JP2004509115A5 - - Google Patents

Download PDF

Info

Publication number
JP2004509115A5
JP2004509115A5 JP2002526858A JP2002526858A JP2004509115A5 JP 2004509115 A5 JP2004509115 A5 JP 2004509115A5 JP 2002526858 A JP2002526858 A JP 2002526858A JP 2002526858 A JP2002526858 A JP 2002526858A JP 2004509115 A5 JP2004509115 A5 JP 2004509115A5
Authority
JP
Japan
Prior art keywords
ring
optionally substituted
aliphatic
phenyl
halo
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.)
Pending
Application number
JP2002526858A
Other languages
English (en)
Japanese (ja)
Other versions
JP2004509115A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2001/028793 external-priority patent/WO2002022605A1/en
Publication of JP2004509115A publication Critical patent/JP2004509115A/ja
Publication of JP2004509115A5 publication Critical patent/JP2004509115A5/ja
Pending legal-status Critical Current

Links

JP2002526858A 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物 Pending JP2004509115A (ja)

Applications Claiming Priority (4)

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
PCT/US2001/028793 WO2002022605A1 (en) 2000-09-15 2001-09-14 Pyrazole compounds useful as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2004509115A JP2004509115A (ja) 2004-03-25
JP2004509115A5 true JP2004509115A5 (enExample) 2005-04-28

Family

ID=27398347

Family Applications (9)

Application Number Title Priority Date Filing Date
JP2002526857A Expired - Fee Related JP4105948B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526856A Expired - Fee Related JP4922539B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526861A Pending JP2004509118A (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526855A Expired - Fee Related JP4105947B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なトリアゾール化合物
JP2002526859A Expired - Fee Related JP4105949B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526854A Expired - Fee Related JP4111824B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526858A Pending JP2004509115A (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526860A Expired - Fee Related JP4170752B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2008015681A Pending JP2008115195A (ja) 2000-09-15 2008-01-25 プロテインキナーゼインヒビターとして有用なピラゾール化合物

Family Applications Before (6)

Application Number Title Priority Date Filing Date
JP2002526857A Expired - Fee Related JP4105948B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526856A Expired - Fee Related JP4922539B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526861A Pending JP2004509118A (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526855A Expired - Fee Related JP4105947B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なトリアゾール化合物
JP2002526859A Expired - Fee Related JP4105949B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2002526854A Expired - Fee Related JP4111824B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2002526860A Expired - Fee Related JP4170752B2 (ja) 2000-09-15 2001-09-14 プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2008015681A Pending JP2008115195A (ja) 2000-09-15 2008-01-25 プロテインキナーゼインヒビターとして有用なピラゾール化合物

Country Status (23)

Country Link
US (7) US6638926B2 (enExample)
EP (8) EP1317450B1 (enExample)
JP (9) JP4105948B2 (enExample)
KR (4) KR20030030005A (enExample)
CN (3) CN1473161A (enExample)
AP (1) AP2003002762A0 (enExample)
AT (8) ATE327991T1 (enExample)
AU (9) AU2001290914A1 (enExample)
BR (1) BR0114088A (enExample)
CA (8) CA2422367C (enExample)
DE (8) DE60120193T2 (enExample)
DK (1) DK1318997T3 (enExample)
ES (3) ES2242771T5 (enExample)
HU (4) HUP0302172A2 (enExample)
IL (6) IL154817A0 (enExample)
MX (8) MXPA03002293A (enExample)
NO (4) NO20031188L (enExample)
NZ (4) NZ525014A (enExample)
PE (1) PE20020451A1 (enExample)
PL (1) PL361676A1 (enExample)
PT (2) PT1317448E (enExample)
TW (1) TWI303636B (enExample)
WO (8) WO2002022605A1 (enExample)

