture and use as pharmaceutical agents
WO2006035061A1 (en) 2004-09-30 2006-04-06 Tibotec Pharmaceuticals Ltd. Hcv inhibiting bi-cyclic pyrimidines
TW200621251A (en) 2004-10-12 2006-07-01 Neurogen Corp Substituted biaryl quinolin-4-ylamine analogues
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
TW200621257A (en) * 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
EP2592075B1 (de) 2004-11-02 2015-04-29 Northwestern University Pyridazinverbindungen zur behandlung von entzündlichen erkrankungen
CA2589102C (en) 2004-11-02 2013-08-13 Northwestern University Pyridazine compounds and methods for using the compounds to treat inflammatory diseases
KR20070086188A (ko) 2004-11-17 2007-08-27 미카나 테라퓨틱스, 인크. 키나제 억제제
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
EP1827434B1 (de) 2004-11-30 2014-01-15 Amgen Inc. Chinolin- und chinazolinanaloge und deren verwendung als medikamente zur krebsbehandlung
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
JP2008525422A (ja) * 2004-12-23 2008-07-17 ファイザー・プロダクツ・インク 抗癌剤として有用な複素芳香族誘導体
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
RU2416616C2 (ru) 2005-01-19 2011-04-20 Райджел Фармасьютикалз, Инк. Пролекарства соединений 2,4-пиримидиндиамина и их применения
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
CA2595514C (en) * 2005-01-26 2012-06-12 Schering Corporation Kinase inhibitors
SI2383268T1 (sl) * 2005-02-04 2016-02-29 Astrazeneca Ab Derivati pirazolilaminopiridina uporabni kot kinazni inhibitorji
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
DK1853588T3 (da) 2005-02-16 2008-09-15 Astrazeneca Ab Kemiske forbindelser
EP1863797A1 (de) * 2005-03-23 2007-12-12 AstraZeneca AB 2-azetidinyl-4-(lh-pyrazol-3-ylamino)pyrimidine als inhibitoren der aktivität des rezeptors für den insulin-like growth factor-i
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
WO2006100310A1 (en) 2005-03-25 2006-09-28 Tibotec Pharmaceuticals Ltd Heterobicylic inhibitors of hcv
ES2310406T3 (es) * 2005-04-05 2009-01-01 Astrazeneca Ab Derivados de pirimidina para uso como agentes anticancerosos.
GB0507347D0 (en) * 2005-04-12 2005-05-18 Astrazeneca Ab Chemical compounds
CA2603204A1 (en) 2005-04-14 2006-10-19 F. Hoffmann-La Roche Ag Aminopyrazole derivatives, their manufacture and use as pharmaceutical agents
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
ES2545382T3 (es) 2005-04-28 2015-09-10 Mitsubishi Tanabe Pharma Corporation Derivado de cianopiridina y su uso como medicamento
EP1885454A2 (de) 2005-05-04 2008-02-13 DeveloGen Aktiengesellschaft Verwendung von gsk-3-hemmern zur prävention und behandlung von pankreatischen autoimmunkrankheiten
WO2006119504A2 (en) * 2005-05-04 2006-11-09 Renovis, Inc. Fused heterocyclic compounds, and compositions and uses thereof
CN101218229A (zh) * 2005-05-05 2008-07-09 阿斯利康(瑞典)有限公司 吡唑基-氨基取代的嘧啶及其在癌症治疗中的应用
AR056347A1 (es) 2005-05-12 2007-10-03 Tibotec Pharm Ltd Uso de compuestos de pteridina para fabricar medicamentos y composiciones farmaceuticas
EP1899323A2 (de) 2005-05-16 2008-03-19 AstraZeneca AB Als tyrosinkinaseinhibitoren geeignete pyrazolylaminopyrimidinderivate
JP2008543888A (ja) 2005-06-24 2008-12-04 ギリアード サイエンシーズ, インコーポレイテッド ピリド(3,2−d)ピリミジン、およびC型肝炎を治療するのに有用な医薬組成物
ES2270715B1 (es) 2005-07-29 2008-04-01 Laboratorios Almirall S.A. Nuevos derivados de pirazina.
CA2619517A1 (en) * 2005-08-18 2007-02-22 Michael Mortimore Pyrazine kinase inhibitors
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
EP2275096A3 (de) 2005-08-26 2011-07-13 Braincells, Inc. Neurogenese durch modulation des Muscarinrezeptors
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
CN101316587B (zh) * 2005-09-30 2013-04-03 迈卡纳治疗股份有限公司 取代的吡唑化合物
BRPI0616630B8 (pt) * 2005-09-30 2021-05-25 Miikana Therapeutics Inc compostos de pirazol substituídos
ES2274712B1 (es) 2005-10-06 2008-03-01 Laboratorios Almirall S.A. Nuevos derivados imidazopiridina.
