ATE346064T1 - Pyrazolverbindungen als protein-kinasehemmer - Google Patents

Pyrazolverbindungen als protein-kinasehemmer

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Publication number
ATE346064T1
ATE346064T1 AT01975210T AT01975210T ATE346064T1 AT E346064 T1 ATE346064 T1 AT E346064T1 AT 01975210 T AT01975210 T AT 01975210T AT 01975210 T AT01975210 T AT 01975210T AT E346064 T1 ATE346064 T1 AT E346064T1
Authority
AT
Austria
Prior art keywords
protein kinase
kinase inhibitors
pyrazole compounds
pyrazole
compounds
Prior art date
Application number
AT01975210T
Other languages
English (en)
Inventor
Robert Davies
David Bebbington
Haley Binch
Ronald Knegtel
Julian M C Golec
Sanjay Patel
Jean-Damien Vertex Ph Charrier
David Kay
Original Assignee
Vertex Pharma
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=ATE346064(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE346064T1 publication Critical patent/ATE346064T1/de

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    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • 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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    • 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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    • 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

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  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
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  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
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AT01975210T 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer ATE346064T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23279500P 2000-09-15 2000-09-15
US25788700P 2000-12-21 2000-12-21
US28694901P 2001-04-27 2001-04-27

Publications (1)

Publication Number Publication Date
ATE346064T1 true ATE346064T1 (de) 2006-12-15

Family

ID=27398347

Family Applications (8)

Application Number Title Priority Date Filing Date
AT01970969T ATE326458T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01977779T ATE326459T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01977783T ATE363284T1 (de) 2000-09-15 2001-09-14 Triazol-verbindungen als protein-kinase- inhibitoren
AT01971006T ATE294797T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01971082T ATE327992T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01973050T ATE327991T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01975210T ATE346064T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01970971T ATE327990T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer

Family Applications Before (6)

Application Number Title Priority Date Filing Date
AT01970969T ATE326458T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01977779T ATE326459T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01977783T ATE363284T1 (de) 2000-09-15 2001-09-14 Triazol-verbindungen als protein-kinase- inhibitoren
AT01971006T ATE294797T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01971082T ATE327992T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer
AT01973050T ATE327991T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer

Family Applications After (1)

Application Number Title Priority Date Filing Date
AT01970971T ATE327990T1 (de) 2000-09-15 2001-09-14 Pyrazolverbindungen als protein-kinasehemmer

Country Status (24)

Country Link
US (7) US7115739B2 (de)
EP (8) EP1317452B1 (de)
JP (9) JP2004509115A (de)
KR (4) KR20030030005A (de)
CN (3) CN100355750C (de)
AP (1) AP2003002762A0 (de)
AT (8) ATE326458T1 (de)
AU (9) AU2001291013A1 (de)
BR (1) BR0114088A (de)
CA (8) CA2422378C (de)
DE (8) DE60128709T2 (de)
DK (1) DK1318997T3 (de)
ES (3) ES2266258T3 (de)
HK (8) HK1057543A1 (de)
HU (4) HUP0302411A2 (de)
IL (6) IL154786A0 (de)
MX (8) MXPA03002297A (de)
NO (4) NO327708B1 (de)
NZ (4) NZ525014A (de)
PE (1) PE20020451A1 (de)
PL (1) PL361676A1 (de)
PT (2) PT1318997E (de)
TW (1) TWI303636B (de)
WO (8) WO2002022602A2 (de)