Families Citing this family (410)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1953417B (zh) * 1996-09-04 2010-12-29 英特托拉斯技术公司 一种从用户站点向外部站点发布使用数据的方法
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
EP1990343B1 (en) 1999-12-24 2012-04-04 Aventis Pharma Limited Azaindoles
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2422367C (en) * 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2004518662A (ja) * 2000-12-19 2004-06-24 スミスクライン ビーチャム パブリック リミテッド カンパニー Gsk−3阻害剤としてのピラゾロ[3,4−c]ピリジン
KR100947185B1 (ko) * 2000-12-21 2010-03-15 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물
CA2432000C (en) * 2000-12-21 2011-03-15 Glaxo Group Limited Pyrimidineamines as angiogenesis modulators
US7276523B2 (en) 2001-03-30 2007-10-02 Smithkline Beecham Corporation Aminopyridine derivatives as estrogen receptor modulators
EP1404669A2 (en) 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
EP1430033A4 (en) 2001-08-31 2004-12-15 Univ Northwestern ANTI-INFLAMMATORY AND PROTEIN-INK-INHIBITING COMPOSITION AND THEIR 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
WO2003028720A1 (en) 2001-09-26 2003-04-10 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
TWI330183B (enExample) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
US20030199526A1 (en) 2001-12-07 2003-10-23 Deborah Choquette Pyrimidine-based compounds useful as GSK-3 inhibitors
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
WO2003051886A1 (en) 2001-12-17 2003-06-26 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
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
CN1627944A (zh) * 2002-01-17 2005-06-15 神经能质公司 取代的喹唑啉-4-基胺类似物作为辣椒辣素调节剂
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
ES2437391T3 (es) * 2002-02-06 2014-01-10 Vertex Pharmaceuticals, Inc. Compuestos de heteroarilo útiles como inhibidores de GSK-3
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
DE60327999D1 (de) 2002-03-15 2009-07-30 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
AU2003220299A1 (en) * 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
EP1494645A2 (en) * 2002-04-05 2005-01-12 Boehringer Ingelheim Pharma GmbH & Co.KG Method of treating mucus hypersecretion
EP1549318B1 (en) 2002-05-01 2010-02-17 Vertex Pharmaceuticals Incorporated Crystal structure of aurora-2 protein and binding pockets thereof
PL375552A1 (en) 2002-05-22 2005-11-28 Amgen Inc. Vanilloid receptor ligands and their medical applications
EP1552842A1 (en) * 2002-06-07 2005-07-13 Kyowa Hakko Kogyo Co., Ltd. Bicyclic pyrimidine derivatives
ES2402855T3 (es) 2002-06-14 2013-05-09 Merck Serono Sa Derivados de cianuro de azol-metilideno y su uso como moduladores de proteína cinasas
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
ES2304531T3 (es) * 2002-07-17 2008-10-16 Pfizer Italia S.R.L. Derivados heterobiciclicos de pirazol como inhibidores de quinasa.
AU2003256783A1 (en) * 2002-07-25 2004-02-16 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
ATE339419T1 (de) * 2002-08-02 2006-10-15 Vertex Pharma Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
EP1739087A1 (en) * 2002-08-02 2007-01-03 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
EP1532120B1 (en) * 2002-08-13 2009-01-14 MERCK SHARP & DOHME LTD. Phenylpyridazine derivatives as ligands for gaba receptors
KR20050042478A (ko) 2002-08-14 2005-05-09 버텍스 파마슈티칼스 인코포레이티드 프로테인 키나아제 억제제 및 이의 용도
FR2844267B1 (fr) * 2002-09-05 2008-02-15 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
JP4648703B2 (ja) 2002-09-05 2011-03-09 アベンティス・ファーマ・ソシエテ・アノニム 医薬としての新規なアミノインダゾール誘導体及びこれらを含む医薬組成物
UA80295C2 (en) 2002-09-06 2007-09-10 Biogen Inc Pyrazolopyridines and using the same
JP2006503043A (ja) * 2002-09-10 2006-01-26 サイオス インク. TGFβ阻害剤
US7312227B2 (en) 2002-11-01 2007-12-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
AU2003286895A1 (en) 2002-11-05 2004-06-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
DK2316831T3 (da) * 2002-11-21 2013-06-10 Novartis Ag 2-(Morpholin-4-yl)pyrimidiner som phosphotidylinositol (PI)-3-kinaseinhibitorer samt deres anvendelse ved behandling af cancer
SI2316831T1 (sl) * 2002-11-21 2013-07-31 Novartis Ag 2-(morfolin-4-il)pirimidini kot inhibitorji fosfotidilinozitol (PI) 3-kinaze in njihova uporaba pri zdravljenju raka
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
CA2507948A1 (fr) 2002-12-12 2004-07-29 Aventis Pharma S.A. Derives d'aminoindazoles et leur utilisation comme inhibiteurs de kinases
FR2848554A1 (fr) * 2002-12-12 2004-06-18 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
JP2006515846A (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モジュレーターとしての2−置換キナゾリン−4−イルアミン類似体
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
US7223766B2 (en) * 2003-03-28 2007-05-29 Scios, Inc. Bi-cyclic pyrimidine inhibitors of TGFβ
AU2004230928B2 (en) * 2003-04-09 2010-12-02 Exelixis, Inc. Tie-2 modulators and methods of use
JP2006524254A (ja) * 2003-04-24 2006-10-26 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害剤
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
BRPI0411514A (pt) * 2003-06-20 2006-08-01 Coley Pharm Gmbh antagonistas de receptor toll-like de molécula pequena
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
GB0317127D0 (en) * 2003-07-22 2003-08-27 Astex Technology Ltd Pharmaceutical compounds
EP2256106B1 (en) 2003-07-22 2015-05-06 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
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
EP1663994B1 (en) * 2003-08-05 2012-03-07 Vertex Pharmaceuticals Incorporated Tetrahydroquinazoline compounds 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
WO2005030776A1 (en) * 2003-09-23 2005-04-07 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
AU2004283137A1 (en) * 2003-10-17 2005-05-06 Astrazeneca Ab 4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer
US8455489B2 (en) * 2003-11-10 2013-06-04 Exelixis, Inc. Substituted pyrimidine compositions and methods of use
US7338951B2 (en) 2003-11-10 2008-03-04 Synta Pharmaceuticals Corp. Pyridine compounds
BRPI0417354A (pt) 2003-12-03 2007-03-13 Cytopia Res Pty Ltd compostos inibidores de tubulina, composições e seus usos
CN1902193B (zh) * 2003-12-04 2011-07-13 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的喹喔啉
CA2548009A1 (en) * 2003-12-09 2005-06-23 Vertex Pharmaceuticals Incorporated Naphthyridine derivatives and their use as modulators of muscarinic receptors
