JP2004509117A5 - - Google Patents

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Publication number
JP2004509117A5
JP2004509117A5 JP2002526860A JP2002526860A JP2004509117A5 JP 2004509117 A5 JP2004509117 A5 JP 2004509117A5 JP 2002526860 A JP2002526860 A JP 2002526860A JP 2002526860 A JP2002526860 A JP 2002526860A JP 2004509117 A5 JP2004509117 A5 JP 2004509117A5
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ring
optionally substituted
aliphatic
con
compound
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JP2002526860A
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JP4170752B2 (ja
JP2004509117A (ja
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Priority claimed from PCT/US2001/028940 external-priority patent/WO2002022607A1/en
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Publication of JP2004509117A5 publication Critical patent/JP2004509117A5/ja
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Publication of JP4170752B2 publication Critical patent/JP4170752B2/ja
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JP2002526860A 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 Expired - Fee Related JP4170752B2 (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/US2001/028940 WO2002022607A1 (en) 2000-09-15 2001-09-14 Pyrazole compounds useful as protein kinase inhibitors

Related Child Applications (1)

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JP2008015681A Division 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

Publications (3)

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JP2004509117A JP2004509117A (ja) 2004-03-25
JP2004509117A5 true JP2004509117A5 (US07585860-20090908-C00112.png) 2005-04-28
JP4170752B2 JP4170752B2 (ja) 2008-10-22

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Family Applications (9)

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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
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
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
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
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
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
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
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 (5)

Application Number Title Priority Date Filing Date
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
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
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
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

Family Applications After (3)

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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
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
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 (24)

Country Link
US (7) US7115739B2 (US07585860-20090908-C00112.png)
EP (8) EP1317448B2 (US07585860-20090908-C00112.png)
JP (9) JP4922539B2 (US07585860-20090908-C00112.png)
KR (4) KR100876069B1 (US07585860-20090908-C00112.png)
CN (3) CN1469875A (US07585860-20090908-C00112.png)
AP (1) AP2003002762A0 (US07585860-20090908-C00112.png)
AT (8) ATE326459T1 (US07585860-20090908-C00112.png)
AU (9) AU2001291013A1 (US07585860-20090908-C00112.png)
BR (1) BR0114088A (US07585860-20090908-C00112.png)
CA (8) CA2422379C (US07585860-20090908-C00112.png)
DE (8) DE60120198T2 (US07585860-20090908-C00112.png)
DK (1) DK1318997T3 (US07585860-20090908-C00112.png)
ES (3) ES2242771T5 (US07585860-20090908-C00112.png)
HK (8) HK1057543A1 (US07585860-20090908-C00112.png)
HU (4) HUP0302172A2 (US07585860-20090908-C00112.png)
IL (6) IL154817A0 (US07585860-20090908-C00112.png)
MX (8) MXPA03002291A (US07585860-20090908-C00112.png)
NO (4) NO326850B1 (US07585860-20090908-C00112.png)
NZ (4) NZ525009A (US07585860-20090908-C00112.png)
PE (1) PE20020451A1 (US07585860-20090908-C00112.png)
PL (1) PL361676A1 (US07585860-20090908-C00112.png)
PT (2) PT1318997E (US07585860-20090908-C00112.png)
TW (1) TWI303636B (US07585860-20090908-C00112.png)
WO (8) WO2002022603A1 (US07585860-20090908-C00112.png)

Families Citing this family (401)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69638122D1 (de) * 1996-09-04 2010-03-18 Intertrust Tech Corp Zuverlässige Infrastrukturhilfssysteme, Verfahren und Techniken für sicheren elektronischen Handel, elektronische Transaktionen, Handelsablaufsteuerung und Automatisierung, verteilte Verarbeitung und Rechteverwaltung
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6982260B1 (en) 1999-11-22 2006-01-03 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
CZ301750B6 (cs) 1999-12-24 2010-06-09 Aventis Pharma Limited Bicyklický pyrrolový derivát, jeho použití pri výrobe léciva, farmaceutická kompozice tento derivát obsahující a pro použití pri lécení
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
EP1317448B2 (en) 2000-09-15 2011-05-04 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
JP4160395B2 (ja) * 2000-12-21 2008-10-01 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なピラゾール化合物
WO2002059110A1 (en) * 2000-12-21 2002-08-01 Glaxo Group Limited Pyrimidineamines as angiogenesis modulators
WO2002079163A1 (en) * 2001-03-30 2002-10-10 Smithkline Beecham Corporation Aminopyridine derivatives as estrogen receptor modulators
JP4316893B2 (ja) * 2001-05-16 2009-08-19 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 Srcおよび他のプロテインキナーゼのインヒビター
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
EP1430033A4 (en) 2001-08-31 2004-12-15 Univ Northwestern PROTEIN KINASE ANTI-INFLAMMATORY AND INHIBITOR COMPOSITION AND METHOD OF USE
WO2003030909A1 (en) * 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
EA007430B1 (ru) 2001-09-26 2006-10-27 Фармация Италия С.П.А. Производные аминоиндазола, активные в качестве ингибиторов киназ, способ их получения и содержащая их фармацевтическая композиция
TWI330183B (US07585860-20090908-C00112.png) * 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
US20030199526A1 (en) 2001-12-07 2003-10-23 Deborah Choquette Pyrimidine-based compounds useful as GSK-3 inhibitors
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
JP2005524609A (ja) 2001-12-17 2005-08-18 スミスクライン ビーチャム コーポレーション ピラゾロピリダジン誘導体