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
GB0520657D0 (en) * 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
EP1940389A2 (de) 2005-10-21 2008-07-09 Braincells, Inc. Modulation von neurogenese durch pde-hemmung
PL1945631T3 (pl) 2005-10-28 2012-12-31 Astrazeneca Ab Pochodne 4-(3-aminopirazolo)pirymidyny do stosowania jako inhibitory kinazy tyrozynowej do leczenia raka
EP1942879A1 (de) 2005-10-31 2008-07-16 Braincells, Inc. Gaba-rezeptor-vermittelte modulation von neurogenese
RU2423361C2 (ru) * 2005-11-03 2011-07-10 Вертекс Фармасьютикалз Инкорпорейтед Аминопиримидины в качестве ингибиторов киназ
ZA200803887B (en) 2005-11-08 2009-12-30 Vertex Pharma Heterocyclic modulators of ATP-Binding Cassette transporters
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
EP1966152A2 (de) * 2005-12-20 2008-09-10 Takeda Pharmaceutical Company Limited Glucokinase-aktivatoren
EP1973911B1 (de) 2006-01-17 2016-01-13 Vertex Pharmaceuticals Incorporated Zur behandlung von (unter anderem) proliferativen, kardiologischen, neurodegenerativen, autoimmun- oder entzündlichen erkrankungen geeignete azaindole
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
DE602007009932D1 (de) 2006-02-16 2010-12-02 Schering Corp Pyrrolidin-derivate als erk-hemmer
US20100216734A1 (en) * 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
CA2643199A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
PE20080145A1 (es) 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
AU2007235237B2 (en) * 2006-04-11 2011-08-18 Vertex Pharmaceuticals Incorporated Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
US8158627B2 (en) 2006-04-28 2012-04-17 Northwestern University Compositions and treatments using pyridazine compounds and cholinesterase inhibitors
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
WO2007134077A2 (en) * 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
CA2656003C (en) 2006-06-27 2014-03-25 Tsuneo Yasuma Fused cyclic compounds
WO2008001070A1 (en) * 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
AU2007269540B2 (en) * 2006-07-05 2013-06-27 Exelixis, Inc. Methods of using IGF1R and Abl kinase modulators
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8003651B2 (en) * 2006-07-06 2011-08-23 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
UA95641C2 (en) * 2006-07-06 2011-08-25 Эррей Биофарма Инк. Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
US8338435B2 (en) 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
BRPI0716604A2 (pt) * 2006-09-08 2013-04-09 Braincells Inc combinaÇÕes contendo um derivado de 4-acilaminopiridina
US20080103165A1 (en) * 2006-09-19 2008-05-01 Braincells, Inc. Ppar mediated modulation of neurogenesis
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
JP2010505961A (ja) * 2006-10-09 2010-02-25 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
KR20090071662A (ko) * 2006-10-21 2009-07-01 애보트 게엠베하 운트 콤파니 카게 헤테로사이클릭 화합물 및 글리코겐 신타제 키나제 3 억제제로서의 이의 용도
WO2008057940A1 (en) * 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
JP2010513567A (ja) * 2006-12-19 2010-04-30 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の阻害剤として有用なアミノピリミジン
WO2008077650A1 (en) 2006-12-26 2008-07-03 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines useful for treating viral infections
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
US8143394B2 (en) 2006-12-26 2012-03-27 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines useful for treating viral infections
AU2008213808B2 (en) 2007-02-06 2011-11-10 Novartis Ag PI 3-kinase inhibitors and methods of their use
WO2008100412A1 (en) * 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
EP2121633A2 (de) * 2007-02-12 2009-11-25 Merck & Co., Inc. Piperazinderivate zur behandlung von alzheimer-krankheit und verwandten leiden
EP2133095A4 (de) 2007-03-05 2012-09-26 Kyowa Hakko Kirin Co Ltd Pharmazeutische zusammensetzung
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
NZ579446A (en) * 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
EP2137183B1 (de) * 2007-03-09 2011-09-28 Vertex Pharmaceuticals Incorporated Als inhibitoren von proteinkinasen geeignete aminopyrimidine
NZ580343A (en) 2007-04-13 2012-03-30 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
EP2155742A1 (de) * 2007-04-18 2010-02-24 AstraZeneca AB 5-aminopyrazol-3-yl-3h-imidazo[4,5-b]pyridinderivate und ihre verwendung zur behandlung von krebs
MX2009011810A (es) 2007-05-02 2010-01-14 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
AU2008247595A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
EP2152696B1 (de) * 2007-05-02 2014-09-24 Vertex Pharmaceuticals Incorporated Aminopyrimidine als kinasehemmer
US20100137398A1 (en) * 2007-05-04 2010-06-03 Novartis Ag Use of hdac inhibitors for the treatment of gastrointestinal cancers
UA99459C2 (en) 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
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
US20090029992A1 (en) * 2007-06-11 2009-01-29 Agoston Gregory E Substituted pyrazole compounds
EP2166854A4 (de) * 2007-06-13 2012-05-16 Merck Sharp & Dohme Triazolderivate zur behandlung von morbus alzheimer und verwandten leiden
CN101687840A (zh) 2007-06-25 2010-03-31 霍夫曼-拉罗奇有限公司 作为激酶抑制剂的苯并咪唑酰胺基衍生物
JP5542282B2 (ja) * 2007-07-05 2014-07-09 アレイ バイオファーマ、インコーポレイテッド Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
ES2551352T3 (es) 2007-07-05 2015-11-18 Array Biopharma, Inc. Pirimido ciclopentanos útiles para el tratamiento de enfermedades inflamatorias o hiperproliferativas
CN101808693A (zh) 2007-07-25 2010-08-18 百时美施贵宝公司 三嗪激酶抑制剂
TW200906818A (en) * 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
CA2694499A1 (en) * 2007-07-31 2009-02-05 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
KR20100088142A (ko) * 2007-11-20 2010-08-06 머크 샤프 앤드 돔 코포레이션 비-뉴클레오사이드 역전사효소 억제제
CA3147290A1 (en) * 2007-12-07 2009-06-18 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
KR20150063170A (ko) 2007-12-07 2015-06-08 버텍스 파마슈티칼스 인코포레이티드 3-(6-(1-(2,2-디플루오로벤조[d][1,3]디옥솔-5-일)사이클로프로판카복스아미도)-3-메틸피리딘-2-일)벤조산의 고체 형태
JP2011032169A (ja) * 2007-12-11 2011-02-17 Genecare Research Institute Co Ltd 4−アミノピリミジン誘導体および該化合物を含有する医薬組成物
US8288397B2 (en) 2007-12-17 2012-10-16 Janssen Pharmaceutica Nv Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
WO2009089454A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
ES2426092T3 (es) * 2008-01-09 2013-10-21 Array Biopharma, Inc. 5H-Ciclopenta[d]pirimidinas como inhibidores de proteínas cinasas AKT
MX2010009268A (es) 2008-02-21 2010-09-14 Schering Corp Compuestos que son inhibidores de erk.
