CN101784545B - 用作raf激酶抑制剂的嘧啶衍生物 - Google Patents

用作raf激酶抑制剂的嘧啶衍生物 Download PDF

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CN101784545B
CN101784545B CN200880022788.9A CN200880022788A CN101784545B CN 101784545 B CN101784545 B CN 101784545B CN 200880022788 A CN200880022788 A CN 200880022788A CN 101784545 B CN101784545 B CN 101784545B
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compound
optionally substituted
synthesis
mmol
nitrogen
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CN101784545A (zh
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陈伟荣
詹妮弗·科斯罗
利奥伊德·富兰克林
关冰
约翰·H·琼斯
格纳纳萨姆班达姆·库玛拉维尔
本杰明·莱恩
亚当·利特克
亚历克西·卢戈夫斯科伊
彭海若
诺埃尔·鲍威尔
布赖恩·雷蒙多
田中弘子
杰弗里·维塞尔斯
托马斯·温
辛智利
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Dot Therapy 1 Co
Viracta Therapeutics Inc
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Millennium Pharmaceuticals Inc
Sunesis Pharmaceuticals Inc
Biogen Idec MA Inc
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Application filed by Millennium Pharmaceuticals Inc, Sunesis Pharmaceuticals Inc, Biogen Idec MA Inc filed Critical Millennium Pharmaceuticals Inc
Priority to CN201611139456.1A priority Critical patent/CN106957314B/zh
Priority to CN201410466320.6A priority patent/CN104370828B/zh
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Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2167497A2 (en) * 2007-06-29 2010-03-31 Sunesis Pharmaceuticals, Inc. Heterocyclic compounds useful as raf kinase inhibitors
AR067354A1 (es) 2007-06-29 2009-10-07 Sunesis Pharmaceuticals Inc Compuestos utiles como inhibidores de la raf quinasa
ES2394126T3 (es) * 2007-07-26 2013-01-22 Novartis Ag Derivados de pirimidina útiles para el tratamiento de estados inflamatorios o alérgicos
MX2010001446A (es) * 2007-08-08 2010-03-01 Merck Serono Sa Derivados de 6-amino-pirimidina-4-carboxamida y compuestos relacionados que se enlazan a los receptores para esfingosina 1-fosfato (s1p) para el tratamiento de esclerosis multiple.
FR2934265B1 (fr) * 2008-07-23 2010-07-30 Sanofi Aventis Derives de carbamates d'alkylthiazoles, leur preparation et leur application en therapeutique
JP5693452B2 (ja) 2008-08-04 2015-04-01 シーエイチディーアイ ファウンデーション,インコーポレーテッド 特定のキヌレニン−3−モノオキシゲナーゼインヒビター、医薬組成物およびそれらの使用方法
WO2010078408A1 (en) * 2008-12-30 2010-07-08 Biogen Idec Ma Inc. Heteroaryl compounds useful as raf kinase inhibitors
CA3121743A1 (en) 2009-01-15 2010-07-22 Incyte Holdings Corporation Processes for preparing jak inhibitors and related intermediate compounds
WO2010111050A1 (en) * 2009-03-23 2010-09-30 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
JP2012521426A (ja) * 2009-03-24 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
WO2010144394A1 (en) 2009-06-09 2010-12-16 Abraxis Bioscience, Llc Benzyl substituted triazine derivatives and their therapeutical applications
KR101457027B1 (ko) 2009-06-09 2014-10-31 캘리포니아 캐피탈 에쿼티, 엘엘씨 트리아진 유도체와 이들의 치료적 용도
BRPI1011247A2 (pt) 2009-06-09 2016-06-21 California Capital Equity Llc derivados de isoquinolina, quinolina e quinazolina como inibidores de sinalização de hedgehog
AU2010297290A1 (en) * 2009-09-21 2012-03-15 F. Hoffmann-La Roche Ag Heterocyclic antiviral compounds
MX2012008346A (es) 2010-01-25 2012-11-12 Chdi Foundation Inc Determinados inhibidores de cinurenina-3-monooxigenasa, composiciones farmceuticas y metodos de uso de los mismos.
WO2011150198A1 (en) 2010-05-27 2011-12-01 Ambit Biosciences Corporation Azolyl urea compounds and methods of use thereof
CN102406646B (zh) * 2010-09-20 2015-09-09 北大方正集团有限公司 芳基脲衍生物用于制备治疗移植排斥药物的用途
CN102153515B (zh) * 2011-02-24 2013-02-27 中国药科大学 N,N′-双取代脲类Raf激酶抑制剂及其制备方法和用途
MX2014002459A (es) 2011-08-30 2014-04-10 Chdi Foundation Inc Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodos de uso de los mismos.
