JP6039683B2 - ピラジンキナーゼ阻害剤 - Google Patents
ピラジンキナーゼ阻害剤 Download PDFInfo
- Publication number
- JP6039683B2 JP6039683B2 JP2014543599A JP2014543599A JP6039683B2 JP 6039683 B2 JP6039683 B2 JP 6039683B2 JP 2014543599 A JP2014543599 A JP 2014543599A JP 2014543599 A JP2014543599 A JP 2014543599A JP 6039683 B2 JP6039683 B2 JP 6039683B2
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- JP
- Japan
- Prior art keywords
- amino
- alkyl
- mmol
- ylamino
- 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.)
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- 0 CC(CCC1N)CC1Nc1cnc(C(N)=O)c(N*)n1 Chemical compound CC(CCC1N)CC1Nc1cnc(C(N)=O)c(N*)n1 0.000 description 10
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Classifications
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- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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| NZ589315A (en) | 2008-04-16 | 2012-11-30 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors |
| US9359308B2 (en) | 2011-11-23 | 2016-06-07 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
| US20130310387A1 (en) | 2012-05-16 | 2013-11-21 | Novartis Ag | Monocyclic Heteroaryl Cycloalkyldiamine Derivatives |
| WO2014060371A1 (en) * | 2012-10-19 | 2014-04-24 | F. Hoffmann-La Roche Ag | Inhibitors of syk |
| CA2932609A1 (en) * | 2013-12-05 | 2015-06-11 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| WO2015138273A1 (en) * | 2014-03-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
| CZ306322B6 (cs) | 2014-12-17 | 2016-11-30 | Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové | Substituovaný 2-(2-fenylhydrazinyl)pyrazin, způsob jeho přípravy, jeho použití a farmaceutický přípravek ho obsahující |
| MA42623A (fr) * | 2015-06-02 | 2018-06-20 | Pharmacyclics Llc | Inhibiteurs de la tyrosine kinase de bruton |
| EP3801525A4 (en) * | 2018-06-08 | 2022-03-23 | The General Hospital Corporation | PROLYL TRNA SYNTHETASE INHIBITORS |
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Family Cites Families (141)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5728536A (en) | 1993-07-29 | 1998-03-17 | St. Jude Children's Research Hospital | Jak kinases and regulation of Cytokine signal transduction |
| US6004981A (en) | 1996-03-08 | 1999-12-21 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| US5691364A (en) * | 1995-03-10 | 1997-11-25 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| WO1996028427A1 (en) | 1995-03-10 | 1996-09-19 | Berlex Laboratories, Inc. | Benzamidine derivatives their preparation and their use as anti-coagulants |
| US6316635B1 (en) | 1995-06-07 | 2001-11-13 | Sugen, Inc. | 2-indolinone derivatives as modulators of protein kinase activity |
| US5811428A (en) | 1995-12-18 | 1998-09-22 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions |
| AU726522B2 (en) | 1995-09-01 | 2000-11-09 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions |
| US6696448B2 (en) | 1996-06-05 | 2004-02-24 | Sugen, Inc. | 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors |
| US6008234A (en) | 1996-09-12 | 1999-12-28 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants |
| DE69717474T2 (de) | 1996-09-12 | 2003-06-26 | Schering Ag | Durch cyclische aminosäuren oder cyclische hydroxysäuren substituierte benzamidinderivate und deren verwendung als antikoagulantien |
| US6004985A (en) | 1996-10-09 | 1999-12-21 | Berlex Laboratories, Inc. | Thio acid derived monocylic N-heterocyclics as anticoagulants |