CN102245573B (zh) 2008-02-28 2013-11-20 沃泰克斯药物股份有限公司 作为cftr调节剂的杂芳基衍生物
JP2011513483A (ja) * 2008-03-10 2011-04-28 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有用なピリミジンおよびピリジン
CL2009000904A1 (es) * 2008-04-21 2010-04-30 Shionogi & Co Compuestos derivados de ciclohexil sulfonamidas que tienen actividad antagonista en el receptor npy y5, composicion farmaceutica y formulacion farmaceutica que los comprende.
US8158656B2 (en) * 2008-05-16 2012-04-17 Shenzhen Chipscreen Biosciences Ltd. 2-indolinone derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
AU2009259026B2 (en) * 2008-06-11 2012-10-04 Astrazeneca Ab Tricyclic 2,4-diamin0-L,3,5-triazine derivatives useful for the treatment of cancer and myeloproliferative disorders
MX2010013726A (es) 2008-06-12 2011-01-14 Janssen Pharmaceutica Nv Moduladores de diamino-piridina, pirimidina, y piridazina del receptor h4 de histamina.
CN102083831B (zh) * 2008-07-03 2014-09-03 默克专利有限公司 用作aurora激酶抑制剂的萘啶酮
WO2010002998A1 (en) 2008-07-03 2010-01-07 Gilead Sciences, Inc. 2,4,6-TRISUBSTITUTED PYRIDO (3,2-d) PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS
UA101676C2 (uk) * 2008-07-31 2013-04-25 Дженентек, Инк. Піримідинові сполуки, композиції і способи застосування
WO2010019392A1 (en) * 2008-08-13 2010-02-18 Merck Sharp & Dohme Corp. Purine derivatives for treatment of alzheimer's disease
EP2323622A1 (de) * 2008-09-03 2011-05-25 Vertex Pharmaceuticals Incorporated Co-kristalle und diese enthaltende pharmazeutische formulierungen
CN102264728B (zh) * 2008-09-15 2015-02-04 加利福尼亚大学董事会 用于调节ire1、src和abl活性的方法和组合物
US20110201628A1 (en) * 2008-09-30 2011-08-18 Astrazeneca Ab Heterocyclic jak kinase inhibitors
CA2744343A1 (en) * 2008-11-19 2010-05-27 Renovis, Inc. 6, 7 -dihydro- 5h- pyrrolo [3, 4-d] pyrimidin-4-yl] -quinolin-3 -ylamine compounds useful as faah modulators and uses thereof
KR101048448B1 (ko) 2008-11-21 2011-07-11 한국화학연구원 신규 피라졸로[4,3-b]피리딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
ME02337B (de) 2009-02-05 2016-06-20 Takeda Pharmaceuticals Co Pyridazinonverbindungen
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
SI2401267T1 (sl) * 2009-02-27 2014-05-30 Ambit Biosciences Corporation Derivati kinazolina, ki modulirajo JAK-kinazo, in njihova uporaba v postopkih
CA2755095A1 (en) * 2009-03-09 2010-09-16 Surface Logix, Inc. Rho kinase inhibitors
US8492397B2 (en) 2009-03-23 2013-07-23 Vertex Pharmaceuticals Incorporated Aminopyridine derivatives having Aurora A selective inhibitory action
EP2411011A4 (de) * 2009-03-24 2012-08-15 Msd Kk Neue aminopyridinderivate mit selektiver aurora-a-hemmung
CA2755810A1 (en) * 2009-03-24 2010-09-30 Msd K.K. Novel aminopyridine derivatives having aurora a selective inhibitory action
US8211901B2 (en) 2009-05-22 2012-07-03 Shenzhen Chipscreen Biosciences Ltd. Naphthamide derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors
CN101906076B (zh) 2009-06-04 2013-03-13 深圳微芯生物科技有限责任公司 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用
AU2010259002B2 (en) * 2009-06-08 2014-03-20 Nantbio, Inc. Triazine derivatives and their therapeutical applications
US20120202818A1 (en) * 2009-06-09 2012-08-09 California Capital Equity, Llc Ureidophenyl substituted triazine derivatives and their therapeutical applications
EP2440057A4 (de) 2009-06-09 2012-12-05 California Capital Equity Llc Triazinderivate und deren therapeutische anwendungen
US20100331305A1 (en) * 2009-06-24 2010-12-30 Genentech, Inc. Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
TWI468402B (zh) * 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β-類澱粉生成之化合物
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
US20110053916A1 (en) 2009-08-14 2011-03-03 Vertex Pharmaceuticals Incorporated Pyrimidine compounds as tuberculosis inhibitors
CN102020657A (zh) * 2009-09-11 2011-04-20 上海艾力斯医药科技有限公司 稠合杂芳基衍生物、制备方法及其应用
CA2778686C (en) 2009-11-12 2015-07-21 F. Hoffmann-La Roche Ag N-9-substituted purine compounds, compositions and methods of use
EP2499143B1 (de) 2009-11-12 2016-03-16 F.Hoffmann-La Roche Ag N7-substituierte purin und pyrazolopyrimidin verbindungen, zusammensetzungen und verfahren zu ihrer verwendung