EP1694686A1 (en) 2003-12-19 2006-08-30 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
EA011402B1 (ru) 2004-01-23 2009-02-27 Эмджен Инк. Азотсодержащие гетероциклические производные и их фармацевтические применения
AU2005207946A1 (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
WO2007056341A1 (en) 2005-11-08 2007-05-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
AU2005212438A1 (en) 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
EP2543376A1 (en) 2004-04-08 2013-01-09 Targegen, Inc. Benzotriazine inhibitors of kinases
CA2561718A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyridines as potassium ion channel modulators
US20050250829A1 (en) * 2004-04-23 2005-11-10 Takeda San Diego, Inc. Kinase inhibitors
US7793137B2 (en) 2004-10-07 2010-09-07 Cisco Technology, Inc. Redundant power and data in a wired data telecommunincations network
PL1771450T3 (pl) 2004-05-14 2008-05-30 Millennium Pharm Inc Związki i sposoby do inhibicji postępu mitozy przez hamowanie kinazy Aurora
EP1598348A1 (en) 2004-05-18 2005-11-23 Aventis Pharma Deutschland GmbH Novel pyridazinone derivatives as inhibitors of CDK2
EP1604988A1 (en) * 2004-05-18 2005-12-14 Sanofi-Aventis Deutschland GmbH Pyridazinone derivatives, methods for producing them and their use as pharmaceuticals
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
EP1778669A2 (en) 2004-08-18 2007-05-02 Takeda San Diego, Inc. 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
US7335672B2 (en) 2004-09-13 2008-02-26 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2006034474A2 (en) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyridine compounds, process for their preparation and compositions containing them
US7285569B2 (en) 2004-09-24 2007-10-23 Hoff Hoffmann-La Roche Inc. Tricycles, their manufacture and use as pharmaceutical agents
TW200624431A (en) 2004-09-24 2006-07-16 Hoffmann La Roche Phthalazinone derivatives, 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
WO2006044687A2 (en) * 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
TW200621257A (en) * 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
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
US8367672B2 (en) 2004-11-02 2013-02-05 Universite De Strasbourg Pyridazine compounds, compositions and methods
EP1812424A4 (en) * 2004-11-17 2009-07-08 Miikana Therapeutics Inc Kinase Inhibitors
DK1814878T3 (da) 2004-11-24 2012-05-07 Rigel Pharmaceuticals Inc Spiro-2, 4-pyrimidindiamin-forbindelser og anvendelser deraf
CA2587642C (en) 2004-11-30 2013-04-09 Amgen Inc. Substituted heterocycles and methods of use
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
CA2588220A1 (en) * 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
PL1856135T3 (pl) 2005-01-19 2010-05-31 Rigel Pharmaceuticals Inc Proleki związków 2,4-pirymidynodiaminy i ich zastosowanie
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
MX2007009017A (es) * 2005-01-26 2007-09-19 Schering Corp Derivados de 3-(indazol-5-il)-(1,2,4)triazina y compuestos relacionados como inhibidores de proteina cinasa para el tratamiento de cancer.
ES2375735T3 (es) * 2005-02-04 2012-03-05 Astrazeneca Ab Derivados de pirazolilaminopiridina útiles como inhibidores de quinasas.
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
ATE398613T1 (de) * 2005-02-16 2008-07-15 Astrazeneca Ab Chemische verbindungen
US20080161278A1 (en) * 2005-03-23 2008-07-03 Astrazeneca Ab 2-Azetidinyl-4-(1H-Pyrazol-3-Ylamino) Pyrimidines as Inhibitors of Insulin-Like Growth Factor-1 Receptor Activity
US7297700B2 (en) 2005-03-24 2007-11-20 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
RU2405783C2 (ru) 2005-03-25 2010-12-10 Тиботек Фармасьютикалз Лтд Гетеробициклические ингибиторы вируса гепатита с (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
KR20070113286A (ko) 2005-04-14 2007-11-28 에프. 호프만-라 로슈 아게 아미노피라졸 유도체, 이의 제조 및 약학 제제로서의 용도
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
CA2607727A1 (en) 2005-04-28 2006-11-09 Mitsubishi Tanabe Pharma Corporation Cyanopyridine derivative and use thereof as medicine
WO2006117212A2 (en) 2005-05-04 2006-11-09 Develogen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
JP5198256B2 (ja) * 2005-05-04 2013-05-15 エボテク エージー 縮合複素環式化合物、並びにそれらの組成物及び使用
JP2008540391A (ja) * 2005-05-05 2008-11-20 アストラゼネカ アクチボラグ ピラゾリルアミノ置換ピリミジン、および癌の処置におけるそれらの使用
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
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.
EP1917259B1 (en) * 2005-08-18 2012-01-25 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
WO2007025177A2 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
WO2007031838A1 (en) 2005-09-16 2007-03-22 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
UA96427C2 (en) * 2005-09-30 2011-11-10 Мийкана Терапьютикс, Инк. Substituted pyrazole compounds
WO2007041358A2 (en) 2005-09-30 2007-04-12 Miikana Therapeutics, Inc. Substituted pyrazole compounds
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
CA2625153A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
PT1945631E (pt) 2005-10-28 2012-10-15 Astrazeneca Ab Derivados de 4-(3-aminopirazole)pirimidina para utilização como inibidores da tirosina-cinase no tratamento do cancro
EP1942879A1 (en) 2005-10-31 2008-07-16 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
MY167260A (en) 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
CA2627808A1 (en) * 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
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
US20070244169A1 (en) * 2005-12-20 2007-10-18 Jun Feng Glucokinase activators
RU2453548C2 (ru) 2006-01-17 2012-06-20 Вертекс Фармасьютикалз Инкорпорейтед Азаиндолы, полезные в качестве ингибиторов янус-киназ
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
ATE485268T1 (de) 2006-02-16 2010-11-15 Schering Corp Pyrrolidin-derivate als erk-hemmer
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP1991212A1 (en) * 2006-03-08 2008-11-19 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
CN101460466B (zh) * 2006-04-11 2012-06-13 沃泰克斯药物股份有限公司 适用作蛋白激酶抑制剂的噻唑类、咪唑类和吡唑类
US8158627B2 (en) 2006-04-28 2012-04-17 Northwestern University Compositions and treatments using pyridazine compounds and cholinesterase inhibitors
US7678808B2 (en) * 2006-05-09 2010-03-16 Braincells, Inc. 5 HT receptor mediated neurogenesis