| US6316429B1 (en) | 1997-05-07 | 2001-11-13 | Sugen, Inc. | Bicyclic protein kinase inhibitors |
| US6486185B1 (en) | 1997-05-07 | 2002-11-26 | Sugen, Inc. | 3-heteroarylidene-2-indolinone protein kinase inhibitors |
| GB9718913D0 (en) | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| US6133305A (en) | 1997-09-26 | 2000-10-17 | Sugen, Inc. | 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity |
| US6686364B2 (en) | 1997-12-08 | 2004-02-03 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| AU1507199A (en) | 1997-12-15 | 1999-07-05 | Yamanouchi Pharmaceutical Co., Ltd. | Novel pyrimidine-5-carboxamide derivatives |
| EP1091739A1 (en) | 1998-06-30 | 2001-04-18 | Parker Hughes Institute | Method for inhibiting c-jun expression using jak-3 inhibitors |
| ATE292121T1 (de) | 1998-08-21 | 2005-04-15 | Parker Hughes Inst | Chinazolinderivate |
| US6262088B1 (en) | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| US6127376A (en) | 1998-12-04 | 2000-10-03 | Berlex Laboratories, Inc. | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| US6841567B1 (en) | 1999-02-12 | 2005-01-11 | Cephalon, Inc. | Cyclic substituted fused pyrrolocarbazoles and isoindolones |
| US6624171B1 (en) | 1999-03-04 | 2003-09-23 | Smithkline Beecham Corporation | Substituted aza-oxindole derivatives |
| GB9904995D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Substituted aza-oxindole derivatives |
| US6080747A (en) | 1999-03-05 | 2000-06-27 | Hughes Institute | JAK-3 inhibitors for treating allergic disorders |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| US7125875B2 (en) | 1999-04-15 | 2006-10-24 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
| WO2000075113A1 (en) | 1999-06-09 | 2000-12-14 | Yamanouchi Pharmaceutical Co., Ltd. | Novel heterocyclic carboxamide derivatives |
| AU5108000A (en) * | 1999-06-10 | 2001-01-02 | Yamanouchi Pharmaceutical Co., Ltd. | Novel nitrogen-contaiing heterocyclic derivatives or salts thereof |
| GB9918035D0 (en) | 1999-07-30 | 1999-09-29 | Novartis Ag | Organic compounds |
| WO2001045641A2 (en) | 1999-11-30 | 2001-06-28 | Parker Hughes Institute | Inhibitors of thrombin induced platelet aggregation |
| AU777911B2 (en) | 1999-12-10 | 2004-11-04 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| ES2245955T3 (es) | 1999-12-21 | 2006-02-01 | Sugen, Inc. | 7-aza-indolin-2-onas 4-sustituidas y su utilizacion como inhibidores de proteina-quinasa. |
| US20020065270A1 (en) | 1999-12-28 | 2002-05-30 | Moriarty Kevin Joseph | N-heterocyclic inhibitors of TNF-alpha expression |
| DE60129926T2 (de) | 2000-01-24 | 2008-06-19 | Genzyme Corp., Cambridge | Inhibitoren des jak/stat-weges und deren verwendung zur behandlung von allgemeiner primärer osteoarthritis |
| CA2396458C (en) | 2000-01-31 | 2006-12-05 | Pfizer Products Inc. | Pyrimidine carboxamides useful as inhibitors of pde4 isozymes |
| EP1196390A2 (en) | 2000-02-05 | 2002-04-17 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of erk |
| KR20010111298A (ko) | 2000-02-05 | 2001-12-17 | 버텍스 파마슈티칼스 인코포레이티드 | Erk의 억제제로서 유용한 피라졸 조성물 |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US6525051B2 (en) | 2000-03-27 | 2003-02-25 | Schering Aktiengesellschaft | N-heterocyclic derivatives as NOS inhibitors |
| US6608048B2 (en) | 2000-03-28 | 2003-08-19 | Wyeth Holdings | Tricyclic protein kinase inhibitors |
| AR028261A1 (es) | 2000-03-28 | 2003-04-30 | Wyeth Corp | Inhibidores triciclicos de la proteina quinasa |