Families Citing this family (400)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1577816A3 (de) * 1996-09-04 2006-08-02 Intertrust Technologies Corp. Vertrauenswürdige Infrastrukturbetreuungssysteme, Verfahren und Techniken zum sicheren elektronischen Handel und zur 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
KR100755622B1 (ko) 1999-12-24 2007-09-04 아벤티스 파마 리미티드 아자인돌
US7115739B2 (en) * 2000-09-15 2006-10-03 Vertex Pharmaceuticals Incorporated Triazole compounds useful as protein kinase inhibitors
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
WO2002050073A1 (en) * 2000-12-19 2002-06-27 Smithkline Beecham P.L.C. Pyrazolo[3,4-c]pyridines as gsk-3 inhibitors
MXPA03005609A (es) * 2000-12-21 2003-10-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de la proteina cinasa.
WO2002059110A1 (en) * 2000-12-21 2002-08-01 Glaxo Group Limited Pyrimidineamines as angiogenesis modulators
US7276523B2 (en) 2001-03-30 2007-10-02 Smithkline Beecham Corporation Aminopyridine derivatives as estrogen receptor modulators
CA2446864C (en) * 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
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
US20030176437A1 (en) 2001-08-31 2003-09-18 D.M. Watterson Anti-inflammatory and protein kinase inhibitor compositions and related methods for downregulation of detrimental cellular responses and inhibition of cell death
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
CA2460145C (en) 2001-09-26 2011-04-26 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
TWI330183B (de) * 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
MXPA04005510A (es) 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
AU2002357164A1 (en) 2001-12-17 2003-06-30 Smithkline Beecham Corporation Pyrazolopyridazine derivatives
US20030158195A1 (en) * 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
WO2003055866A1 (en) * 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
RS63204A (en) 2002-01-17 2006-10-27 Neurogen Corporation Substituted quinazolin-4-ylamine analogues as modulators of capsaicin
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
PL372198A1 (en) * 2002-02-06 2005-07-11 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
ATE433973T1 (de) 2002-03-15 2009-07-15 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
AU2003218215A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
DE60332433D1 (de) 2002-03-15 2010-06-17 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
PL372963A1 (en) * 2002-04-05 2005-08-08 Boehringer Ingelheim Pharma Gmb & Co.Kg Method of treating mucus hypersecretion
ES2340475T3 (es) 2002-05-01 2010-06-04 Vertex Pharmaceuticals Incorporated Estructura cristalizada de proteina aurora-2 y sus bolsillos de union.
ES2355472T3 (es) 2002-05-22 2011-03-28 Amgen Inc. Derivados de aminopirimidina para su uso como ligandos del receptor vaniloide para el tratamiento del dolor.
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
AU2003251721A1 (en) 2002-06-14 2003-12-31 Laboratoires Serono Sa 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
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
JP2006501191A (ja) * 2002-07-17 2006-01-12 ファルマシア・イタリア・エス・ピー・エー キナーゼ阻害剤としてのヘテロ二環式ピラゾール誘導体
CA2494367A1 (en) * 2002-07-25 2004-02-05 Scios Inc. Methods for improvement of lung function using tgf-.beta. inhibitors
JP2006514989A (ja) 2002-07-29 2006-05-18 ライジェル ファーマシューティカルズ 2,4−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法
SI1532145T1 (sl) * 2002-08-02 2007-02-28 Vertex Pharma Pirazolni sestavki, koristni kot inhibitorji GSK-3
ATE339419T1 (de) * 2002-08-02 2006-10-15 Vertex Pharma Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
CA2495285A1 (en) * 2002-08-13 2004-02-19 Merck Sharp & Dohme Limited Phenylpyridazine derivatives as ligands for gaba receptors
AU2003262642B2 (en) * 2002-08-14 2010-06-17 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
AU2003278249B8 (en) 2002-09-05 2010-11-18 Aventis Pharma S.A. Novel aminoindazole derivatives as medicines and pharmaceutical compositions containing same
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
RU2005110656A (ru) * 2002-09-10 2006-01-20 Сайос Инк. (Us) Ингибиторы tgf
EP1562911B1 (de) 2002-11-01 2010-01-06 Vertex Pharmaceuticals Incorporated Verbindungen, die sich als inhibitoren vonjak und anderen proteinkinasen eignen
WO2004041810A1 (en) 2002-11-05 2004-05-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
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
US7423148B2 (en) * 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
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
PL376789A1 (pl) 2002-12-12 2006-01-09 Aventis Pharma S.A. Pochodne aminoindazoli i ich zastosowanie jako inhibitorów kinazy
JP2006515847A (ja) 2002-12-13 2006-06-08 ニューロジェン・コーポレーション カプサイシン受容体調節剤としてのカルボン酸、ホスフェート又はホスホネート置換キナゾリン−4−イルアミン類縁体
WO2004072029A2 (en) * 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
US7157455B2 (en) * 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
JP2006521398A (ja) * 2003-03-28 2006-09-21 サイオス・インコーポレーテツド TGFβの二−環式ピリミジン阻害剤
CA2520323C (en) * 2003-04-09 2013-07-09 Exelixis, Inc. Tie-2 modulators and methods of use
WO2004096130A2 (en) * 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
WO2004096808A1 (en) * 2003-04-28 2004-11-11 De Novo Pharmaceuticals Limited Triazine compounds and their use
AU2004260636A1 (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
CA2528774A1 (en) * 2003-06-20 2005-01-27 Coley Pharmaceutical Gmbh Small molecule toll-like receptor (tlr) antagonists
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
WO2005012256A1 (en) 2003-07-22 2005-02-10 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
AU2004265288A1 (en) 2003-07-30 2005-02-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
AR045445A1 (es) * 2003-08-05 2005-10-26 Vertex Pharma Compuestos ihinibidores de canales ionicos regulados por voltaje