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
PT2248812E (pt) 2006-06-27 2014-03-12 Takeda Pharmaceutical Compostos cíclicos fundidos como moduladores do receptor gpr40
UY30444A1 (es) * 2006-06-30 2008-01-31 Astrazeneca Ab Derivados de pirimidina, procesos para su preparacinn, composiciones farmaccuticos y usos de los mismos.
US8222256B2 (en) 2006-07-05 2012-07-17 Exelixis, Inc. Methods of using IGFIR and ABL kinase modulators
UA95641C2 (xx) * 2006-07-06 2011-08-25 Эррей Биофарма Инк. Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы
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
CA2662491A1 (en) 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP2066355A2 (en) * 2006-09-19 2009-06-10 Braincells, Inc. Combination comprising a peroxisome proliferator activated receptor agent and a second neurogenic agent for treating a nervous system disorder, increasing neurodifferentiation and increasing neurogenesis
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
AU2007312165A1 (en) 2006-10-21 2008-04-24 Abbott Gmbh & Co. Kg Heterocyclic compounds and their use as glycogen synthase kinase 3 inhibitors
NZ576750A (en) * 2006-11-02 2012-01-12 Vertex Pharma Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
CA2673353A1 (en) * 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
US8143394B2 (en) 2006-12-26 2012-03-27 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
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
EP2118087B1 (en) 2007-02-06 2012-03-28 Novartis AG Pi 3-kinase inhibitors and methods of their use
EP2120573A4 (en) * 2007-02-12 2011-05-25 Merck Sharp & Dohme piperidine
US20100204230A1 (en) * 2007-02-12 2010-08-12 Peter Blurton Piperazine derivatives for treatment of ad and related conditions
TW200901975A (en) 2007-03-05 2009-01-16 Kyowa Hakko Kogyo Kk Pharmaceutical composition
JP5520057B2 (ja) * 2007-03-09 2014-06-11 バーテックス ファーマシューティカルズ インコーポレイテッド 蛋白キナーゼの阻害剤として有用なアミノピリミジン
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
NZ579485A (en) * 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
JP2010523700A (ja) 2007-04-13 2010-07-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリミジン
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
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
AU2008247592A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
JP5572087B2 (ja) * 2007-05-02 2014-08-13 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 キナーゼ阻害として有用なアミノピリミジン
JP2010526048A (ja) * 2007-05-04 2010-07-29 アストラゼネカ アクチボラグ アミノ−チアゾリル−ピリミジン誘導体、および癌の治療のための該誘導体の使用
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
CN104447716A (zh) 2007-05-09 2015-03-25 沃泰克斯药物股份有限公司 Cftr调节剂
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
CA2683152A1 (en) * 2007-06-11 2008-12-18 Miikana Therapeutics, Inc. Substituted pyrazole compounds
US8242150B2 (en) * 2007-06-13 2012-08-14 Merck Sharp & Dohme Corp. 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
ATE522509T1 (de) * 2007-07-05 2011-09-15 Array Biopharma Inc Pyrimidylcyclopentane als inhibitoren der akt- proteinkinase
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
EP2170863B1 (en) * 2007-07-05 2015-09-02 Array Biopharma, Inc. Pyrimido cyclopentanes useful for the treatment of inflammatory or hyperproliferative diseases
KR20100038108A (ko) 2007-07-25 2010-04-12 브리스톨-마이어스 스큅 컴퍼니 트리아진 키나제 억제제
TW200906818A (en) * 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
NZ582879A (en) * 2007-07-31 2012-03-30 Vertex Pharma Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
WO2009067166A2 (en) * 2007-11-20 2009-05-28 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
EP3683218B1 (en) 2007-12-07 2024-09-18 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
HUE031871T2 (en) 2007-12-07 2017-08-28 Vertex Pharma Methods for the preparation of cycloalkylcarboxamide pyridine benzoic acids
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
WO2009078999A1 (en) 2007-12-17 2009-06-25 Janssen Pharmaceutica N.V. Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1
CN101970415A (zh) * 2008-01-09 2011-02-09 阵列生物制药公司 作为AKT蛋白激酶抑制剂的5H-环戊二烯并[d]嘧啶
CA2714888C (en) 2008-01-09 2017-03-14 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
AU2009215534B8 (en) 2008-02-21 2014-07-10 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
NZ736561A (en) 2008-02-28 2018-02-23 Vertex Pharma Heteroaryl derivatives as cftr modulators
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
EP3210609A1 (en) 2008-05-21 2017-08-30 Ariad Pharmaceuticals, Inc. Phosphorous derivatives as kinase inhibitors
WO2009150462A1 (en) * 2008-06-11 2009-12-17 Astrazeneca Ab Tricyclic 2,4-diamin0-l,3,5-triazine derivatives useful for the treatment of cancer and myeloproliferative disorders
MY158927A (en) 2008-06-12 2016-11-30 Janssen Pharmaceutica Nv Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h4 receptor
WO2010002779A2 (en) * 2008-07-03 2010-01-07 Merck Serono S.A. Naphthyridininones as aurora kinase inhibitors
US8536187B2 (en) 2008-07-03 2013-09-17 Gilead Sciences, Inc. 2,4,6-trisubstituted pyrido(3,2-d)pyrimidines useful for treating viral infections
WO2010014939A1 (en) * 2008-07-31 2010-02-04 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
US20110251172A1 (en) * 2008-08-13 2011-10-13 Rivkin Alexey A Purine derivatives for treatment of alzheimer's disease
JP2012501971A (ja) * 2008-09-03 2012-01-26 バーテックス ファーマシューティカルズ インコーポレイテッド 共結晶および共結晶を含む薬学的処方物
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
WO2010038060A1 (en) * 2008-09-30 2010-04-08 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
RS54504B1 (sr) 2009-02-05 2016-06-30 Takeda Pharmaceutical Company Limited Jedinjenja piridazinona
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2010099379A1 (en) * 2009-02-27 2010-09-02 Ambit Biosciences Corporation Jak kinase modulating quinazoline derivatives and methods of use thereof
AU2010222848A1 (en) * 2009-03-09 2011-10-20 Surface Logix, Inc. Rho kinase inhibitors
AU2010229134A1 (en) * 2009-03-23 2011-11-10 Msd K.K. Novel aminopyridine derivatives having Aurora A selective inhibitory action
EP2411012A4 (en) * 2009-03-24 2012-08-22 Msd Kk NEW AMINO-PYRIDINE DERIVATIVES WITH SELECTIVE AURORA A INHIBITION
AU2010229140A1 (en) * 2009-03-24 2011-11-10 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