BR112012020273A8 (pt) 2010-02-11 2017-12-26 Univ Vanderbilt compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica
WO2011127241A2 (en) 2010-04-07 2011-10-13 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof
AU2011254550B2 (en) 2010-05-21 2013-11-07 Noviga Research Ab Novel pyrimidine derivatives
SI2576541T1 (sl) 2010-06-04 2016-07-29 F. Hoffmann-La Roche Ag Aminopirimidinski derivati kot modulatorji lrrk2
US20110319409A1 (en) * 2010-06-23 2011-12-29 Cox Christopher D 7-aza-quinazoline pde10 inhibitors
MX2013002384A (es) 2010-09-01 2013-07-05 Ambit Biosciences Corp Compuestos quinazolina y metodos para utilizarlos.
US9266855B2 (en) 2010-09-27 2016-02-23 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
RS59106B1 (sr) 2010-11-10 2019-09-30 Genentech Inc Derivati pirazol aminopirimidina kao lrrk2 modulatori
CN104906103B (zh) 2010-12-14 2018-05-18 电泳有限公司 酪蛋白激酶1δ(CK1δ)抑制剂
WO2012085815A1 (en) 2010-12-21 2012-06-28 Novartis Ag Bi-heteroaryl compounds as vps34 inhibitors
US9090592B2 (en) 2010-12-30 2015-07-28 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
US9481670B2 (en) * 2011-01-25 2016-11-01 Sphaera Pharma Pte. Ltd. Triazine compounds
BR112013024378A2 (pt) 2011-03-24 2016-12-13 Chemilia Ab novos derivados de pirimidina
EP2694073B1 (de) 2011-04-01 2018-08-08 Genentech, Inc. Kombinationen aus akt- und mek-hemmer zur behandlung von krebs
AU2012236138A1 (en) 2011-04-01 2013-11-14 Genentech, Inc. Combinations of AKT inhibitor compounds and erlotinib, and methods of use
RU2477723C2 (ru) 2011-06-16 2013-03-20 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе
JP6027610B2 (ja) 2011-07-19 2016-11-16 インフィニティー ファーマシューティカルズ, インコーポレイテッド 複素環式化合物及びその使用
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
CA2844729A1 (en) 2011-08-25 2013-02-28 F. Hoffmann-La Roche Ag Serine/threonine pak1 inhibitors
RU2627693C2 (ru) 2011-09-14 2017-08-10 СЭМЬЮМЕД, ЭлЭлСи ИНДАЗОЛ-3-КАРБОКСАМИДЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ СИГНАЛЬНОГО ПУТИ WNT/b-КАТЕНИНА
KR20140059246A (ko) 2011-09-22 2014-05-15 화이자 인코포레이티드 피롤로피리미딘 및 퓨린 유도체
CU24269B1 (es) 2011-09-27 2017-08-08 Novartis Ag 3- pirimidin- 4-il- oxazolidin- 2- onas inhibidores de la idh mutante
CA2854248A1 (en) 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag 2,4-diamine-pyrimidine derivative as serine/threonine kinase inhibitors
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
WO2013138613A1 (en) * 2012-03-16 2013-09-19 Axikin Pharmaceuticals, Inc. 3,5-diaminopyrazole kinase inhibitors
WO2013140148A1 (en) * 2012-03-19 2013-09-26 Imperial Innovations Limited Quinazoline compounds and their use in therapy
US20130303519A1 (en) 2012-03-20 2013-11-14 Millennium Pharmaceuticals, Inc. Methods of treating cancer using aurora kinase inhibitors
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
PT2841428T (pt) 2012-04-24 2018-11-29 Vertex Pharma Inibidores de adn-pk
CN106279202A (zh) * 2012-05-03 2017-01-04 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂用于治疗帕金森病的吡唑氨基嘧啶衍生物
CN106220615A (zh) * 2012-05-03 2016-12-14 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂的吡唑氨基嘧啶衍生物
WO2014004376A2 (en) 2012-06-26 2014-01-03 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
KR102215272B1 (ko) * 2012-09-28 2021-02-15 이그니타, 인코포레이티드 비정형 단백질 키나제 c의 아자퀴나졸린 억제제
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
DK2909181T3 (da) * 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
WO2014081718A1 (en) * 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
KR102275676B1 (ko) 2012-11-21 2021-07-12 피티씨 테라퓨틱스, 인크. 치환된 리버스 피리미딘 bmi-1 저해제
CN103012428A (zh) 2013-01-08 2013-04-03 中国药科大学 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途
WO2014110086A2 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
EP2951170B1 (de) 2013-02-04 2018-10-24 Janssen Pharmaceutica NV Flap-modulatoren
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Flap調節劑
EP2769722A1 (de) * 2013-02-22 2014-08-27 Ruprecht-Karls-Universität Heidelberg Verbindungen zur Verwendung bei der Hemmung einer HIV-Kapsid-Anordnung
JO3377B1 (ar) * 2013-03-11 2019-03-13 Takeda Pharmaceuticals Co مشتقات بيريدينيل وبيريدينيل مندمج
US9340557B2 (en) 2013-03-12 2016-05-17 Vertex Pharmaceuticals Incorporated Substituted quinoxaline DNA-PK inhibitors