JP4889489B2 (ja) * 2003-08-06 2012-03-07 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アミノトリアゾール化合物
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
KR20060123164A (ko) 2003-10-17 2006-12-01 아스트라제네카 아베 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체
EP1687004A4 (de) 2003-11-10 2009-04-08 Synta Pharmaceuticals Corp Pyridin-verbindungen
US8455489B2 (en) * 2003-11-10 2013-06-04 Exelixis, Inc. Substituted pyrimidine compositions and methods of use
CN1890218B (zh) 2003-12-03 2011-08-03 Ym生物科学澳大利亚私人有限公司 微管蛋白抑制剂
US7592340B2 (en) * 2003-12-04 2009-09-22 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
KR20060123452A (ko) * 2003-12-09 2006-12-01 버텍스 파마슈티칼스 인코포레이티드 나프티리딘 유도체 및 무스카린 수용체의 조절자로서의이의 용도
WO2005061519A1 (en) * 2003-12-19 2005-07-07 Takeda San Diego, Inc. Kinase inhibitors
TW200530235A (en) 2003-12-24 2005-09-16 Renovis Inc Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
US7626030B2 (en) 2004-01-23 2009-12-01 Amgen Inc. Compounds and methods of use
TW200536851A (en) 2004-01-23 2005-11-16 Amgen Inc Compounds and methods of use
EP1745034A1 (de) 2004-02-11 2007-01-24 Amgen Inc. Vanilloidrezeptorliganden und deren verwendung bei behandlungen
CA2561718A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyridines as potassium ion channel modulators
WO2005105788A1 (en) * 2004-04-23 2005-11-10 Takeda San Diego, Inc. Indole derivatives and use thereof as kinase inhibitors
US7793137B2 (en) 2004-10-07 2010-09-07 Cisco Technology, Inc. Redundant power and data in a wired data telecommunincations network
RS50568B8 (sr) * 2004-05-14 2019-08-30 Millennium Pharm Inc Jedinjenja i postupci za inhibiciju mitotičke progresije inhibiranjem aurora kinaze
EP1598348A1 (de) * 2004-05-18 2005-11-23 Aventis Pharma Deutschland GmbH Pyridazinonderivate als CDK2-Inhibitoren
EP1604988A1 (de) * 2004-05-18 2005-12-14 Sanofi-Aventis Deutschland GmbH Pyridazinonderivate, Methoden, um selbige herzustellen, und ihre Verwendung als Pharmazeutika
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
WO2006012624A2 (en) * 2004-07-21 2006-02-02 The Regents Of The University Of California Mechanism-based crosslinkers
EP1778669A2 (de) 2004-08-18 2007-05-02 Takeda San Diego, Inc. Kinase-inhibitoren
DE602005027081D1 (de) 2004-08-19 2011-05-05 Dsm Ip Assets Bv Verfahren zur rektifikation von vitamin e acetat
GB0419416D0 (en) * 2004-09-01 2004-10-06 Inst Of Ex Botany Ascr 4-Arylazo-3,5-Diamino-Pyrazole compounds and use thereof
AU2005284904A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
CA2581623A1 (en) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyridine compounds, process for their preparation and compositions containing them
AR050948A1 (es) 2004-09-24 2006-12-06 Hoffmann La Roche Derivados de ftalazinona; su obtencion y su utilizacion en la fabricacion de medicamentos para el tratamiento del cancer.
US7285569B2 (en) 2004-09-24 2007-10-23 Hoff Hoffmann-La Roche Inc. Tricycles, their manufacture and use as pharmaceutical agents
BRPI0516751A (pt) 2004-09-30 2008-09-16 Tibotec Pharm Ltd pirimidinas bicìclicas que inibem hcv
TW200621251A (en) 2004-10-12 2006-07-01 Neurogen Corp Substituted biaryl quinolin-4-ylamine analogues
ATE479687T1 (de) 2004-10-15 2010-09-15 Takeda Pharmaceutical Kinaseinhibitoren
TW200621257A (en) * 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
ES2543813T3 (es) 2004-11-02 2015-08-24 Northwestern University Compuestos de piridazina para el tratamiento de enfermedades inflamatorias
JP2008518955A (ja) 2004-11-02 2008-06-05 ノースウェスタン ユニバーシティ ピリダジン化合物および方法
AU2005306458B2 (en) * 2004-11-17 2011-02-17 Miikana Therapeutics, Inc. Kinase inhibitors
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
JP2008521900A (ja) 2004-11-30 2008-06-26 アムジエン・インコーポレーテツド キノリン及びキナゾリン類似体並びにがん治療のための医薬としてのその使用
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
WO2006067614A2 (en) * 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
ATE519759T1 (de) * 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
NZ555947A (en) 2005-01-19 2010-11-26 Rigel Pharmaceuticals Inc Prodrugs of 2,4-pyrimidinediamine compounds and their uses
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.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
CA2595514C (en) * 2005-01-26 2012-06-12 Schering Corporation Kinase inhibitors
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
MX2007009437A (es) 2005-02-04 2007-08-16 Astrazeneca Ab Derivados de pirazolilaminopiridina utiles como inhibidores de cinasa.
ES2308731T3 (es) * 2005-02-16 2008-12-01 Astrazeneca Ab Compuestos quimicos.
WO2006100461A1 (en) * 2005-03-23 2006-09-28 Astrazeneca Ab 2-AZETIDINYL-4-(lH-PYRAZOL-3-YLAMINO)PYRIMIDINES AS INHIBITORS OF INSULIN-LIKE GROWTH FACTOR-I RECEPTOR ACTIVITY
US7297700B2 (en) 2005-03-24 2007-11-20 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
EP1869037B1 (de) 2005-03-25 2011-07-27 Tibotec Pharmaceuticals Heterobicyclische inhibitoren von hvc
DE602006002271D1 (de) * 2005-04-05 2008-09-25 Astrazeneca Ab Pyrimidinderivate zur verwendung als antikrebsmittel
GB0507347D0 (en) * 2005-04-12 2005-05-18 Astrazeneca Ab Chemical compounds
AU2006233537A1 (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
AU2006241825A1 (en) 2005-04-28 2006-11-09 Mitsubishi Tanabe Pharma Corporation Cyanopyridine derivative and use thereof as medicine
EP1885454A2 (de) 2005-05-04 2008-02-13 DeveloGen Aktiengesellschaft Verwendung von gsk-3-hemmern zur prävention und behandlung von pankreatischen autoimmunkrankheiten
CA2606760C (en) 2005-05-04 2014-12-23 Renovis, Inc. Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and disfunctions
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
KR20080015409A (ko) 2005-05-16 2008-02-19 아스트라제네카 아베 티로신 키나제 억제제로서 유용한 피라졸릴아미노피리미딘 유도체