EP2440050A4 (en) * 2009-06-08 2013-04-03 California Capital Equity Llc TRIAZINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATION
KR20120016676A (ko) * 2009-06-09 2012-02-24 아브락시스 바이오사이언스, 엘엘씨 우레이도페닐치환 트리아진 유도체와 이들의 치료적 용도
CA2765030C (en) * 2009-06-09 2015-10-27 California Capital Equity, Llc Triazine derivatives and their therapeutical applications
CN102480961A (zh) * 2009-06-24 2012-05-30 健泰科生物技术公司 与含氧杂环稠合的嘧啶化合物、组合物和使用方法
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
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
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
JP5579864B2 (ja) * 2009-11-12 2014-08-27 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト N−9−置換プリン化合物、組成物及び使用の方法
US8828990B2 (en) 2009-11-12 2014-09-09 Genentech, Inc. N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use
KR20130029368A (ko) 2010-02-11 2013-03-22 벤더르빌트 유니버시티 Mglur4 알로스테릭 강화제로서 피라졸로피리딘, 피라졸로피라진, 피라졸로피리미딘, 피라졸로티오펜 및 피라졸로티아졸 화합물, 조성물, 및 신경 기능이상을 치료하는 방법
EP3150198B1 (en) 2010-04-07 2021-09-22 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
BR112012029647A2 (pt) 2010-05-21 2016-08-02 Chemilia Ab novos derivados de pirimidinas
AU2011260323A1 (en) 2010-06-04 2012-11-15 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as LRRK2 modulators
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.
CN103119035B (zh) 2010-09-27 2015-09-30 雅培股份有限两合公司 杂环化合物和它们作为糖原合成酶激酶-3抑制剂的用途
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
CA3017869C (en) 2010-11-10 2021-07-27 Genentech, Inc. Pyrazole aminopyrimidine derivatives as lrrk2 modulators
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
KR20130130030A (ko) 2010-12-21 2013-11-29 노파르티스 아게 Vps34 억제제로서의 비-헤테로아릴 화합물
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
DK2688883T3 (en) 2011-03-24 2016-09-05 Noviga Res Ab pyrimidine
US9682082B2 (en) 2011-04-01 2017-06-20 Genentech, Inc. Combinations of AKT and MEK inhibitor compounds, and methods of use
CN103857395A (zh) 2011-04-01 2014-06-11 基因泰克公司 Akt抑制剂化合物和阿比特龙的组合及使用方法
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
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
CN104024248A (zh) 2011-08-25 2014-09-03 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸pak1抑制剂
PT2755483T (pt) 2011-09-14 2019-02-18 Samumed Llc Indazol-3-carboxamidas e sua utilização como inibidores da via de sinalização de wnt/β-catenina
MD20140023A2 (ro) 2011-09-22 2014-06-30 Pfizer Inc. Derivaţi de pirolpirimidină şi purină
TWI547493B (zh) 2011-09-27 2016-09-01 諾華公司 作為突變idh之抑制劑之3-嘧啶-4-基-唑啶-2-酮
BR112014015549A8 (pt) 2011-12-22 2017-07-04 Hoffmann La Roche composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção
CA3128556A1 (en) 2012-01-25 2013-08-01 Vertex Pharmaceuticals Incorporated Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
NZ628084A (en) * 2012-03-16 2016-09-30 Axikin Pharmaceuticals Inc 3,5-diaminopyrazole kinase inhibitors
AU2013237226A1 (en) * 2012-03-19 2014-10-09 Emory University 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
SI3459942T1 (sl) 2012-04-24 2021-05-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
CN104271569B (zh) * 2012-05-03 2016-08-24 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
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
KR102427777B1 (ko) 2012-06-26 2022-08-01 델 마 파마슈티컬스 디안하이드로갈락티톨, 디아세틸디안하이드로갈락티톨, 디브로모둘시톨, 또는 그의 유사체 또는 유도체를 이용하여 유전학적 다형성이 있는 환자에 있어서 티로신-키나아제-억제제 내성 악성종양, ahi1 조절곤란 또는 돌연변이를 치료하는 방법
CA2886495C (en) * 2012-09-28 2023-09-19 Ignyta, Inc. Azaquinazoline inhibitors of atypical protein kinase 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
ES2644758T3 (es) 2012-10-16 2017-11-30 Tolero Pharmaceuticals, Inc. Moduladores de PKM2 y métodos para su uso
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
EP3181564B1 (en) * 2012-11-20 2019-09-18 H. Hoffnabb-La Roche Ag Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
UA118094C2 (uk) 2012-11-21 2018-11-26 Пітісі Терап'Ютикс, Інк. Заміщені зворотні піримідинові інгібітори bmi-1
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
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.
JP6424173B2 (ja) 2013-02-04 2018-11-14 ヤンセン ファーマシューティカ エヌ.ベー. Flap調節因子
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Flap調節劑
EP2769722A1 (en) * 2013-02-22 2014-08-27 Ruprecht-Karls-Universität Heidelberg Compounds for use in inhibiting HIV capsid assembly
JO3377B1 (ar) * 2013-03-11 2019-03-13 Takeda Pharmaceuticals Co مشتقات بيريدينيل وبيريدينيل مندمج
HRP20211855T1 (hr) 2013-03-12 2022-03-04 Vertex Pharmaceuticals Incorporated Inhibitori dnk-pk
MX355945B (es) 2013-03-14 2018-05-07 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
CN105209042B (zh) 2013-03-22 2019-03-08 米伦纽姆医药公司 催化性mtorc 1/2抑制剂与选择性极光a激酶抑制剂的组合
CN105764501A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群治疗效益的组合物
WO2015030847A1 (en) 2013-08-30 2015-03-05 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
RS57058B1 (sr) 2013-10-03 2018-05-31 Kura Oncology Inc Ekr inhibitori i postupci primene
CN104903312B (zh) * 2013-10-07 2019-01-29 卡德门企业有限公司 Rho激酶抑制剂
SI3424920T1 (sl) 2013-10-17 2020-08-31 Vertex Pharmaceuticals Incorporated Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk
HRP20210516T2 (hr) 2013-11-12 2021-10-01 Vertex Pharmaceuticals Incorporated Postupak proizvodnje farmaceutskih pripravaka za liječenje bolesti koje su posredovane putem cftr
EP3071553A4 (en) * 2013-11-21 2017-08-02 PTC Therapeutics, Inc. Substituted pyridine and pyrazine bmi-1 inhibitors
US9975878B2 (en) 2013-11-21 2018-05-22 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
CA2935392C (en) 2014-01-01 2022-07-26 Medivation Technologies, Inc. Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity
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
CN104926794B (zh) * 2014-03-17 2017-12-05 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
CA2945263A1 (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
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
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
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
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
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
WO2016081556A1 (en) 2014-11-18 2016-05-26 Vertex Pharmaceuticals Incorporated Process of conducting high throughput testing high performance liquid chromatography