EA028033B1 (ru) 2013-03-14 2017-09-29 Новартис Аг 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантного idh
JP6360881B2 (ja) 2013-03-22 2018-07-18 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. 触媒的mtorc1/2阻害薬及びオーロラaキナーゼの選択的阻害薬の組合せ
CA2928568A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Combinatorial methods to improve the therapeutic benefit of bisantrene
EP3039015B1 (de) 2013-08-30 2019-10-30 PTC Therapeutics, Inc. Substituierte pyrimidin-bmi-1 inhibitoren
WO2015028848A1 (en) * 2013-09-02 2015-03-05 Piramal Enterprises Limited Bicyclic heterocyclic compounds as multi-kinase inhibitors
EA032196B1 (ru) 2013-10-03 2019-04-30 Кура Онколоджи, Инк. Ингибиторы erk и способы применения
CN104903312B (zh) 2013-10-07 2019-01-29 卡德门企业有限公司 Rho激酶抑制剂
LT3424920T (lt) 2013-10-17 2020-08-10 Vertex Pharmaceuticals Incorporated (s)-n-metil-8-(1-((2`-metil-[4,5`-bipirimidin]-6-il)amino)propan-2-il)chinolin-4-karboksamido ir jo deuterintų darinių, kaip dnr-pk inhibitorių, bendri kristalai
NZ720958A (en) 2013-11-12 2022-02-25 Vertex Pharma Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases
US9975878B2 (en) 2013-11-21 2018-05-22 Ptc Therapeutics, Inc. Substituted triazine BMI-1 inhibitors
EP3071553A4 (de) * 2013-11-21 2017-08-02 PTC Therapeutics, Inc. Substituierte pyridin- und pyrazin-bmi-1-hemmer
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
CN104672250B (zh) * 2013-11-29 2017-11-07 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
CN109045032A (zh) 2014-01-01 2018-12-21 麦迪威森技术有限责任公司 氨基吡啶类化合物和使用方法
WO2015112739A1 (en) * 2014-01-22 2015-07-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Compounds and method for treating parp1-deficient cancers
CN104926795B (zh) * 2014-03-17 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
TWI675836B (zh) * 2014-03-25 2019-11-01 美商伊格尼塔公司 非典型蛋白質激酶c之氮雜喹唑啉抑制劑
US20170165230A1 (en) 2014-04-09 2017-06-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
CN105367555B (zh) * 2014-08-07 2019-06-25 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
BR112017010406B1 (pt) 2014-11-18 2021-03-09 Vertex Pharmaceuticals Incorporated processo de realização de teste de alta produtividade de cromatografia líquida de alta eficiência
TWI704151B (zh) * 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
US9879029B2 (en) * 2014-12-22 2018-01-30 Eli Lilly And Company ERK inhibitors
US10227343B2 (en) 2015-01-30 2019-03-12 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
EP3070084A1 (de) * 2015-03-18 2016-09-21 Rottapharm Biotech S.r.l. Neue fyn-kinase-inhibitoren
US10752612B2 (en) 2015-04-17 2020-08-25 Ludwig Institute For Cancer Research Ltd PLK4 inhibitors
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
WO2017023984A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024025A1 (en) 2015-08-03 2017-02-09 Sunil Kumar Kc 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024015A1 (en) * 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023987A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023975A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10206909B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023996A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023988A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023980A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10544139B2 (en) 2015-11-06 2020-01-28 Samumed, Llc Treatment of osteoarthritis
GB201604647D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
KR20190062485A (ko) 2016-09-27 2019-06-05 버텍스 파마슈티칼스 인코포레이티드 Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법
JP2019535672A (ja) 2016-10-21 2019-12-12 サミュメッド リミテッド ライアビリティ カンパニー インダゾール−3−カルボキサミドの使用方法およびwnt/β−カテニンシグナル伝達経路阻害剤としてのそれらの使用
EP3534888B1 (de) * 2016-11-01 2022-04-06 Merck Sharp & Dohme Corp. Substituierte bicyclische heteroaryl-allosterische modulatoren von nikotinischen acetylcholin-rezeptoren
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
IT201700047189A1 (it) * 2017-05-02 2018-11-02 Fondazione St Italiano Tecnologia Composti e composizioni per il trattamento di cancro, disordini della retina e cardiomiopatie
AR112027A1 (es) * 2017-06-15 2019-09-11 Biocryst Pharm Inc Inhibidores de alk 2 quinasa que contienen imidazol