| WO2001085700A2 (en) | 2000-05-08 | 2001-11-15 | Janssen Pharmaceutica N.V. | Hiv replication inhibiting pyrimidines and triazines |
| AP1911A (en) | 2000-06-26 | 2008-10-30 | Pfizer Prod Inc | Pyrrolo[2,3-d]pyrimidine compounds. |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| WO2002043735A1 (en) | 2000-11-29 | 2002-06-06 | Parker Hughes Institute | Inhibitors of thrombin induced platelet aggregation |
| US20020115173A1 (en) | 2000-12-11 | 2002-08-22 | Children's Medical Center Corporation | Short peptides from the 'A-region' of protein kinases which selectively modulate protein kinase activity |
| JP2004518669A (ja) | 2000-12-20 | 2004-06-24 | スージェン・インコーポレーテッド | 4−アリール置換インドリノン |
| CA2432000C (en) | 2000-12-21 | 2011-03-15 | Glaxo Group Limited | Pyrimidineamines as angiogenesis modulators |
| FR2818642B1 (fr) | 2000-12-26 | 2005-07-15 | Hoechst Marion Roussel Inc | Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilistion |
| AUPR279101A0 (en) | 2001-01-30 | 2001-02-22 | Cytopia Pty Ltd | Protein kinase signalling |
| EP1363702A4 (en) | 2001-01-30 | 2007-08-22 | Cytopia Pty Ltd | PROCESS FOR INHIBITING KINASES |
| SE0101675D0 (sv) | 2001-05-11 | 2001-05-11 | Astrazeneca Ab | Novel composition |
| JP4291135B2 (ja) | 2001-05-29 | 2009-07-08 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | Cdk阻害性ピリミジン、それらの製造および薬剤としての使用 |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| CA2450769A1 (en) | 2001-06-15 | 2002-12-27 | Vertex Pharmaceuticals Incorporated | 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors |
| US6433018B1 (en) | 2001-08-31 | 2002-08-13 | The Research Foundation Of State University Of New York | Method for reducing hypertrophy and ischemia |
| WO2003020698A2 (en) | 2001-09-06 | 2003-03-13 | Prochon Biotech Ltd. | Protein tyrosine kinase inhibitors |
| JP2005506982A (ja) | 2001-09-10 | 2005-03-10 | スージェン・インコーポレーテッド | キナーゼ阻害剤としての3−(4,5,6,7−テトラヒドロインドール−2−イルメチリデン)−2−インドリノン誘導体 |
| 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 |
| WO2003031438A1 (en) | 2001-10-10 | 2003-04-17 | Sugen, Inc. | 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors |
| GT200200234A (es) | 2001-12-06 | 2003-06-27 | Compuestos cristalinos novedosos | |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| US6998391B2 (en) | 2002-02-07 | 2006-02-14 | Supergen.Inc. | Method for treating diseases associated with abnormal kinase activity |
| WO2003066601A1 (en) | 2002-02-08 | 2003-08-14 | Smithkline Beecham Corporation | Pyrimidine compounds |
| CA2477505A1 (en) | 2002-03-01 | 2003-09-12 | Smithkline Beecham Corporation | Diamino-pyrimidines and their use as angiogenesis inhibitors |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| WO2003095448A1 (en) | 2002-05-06 | 2003-11-20 | Bayer Pharmaceuticals Corporation | Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders |
| JP4681302B2 (ja) | 2002-05-06 | 2011-05-11 | 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 | チアジアゾールまたはオキサジアゾール、およびこれらの、jakプロテインキナーゼのインヒビターとしての使用 |
| AU2003231880A1 (en) | 2002-05-30 | 2003-12-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of jak and cdk2 protein kinases |
| EP1515955A4 (en) | 2002-06-17 | 2006-05-03 | Smithkline Beecham Corp | CHEMICAL PROCESS |
| AU2003244098A1 (en) | 2002-06-28 | 2004-01-19 | Yamanouchi Pharmaceutical Co., Ltd. | Diaminopyrimidinecarboxa mide derivative |
| 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 |
| KR20050042478A (ko) | 2002-08-14 | 2005-05-09 | 버텍스 파마슈티칼스 인코포레이티드 | 프로테인 키나아제 억제제 및 이의 용도 |