TWI704151B (zh) * 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
JP6322770B2 (ja) * 2014-12-22 2018-05-09 イーライ リリー アンド カンパニー Erk阻害剤
WO2016123627A1 (en) 2015-01-30 2016-08-04 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction
EP3070084A1 (en) * 2015-03-18 2016-09-21 Rottapharm Biotech S.r.l. New fyn kinase inhibitors
US10752612B2 (en) 2015-04-17 2020-08-25 Ludwig Institute For Cancer Research Ltd PLK4 inhibitors
HK1252425A1 (zh) 2015-06-05 2019-05-24 Vertex Pharmaceuticals Incorporated 用於治疗脱髓鞘疾病的三唑类药物
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
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017023989A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]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
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
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
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
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
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
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-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
US10195185B2 (en) 2015-08-03 2019-02-05 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10188634B2 (en) 2015-08-03 2019-01-29 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-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
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
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
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
NZ742200A (en) 2015-11-06 2023-01-27 Samumed Llc Treatment of osteoarthritis
GB201604647D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
AU2017274350B2 (en) 2016-06-01 2022-03-03 Samumed, Llc Process for preparing N-(5-(3-(7-(3-fluorophenyl)-3H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide
MX394860B (es) 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
CA3041291A1 (en) 2016-10-21 2018-04-26 Samumed, Llc Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
US10870630B2 (en) 2016-11-01 2020-12-22 Merck Sharp & Dohme Corp. Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors
WO2018085865A1 (en) 2016-11-07 2018-05-11 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
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
ES2969536T3 (es) 2017-06-30 2024-05-21 Beijing Tide Pharmaceutical Co Ltd Inhibidor de la proteína cinasa asociada a rho, composición farmacéutica que lo comprende, y su método de preparación y uso
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
CA3074034A1 (en) 2017-10-27 2019-05-02 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
US12030857B2 (en) * 2018-06-25 2024-07-09 Kadmon Corporation, Llc Glucose uptake inhibitors
CN113164479A (zh) 2018-08-17 2021-07-23 Ptc医疗公司 用于治疗胰腺癌的方法
CN112739698A (zh) 2018-08-24 2021-04-30 捷豹治疗有限公司 作为ahr调节剂的四氢嘧啶衍生物
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
ES2942310T3 (es) * 2018-12-27 2023-05-31 Servier Lab Inhibidores aza-heterobicíclicos de MAT2A y métodos de uso para el tratamiento del cáncer
JP7566753B2 (ja) 2019-01-03 2024-10-15 ユニバーシティ オブ ピッツバーグ -オブ ザ コモンウェルス システム オブ ハイヤー エデュケイション 転写因子ebポリペプチドレベルを増加させるための方法および材料
US20220133740A1 (en) 2019-02-08 2022-05-05 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
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
JP7547360B2 (ja) 2019-03-22 2024-09-09 スミトモ ファーマ オンコロジー, インコーポレイテッド Pkm2モジュレーターを含む組成物およびそれを使用する処置の方法
WO2020192750A1 (zh) 2019-03-28 2020-10-01 江苏恒瑞医药股份有限公司 噻吩并杂环类衍生物、其制备方法及其在医药上的应用
US20220185818A1 (en) 2019-03-29 2022-06-16 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
US11919904B2 (en) 2019-03-29 2024-03-05 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
AU2020260629A1 (en) * 2019-04-22 2021-12-09 Betta Pharmaceuticals Co., Ltd Quinazoline compound and pharmaceutical application thereof
PL3958969T3 (pl) 2019-04-24 2024-05-20 Theravance Biopharma R&D Ip, Llc Estrowe i węglanowe związki pirymidynowe jako inhibitory kinaz
AR118767A1 (es) 2019-04-24 2021-10-27 Theravance Biopharma R&D Ip Llc Pirimidinas sustituidas como inhibidores de jak y su uso para el tratamiento de enfermedades inflamatorias o autoinmunes cutáneas
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
WO2020223558A1 (en) 2019-05-01 2020-11-05 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
JP2022535743A (ja) * 2019-05-29 2022-08-10 アイエフエム デュー インコーポレイテッド Sting活性に関連する状態を治療するための化合物および組成物
CR20220066A (es) 2019-08-14 2022-11-28 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2
JP2022547882A (ja) * 2019-09-06 2022-11-16 インフレイゾーム リミテッド Nlrp3阻害剤
WO2021064142A1 (en) 2019-10-02 2021-04-08 Tolremo Therapeutics Ag Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer
CN119930610A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
TWI885039B (zh) 2020-01-13 2025-06-01 美商邊際分析公司 經取代吡唑并嘧啶及其用途
JP2023515128A (ja) * 2020-02-26 2023-04-12 ジャガー セラピューティクス ピーティーイーリミテッド Ahrシグナル伝達の調節に有用なピリドピリミジン誘導体
BR112022019387A2 (pt) * 2020-03-27 2022-11-16 Dong A St Co Ltd Derivados de aminopirimidina e seu uso como moduladores de receptores de aril hidrocarbonetos
CA3184076A1 (en) 2020-06-25 2021-12-30 Stefanie Fluckiger-Mangual Combination of a cbp/p300 bromodomain inhibitor and a kras inhibitor for the treatment of cancer
CN116096719B (zh) * 2020-07-15 2025-09-30 奇斯药制品公司 作为alk5抑制剂的哒嗪基氨基衍生物
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
CN114149410B (zh) * 2020-09-07 2025-02-25 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
US20230331731A1 (en) 2020-09-29 2023-10-19 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Crystal form of pyrrolo heterocyclic derivative and preparation method therefor
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
CN117355516A (zh) * 2021-03-24 2024-01-05 阿索斯治疗公司 用于治疗激酶相关疾病的小分子
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11932648B2 (en) 2021-06-28 2024-03-19 Blueprint Medicines Corporation CDK2 inhibitors
AR127108A1 (es) 2021-09-21 2023-12-20 Chiesi Farm Spa Derivados de amino piridazinilo como inhibidores de alk5
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
US20250100997A1 (en) 2022-01-11 2025-03-27 Chiesi Farmaceutici S.P.A. Pyridazinyl amino derivatives as alk5 inhibitors
WO2024206628A1 (en) * 2023-03-30 2024-10-03 Nalo Therapeutics Modulators of myc family proto-oncogene protein