AU2002361846A1 (en) * 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
WO2003062209A2 (en) 2002-01-17 2003-07-31 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
DE60332604D1 (de) * 2002-03-15 2010-07-01 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
US7179826B2 (en) 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
ATE466580T1 (de) 2002-03-15 2010-05-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
RU2004132847A (ru) * 2002-04-05 2006-08-20 Берингер Ингельхайм Фарма Гмбх Унд Ко.Кг (De) Способ лечения гиперсекреции слизи
DE60331329D1 (de) * 2002-05-01 2010-04-01 Vertex Pharma Kristallstruktur des aurora-2 proteins und dessen bindungstaschen
AU2003247425B2 (en) * 2002-05-22 2007-03-08 Amgen Inc. Amino-pyridine, -pyridine and pyridazine derivatives for use as vanilloid receptor ligands for the treatment of pain
AU2003242252A1 (en) * 2002-06-07 2003-12-22 Kyowa Hakko Kogyo Co., Ltd. Bicyclic pyrimidine derivatives
CA2487948A1 (en) 2002-06-14 2003-12-24 Applied Research Systems Ars Holding N.V. Azole methylidene cyanide derivatives and their use as protein kinase modulators
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004000318A2 (en) 2002-06-21 2003-12-31 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
CA2492673A1 (en) * 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Heterobicyclic pyrazole derivatives as kinase inhibitors
CA2494367A1 (en) * 2002-07-25 2004-02-05 Scios Inc. Methods for improvement of lung function using tgf-.beta. inhibitors
CN1678321A (zh) 2002-07-29 2005-10-05 里格尔药品股份有限公司 用2,4-嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法
EP1739087A1 (en) * 2002-08-02 2007-01-03 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
EP1532145B1 (en) * 2002-08-02 2006-09-13 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
ATE420867T1 (de) * 2002-08-13 2009-01-15 Merck Sharp & Dohme Phenylpyridazin derivative als liganden für gaba- rezeptoren
US7304071B2 (en) * 2002-08-14 2007-12-04 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
MXPA05001807A (es) 2002-09-05 2005-04-19 Aventis Pharma Sa Nuevos derivados de aminoindazol utilizados como medicamentos y composiciones farmaceuticas que los contienen.
FR2844267B1 (fr) * 2002-09-05 2008-02-15 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
UA80295C2 (en) 2002-09-06 2007-09-10 Biogen Inc Pyrazolopyridines and using the same
BR0314196A (pt) * 2002-09-10 2005-07-26 Scios Inc Inibidores de tgf-beta
AU2003286876A1 (en) 2002-11-01 2004-06-07 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
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
ES2412273T3 (es) 2002-11-21 2013-07-10 Novartis Ag Inhibidores de 2-morfolín-4-pirimidinas como inhibidores de fosfotidilinositol (PI) 3-quinasa y su uso en el tratamiento del cáncer.
WO2004052862A1 (ja) * 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 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
KR20050084271A (ko) 2002-12-12 2005-08-26 아방티 파르마 소시에테 아노님 아미노인다졸 유도체 및 키나제 억제제로서의 이의 용도
WO2004055004A1 (en) 2002-12-13 2004-07-01 Neurogen Corporation Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
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
CA2522430A1 (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
WO2005007672A2 (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
EP1656372B1 (en) 2003-07-30 2013-04-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
MXPA06001494A (es) * 2003-08-05 2007-05-11 Vertex Pharma Compuestos de piramidina condensados como inhibidores de canales ionicos gatillados por tension.
WO2005013982A1 (en) * 2003-08-06 2005-02-17 Vertex Pharmaceuticals Incorporated Aminotriazole compounds useful as inhibitors of protein kinases
US7652135B2 (en) * 2003-09-23 2010-01-26 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
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
AU2004289304A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Pyridine compounds
WO2005047268A2 (en) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
US7981900B2 (en) * 2003-12-03 2011-07-19 Ym Biosciences Australia Pty Ltd 2-phenyl pyrimidines which are tubulin inhibitors
CA2548172A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
WO2005056552A1 (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
GEP20084439B (en) 2004-01-23 2008-07-25 Amgen Inc Nitrogen-containing heterocyclic derivatives and pharmaceutical use thereof
JP2007518823A (ja) 2004-01-23 2007-07-12 アムゲン インコーポレイテッド キノリン、キナゾリン、ピリジン、及びピリミジン化合物と炎症、血管新生、及び癌に対する治療におけるそれら化合物の用途
US7534798B2 (en) 2004-02-11 2009-05-19 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2005100340A2 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyridines as potassium ion channel modulators
JP2007533753A (ja) * 2004-04-23 2007-11-22 タケダ サン ディエゴ インコーポレイテッド インドール誘導体及びキナーゼ阻害剤としてのその使用
US7793137B2 (en) 2004-10-07 2010-09-07 Cisco Technology, Inc. Redundant power and data in a wired data telecommunincations network
WO2005111039A2 (en) 2004-05-14 2005-11-24 Millennium Pharmaceuticals, Inc. Compounds and methods for inhibiting mitotic progression by inhibition of aurora kinase
EP1604988A1 (en) * 2004-05-18 2005-12-14 Sanofi-Aventis Deutschland GmbH Pyridazinone derivatives, methods for producing them and their use as pharmaceuticals
EP1598348A1 (en) * 2004-05-18 2005-11-23 Aventis Pharma Deutschland GmbH Novel pyridazinone derivatives as inhibitors of CDK2
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
JP2008510734A (ja) * 2004-08-18 2008-04-10 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
JP5006194B2 (ja) 2004-08-19 2012-08-22 ディーエスエム アイピー アセッツ ビー.ブイ. 高沸点の空気および/または温度感受性有用生成物の混合物の精留方法
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
JP2008538544A (ja) * 2004-09-23 2008-10-30 レディ ユーエス セラピューティックス, インコーポレイテッド 新規ピリミジン化合物、それらの調製のためのプロセスおよびそれらを含む組成物
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
AR052771A1 (es) 2004-09-30 2007-04-04 Tibotec Pharm Ltd Pirimidinas biciclicas inhibidoras del vhc
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
WO2006050359A2 (en) 2004-11-02 2006-05-11 Northwestern University Pyridazine compounds and methods
MX2007005247A (es) 2004-11-02 2008-03-13 Univ Northwestern Compuestos de piridazina, composiciones y metodos.