CN110582491B (zh) 2017-06-30 2023-09-29 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
JP7311228B2 (ja) 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Rho-関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
KR102563325B1 (ko) * 2017-06-30 2023-08-03 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Rho-관련 단백질 키나아제 억제제, Rho-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
CN109384774B (zh) * 2017-08-11 2023-02-17 中国科学院上海药物研究所 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用
US10308646B2 (en) 2017-10-27 2019-06-04 Theravance Biopharma R&D Ip, Llc Pyrimidine compound as JAK kinase inhibitor
GB201801226D0 (en) 2018-01-25 2018-03-14 Redx Pharma Plc Modulators of Rho-associated protein kinase
WO2020005935A1 (en) * 2018-06-25 2020-01-02 Kadmon Corporation, Llc Glucose uptake inhibitors
KR102328682B1 (ko) * 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
WO2020045941A1 (ko) * 2018-08-27 2020-03-05 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
DK3902803T3 (da) 2018-12-27 2023-02-13 Servier Lab Aza-heterobicykliske inhibitorer af mat2a og anvendelsesfremgangsmåder til behandling af kræft
KR20210111787A (ko) 2019-01-03 2021-09-13 유니버시티 오브 피츠버그-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 전사 인자 eb 폴리펩티드 수준을 증가시키기 위한 방법 및 물질
WO2020163812A1 (en) 2019-02-08 2020-08-13 Frequency Therapeutics, Inc. Valproic acid compounds and wnt agonists for treating ear disorders
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
EP3941463A1 (de) 2019-03-22 2022-01-26 Sumitomo Dainippon Pharma Oncology, Inc. Zusammensetzungen mit pkm2-modulatoren und behandlungsverfahren damit
TW202102511A (zh) 2019-03-28 2021-01-16 大陸商江蘇恆瑞醫藥股份有限公司 噻吩并雜環類衍生物、其製備方法及其在醫藥上的應用
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
CN113544131B (zh) 2019-03-29 2024-03-15 江苏恒瑞医药股份有限公司 吡咯并杂环类衍生物、其制备方法及其在医药上的应用
CN109826608A (zh) * 2019-04-08 2019-05-31 中国科学院地质与地球物理研究所 一种分段压裂装置
AR118768A1 (es) 2019-04-24 2021-10-27 Theravance Biopharma R&D Ip Llc Derivados de pirimidina como inhibidores de las cinasas jak
WO2020219640A1 (en) 2019-04-24 2020-10-29 Theravance Biopharma R&D Ip, Llc Pyrimidine jak inhibitors for the treatment of skin diseases
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
EP3978498A1 (de) 2019-05-24 2022-04-06 Jiangsu Hengrui Medicine Co., Ltd. Substituierte kondensierte bicyclische derivate, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
MA56047A (fr) * 2019-05-29 2022-04-06 Ifm Due Inc Composés et compositions destinés au traitement d'états pathologiques associés à une activité de sting
CN116348458A (zh) 2019-08-14 2023-06-27 因赛特公司 作为cdk2抑制剂的咪唑基嘧啶基胺化合物
WO2021043966A1 (en) * 2019-09-06 2021-03-11 Inflazome Limited Nlrp3 inhibitors
EP4041399A1 (de) * 2019-10-02 2022-08-17 Tolremo Therapeutics AG Heterocyclische derivate, pharmazeutische zusammensetzungen und deren verwendung zur behandlung oder linderung von krebs
BR112022006977A2 (pt) 2019-10-11 2022-09-20 Incyte Corp Aminas bicíclicas como inibidores de cdk2
WO2021173082A1 (en) * 2020-02-26 2021-09-02 Jaguahr Therapeutics Pte Ltd Pyridopyrimidine derivatives useful in modulation of ahr signalling
JP2023533849A (ja) 2020-07-15 2023-08-04 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ Alk5阻害剤としてのピリダジニルアミノ誘導体
WO2022032484A1 (zh) * 2020-08-11 2022-02-17 北京诺诚健华医药科技有限公司 哒嗪-3-甲酰胺类化合物、其制备方法及其在医药学上的应用
TW202221001A (zh) 2020-09-29 2022-06-01 大陸商江蘇恒瑞醫藥股份有限公司 吡咯並雜環類衍生物的晶型及其製備方法
WO2022107919A1 (ko) * 2020-11-19 2022-05-27 주식회사 보로노이 N을 포함하는 헤테로아릴 유도체 및 이를 유효성분으로 포함하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
TW202317574A (zh) 2021-06-28 2023-05-01 美商纜圖藥品公司 Cdk2抑制劑
WO2023046698A1 (en) 2021-09-21 2023-03-30 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors
CN116023380B (zh) * 2021-10-26 2024-01-23 沈阳药科大学 一类吡唑并嘧啶衍生物及制备方法和应用
WO2023135107A1 (en) 2022-01-11 2023-07-20 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors

Family Cites Families (120)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) * 1964-05-12 J-aminoindazole derivatives
US665330A (en) * 1899-12-18 1901-01-01 Antoine J Langelier Machine for making blanks for sewing-machine needles or similar articles.