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
EP0672042B1 (en) 1993-10-01 2006-05-03 Novartis AG Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof
ATE262902T1 (de) 1994-11-10 2004-04-15 Millennium Pharm Inc 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
AU726058B2 (en) 1995-09-01 2000-10-26 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
JP4205168B2 (ja) * 1996-10-02 2009-01-07 ノバルティス アクチエンゲゼルシヤフト ピリミジン誘導体およびその製造法
EP0932598A1 (en) 1996-10-11 1999-08-04 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME
BR9814817A (pt) 1997-10-10 2002-01-08 Cytovia Inc Inibidores de apoptose de dipeptìdio e o uso dos mesmos
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
CA2334200C (en) 1998-06-02 2011-01-25 Cadus Pharmaceutical Corporation Pyrrolo[2,3d]pyrimidine compositions and their use
AU4956699A (en) 1998-06-19 2000-01-05 Chiron Corporation Inhibitors of glycogen synthase kinase 3
AU5777299A (en) * 1998-08-21 2000-03-14 Du Pont Pharmaceuticals Company Isoxazolo(4,5-d)pyrimidines as CRF antagonists
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
HK1039126B (en) * 1998-10-08 2005-09-30 阿斯特拉曾尼卡有限公司 Quinazoline derivatives
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
EE200100374A (et) * 1999-01-13 2002-12-16 Warner-Lambert Company 1-heterotsükliga asendatud diarüülamiinid
US6921748B1 (en) 1999-03-29 2005-07-26 Uutech Limited Analogs of gastric inhibitory polypeptide and their use for treatment of diabetes
CA2366857C (en) 1999-03-30 2010-12-14 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
WO2000078757A1 (en) 1999-06-17 2000-12-28 Shionogi Bioresearch Corp. Inhibitors of il-12 production
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
JP2001042764A (ja) 1999-08-04 2001-02-16 Sony Corp 地図表示装置
AU6909600A (en) 1999-08-13 2001-03-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
MXPA02003436A (es) 1999-10-07 2002-08-20 Amgen Inc Inhibidores de triazina cinasa.
EA200200411A1 (ru) 1999-11-30 2002-10-31 Пфайзер Продактс Инк. 2,4-диаминопиримидиновые соединения, полезные в качестве иммуносупрессоров
DK1246623T3 (da) * 1999-12-02 2006-11-13 Osi Pharm Inc Forbindelser, som er specifikke for adenosin A1-, A2a- og A3-receptor og anvendelser deraf
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
KR20010111298A (ko) 2000-02-05 2001-12-17 버텍스 파마슈티칼스 인코포레이티드 Erk의 억제제로서 유용한 피라졸 조성물
AU2001237041B9 (en) * 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
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
EP1268519B1 (en) 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
EP1274706A1 (en) 2000-04-18 2003-01-15 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinases
CA2412592A1 (en) * 2000-06-28 2002-01-03 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
MXPA03000627A (es) 2000-07-21 2004-07-30 Schering Corp Nuevos peptidos como inhibidores de proteasa serina-ns3 del virus de la hepatitis c.
HUP0302669A3 (en) 2000-08-31 2004-03-29 Pfizer Prod Inc Pyrazole derivatives and pharmaceutical compositions containing them for treating diseases comprising abnormal cell growth and neurodegenerative diseases
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
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ZA200301696B (en) 2000-09-15 2004-04-28 Vertex Pharma Isoxazoles and their use as inhibitors of erk.
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2422367C (en) 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2001293817A1 (en) 2000-09-20 2002-04-02 Merck Patent Gmbh 4-amino-quinazolines
EP1351691A4 (en) 2000-12-12 2005-06-22 Cytovia Inc SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND ANALOGUES AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCERS, AND USE THEREOF
DE10061863A1 (de) 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
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
KR100947185B1 (ko) 2000-12-21 2010-03-15 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US6949544B2 (en) 2001-03-29 2005-09-27 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
DE60214701T2 (de) 2001-04-13 2007-09-13 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren von c-jun-n-terminalen-kinasen (jnk) und anderen proteinkinasen
US20030096813A1 (en) 2001-04-20 2003-05-22 Jingrong Cao Compositions useful as inhibitors of GSK-3
EP1404669A2 (en) 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
MXPA03010961A (es) 2001-05-31 2004-02-27 Vertex Pharma Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
EP1392684B1 (en) 2001-06-01 2006-09-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinases
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
US6689778B2 (en) 2001-07-03 2004-02-10 Vertex Pharmaceuticals Incorporated Inhibitors of Src and Lck protein kinases
WO2003011287A1 (en) * 2001-08-03 2003-02-13 Vertex Pharmaceuticals Incorporated Pyrazolon derivatives as inhibitors of gsk-3
US20030199526A1 (en) 2001-12-07 2003-10-23 Deborah Choquette Pyrimidine-based compounds useful as GSK-3 inhibitors
ES2437391T3 (es) 2002-02-06 2014-01-10 Vertex Pharmaceuticals, Inc. Compuestos de heteroarilo útiles como inhibidores de GSK-3
DE60327999D1 (de) 2002-03-15 2009-07-30 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
US7863282B2 (en) 2003-03-14 2011-01-04 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2003220299A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
AU2003220300A1 (en) 2002-03-15 2003-09-29 Binch, Hayley Compositions useful as inhibitors of protein kinases
US20030207873A1 (en) 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2003237121A1 (en) 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
US7361665B2 (en) 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
ATE339419T1 (de) 2002-08-02 2006-10-15 Vertex Pharma Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
WO2004041814A1 (en) 2002-11-04 2004-05-21 Vertex Pharmaceuticals Incorporated Heteroaryl-pyramidine derivatives as jak inhibitors
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
EP1605946B1 (en) 2003-03-25 2008-05-28 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
US20040235834A1 (en) 2003-03-25 2004-11-25 Farmer Luc J. Thiazoles useful as inhibitors of protein kinases
AU2004283137A1 (en) 2003-10-17 2005-05-06 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
EP1917259B1 (en) 2005-08-18 2012-01-25 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
CA2627808A1 (en) 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CN101360740A (zh) 2005-11-16 2009-02-04 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
NZ576750A (en) 2006-11-02 2012-01-12 Vertex Pharma Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
CA2673353A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
NZ579485A (en) 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
JP5520057B2 (ja) 2007-03-09 2014-06-11 バーテックス ファーマシューティカルズ インコーポレイテッド 蛋白キナーゼの阻害剤として有用なアミノピリミジン
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
WO2008115973A2 (en) 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2008131103A2 (en) 2007-04-17 2008-10-30 Vertex Pharmaceuticals Incorporated Drug discovery methods for aurora 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
AU2008247592A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
JP5572087B2 (ja) 2007-05-02 2014-08-13 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 キナーゼ阻害として有用なアミノピリミジン
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