SI2750677T1 (sl) 2011-08-30 2017-10-30 Chdi Foundation, Inc. Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
CN104428001A (zh) * 2012-03-30 2015-03-18 武田药品工业有限公司 Raf抑制剂和mek抑制剂在黑素瘤治疗中的投与
JP2016501203A (ja) 2012-11-20 2016-01-18 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Vertex Pharmaceuticals Incorporated インドールアミン2,3−ジオキシゲナーゼの阻害剤として有用な化合物
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
US9186361B2 (en) 2013-03-15 2015-11-17 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
US9233961B2 (en) 2013-03-15 2016-01-12 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
US9296754B2 (en) 2013-03-15 2016-03-29 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
TWI674263B (zh) 2013-12-19 2019-10-11 瑞士商諾華公司 用於治療寄生蟲疾病之化合物及組合物
UY36046A (es) * 2014-03-26 2015-10-30 Millennium Pharm Inc Formulaciones farmacéuticas, procesos para la preparación y métodos de uso
CN106715421A (zh) 2014-07-17 2017-05-24 Chdi基金会股份有限公司 用于治疗hiv相关病症的方法和组合物
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
WO2016106351A1 (en) * 2014-12-23 2016-06-30 Millennium Pharmaceuticals, Inc. Combination of raf inhibitors and mtor inhibitors
ES2827024T3 (es) * 2014-12-23 2021-05-19 Dot Therapeutics 1 Inc Combinación de inhibidores de Raf y de taxanos
WO2016106357A1 (en) * 2014-12-23 2016-06-30 Millennnium Pharmaceuticals, Inc. Combination of raf inhibitors and aurora kinase inhibitors
JP6666673B2 (ja) * 2015-09-07 2020-03-18 キリンホールディングス株式会社 細胞内送達ベヒクル
WO2017066664A1 (en) * 2015-10-16 2017-04-20 Millennium Pharmaceuticals, Inc. Combination therapy including a raf inhibitor for the treatment of colorectal cancer
SG11201804359SA (en) * 2015-12-11 2018-06-28 Teijin Pharma Ltd Aminoazole derivative
MA44483A (fr) 2016-03-24 2019-01-30 Millennium Pharm Inc Procédés pour traiter des événements indésirables gastro-intestinaux d'origine immunitaire dans des traitements oncologiques immunitaires
WO2017165491A1 (en) * 2016-03-24 2017-09-28 Millennium Pharmaceuticals, Inc. Use of a pd-1 antagonist and a raf inhibitor in the treatment of cancer
WO2017165742A1 (en) 2016-03-24 2017-09-28 Millennium Pharmaceuticals, Inc. Methods of treating gastrointestinal immune-related adverse events in anti-ctla4 anti-pd-1 combination treatments
KR101725292B1 (ko) * 2016-03-30 2017-04-10 한국과학기술연구원 항암 활성을 갖는 신규 피리미딘-4-카르복시산 유도체
JP2019196307A (ja) * 2016-09-15 2019-11-14 武田薬品工業株式会社 複素環アミド化合物
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
JP7341060B2 (ja) 2017-02-10 2023-09-08 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Mapk経路の活性化に関連付けられる癌の処置のための方法及び医薬組成物
US10787443B2 (en) * 2017-04-28 2020-09-29 Zamboni Chem Solutions Inc. RAF-degrading conjugate compounds
ES2952265T3 (es) 2017-05-02 2023-10-30 Novartis Ag Terapia combinada que comprende un inhibidor de Raf y trametinib
MX391164B (es) * 2017-05-30 2025-03-21 Dot Therapeutics 1 Inc Metodo para producir compuesto opticamente activo
EP3732285A1 (en) 2017-12-28 2020-11-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
US10927111B2 (en) 2019-05-03 2021-02-23 Kinnate Biopharma Inc. Inhibitors of RAF kinases
ES3025633T3 (en) 2019-05-13 2025-06-09 Novartis Ag New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
EP4045498B1 (en) * 2019-10-14 2025-12-03 The Regents of the University of California Broad spectrum anti-cancer compounds
BR112022007612A2 (pt) 2019-10-24 2022-09-20 Kinnate Biopharma Inc Inibidores de raf quinases
WO2021108616A1 (en) * 2019-11-27 2021-06-03 Dot Therapeutics-1, Inc. Solid dispersion of pan-raf kinase inhibitor
WO2021117759A1 (ja) 2019-12-10 2021-06-17 塩野義製薬株式会社 含窒素芳香族複素環式基を有するヒストン脱アセチル化酵素阻害剤
JP7807381B2 (ja) * 2020-03-02 2026-01-27 シロナックス リミテッド. フェロトーシス阻害剤ジアリールアミンパラアセトアミド類
EP4149929B1 (en) 2020-05-12 2026-01-28 Bayer Aktiengesellschaft Triazine and pyrimidine (thio)amides as fungicidal compounds
US11407737B2 (en) 2020-09-18 2022-08-09 Kinnate Biopharma Inc. Inhibitors of RAF kinases
WO2022081469A1 (en) 2020-10-12 2022-04-21 Kinnate Biopharma Inc. Inhibitors of raf kinases
JP2024509269A (ja) * 2021-03-09 2024-02-29 ジェネンテック, インコーポレイテッド 脳がんの治療における使用のためのベルバラフェニブ