RU2007122485A (ru) 2004-11-17 2008-12-27 Мийкана Терапьютикс Ингибиторы киназы
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
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
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
PT1856135E (pt) 2005-01-19 2010-02-26 Rigel Pharmaceuticals Inc Pró-fármacos de compostos 2,4-pirimidinodiamina e suas utilizações
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
WO2006081230A2 (en) * 2005-01-26 2006-08-03 Schering Corporation 3-(indazol-5-yl)-(1,2, 4) triazine derivatives and related compounds as protein kinase inhibitors for the treatment of cancer
PT1846394E (pt) 2005-02-04 2012-01-05 Astrazeneca Ab Derivados de pirazolilaminopiridina úteis como inibidores da quinase
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
BRPI0607455A2 (pt) * 2005-02-16 2009-09-01 Astrazeneca Ab composto, processo para a preparação do mesmo, uso de um composto, e composição farmacêutica
EP1863797A1 (en) * 2005-03-23 2007-12-12 AstraZeneca AB 2-AZETIDINYL-4-(lH-PYRAZOL-3-YLAMINO)PYRIMIDINES AS INHIBITORS OF INSULIN-LIKE GROWTH FACTOR-I RECEPTOR ACTIVITY
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
MX2007011850A (es) 2005-03-25 2007-10-03 Tibotec Pharm Ltd Inhibidores heterobiciclicos de virus de hepatitis c.
ATE404554T1 (de) * 2005-04-05 2008-08-15 Astrazeneca Ab Pyrimidinderivate zur verwendung als antikrebsmittel
GB0507347D0 (en) * 2005-04-12 2005-05-18 Astrazeneca Ab Chemical compounds
BRPI0608178A2 (pt) 2005-04-14 2009-11-17 Hoffmann La Roche derivados de aminopirazol, sua fabricação, composição farmacêutica e uso como agentes farmacêuticos
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
US7928126B2 (en) 2005-04-28 2011-04-19 Mitsubishi Tanabe Pharma Corporation Cyanopyridine derivative and use thereof as medicine
EP1885369B1 (en) 2005-05-04 2015-09-23 Evotec AG Fused heterocyclic compounds, and compositions and uses thereof
US20080207594A1 (en) 2005-05-04 2008-08-28 Davelogen Aktiengesellschaft Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders
US20080194606A1 (en) * 2005-05-05 2008-08-14 Astrazeneca Pyrazolyl-Amino-Substituted Pyrimidines and Their Use in the Treatment of Cancer
AR056347A1 (es) 2005-05-12 2007-10-03 Tibotec Pharm Ltd Uso de compuestos de pteridina para fabricar medicamentos y composiciones farmaceuticas
EP1899323A2 (en) 2005-05-16 2008-03-19 AstraZeneca AB Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
EP1899332A1 (en) 2005-06-24 2008-03-19 Gilead Sciences, Inc. 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.
JP2009504771A (ja) * 2005-08-18 2009-02-05 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 ピラジンキナーゼ阻害剤
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
CN101316587B (zh) * 2005-09-30 2013-04-03 迈卡纳治疗股份有限公司 取代的吡唑化合物
KR20140025610A (ko) * 2005-09-30 2014-03-04 미카나 테라퓨틱스, 인크. 치환된 피라졸 화합물
ES2274712B1 (es) 2005-10-06 2008-03-01 Laboratorios Almirall S.A. Nuevos derivados imidazopiridina.
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
GB0520657D0 (en) * 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
EP1940389A2 (en) 2005-10-21 2008-07-09 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
WO2007053596A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
JP5249771B2 (ja) * 2005-11-03 2013-07-31 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
EP1945632B1 (en) 2005-11-08 2013-09-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
WO2007075847A2 (en) * 2005-12-20 2007-07-05 Takeda Pharmaceutical Company Limited Glucokinase activators
KR20130041313A (ko) 2006-01-17 2013-04-24 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
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
WO2007104035A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
PE20080145A1 (es) * 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
EP2007732B1 (en) * 2006-04-11 2011-11-23 Vertex Pharmaceuticals, Inc. Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
CA2650711A1 (en) 2006-04-28 2007-11-08 Northwestern University Compositions and treatments using pyridazine compounds and cholinesterase inhibitors
CA2651813A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
EP2026813A2 (en) 2006-05-09 2009-02-25 Braincells, Inc. 5 ht receptor mediated neurogenesis
PE20080993A1 (es) 2006-06-27 2008-10-06 Takeda Pharmaceutical Compuestos ciclicos fusionados como moduladores del receptor gpr40
MX2008016523A (es) * 2006-06-30 2009-01-19 Astrazeneca Ab Derivados de pirimidina utiles en el tratamiento de cancer.