CA2612788A1 (en) 2005-06-24 2006-12-28 Steven Cesar Alfons De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c
ES2270715B1 (es) 2005-07-29 2008-04-01 Laboratorios Almirall S.A. Nuevos derivados de pirazina.
US7737151B2 (en) * 2005-08-18 2010-06-15 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
EP1928437A2 (de) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenese mittels muscarinrezeptormodulation
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
WO2007041358A2 (en) 2005-09-30 2007-04-12 Miikana Therapeutics, Inc. Substituted pyrazole compounds
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
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
US7985756B2 (en) 2005-10-21 2011-07-26 Braincells Inc. Modulation of neurogenesis by PDE inhibition
AU2006307657B2 (en) * 2005-10-28 2010-10-28 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
NZ594385A (en) * 2005-11-03 2013-02-22 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
PL2395002T3 (pl) 2005-11-08 2015-04-30 Vertex Pharma Kompozycja farmaceutyczna zawierająca heterocykliczny modulator transporterów zawierających kasetę wiążącą ATP
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
KR101235103B1 (ko) 2006-01-17 2013-02-21 버텍스 파마슈티칼스 인코포레이티드 야누스 키나제의 억제제로서 유용한 아자인돌
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US7807672B2 (en) 2006-02-16 2010-10-05 Schering Corporation Compounds that are ERK inhibitors
US20070244143A1 (en) * 2006-03-08 2007-10-18 Braincells, Inc Modulation of neurogenesis by nootropic agents
US20100216734A1 (en) * 2006-03-08 2010-08-26 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
US7589214B2 (en) * 2006-04-11 2009-09-15 Vertex Pharmaceuticals Incorporated Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
EP2015750A2 (de) 2006-04-28 2009-01-21 Northwestern University Zusammensetzungen und behandlungen mit pyridazinverbindungen und cholisterinasehemmern
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
EP2026813A2 (de) * 2006-05-09 2009-02-25 Braincells, Inc. 5-ht-rezeptor-vermittelte neurogenese
EP2743268A3 (de) 2006-06-27 2014-10-08 Takeda Pharmaceutical Company Limited Kondensierte zyklische Verbindungen als GPR40 Modulatoren
CA2654852A1 (en) * 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
EP2043651A2 (de) * 2006-07-05 2009-04-08 Exelixis, Inc. Verfahren zur verwendung von igf1r und abl-kinase-modulatoren
UA95641C2 (en) * 2006-07-06 2011-08-25 Эррей Биофарма Инк. Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
SI2049500T1 (sl) 2006-07-06 2012-01-31 Array Biopharma Inc Ciklopenta (d) pirimidini kot AKT protein kinazni inhibitorji
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes 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
KR20090064418A (ko) 2006-09-08 2009-06-18 브레인셀즈 인코퍼레이션 4-아실아미노피리딘 유도체 포함 조합물
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
US20080103165A1 (en) * 2006-09-19 2008-05-01 Braincells, Inc. Ppar mediated modulation of neurogenesis
EP2223925A1 (de) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase-Inhibitoren
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
US8642598B2 (en) * 2006-10-21 2014-02-04 Abbvie Inc. Heterocyclic compounds and their use as glycogen synthase kinase 3 inhibitors
MX2009004807A (es) * 2006-11-02 2009-06-15 Vertex Pharma Aminopiridinas y aminopirimidinas utiles como inhibidores de proteina cinasa.
CA2673353A1 (en) * 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
US8637531B2 (en) 2006-12-26 2014-01-28 Gilead Sciences, Inc. Pyrido(3,2-d)pyridmidines 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
MX2009008341A (es) 2007-02-06 2009-08-12 Novartis Ag Inhibidores de cinasa de pi3 y metodos para su uso.
JP2010518064A (ja) * 2007-02-12 2010-05-27 メルク・シャープ・エンド・ドーム・コーポレイション Adおよび関連状態の治療のためのピペラジン誘導体
EP2120573A4 (de) * 2007-02-12 2011-05-25 Merck Sharp & Dohme Piperidinderivate
TW200901975A (en) 2007-03-05 2009-01-16 Kyowa Hakko Kogyo Kk Pharmaceutical composition
CA2679701A1 (en) * 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
RU2009137390A (ru) * 2007-03-09 2011-04-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Аминопиримидины, пригодные в качестве ингибиторов протеинкиназ
CA2679884A1 (en) * 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CN101679386A (zh) 2007-04-13 2010-03-24 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶类化合物
WO2008129255A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
AU2008247595A1 (en) * 2007-05-02 2008-11-13 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
CN101801959A (zh) * 2007-05-02 2010-08-11 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶类化合物
CN101687863B (zh) * 2007-05-04 2012-09-12 阿斯利康(瑞典)有限公司 氨基-噻唑基-嘧啶衍生物及其治疗癌症的用途
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
EP2164840A2 (de) 2007-05-09 2010-03-24 Vertex Pharmaceuticals Incorporated Modulatoren von cftr
MX2009012719A (es) * 2007-05-24 2010-02-04 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
EP2166849A4 (de) * 2007-06-11 2010-09-15 Miikana Therapeutics Inc Substituierte pyrazol-verbindungen
WO2008156580A1 (en) * 2007-06-13 2008-12-24 Merck & Co., Inc. Triazole derivatives for treating alzheimer's disease and related conditions
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
KR20150089099A (ko) * 2007-07-05 2015-08-04 어레이 바이오파마 인크. Akt 단백질 키나제 억제제로서의 피리미딜 시클로펜탄
AU2008272832B2 (en) * 2007-07-05 2014-02-20 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
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8415340B2 (en) 2007-07-25 2013-04-09 Bristol-Myers Squibb Company Triazine kinase inhibitors
WO2009018415A1 (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
TW200906818A (en) * 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
CN101952274A (zh) 2007-11-20 2011-01-19 默沙东公司 非核苷逆转录酶抑制剂
RS55298B1 (sr) 2007-12-07 2017-03-31 Vertex Pharma Proces za proizvodnju cikloalkilkarboksiamido-piridin benzoevih kiselina