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
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
JP2657760B2 (ja) 1992-07-15 1997-09-24 小野薬品工業株式会社 4−アミノキナゾリン誘導体およびそれを含有する医薬品
ES2262137T3 (es) 1993-10-01 2006-11-16 Novartis Ag Derivados de pirimidinamina farmacologicamente activos y procedimientos para su preparacion.
CA2203517A1 (en) 1994-11-10 1996-05-23 Alan M. Laibelman Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
US5658902A (en) 1994-12-22 1997-08-19 Warner-Lambert Company Quinazolines as inhibitors of endothelin converting enzyme
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
CA2230896A1 (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
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
ES2186908T3 (es) 1996-07-13 2003-05-16 Glaxo Group Ltd Compuestos heterociciclos condensados como inhibidores de pproteina-tirosina-quinasas.
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
ES2239779T3 (es) 1996-10-02 2005-10-01 Novartis Ag Derivados de pirimidina y procedimientos para la preparacion de los mismos.
BR9712530A (pt) 1996-10-11 1999-10-19 Warner Lambert Co Inibidores de ésteres de asparato de enzima de conversão de interleucina-1beta
JP4439111B2 (ja) 1997-10-10 2010-03-24 サイトビア インコーポレイテッド ジペプチドのアポトーシスインヒビターおよびそれらの使用
DE19756388A1 (de) 1997-12-18 1999-06-24 Hoechst Marion Roussel De Gmbh Substituierte 2-Aryl-4-amino-chinazoline
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
ATE245641T1 (de) * 1998-02-17 2003-08-15 Tularik Inc Antivirale pyrimidinderivate
AU755273B2 (en) 1998-03-16 2002-12-05 Cytovia, Inc. Dipeptide caspase inhibitors and the use thereof
BR9911612A (pt) * 1998-06-02 2001-02-06 Osi Pharm Inc Composições de pirrolo[2,3d]pirimidina e seus usos
EP1087963B1 (de) 1998-06-19 2004-08-25 Chiron Corporation Glycogen synthase kinase 3 inhibitoren
EP1105394A1 (de) * 1998-08-21 2001-06-13 Du Pont Pharmaceuticals Company Isoxazolo[4,5-d]pyrimidine als crf antagonisten
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
BR9914326A (pt) * 1998-10-08 2001-06-26 Astrazeneca Ab Uso de um composto, composto, processo para a preparação do mesmo, composição farmacêutica, e, método para produzir um efeito antiangiogênico e/ou de redução da permeabilidade vascular em animais de sangue quente em necessidade de um tal tratamento
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
ATE302761T1 (de) 1999-01-13 2005-09-15 Warner Lambert Co 1-heterozyklus-substituierte diarylaminen
US6921748B1 (en) 1999-03-29 2005-07-26 Uutech Limited Analogs of gastric inhibitory polypeptide and their use for treatment of diabetes
AU766081B2 (en) 1999-03-30 2003-10-09 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
AU781849C (en) 1999-06-17 2006-03-02 Synta Pharmaceuticals Corp. Inhibitors of IL-12 production
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
JP2001042764A (ja) 1999-08-04 2001-02-16 Sony Corp 地図表示装置
BR0013551A (pt) 1999-08-13 2003-06-17 Vertex Pharma Inibidores de cinases n-terminal cjun (jnk) e outras cinases de proteìnas
AU770600B2 (en) 1999-10-07 2004-02-26 Amgen, Inc. Triazine kinase inhibitors
AP2002002530A0 (en) 1999-11-30 2002-06-30 Pfizer Prod Inc 2,4 diaminopyrimidine compounds useful as immunosuppressants.
CA2393179A1 (en) 1999-12-02 2001-06-07 Osi Pharmaceuticals, Inc. Compounds specific to adenosine a1 a2a, and a3 receptors and uses thereof
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
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
CA2394727A1 (en) 1999-12-28 2001-07-05 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
CN1362953A (zh) * 2000-02-05 2002-08-07 沃泰克斯药物股份有限公司 用作erk抑制剂的吡唑组合物
CN1429222A (zh) * 2000-02-17 2003-07-09 安姆根有限公司 激酶抑制剂
GB0004890D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
WO2001074768A2 (en) 2000-04-03 2001-10-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
JP2004501083A (ja) 2000-04-18 2004-01-15 アゴーロン・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を阻害するためのピラゾール
IL153246A0 (en) * 2000-06-28 2003-07-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
WO2002008244A2 (en) 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
EA200300205A1 (ru) 2000-08-31 2003-06-26 Пфайзер Продактс Инк. Производные пиразола и их применение в качестве ингибиторов протеинкиназы
CA2422376A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Isoxazoles and their use as inhibitors of erk
US7473691B2 (en) * 2000-09-15 2009-01-06 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
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
ES2242771T5 (es) * 2000-09-15 2011-10-14 Vertex Pharmaceuticals Incorporated Compuestos de pirazol útiles como inhibidores de proteína quinasas.