| US7312227B2 (en) | 2002-11-01 | 2007-12-25 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| WO2004041814A1 (en) | 2002-11-04 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as jak inhibitors |
| AU2003286895A1 (en) | 2002-11-05 | 2004-06-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of jak and other protein kinases |
| CL2003002353A1 (es) | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| RS20050380A (sr) | 2002-11-21 | 2007-11-15 | Pfizer Products Inc., | Derivati 3-aminopiperidina i postupci njihove proizvodnje |
| KR20050086784A (ko) | 2002-11-26 | 2005-08-30 | 화이자 프로덕츠 인크. | 이식 거부반응의 치료 방법 |
| WO2004058749A1 (en) | 2002-12-18 | 2004-07-15 | Vertex Pharmaceuticals Incorporated | Benzisoxazole derivatives useful as inhibitors of protein kinases |
| ATE433447T1 (de) | 2003-02-20 | 2009-06-15 | Smithkline Beecham Corp | Pyrimiidinverbindungen |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| AU2004230841A1 (en) | 2003-04-03 | 2004-10-28 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| JP2006528629A (ja) | 2003-07-24 | 2006-12-21 | メルク エンド カムパニー インコーポレーテッド | チロシンキナーゼ阻害薬 |
| 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 |
| BRPI0413469A (pt) | 2003-08-14 | 2006-10-17 | Pfizer | derivados de piperazina para o tratamento de infecções por hiv |
| BR122019017579B8 (pt) | 2003-08-15 | 2021-07-27 | Novartis Ag | 2,4-pirimidinadiaminas, seus usos, combinação e composição farmacêutica |
| AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| US7189729B2 (en) | 2003-09-30 | 2007-03-13 | Irm Llc | Methods and compositions as protein kinase inhibitors |
| JP4874107B2 (ja) | 2003-10-03 | 2012-02-15 | ファイザー・インク | Hiv及び炎症の治療のためのccr5受容体拮抗活性を有するイミダゾピリジン置換トロパン誘導体 |
| DE10349423A1 (de) | 2003-10-16 | 2005-06-16 | Schering Ag | Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| ZA200602666B (en) | 2004-01-12 | 2007-09-26 | Cytopia Res Pty Ltd | Selective kinase inhibitors |
| KR101298967B1 (ko) | 2004-03-30 | 2013-09-02 | 버텍스 파마슈티칼스 인코포레이티드 | Jak 및 기타 단백질 키나제의 억제제로서 유용한 아자인돌 |
| GB0407723D0 (en) | 2004-04-05 | 2004-05-12 | Novartis Ag | Organic compounds |
| WO2005122294A1 (ja) | 2004-06-14 | 2005-12-22 | Nec Corporation | フィルム外装電気デバイス |
| CA2579017A1 (en) | 2004-09-10 | 2006-03-16 | Altana Pharma Ag | Roflumilast and syk inhibitor combination and methods of use thereof |
| AU2005281735A1 (en) | 2004-09-10 | 2006-03-16 | Nycomed Gmbh | Ciclesonide and syk inhibitor combination and methods of use thereof |
| DK1814878T3 (da) | 2004-11-24 | 2012-05-07 | Rigel Pharmaceuticals Inc | Spiro-2, 4-pyrimidindiamin-forbindelser og anvendelser deraf |
| PL1856135T3 (pl) | 2005-01-19 | 2010-05-31 | Rigel Pharmaceuticals Inc | Proleki związków 2,4-pirymidynodiaminy i ich zastosowanie |
| WO2007027238A2 (en) | 2005-05-03 | 2007-03-08 | Rigel Pharmaceuticals, Inc. | Jak kinase inhibitors and their uses |
| BRPI0617241A2 (pt) | 2005-10-13 | 2016-11-08 | Glaxo Group Ltd | composto ou um sal ou solvato do mesmo, composição farmacêutica, método para tratar uma doença ou condição mediada por atividade syk inadequada em um mamífero, e, uso de um composto ou um sal ou solvato farmaceuticamente aceitável do mesmo |
| WO2007046112A1 (en) | 2005-10-19 | 2007-04-26 | Suven Life Sciences Inc. | Arylthioether tryptamine derivatives as functional 5-ht6 ligands |
| EP1960372B1 (en) | 2005-12-15 | 2015-12-09 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| GB0526246D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| WO2007113254A1 (en) | 2006-03-30 | 2007-10-11 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-amido substituted pyrimidines |