LT2225230T (lt) 2007-12-07 2017-01-25 Vertex Pharmaceuticals Incorporated 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzoinės rūgšties kietos formos
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
CL2008003749A1 (es) 2007-12-17 2010-01-15 Janssen Pharmaceutica Nv Compuestos derivados de imidazol, oxazol, y tiazol pirimidina, moduladores de trpv1, proceso de preparacion, composicion farmaceutica y su uso en el tratamiento de enfermedades, trastornos o condicion de dolor, prurito, artritis, tos, asma, trastorno del oido interno y enfermedad inflamatoria intestinal, entre otras.
EP2250155B1 (de) * 2008-01-09 2013-07-03 Array Biopharma, Inc. 5h-cyclopenta[d]pyrimidine als akt-proteinkinase-inhibitoren
ES2403284T3 (es) * 2008-01-09 2013-05-17 Array Biopharma, Inc. Pirimidil ciclopentanos como inhibidores de la proteína quinasa AKT
BRPI0908120A8 (pt) 2008-02-21 2017-10-24 Schering Corp Compostos que são inibidores de erk, composição faramacêutica e uso
CA2716109C (en) 2008-02-28 2016-07-19 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as cftr modulators
WO2009145814A2 (en) * 2008-03-10 2009-12-03 Vertex Pharmaceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
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
MX353308B (es) 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
AR072085A1 (es) * 2008-06-11 2010-08-04 Astrazeneca Ab Compuestos triciclicos, metodos para su preparacion, composicion farma-ceutica que los comprende y su uso en el tratamiento de enfermedades me-diadas por la actividad de las proteinas quinasas
CA2727684C (en) 2008-06-12 2017-01-31 Janssen Pharmaceutica Nv Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h4 receptor
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
EA201100126A1 (ru) * 2008-07-03 2011-08-30 Мерк Патент Гмбх Нафтиридиноны в качестве ингибиторов протеинкиназ
AR073354A1 (es) * 2008-07-31 2010-11-03 Genentech Inc Compuestos de pirimidina, composiciones farmaceuticas y su uso en el tratamiento del cancer.
EP2312945A4 (de) * 2008-08-13 2012-05-09 Merck Sharp & Dohme Purinderivate zur behandlung von morbus alzheimer
RU2011112802A (ru) * 2008-09-03 2012-10-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Сокристаллы и содержащие их фармацевтические композиции
EP2340248B1 (de) * 2008-09-15 2017-05-31 The Regents of The University of California Verfahren und zusammensetzungen zur modulation der ire1-, src- und abl-aktivität
US20110201628A1 (en) * 2008-09-30 2011-08-18 Astrazeneca Ab Heterocyclic jak kinase inhibitors
WO2010059610A1 (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
MX2011008305A (es) 2009-02-05 2012-08-15 Takeda Pharmaceutical Compuestos de piridazinona.
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CN105601619A (zh) * 2009-02-27 2016-05-25 埃姆比特生物科学公司 调控jak激酶的喹唑啉衍生物和其使用方法
EP2406236A4 (de) * 2009-03-09 2013-07-24 Surface Logix Inc Rho-kinase-hemmer
JP2012521425A (ja) * 2009-03-23 2012-09-13 Msd株式会社 オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
CA2755810A1 (en) * 2009-03-24 2010-09-30 Msd K.K. Novel 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
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
CA2764785C (en) * 2009-06-08 2015-10-27 California Capital Equity, Llc Triazine derivatives and their therapeutical applications
CN102573481A (zh) * 2009-06-09 2012-07-11 加利福尼亚资本权益有限责任公司 脲基苯基取代的三嗪衍生物及其治疗应用
CN102573480B (zh) * 2009-06-09 2015-06-10 加利福尼亚资本权益有限责任公司 三嗪衍生物及其治疗应用
SG176959A1 (en) * 2009-06-24 2012-01-30 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
WO2011058027A2 (en) 2009-11-12 2011-05-19 F. Hoffmann-La Roche Ag N-9-substituted purine compounds, compositions and methods of use
ES2567168T3 (es) 2009-11-12 2016-04-20 F. Hoffmann-La Roche Ag Compuestos purina y pirazolopirimidina N7-sustituidos, composiciones y métodos de utilización
AU2011215638B2 (en) * 2010-02-11 2016-04-28 Vanderbilt University Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mGluR4 allosteric potentiators, compounds, and methods of treating neurological dysfunction
AU2011237601B2 (en) 2010-04-07 2015-08-20 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
US8927547B2 (en) 2010-05-21 2015-01-06 Noviga Research Ab Pyrimidine derivatives
US8354420B2 (en) 2010-06-04 2013-01-15 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 inhibitors
US20110319409A1 (en) * 2010-06-23 2011-12-29 Cox Christopher D 7-aza-quinazoline pde10 inhibitors
EP2611789A1 (de) 2010-09-01 2013-07-10 Ambit Biosciences Corporation Chinazolinverbindungen und anwendungsverfahren dafür
CA2810954A1 (en) 2010-09-27 2012-04-05 Abbott 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
AU2010363329A1 (en) 2010-11-07 2013-05-09 Targegen, Inc. Compositions and methods for treating myelofibrosis
ES2746134T3 (es) 2010-11-10 2020-03-04 Genentech Inc Derivados de pirazol aminopirimidina como moduladores de LRRK2
US20140018540A1 (en) 2010-12-14 2014-01-16 Electrophoretics Limited Casein kinase 1delta (ck 1delta) inhibitors
AU2011346567A1 (en) 2010-12-21 2013-07-25 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
JP5886411B2 (ja) 2011-03-24 2016-03-16 ノビガ・リサーチ・エービーNoviga Research AB 新規のピリミジン誘導体
KR102021157B1 (ko) 2011-04-01 2019-09-11 제넨테크, 인크. Akt 억제제 화합물 및 아비라테론의 조합물, 및 사용 방법
ES2688809T3 (es) 2011-04-01 2018-11-07 Genentech, Inc. Combinaciones de compuestos inhibidores de AKT y MEK para tratar el cáncer
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
EP2734520B1 (de) 2011-07-19 2016-09-14 Infinity Pharmaceuticals, Inc. Heterocyclische verbindungen und ihre verwendung
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
KR20140062079A (ko) 2011-08-25 2014-05-22 에프. 호프만-라 로슈 아게 세린/트레오닌 pak1 억제제
CA2848659C (en) 2011-09-14 2021-03-09 Samumed, Llc Indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
AU2012311184A1 (en) 2011-09-22 2014-03-06 Pfizer Inc. Pyrrolopyrimidine and purine derivatives