EP1318984A1 (de) 2000-09-20 2003-06-18 MERCK PATENT GmbH 4-amino-chinazoline
WO2002047690A1 (en) 2000-12-12 2002-06-20 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the 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)
ATE327989T1 (de) * 2000-12-21 2006-06-15 Vertex Pharma Pyrazolverbindungen als protein-kinase- inhibitoren
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
MXPA03008888A (es) * 2001-03-29 2005-03-07 Vertex Pharma Inhibidores de n-terminal c-jun cinasas (jnk) y otras proteinas cinasas.
ATE339416T1 (de) * 2001-04-13 2006-10-15 Vertex Pharma Inhibitoren von c-jun-n-terminalen-kinasen (jnk) und anderen proteinkinasen
EP1383771A1 (de) * 2001-04-20 2004-01-28 Vertex Pharmaceuticals Incorporated 9-deazaguaninderivate als gsk-3 inhibitoren
EP1404669A2 (de) * 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclisch substituierte pyrazole als inhibitoren von src und anderen protein kinasen
US6762179B2 (en) * 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
ES2274035T3 (es) * 2001-06-01 2007-05-16 Vertex Pharmaceuticals Incorporated Compuestos de tiazol utiles como inhibidores de proteina quinasas.
MXPA03011652A (es) * 2001-06-15 2004-05-31 Vertex Pharma 5-(2-aminopirimidin-4-il) benzioxazoles como inhibidores de proteinas cinasa.
DE60214198T2 (de) * 2001-07-03 2007-08-09 Vertex Pharmaceuticals Inc., Cambridge Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen
WO2003011287A1 (en) * 2001-08-03 2003-02-13 Vertex Pharmaceuticals Incorporated Pyrazolon derivatives as inhibitors of gsk-3
CA2469316A1 (en) * 2001-12-07 2003-06-19 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as gsk-3 inhibitors
EP2322521B1 (de) * 2002-02-06 2013-09-04 Vertex Pharmaceuticals, Inc. Heteroaryl-Verbindungen und Ihre Anwendung als GSK-3-Hemmer
US7863282B2 (en) 2003-03-14 2011-01-04 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2003220300A1 (en) * 2002-03-15 2003-09-29 Binch, Hayley Compositions useful as inhibitors of protein kinases
DE60332604D1 (de) 2002-03-15 2010-07-01 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
EP1485100B1 (de) * 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azolylaminoazine als proteinkinasehemmer
US7179826B2 (en) * 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
EP1506189A1 (de) * 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrol-derivate als inhibitoren von erk2 und deren verwendung
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
AU2003247959B2 (en) * 2002-07-09 2010-07-29 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
KR20050032105A (ko) 2002-08-02 2005-04-06 버텍스 파마슈티칼스 인코포레이티드 Gsk-3의 억제제로서 유용한 피라졸 조성물
JP4688498B2 (ja) * 2002-11-04 2011-05-25 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 Jakインヒビターとしてのヘテロアリール−ピリミジン誘導体
JP2006518381A (ja) * 2003-02-07 2006-08-10 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のインヒビターとして有用なヘテロアリール置換ピロール
ATE396731T1 (de) * 2003-03-25 2008-06-15 Vertex Pharma Thiazole zur verwendung als inhibitoren von protein-kinasen
WO2004087698A2 (en) * 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
US7579349B2 (en) 2003-10-17 2009-08-25 Astrazeneca Ab 4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer
JP4329649B2 (ja) 2004-08-30 2009-09-09 ソニー株式会社 撮像装置及び光学系の駆動方法
CA2619517A1 (en) 2005-08-18 2007-02-22 Michael Mortimore Pyrazine kinase inhibitors
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
BRPI0616630B8 (pt) 2005-09-30 2021-05-25 Miikana Therapeutics Inc compostos de pirazol substituídos
RU2423361C2 (ru) 2005-11-03 2011-07-10 Вертекс Фармасьютикалз Инкорпорейтед Аминопиримидины в качестве ингибиторов киназ
WO2007059299A1 (en) 2005-11-16 2007-05-24 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2008057940A1 (en) 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
JP2010513567A (ja) 2006-12-19 2010-04-30 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の阻害剤として有用なアミノピリミジン
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
EP2137183B1 (de) 2007-03-09 2011-09-28 Vertex Pharmaceuticals Incorporated Als inhibitoren von proteinkinasen geeignete aminopyrimidine
NZ579446A (en) 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
AU2008228963A1 (en) 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
EP2148931A2 (de) 2007-04-17 2010-02-03 Vertex Pharmaceuticals Incorporated Wirkstoffentdeckungsverfahren für aurora-kinase-inhibitoren
MX2009011810A (es) 2007-05-02 2010-01-14 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
EP2152696B1 (de) 2007-05-02 2014-09-24 Vertex Pharmaceuticals Incorporated Aminopyrimidine als kinasehemmer
AU2008247595A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
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

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