Similar Documents

Publication Publication Date Title
JP2004509115A5 (enExample)
JP2004509118A5 (enExample)
JP2004525075A5 (enExample)
JP2004509116A5 (enExample)
JP2004509113A5 (enExample)
JP2004509114A5 (enExample)
JP2004509117A5 (enExample)
JP2004512277A5 (enExample)
CA2422377A1 (en) Pyrazole compounds useful as protein kinase inhibitors
JP2010509231A5 (enExample)
EP1857443B1 (en) Therapeutic morpholino-substituted compounds
EP2894149B1 (en) Cyanoguanidine prodrugs
RU2003122209A (ru) Производные пиразола, полезные в качестве ингибиторов протеинкиназы
JP6786086B2 (ja) 1,3,5−トリアジン誘導体及びその使用方法
JP2004517894A5 (enExample)
JP2019135258A (ja) 第Xa因子阻害剤の結晶形態
JP2015522028A (ja) 化合物とその治療用途
CN1434796A (zh) 酰基苯基脲衍生物,其制备方法和作为药物的用途
JP2008540493A (ja) Hcv阻害剤として有用なプテリジンおよびその製造方法
JP2010513567A5 (enExample)
US20070249676A1 (en) Cyanoguanidine prodrugs
MXPA03010669A (es) Nuevos compuestos de cianoguanidina de piridilo.
SK61496A3 (en) Prodrugs of an inhibitor of hiv protease and pharmaceutical agents containing them
JPS61254524A (ja) 抗血栓形成性医薬組成物
PT87604B (pt) Processo para a preparacao de agentes anti-alergicos e anti-inflamatorios di-hidropiridinicos