KR20140069235A (ko) 2011-09-27 2014-06-09 노파르티스 아게 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
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
US9365556B2 (en) * 2012-03-16 2016-06-14 Axikin Pharmaceuticals, Inc. 3,5-diaminopyrazole kinase inhibitors
EP2828250B1 (de) * 2012-03-19 2021-03-10 Imperial College Innovations Limited Chinazolin-verbindungen und ihre therapeutische verwendung
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
PT3459942T (pt) 2012-04-24 2021-03-26 Vertex Pharma Inibidores de adn-pk
WO2013164323A1 (en) * 2012-05-03 2013-11-07 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease
RU2637947C2 (ru) * 2012-05-03 2017-12-08 Дженентек, Инк. Производные пиразоламинопиримидина в качестве модуляторов обогащенной лейциновыми повторами киназы 2
AU2013280644B2 (en) 2012-06-26 2018-08-02 Jeffrey A. BACHA 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
EP2900666B1 (de) 2012-09-28 2020-11-04 Cancer Research Technology Limited Azaquinazolininhibitoren von atypischer proteinkinase c
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
JP6243918B2 (ja) 2012-10-16 2017-12-06 トレロ ファーマシューティカルズ, インコーポレイテッド Pkm2調節因子およびそれらの使用方法
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
CN104955824B (zh) * 2012-11-20 2017-09-22 豪夫迈·罗氏有限公司 作为含t790m的egfr突变体的抑制剂的氨基嘧啶化合物
PE20151413A1 (es) 2012-11-21 2015-10-23 Ptc Therapeutics Inc Inhibidores de bmi-1 de pirimidina inversa sustituida
MX370487B (es) 2013-01-08 2019-12-16 Samumed Llc Inhibidores de 3-(benzo-imidazol-2-il)-indazol de la senda de señalización de wnt y usos terapéuticos de los mismos.
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
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Flap調節劑
WO2014121055A2 (en) * 2013-02-04 2014-08-07 Janssen Pharmaceutica Nv Flap modulators
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
ME03336B (de) 2013-03-12 2019-10-20 Vertex Pharma Dna-pk-hemmer
CA2903979A1 (en) 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
CA2907726A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase
US9993460B2 (en) 2013-07-26 2018-06-12 Race Oncology Ltd. Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US10370371B2 (en) 2013-08-30 2019-08-06 Ptc Therapeutics, Inc. Substituted pyrimidine Bmi-1 inhibitors
WO2015028848A1 (en) * 2013-09-02 2015-03-05 Piramal Enterprises Limited Bicyclic heterocyclic compounds as multi-kinase inhibitors
HUE036600T2 (hu) 2013-10-03 2018-07-30 Kura Oncology Inc ERK inhibitorok és alkalmazási eljárások
ES2779152T3 (es) * 2013-10-07 2020-08-13 Kadmon Corporation Llc Derivados de (2-(5-isoindolin-2-il)pirimidin-4-il)-amina como inhibidores de Rho-quinasa para tratar enfermedades autoinmunes
HUE051275T2 (hu) 2013-10-17 2021-03-01 Vertex Pharma (S)-N-Metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propán-2-il)kinolin-4-karboxamid és deuterált származékainak kokristályai DNS-PK inhibitorokként
NZ720958A (en) 2013-11-12 2022-02-25 Vertex Pharma Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases
EP3071553A4 (de) 2013-11-21 2017-08-02 PTC Therapeutics, Inc. Substituierte pyridin- und pyrazin-bmi-1-hemmer
WO2015076801A1 (en) * 2013-11-21 2015-05-28 Ptc Therapeutics, Inc. Substituted triazine bmi-1 inhibitors
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
CN104926824B (zh) * 2014-03-17 2017-07-07 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
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
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
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
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
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
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
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
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
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
CN107110831B (zh) 2014-11-18 2020-02-21 弗特克斯药品有限公司 进行高通量试验高效液相色谱的方法
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
WO2016166604A1 (en) 2015-04-17 2016-10-20 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
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
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10329309B2 (en) 2015-08-03 2019-06-25 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-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
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]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
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]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
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
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
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
WO2017024004A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]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
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
WO2017023993A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
EP3371187A4 (de) 2015-11-06 2019-09-04 Samumed, LLC 2-(1h-indazol-3-yl)-3h-imidazo[4,5-c]pyridine und deren verwendung als entzündungshemmer
GB201604647D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
KR102477407B1 (ko) 2016-06-01 2022-12-13 사뮤메드, 엘엘씨 N-(5-(3-(7-(3-플루오로페닐)-3h-이미다조[4,5-c]피리딘-2-일)-1h-인다졸-5-일)피리딘-3-일)-3-메틸부탄아미드를 제조하기 위한 공정
EP3518931A4 (de) 2016-09-27 2020-05-13 Vertex Pharmaceuticals Incorporated Verfahren zur behandlung von krebs mit einer kombination aus dna-schädigenden substanzen und dna-pk-inhibitoren
BR112019008061A2 (pt) 2016-10-21 2019-09-17 Samumed Llc métodos de uso de indazol-3-carboxamidas e seu uso como inibidores da via de sinalização de wnt/b-catenina
JP7041141B2 (ja) * 2016-11-01 2022-03-23 メルク・シャープ・アンド・ドーム・コーポレーション 置換された二環式ヘテロアリール系ニコチン性アセチルコリン受容体アロステリック調節剤
MA46696A (fr) 2016-11-07 2019-09-11 Samumed Llc Formulations injectables à dose unique prêtes à l'emploi