CA2656290A1 (en) * 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
UA95641C2 (en) * 2006-07-06 2011-08-25 Эррей Биофарма Инк. Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
JP5268904B2 (ja) * 2006-07-06 2013-08-21 アレイ バイオファーマ、インコーポレイテッド Aktプロテインキナーゼ阻害剤としてのシクロペンタ[d]ピリミジン
US8338435B2 (en) 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
EP2068872A1 (en) 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
AU2007299920A1 (en) * 2006-09-19 2008-03-27 Braincells, Inc. PPAR Mediated Modulation of Neurogenesis
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EA200970361A1 (ru) 2006-10-09 2010-02-26 Такеда Фармасьютикал Компани Лимитед Ингибиторы киназы
JP2010505961A (ja) * 2006-10-09 2010-02-25 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
CN101573352A (zh) 2006-10-21 2009-11-04 艾博特股份有限两合公司 杂环化合物和其作为糖原合酶激酶3抑制剂的用途
JP2010509231A (ja) * 2006-11-02 2010-03-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼの阻害剤として有用なアミノピリジンおよびアミノピリミジン
MX2009006690A (es) * 2006-12-19 2009-07-31 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
WO2008077650A1 (en) 2006-12-26 2008-07-03 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines useful for treating viral infections
WO2008077649A1 (en) 2006-12-26 2008-07-03 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines useful for treating viral infectons
KR20090108124A (ko) 2007-02-06 2009-10-14 노파르티스 아게 Pi 3-키나제 억제제 및 그의 사용 방법
US20100204230A1 (en) * 2007-02-12 2010-08-12 Peter Blurton Piperazine derivatives for treatment of ad and related conditions
EP2120573A4 (en) * 2007-02-12 2011-05-25 Merck Sharp & Dohme DERIVATIVES OF PIPERIDINE
TW200901975A (en) 2007-03-05 2009-01-16 Kyowa Hakko Kogyo Kk Pharmaceutical composition
EP2134709A1 (en) * 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
CA2680029A1 (en) * 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
ES2435997T3 (es) * 2007-03-09 2013-12-26 Vertex Pharmaceuticals, Inc. Aminopirimidinas útiles como inhibidores de las proteínas cinasas
MX2009011059A (es) 2007-04-13 2009-11-26 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasas.
US20100204246A1 (en) * 2007-04-18 2010-08-12 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo (4,5-b) pyridine derivatives and their use for the treatment of cancer
AU2008247594A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247595A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247592A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
ATE521609T1 (de) * 2007-05-04 2011-09-15 Astrazeneca Ab Aminothiazolylpyrimidinderivate und ihre verwendung bei der behandlung von krebs
UA99459C2 (en) 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
AU2008257044A1 (en) * 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
JP2010529193A (ja) * 2007-06-11 2010-08-26 ミイカナ セラピューティクス インコーポレイテッド 置換ピラゾール化合物
US8242150B2 (en) * 2007-06-13 2012-08-14 Merck Sharp & Dohme Corp. Triazole derivatives for treating alzheimer'S disease and related conditions
US7956190B2 (en) 2007-06-25 2011-06-07 Hoffmann-La Roche Inc. Benzimidazole amido derivatives as kinase inhibitors
RU2486181C2 (ru) * 2007-07-05 2013-06-27 Эррэй Биофарма Инк. Пиримидилциклопентаны как ингибиторы акт-протеинкиназ
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
MX2009014013A (es) * 2007-07-05 2010-01-28 Array Biopharma Inc Pirimidil ciclopentanos como inhibidores de la proteina cinasa akt.
JP5282091B2 (ja) 2007-07-25 2013-09-04 ブリストル−マイヤーズ スクイブ カンパニー トリアジンキナーゼ阻害剤
CA2694499A1 (en) 2007-07-31 2009-02-05 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
TW200906818A (en) * 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
WO2009067166A2 (en) * 2007-11-20 2009-05-28 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
NZ702159A (en) 2007-12-07 2016-03-31 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
DK2639224T3 (en) 2007-12-07 2016-10-17 Vertex Pharma A process for the preparation of cycloalkylcarboxiamido-pyridinbenzoesyrer
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
JP5562865B2 (ja) 2007-12-17 2014-07-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Trpv1のイミダゾロ−、オキサゾロ−、及びチアゾロピリミジン・モジュレーター
ES2426092T3 (es) * 2008-01-09 2013-10-21 Array Biopharma, Inc. 5H-Ciclopenta[d]pirimidinas como inhibidores de proteínas cinasas AKT
JP5512545B2 (ja) 2008-01-09 2014-06-04 アレイ バイオファーマ、インコーポレイテッド Aktタンパク質キナーゼ阻害剤としてのピリミジルシクロペンタン類
MX2010009268A (es) 2008-02-21 2010-09-14 Schering Corp Compuestos que son inhibidores de erk.
NZ720282A (en) 2008-02-28 2017-12-22 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
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
CN102119157A (zh) * 2008-06-11 2011-07-06 阿斯利康(瑞典)有限公司 用于治疗癌症和骨髓增生性疾病的三环2,4-二氨基-l,3,5-三嗪衍生物
MX2010013726A (es) 2008-06-12 2011-01-14 Janssen Pharmaceutica Nv Moduladores de diamino-piridina, pirimidina, y piridazina del receptor h4 de histamina.