| JP2009542604A (ja) | 2006-07-06 | 2009-12-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 4−ヘテロシクロアルキルピリミジン、それらの調製方法及び医薬としての使用 |
| KR20090031787A (ko) | 2006-07-21 | 2009-03-27 | 노파르티스 아게 | Jak 키나제 억제제로서의 2,4-디(아릴아미노)-피리미딘-5-카르복스아미드 화합물 |
| US20080076800A1 (en) | 2006-08-24 | 2008-03-27 | Huang Kenneth H | Benzene, Pyridine, and Pyridazine Derivatives |
| JP5512274B2 (ja) | 2006-10-23 | 2014-06-04 | セファロン、インク. | ALK阻害剤およびc−MET阻害剤としての2,4−ジアミノピリミジンの縮合二環式誘導体 |
| US20080139531A1 (en) | 2006-12-04 | 2008-06-12 | Alcon Manufacturing Ltd. | Use of connective tissue mast cell stabilizers to facilitate ocular surface re-epithelization and wound repair |
| KR20090094084A (ko) | 2006-12-29 | 2009-09-03 | 티보텍 파마슈티칼즈 리미티드 | Hiv를 억제하는 5,6-치환된 피리미딘 |
| KR20100015353A (ko) | 2007-04-02 | 2010-02-12 | 팔라우 파르마 에스에이 | Jak3 억제제로서의 피롤로피리미딘 유도체 |
| 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 |
| EP2157090A4 (en) | 2007-06-21 | 2011-09-07 | Taisho Pharmaceutical Co Ltd | PYRAZINAMIDE COMPOUND |
| JP2010538004A (ja) | 2007-08-28 | 2010-12-09 | アイアールエム・リミテッド・ライアビリティ・カンパニー | キナーゼ阻害剤としての2−ビフェニルアミノ−4−アミノピリミジン誘導体 |
| WO2009046840A1 (en) | 2007-10-12 | 2009-04-16 | Merck Patent Gmbh | Method and agent for refolding proteins |
| US20090270418A1 (en) * | 2008-01-09 | 2009-10-29 | Marianne Sloss | Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith |
| WO2009097541A1 (en) | 2008-02-01 | 2009-08-06 | Rich Products Corporation | Foam compositions |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| NZ589315A (en) | 2008-04-16 | 2012-11-30 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors |
| JP5802127B2 (ja) * | 2008-04-16 | 2015-10-28 | ポートラ ファーマシューティカルズ, インコーポレイテッド | Syk又はjakキナーゼ阻害剤としての2,6−ジアミノ−ピリミジン−5−イル−カルボキサミド類 |
| CN102066340B (zh) | 2008-04-16 | 2014-05-14 | 波托拉医药品公司 | 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物 |
| BRPI0910668A2 (pt) | 2008-04-22 | 2019-09-24 | Portola Pharmaceutiacals Inc | inibidores de proteína quinases |
| CA2737738A1 (en) * | 2008-09-18 | 2010-03-25 | Astellas Pharma Inc. | Heterocyclic carboxamide compounds |
| WO2010058846A1 (ja) | 2008-11-21 | 2010-05-27 | アステラス製薬株式会社 | 4,6-ジアミノニコチンアミド化合物 |
| KR101361027B1 (ko) | 2008-11-28 | 2014-02-11 | 코와 가부시키가이샤 | 피리딘-3-카르복시아미드 유도체 |
| CN102348707A (zh) | 2009-01-13 | 2012-02-08 | 葛兰素集团有限公司 | 作为syk激酶抑制剂的嘧啶甲酰胺衍生物 |
| WO2010129802A1 (en) | 2009-05-06 | 2010-11-11 | Portola Pharmaceuticals, Inc. | Inhibitors of jak |
| RS54552B1 (sr) | 2009-05-08 | 2016-06-30 | Astellas Pharma Inc. | Jedinjenje diamino heterocikličnog karboksamida |
| WO2012044936A1 (en) | 2010-09-30 | 2012-04-05 | Portola Pharmaceuticals, Inc. | Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide |
| EP2621489A1 (en) | 2010-09-30 | 2013-08-07 | Portola Pharmaceuticals, Inc. | Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine |
| JP2014005206A (ja) | 2010-10-22 | 2014-01-16 | Astellas Pharma Inc | アリールアミノヘテロ環カルボキサミド化合物 |
| TW201300360A (zh) | 2010-11-01 | 2013-01-01 | Portola Pharm Inc | 做為jak激酶調節劑之菸鹼醯胺 |
| WO2012061415A1 (en) | 2010-11-01 | 2012-05-10 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
| US9359308B2 (en) | 2011-11-23 | 2016-06-07 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
| WO2013078468A1 (en) | 2011-11-23 | 2013-05-30 | Portola Pharmaceuticals, Inc. | Selective kinase inhibitors |
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