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
WO2019000682A1 (zh) * 2017-06-30 2019-01-03 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
CA3063616A1 (en) 2017-06-30 2019-12-06 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
EP3421464B1 (de) 2017-06-30 2021-11-24 Beijing Tide Pharmaceutical Co., Ltd. Rho-assoziierte proteinkinasehemmer, pharmazeutische zusammensetzung damit sowie herstellungsverfahren und verwendung davon
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
EA202091016A1 (ru) 2017-10-27 2020-07-17 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Пиримидиновое соединение в качестве ингибитора jak киназы
GB201801226D0 (en) 2018-01-25 2018-03-14 Redx Pharma Plc Modulators of Rho-associated protein kinase
US12030857B2 (en) * 2018-06-25 2024-07-09 Kadmon Corporation, Llc Glucose uptake inhibitors
US12023335B2 (en) 2018-08-17 2024-07-02 Ptc Therapeutics, Inc. Method for treating pancreatic cancer
WO2020045941A1 (ko) * 2018-08-27 2020-03-05 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
KR102328682B1 (ko) * 2018-08-27 2021-11-18 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
GEP20237519B (en) 2018-12-27 2023-07-10 Servier Lab Aza-heterobicyclic inhibitors of mat2a and methods of use for treating cancer
SG11202105685TA (en) * 2019-01-03 2021-06-29 Univ Pittsburgh Commonwealth Sys Higher Education Methods and materials for increasing transcription factor eb polypeptide levels
AU2020218366A1 (en) 2019-02-08 2021-09-16 Frequency Therapeutics, Inc. Valproic acid compounds and Wnt agonists for treating ear disorders
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones 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
AU2020245437A1 (en) 2019-03-22 2021-09-30 Sumitomo Pharma Oncology, Inc. Compositions comprising PKM2 modulators and methods of treatment using the same
US20220213119A1 (en) 2019-03-28 2022-07-07 Jiangsu Hengrui Medicine Ca, Lid. Thienoheterocyclic derivative, preparation method therefor and medical use thereof
CA3135070A1 (en) 2019-03-29 2020-10-08 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
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
WO2020219639A1 (en) 2019-04-24 2020-10-29 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as jak kinase inhibitors
JP7482152B2 (ja) 2019-04-24 2024-05-13 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー 皮膚疾患の処置のためのピリミジンjak阻害剤 発明の背景
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
TW202110848A (zh) 2019-05-24 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 取代的稠合雙環類衍生物、其製備方法及其在醫藥上的應用
WO2020243519A1 (en) * 2019-05-29 2020-12-03 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
MX2022001940A (es) 2019-08-14 2022-05-10 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2.
US20220289692A1 (en) * 2019-09-06 2022-09-15 Inflazome Limited Nlrp3 inhibitors
CA3153456A1 (en) * 2019-10-02 2021-04-08 Stefanie Fluckiger-Mangual Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer
CA3157681A1 (en) 2019-10-11 2021-04-15 Incyte Corporation Bicyclic amines as cdk2 inhibitors
KR20220153595A (ko) * 2020-02-26 2022-11-18 재규어 테라퓨틱스 피티이 리미티드 AhR 신호전달의 조절에 유용한 피리도피리미딘 유도체
EP4126839A4 (de) * 2020-03-27 2024-04-17 Dong-A ST Co., Ltd. Aminopyrimidinderivate und deren verwendung als arylkohlenwasserstoffrezeptormodulatoren
MX2023000521A (es) 2020-07-15 2023-02-13 Chiesi Farm Spa Derivados de piridazinil-amino como inhibidores de el receptor tipo i de factor de crecimiento transformante beta (alk5).
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
CN114149410A (zh) * 2020-09-07 2022-03-08 四川科伦博泰生物医药股份有限公司 吡啶并环类化合物及其制备方法和用途
EP4223758A4 (de) 2020-09-29 2024-04-03 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Kristalline form eines heterocyclischen pyrroloderivats und herstellungsverfahren dafür
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
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
IL309118A (en) 2021-06-28 2024-02-01 Blueprint Medicines Corp CDK2 inhibitors
AU2022351219A1 (en) 2021-09-21 2024-05-02 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
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
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
WO1995009851A1 (en) 1993-10-01 1995-04-13 Ciba-Geigy Ag Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof
DE69532817T2 (de) 1994-11-10 2005-01-13 Millenium Pharmaceuticals, Inc., Cambridge Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose
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
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
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
ID19609A (id) * 1996-07-13 1998-07-23 Glaxo Group Ltd Senyawa-senyawa heterosiklik
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.
AU738341B2 (en) 1996-10-11 2001-09-13 Abbott Gmbh & Co. Kg Asparate ester inhibitors of interleukin-1beta 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
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
EA200000840A1 (ru) 1998-02-17 2001-02-26 Туларик, Инк. Антивирусные производные пиримидина
ATE295177T1 (de) 1998-03-16 2005-05-15 Cytovia Inc Dipeptid kaspase inhibitoren und deren verwendung
CA2334200C (en) * 1998-06-02 2011-01-25 Cadus Pharmaceutical Corporation Pyrrolo[2,3d]pyrimidine compositions and their use
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
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
PT1119567E (pt) * 1998-10-08 2005-08-31 Astrazeneca Ab Derivados de quinazolina
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
EP1144394B1 (de) 1999-01-13 2005-08-24 Warner-Lambert Company LLC 1-heterozyklus-substituierte diarylaminen
CA2367856C (en) 1999-03-29 2013-10-15 Uutech Limited Analogs of gastric inhibitory peptide and their use for treatment of diabetes
AU766081B2 (en) 1999-03-30 2003-10-09 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