US20110269758A1 (en) * 2008-07-03 2011-11-03 Merck Patent Gmbh Naphthyridinones as protein kinase inhibitors
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
AR073354A1 (es) 2008-07-31 2010-11-03 Genentech Inc Compuestos de pirimidina, composiciones farmaceuticas y su uso en el tratamiento del cancer.
WO2010019392A1 (en) * 2008-08-13 2010-02-18 Merck Sharp & Dohme Corp. Purine derivatives for treatment of alzheimer's disease
KR20110050549A (ko) * 2008-09-03 2011-05-13 버텍스 파마슈티칼스 인코포레이티드 공-결정 및 이를 포함하는 제약 제제
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
TW201018693A (en) * 2008-09-30 2010-05-16 Astrazeneca Ab Chemical compounds 496-1p
CA2744343A1 (en) * 2008-11-19 2010-05-27 Renovis, Inc. 6, 7 -dihydro- 5h- pyrrolo [3, 4-d] pyrimidin-4-yl] -quinolin-3 -ylamine compounds useful as faah modulators and uses thereof
KR101048448B1 (ko) 2008-11-21 2011-07-11 한국화학연구원 신규 피라졸로[4,3-b]피리딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
ME02337B (me) 2009-02-05 2016-06-20 Takeda Pharmaceuticals Co Jedinjenja piridazinona
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
DK2401267T3 (en) * 2009-02-27 2014-03-10 Ambit Biosciences Corp JAK-kinase modulating quinazoline derivatives AND THEIR APPLICATION IN PROCESSES
EP2406236A4 (en) * 2009-03-09 2013-07-24 Surface Logix Inc INHIBITORS OF RHO KINASE
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
WO2010111057A1 (en) * 2009-03-24 2010-09-30 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
EP2411011A4 (en) * 2009-03-24 2012-08-15 Msd Kk NEW AMINO-PYRIDINE DERIVATIVES WITH SELECTIVE AURORA A INHIBITION
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
BRPI1010881A2 (pt) * 2009-06-08 2016-05-31 California Capital Equity Llc derivados de triazina e suas aplicações terapêuticas.
WO2010144522A1 (en) * 2009-06-09 2010-12-16 Abraxis Bioscience, Llc Ureidophenyl substituted triazine derivatives and their therapeutical applications
JP5785940B2 (ja) * 2009-06-09 2015-09-30 アブラクシス バイオサイエンス, エルエルシー トリアジン誘導体類及びそれらの治療応用
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
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
MX2012009378A (es) * 2010-02-11 2012-09-12 Univ Vanderbilt Compuestos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno y pirazolotiazol como potenciadores alostericos mglur4, composiciones y metodos para tratar disfunciones neurologicas.
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
RU2528386C2 (ru) 2010-05-21 2014-09-20 Кемилиа Аб Новые производные пиримидина
RS54865B1 (sr) 2010-06-04 2016-10-31 Hoffmann La Roche Derivati aminopirimidina kao modulatori lrrk2
US20110319409A1 (en) * 2010-06-23 2011-12-29 Cox Christopher D 7-aza-quinazoline pde10 inhibitors
EP2611789A1 (en) 2010-09-01 2013-07-10 Ambit Biosciences Corporation Quinazoline compounds and methods of use thereof
US9266855B2 (en) 2010-09-27 2016-02-23 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
SG189043A1 (en) 2010-11-10 2013-05-31 Hoffmann La Roche Pyrazole aminopyrimidine derivatives as lrrk2 modulators
EP2651404B1 (en) * 2010-12-14 2015-10-14 Electrophoretics Limited Casein kinase 1delta (ck1delta) inhibitors
WO2012085815A1 (en) 2010-12-21 2012-06-28 Novartis Ag Bi-heteroaryl compounds as vps34 inhibitors
US9090592B2 (en) 2010-12-30 2015-07-28 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
WO2012101654A2 (en) * 2011-01-25 2012-08-02 Sphaera Pharma Pvt. Ltd Novel triazine compounds
ES2587864T3 (es) 2011-03-24 2016-10-27 Noviga Research Ab Derivados de pirimidina
ES2657750T3 (es) 2011-04-01 2018-03-06 Genentech, Inc. Combinación de compuesto inhibidor de AKT y vemurafenib para su uso en tratamientos terapéuticos
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
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
KR20140062079A (ko) 2011-08-25 2014-05-22 에프. 호프만-라 로슈 아게 세린/트레오닌 pak1 억제제
MX362494B (es) 2011-09-14 2019-01-21 Samumed Llc Indazol-3-carboxamidas y su uso como inhibidores de la trayectoria de señalizacion de wnt/b-catenina.
ES2575710T3 (es) 2011-09-22 2016-06-30 Pfizer Inc Derivados de pirrolopirimidina y purina
GEP20166432B (en) 2011-09-27 2016-02-10 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
US8815877B2 (en) 2011-12-22 2014-08-26 Genentech, Inc. Serine/threonine kinase inhibitors
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
CN104334545A (zh) * 2012-03-16 2015-02-04 埃克希金医药品有限公司 3,5-二氨基吡唑激酶抑制剂
WO2013140148A1 (en) * 2012-03-19 2013-09-26 Imperial Innovations Limited Quinazoline compounds and their use in therapy
US20130303519A1 (en) 2012-03-20 2013-11-14 Millennium Pharmaceuticals, Inc. Methods of treating cancer using aurora kinase inhibitors
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
BR112014026703B1 (pt) 2012-04-24 2022-10-25 Vertex Pharmaceuticals Incorporated Inibidores de dna-pk e seus usos, composição farmacêutica e seus usos, e método de sensibilização de uma célula
EP2844658B1 (en) * 2012-05-03 2019-03-20 Genentech, Inc. Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease
KR102091894B1 (ko) * 2012-05-03 2020-03-20 제넨테크, 인크. Lrrk2 조절제로서의 피라졸 아미노피리미딘 유도체
CN104797267A (zh) 2012-06-26 2015-07-22 德玛医药 使用卫康醇、二乙酰二脱水卫矛醇、二溴卫矛醇或类似物或其衍生物治疗具有基因多型性或ahi1失调或突变患者的抗酪氨酸激酶抑制剂的恶性肿瘤的方法
SG11201502301YA (en) 2012-09-28 2015-04-29 Cancer Rec Tech Ltd 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
CA2891655A1 (en) * 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
EA035349B1 (ru) 2012-11-21 2020-05-29 ПиТиСи ТЕРАПЬЮТИКС, ИНК. ЗАМЕЩЕННЫЕ ПИРИМИДИНОВЫЕ ОБРАТНЫЕ ИНГИБИТОРЫ Bmi-1
WO2014110086A2 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
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
EP2951170B1 (en) 2013-02-04 2018-10-24 Janssen Pharmaceutica NV Flap modulators
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
PT3527563T (pt) 2013-03-12 2021-12-09 Vertex Pharma Inibidores de adn-pk
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
CN105764502A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群及其类似物及衍生物的治疗益处的组合方法
AU2013399092A1 (en) 2013-08-30 2016-03-17 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
LT3052096T (lt) 2013-10-03 2018-04-10 Kura Oncology, Inc. Erk inhibitoriai ir jų panaudojimo būdai
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
ES2705342T3 (es) 2013-10-17 2019-03-22 Vertex Pharma Co-cristales de (S)-N-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolin-4-carboxamida y derivados deuterados de la misma como inhibidores de DNA-PK
KR102280372B1 (ko) 2013-11-12 2021-07-22 버텍스 파마슈티칼스 인코포레이티드 Cftr 매개된 질환 치료용 약제학적 조성물의 제조 방법
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
WO2015076800A1 (en) * 2013-11-21 2015-05-28 Ptc Therapeutics, Inc. Substituted pyridine and pyrazine bmi-1 inhibitors
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
CN104926795B (zh) * 2014-03-17 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
TWI675836B (zh) 2014-03-25 2019-11-01 美商伊格尼塔公司 非典型蛋白質激酶c之氮雜喹唑啉抑制劑
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
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
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
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
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
HUE055423T2 (hu) 2014-11-18 2021-11-29 Vertex Pharma Eljárás nagy áteresztõképességû tesztelõ nagy teljesítményû folyadék-kromatográfia elvégzésére
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
TWI704151B (zh) * 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
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
AU2016247858B2 (en) 2015-04-17 2020-10-15 Ludwig Institute For Cancer Research Ltd. PLK4 inhibitors
US10118904B2 (en) 2015-06-05 2018-11-06 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of Demyelinating Diseases
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
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
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
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles 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
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
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
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
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
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
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023996A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
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
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
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
US10226448B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]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
EP3371187A4 (en) 2015-11-06 2019-09-04 Samumed, LLC 2- (1H-INDAZOLE-3-YL) -3H-IMIDAZO [4,5-C] PYRIDINE AND ITS USE AS AN INHIBITOR OF INHIBITOR
GB201604647D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
JP7010851B2 (ja) 2016-06-01 2022-02-10 バイオスプライス セラピューティクス インコーポレイテッド N-(5-(3-(7-(3-フルオロフェニル)-3H-イミダゾ[4,5-c]ピリジン-2-イル)-1H-インダゾール-5-イル)ピリジン-3-イル)-3-メチルブタンアミドを調製するための方法
WO2018064092A1 (en) 2016-09-27 2018-04-05 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors
MX2019004616A (es) 2016-10-21 2019-11-21 Samumed Llc Métodos de uso de indazol-3-carboxamidas y su uso como inhibidores de la ruta de señalización de wnt/b-catenina.