JP2001042764A (ja) 1999-08-04 2001-02-16 Sony Corp 地図表示装置
CA2381882C (en) 1999-08-13 2011-01-25 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1218360B1 (de) 1999-10-07 2008-05-28 Amgen Inc., Triazin-kinase-hemmer
TR200201431T2 (tr) 1999-11-30 2002-09-23 Pfizer Products Inc. İmünosupresanlar olarak faydalı 2,4-diaminopirimidin bileşikleri
EP1246623B1 (de) 1999-12-02 2006-08-09 OSI Pharmaceuticals, Inc. Für adenosin a3, a2a und a3 rezeptoren spezifische verbindungen und deren verwendungen
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
CA2396693A1 (en) 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
HUP0202332A2 (en) 2000-02-05 2002-10-28 Vertex Pharma Pyrazole compositions useful as inhibitors of erk
CA2400447C (en) 2000-02-17 2008-04-22 Amgen Inc. Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
EP1268519B1 (de) 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
BR0110302A (pt) 2000-04-18 2003-01-14 Agouron Pharma Compostos de pirazol para inibição de proteìnas cinase, sal e pró-droga farmaceuticamente aceitável, metabólito farmaceuticamente ativo ou sal farmaceuticamente aceitável de metabólito, composição farmacêutica, método de tratamento de condição doentia em mamìferos mediada pela atividade de proteìna cinase, método de modulação ou inibição da atividade de um receptor de proteìna cinase
EE200200715A (et) * 2000-06-28 2004-08-16 Astrazeneca Ab Asendatud kinasoliini derivaadid ja nende kasutamine inhibiitoritena
AU2001276988B2 (en) 2000-07-21 2007-01-25 Dendreon Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
EP1313710A1 (de) 2000-08-31 2003-05-28 Pfizer Products Inc. Pyrazolderivate und ihre verwendung als proteinkinase inhibitoren
EP1317453B1 (de) 2000-09-15 2006-08-09 Vertex Pharmaceuticals Incorporated 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
US7115739B2 (en) 2000-09-15 2006-10-03 Vertex Pharmaceuticals Incorporated Triazole 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
BR0114020A (pt) 2000-09-20 2003-07-22 Merck Patent Gmbh 4-amino-quinazolinas
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
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
DE10061863A1 (de) 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
MXPA03005609A (es) 2000-12-21 2003-10-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de la proteina cinasa.
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
ES2292753T4 (es) 2001-03-29 2009-02-16 Vertex Pharmaceuticals Incorporated Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas.
US6642227B2 (en) 2001-04-13 2003-11-04 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
WO2002085909A1 (en) 2001-04-20 2002-10-31 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
US6762179B2 (en) 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
CA2446756C (en) 2001-06-01 2011-03-08 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
EP1417205B1 (de) 2001-07-03 2006-08-23 Vertex Pharmaceuticals Incorporated 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
MXPA04005510A (es) 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
PL372198A1 (en) 2002-02-06 2005-07-11 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
ATE433973T1 (de) 2002-03-15 2009-07-15 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
US7863282B2 (en) 2003-03-14 2011-01-04 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
DE60332433D1 (de) 2002-03-15 2010-06-17 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
EP1485376B1 (de) 2002-03-15 2007-06-27 Vertex Pharmaceuticals Incorporated Zusammensetzungen brauchbar als protein-kinase- inhibitoren
AU2003218215A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azolylaminoazines 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
JP4570955B2 (ja) 2002-07-09 2010-10-27 バーテクス ファーマスーティカルズ インコーポレイテッド プロテインキナーゼ阻害活性を持つイミダゾール類
ATE339419T1 (de) 2002-08-02 2006-10-15 Vertex Pharma Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
EP1611125A1 (de) 2003-02-07 2006-01-04 Vertex Pharmaceuticals Incorporated Heteroaryl-substituierte pyrrole als proteinkinase-hemmer
US7276502B2 (en) 2003-03-25 2007-10-02 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
JP2006524688A (ja) 2003-03-25 2006-11-02 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チアゾール
KR20060123164A (ko) 2003-10-17 2006-12-01 아스트라제네카 아베 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체
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
US7737151B2 (en) 2005-08-18 2010-06-15 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
WO2007041358A2 (en) 2005-09-30 2007-04-12 Miikana Therapeutics, Inc. Substituted pyrazole compounds
NZ594385A (en) 2005-11-03 2013-02-22 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
AU2006315334B2 (en) 2005-11-16 2011-05-19 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
MX2009004807A (es) 2006-11-02 2009-06-15 Vertex Pharma Aminopiridinas y aminopirimidinas utiles como inhibidores de proteina cinasa.
CA2673353A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CA2679884A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
RU2009137390A (ru) 2007-03-09 2011-04-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Аминопиримидины, пригодные в качестве ингибиторов протеинкиназ
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
AU2008228963A1 (en) 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
JP2010524962A (ja) 2007-04-17 2010-07-22 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 オーロラキナーゼ阻害剤のための創薬法
AU2008247595A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CN101801959A (zh) 2007-05-02 2010-08-11 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶类化合物
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
MX2009012719A (es) 2007-05-24 2010-02-04 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.

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