US10870630B2 (en) 2016-11-01 2020-12-22 Merck Sharp & Dohme Corp. Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
IT201700047189A1 (it) * 2017-05-02 2018-11-02 Fondazione St Italiano Tecnologia Composti e composizioni per il trattamento di cancro, disordini della retina e cardiomiopatie
AR112027A1 (es) * 2017-06-15 2019-09-11 Biocryst Pharm Inc Inhibidores de alk 2 quinasa que contienen imidazol
JP7311228B2 (ja) 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Rho-関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
WO2019000683A1 (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
JP2020525525A (ja) * 2017-06-30 2020-08-27 ベイジン タイド ファーマシューティカル カンパニー リミテッドBeijing Tide Pharmaceutical Co., Ltd. Rho−関連プロテインキナーゼ阻害剤、rho−関連プロテインキナーゼ阻害剤を含む医薬組成物、当該医薬組成物の調製方法及び使用
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
LT3672965T (lt) 2017-10-27 2022-10-10 Theravance Biopharma R&D Ip, Llc Pirimidino junginys, kaip jak kinazės inhibitorius
GB201801226D0 (en) * 2018-01-25 2018-03-14 Redx Pharma Plc Modulators of Rho-associated protein kinase
WO2020005935A1 (en) * 2018-06-25 2020-01-02 Kadmon Corporation, Llc Glucose uptake inhibitors
AU2019340402A1 (en) 2018-08-17 2021-03-25 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
JOP20210172A1 (ar) * 2018-12-27 2023-01-30 Les Laboratoires Servier Sas مثبطات أزا-غير متجانسة ثنائية الحلقة لـ mat2a وطرق الاستخدام لعلاج السرطان
AU2020204717A1 (en) * 2019-01-03 2021-06-10 University Of Pittsburgh - Of The Commonwealth System Of 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
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
CA3133460A1 (en) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
CN113518779B (zh) 2019-03-28 2024-03-15 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
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
AU2020251621A1 (en) 2019-03-29 2021-11-04 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
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
JP7470713B2 (ja) 2019-04-24 2024-04-18 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 Jakキナーゼ阻害剤としてのエステルおよびカルボナートピリミジン化合物
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
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US20220204512A1 (en) 2019-05-24 2022-06-30 Jiangsu Hengrui Medicine Co., Ltd. Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines
WO2020243519A1 (en) * 2019-05-29 2020-12-03 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
JP2023509260A (ja) 2019-08-14 2023-03-08 インサイト・コーポレイション Cdk2阻害剤としてのイミダゾリルピリミジニルアミン化合物
CN114302876A (zh) * 2019-09-06 2022-04-08 英夫拉索姆有限公司 Nlrp3抑制剂
BR112022006394A2 (pt) * 2019-10-02 2022-07-26 Tolremo Therapeutics Ag Derivados heterocíclicos, composições farmacêuticas e seu uso no tratamento ou melhora do câncer
AR120184A1 (es) 2019-10-11 2022-02-02 Incyte Corp Aminas bicíclicas como inhibidoras de la cdk2
KR20220153595A (ko) * 2020-02-26 2022-11-18 재규어 테라퓨틱스 피티이 리미티드 AhR 신호전달의 조절에 유용한 피리도피리미딘 유도체
EP4126839A4 (en) * 2020-03-27 2024-04-17 Dong-A ST Co., Ltd. AMINOPYRIMIDINE DERIVATIVES AND THEIR USE AS ARYL HYDROCARBON RECEPTOR MODULATORS
DK4182308T3 (da) 2020-07-15 2024-10-21 Chiesi Farm Spa Pyridazinylamino-derivater som ALK5-inhibitorer
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
CN116437915A (zh) 2020-09-29 2023-07-14 江苏恒瑞医药股份有限公司 一种吡咯并杂环类衍生物的晶型及其制备方法
WO2022107919A1 (ko) * 2020-11-19 2022-05-27 주식회사 보로노이 N을 포함하는 헤테로아릴 유도체 및 이를 유효성분으로 포함하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
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
JP2024534510A (ja) 2021-09-21 2024-09-20 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ Alk5阻害剤としてのピリダジニルアミノ誘導体
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
CN118541362A (zh) 2022-01-11 2024-08-23 奇斯药制品公司 作为alk5抑制剂的哒嗪基氨基衍生物
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
JP3588116B2 (ja) 1993-10-01 2004-11-10 ノバルティス アクチェンゲゼルシャフト 薬理活性のピリミジンアミン誘導体およびその製造方法
JPH10509708A (ja) 1994-11-10 1998-09-22 コア セラピューティクス,インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
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
JPH11512390A (ja) 1995-09-01 1999-10-26 シグナル ファーマシューティカルズ,インコーポレイテッド ピリミジンカルボキシレートおよび関連化合物ならびに炎症状態を処置するための方法
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
WO1997020820A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
AR007857A1 (es) * 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
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
EP0929553B1 (en) * 1996-10-02 2005-03-16 Novartis AG Pyrimidine derivatives and processes for the preparation thereof
WO1998016502A1 (en) 1996-10-11 1998-04-23 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
CA2306692C (en) 1997-10-10 2010-09-21 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
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
NZ506417A (en) 1998-02-17 2003-05-30 Tularik Inc Anti-viral pyrimidine derivatives
CN1297354A (zh) 1998-03-16 2001-05-30 西托维亚公司 二肽卡斯帕酶抑制剂及其用途
WO1999062518A1 (en) * 1998-06-02 1999-12-09 Osi Pharmaceuticals, Inc. PYRROLO[2,3d]PYRIMIDINE COMPOSITIONS AND THEIR USE
DE69919707T2 (de) 1998-06-19 2005-09-01 Chiron Corp., Emeryville Glycogen synthase kinase 3 inhibitoren
WO2000011003A1 (en) * 1998-08-21 2000-03-02 Du Pont Pharmaceuticals Company ISOXAZOLO[4,5-d]PYRIMIDINES AS CRF ANTAGONISTS
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
ES2241324T3 (es) * 1998-10-08 2005-10-16 Astrazeneca Ab Derivados de quinazolina.
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
WO2000042029A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company 1-heterocycle substituted diarylamines
PT1171465E (pt) 1999-03-29 2004-12-31 Uutech Ltd Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes
JP4673977B2 (ja) 1999-03-30 2011-04-20 ノバルティス アーゲー 炎症性疾患治療用フタラジン誘導体
AU781849C (en) 1999-06-17 2006-03-02 Synta Pharmaceuticals Corp. Inhibitors of IL-12 production
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
JP2001042764A (ja) 1999-08-04 2001-02-16 Sony Corp 地図表示装置
JP2003531103A (ja) 1999-08-12 2003-10-21 バーテックス ファーマシューティカルズ インコーポレイテッド c−JUNN−末端キナーゼ(JNK)および他のタンパク質キナーゼの阻害剤
AU770600B2 (en) 1999-10-07 2004-02-26 Amgen, Inc. Triazine kinase inhibitors
CN1402720A (zh) 1999-11-30 2003-03-12 辉瑞产品公司 用作免疫抑制剂的2,4-二氨基嘧啶化合物
IL149935A0 (en) * 1999-12-02 2002-11-10 Osi Pharm Inc Compounds specific to adenosine a1, a2a and a3 receptors and uses thereof
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
JP4794793B2 (ja) 1999-12-28 2011-10-19 ファーマコペイア, インコーポレイテッド N−ヘテロ環TNF−α発現阻害剤
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
AU782775B2 (en) 2000-02-05 2005-08-25 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of ERK
EP1257546A1 (en) * 2000-02-17 2002-11-20 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
ES2240446T3 (es) 2000-04-03 2005-10-16 Vertex Pharma Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
MXPA02010222A (es) 2000-04-18 2003-05-23 Agouron Pharma Pirazoles para inhibir proteina cinasa.
MXPA02011974A (es) * 2000-06-28 2004-09-06 Astrazeneca Ab Derivados de quinazolina sustituidos y su uso como inhibidores.
BR0112540A (pt) 2000-07-21 2003-06-24 Schering Corp Peptìdios como inibidores da ns-3-serina protease do vìrus da hepatite c
JP2004507526A (ja) 2000-08-31 2004-03-11 ファイザー・プロダクツ・インク ピラゾール誘導体及びそのプロテインキナーゼ阻害剤としての使用
US6495582B1 (en) 2000-09-15 2002-12-17 Vertex Pharmaceuticals Incorporated Isoxazole compositions useful as inhibitors of ERK
US7473691B2 (en) * 2000-09-15 2009-01-06 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
US6610677B2 (en) * 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317448B2 (en) * 2000-09-15 2011-05-04 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2004509876A (ja) 2000-09-20 2004-04-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング 4−アミノ−キナゾリン
DE10061863A1 (de) * 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
AU2002228922A1 (en) 2000-12-12 2002-06-24 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
US6716851B2 (en) * 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
JP4160395B2 (ja) * 2000-12-21 2008-10-01 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なピラゾール化合物
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
EP1373257B9 (en) 2001-03-29 2008-10-15 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
WO2002085909A1 (en) 2001-04-20 2002-10-31 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
JP4316893B2 (ja) * 2001-05-16 2009-08-19 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 Srcおよび他のプロテインキナーゼのインヒビター
MXPA03010961A (es) * 2001-05-31 2004-02-27 Vertex Pharma Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
JP4523271B2 (ja) * 2001-06-01 2010-08-11 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 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化合物
EP1399440B1 (en) 2001-06-15 2009-06-03 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors
ATE337312T1 (de) 2001-07-03 2006-09-15 Vertex Pharma 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
US20030199526A1 (en) * 2001-12-07 2003-10-23 Deborah Choquette Pyrimidine-based compounds useful as GSK-3 inhibitors
PL372198A1 (en) * 2002-02-06 2005-07-11 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
DE60332604D1 (de) * 2002-03-15 2010-07-01 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
US7863282B2 (en) 2003-03-14 2011-01-04 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US7179826B2 (en) * 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
ATE466580T1 (de) * 2002-03-15 2010-05-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
DE60314603T2 (de) * 2002-03-15 2008-02-28 Vertex Pharmaceuticals Inc., Cambridge Zusammensetzungen brauchbar als protein-kinase-inhibitoren
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
US7304061B2 (en) * 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
AU2003247959B2 (en) * 2002-07-09 2010-07-29 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
EP1532145B1 (en) 2002-08-02 2006-09-13 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
DE60316013T2 (de) * 2002-11-04 2008-05-29 Vertex Pharmaceuticals Inc., Cambridge Heteroaryl-pyrimidinderivate als jak-inhibitoren
WO2004072063A1 (en) * 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
US7276502B2 (en) * 2003-03-25 2007-10-02 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
AU2004225965A1 (en) * 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
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
JP2009504771A (ja) 2005-08-18 2009-02-05 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 ピラジンキナーゼ阻害剤
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
KR20140025610A (ko) 2005-09-30 2014-03-04 미카나 테라퓨틱스, 인크. 치환된 피라졸 화합물
JP5249771B2 (ja) 2005-11-03 2013-07-31 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
ATE508126T1 (de) 2005-11-16 2011-05-15 Vertex Pharma Als kinaseinhibitoren geeignete aminopyrimidine
JP2010509231A (ja) 2006-11-02 2010-03-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼの阻害剤として有用なアミノピリジンおよびアミノピリミジン
MX2009006690A (es) 2006-12-19 2009-07-31 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
CA2680029A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
ES2435997T3 (es) 2007-03-09 2013-12-26 Vertex Pharmaceuticals, Inc. Aminopirimidinas útiles como inhibidores de las proteínas cinasas
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
JP2010522194A (ja) 2007-03-20 2010-07-01 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 キナーゼ阻害薬として有用なアミノピリミジン
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
AU2008247592A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
AU2008247594A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247595A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008257044A1 (en) 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors

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