CN117561057A (zh) 2021-04-23 2024-02-13 金耐特生物制药公司 用raf抑制剂治疗癌症
EP4448492B1 (en) 2021-12-17 2026-03-04 Reglagene, Inc. Compositions and methods of making and using small molecules in the treatment of cancer
US12215102B2 (en) 2023-02-28 2025-02-04 Reglagene, Inc. Compositions and methods for making and using small molecules for tubulin-targeted therapy in the treatment of cancers and related conditions
CN117567388B (zh) * 2023-11-14 2024-04-16 济南悟通生物科技有限公司 一种2-乙酰基-5-噻唑甲酸的合成方法
WO2025264645A1 (en) * 2024-06-18 2025-12-26 Latigo Biotherapeutics, Inc. Sodium channel blocking compounds, derivatives thereof, and methods of their use
WO2026028053A2 (en) 2024-07-27 2026-02-05 Assia Chemical Industries Ltd. Process for the preparation of tovorafenib
CN119241529B (zh) * 2024-09-20 2026-04-10 武汉九州钰民医药科技有限公司 一种Tovorafenib的制备方法
CN119241530B (zh) * 2024-09-20 2026-04-10 武汉九州钰民医药科技有限公司 一种Tovorafenib的药物合成工艺

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005082367A1 (en) * 2004-02-18 2005-09-09 Devgen Nv Kinase inhibitors
WO2006065703A1 (en) * 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors

Family Cites Families (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
US5563158A (en) 1993-12-28 1996-10-08 The Dupont Merck Pharmaceutical Company Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
EP0852498A1 (en) 1995-09-26 1998-07-15 Takeda Chemical Industries, Ltd. Phosphorylamides, their preparation and use
EP0939757A1 (en) 1995-12-22 1999-09-08 Dupont Pharmaceuticals Company Novel integrin receptor antagonists
US5760028A (en) 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
AU706150B2 (en) 1996-04-03 1999-06-10 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5872136A (en) 1996-04-03 1999-02-16 Merck & Co., Inc. Arylheteroaryl inhibitors of farnesyl-protein transferase
CN1219171A (zh) 1996-05-20 1999-06-09 达尔文发现有限公司 苯并呋喃甲酰胺及其治疗用途
US5877182A (en) 1996-09-13 1999-03-02 Merck & Co., Inc. Piperidines promote release of growth hormone
US6174905B1 (en) 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
BR9713507A (pt) * 1996-11-15 2000-02-29 Darwin Discovery Ltd Aril carboxamidas bicìclicas e seu uso terapêutico
US6017925A (en) 1997-01-17 2000-01-25 Merck & Co., Inc. Integrin antagonists
WO1998042323A1 (en) 1997-03-25 1998-10-01 Takeda Chemical Industries, Ltd. Stabilized urease inhibitor
WO1998043962A1 (en) 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Heterocyclic integrin inhibitor prodrugs
SE9704545D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
US6632823B1 (en) 1997-12-22 2003-10-14 Merck & Co., Inc. Substituted pyridine compounds useful as modulators of acetylcholine receptors
JPH11209366A (ja) 1998-01-23 1999-08-03 Nissan Chem Ind Ltd クロマン誘導体及び心不全治療薬
EP0982030A3 (en) 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
WO2000053602A1 (en) 1999-03-10 2000-09-14 Merck & Co., Inc. 6-azaindole compounds as antagonists of gonadotropin releasing hormone
AU3514200A (en) 1999-03-10 2000-09-28 Merck & Co., Inc. 6-azaindole compounds as antagonists of gonadotropin releasing hormone
WO2000058300A1 (en) 1999-03-25 2000-10-05 Nissan Chemical Industries, Ltd. Chroman derivatives
DE19915364A1 (de) 1999-04-06 2000-10-12 Merck Patent Gmbh Verwendung von Arylalkanoylpyridazinen
US6127382A (en) 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
WO2001038309A1 (en) 1999-11-24 2001-05-31 Cor Therapeutics, Inc. β-AMINO ACID-, ASPARTIC ACID- AND DIAMINOPROPIONIC-BASED INHIBITORS OF FACTOR Xa
GB0007245D0 (en) 2000-03-24 2000-05-17 Zeneca Ltd Chemical compounds
AU7002501A (en) 2000-06-21 2002-01-02 Du Pont Pharm Co Vitronectin receptor antagonist pharmaceuticals for use in combination therapy
WO2002080928A1 (en) 2001-04-03 2002-10-17 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
CA2471566A1 (en) 2002-01-10 2003-07-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Combination of mtp inhibitors or apob-secretion inhibitors with fibrates for use as pharmaceuticals
US20040048866A1 (en) 2002-03-08 2004-03-11 Teodozyj Kolasa Indazole derivatives that are activators of soluble guanylate cyclase
US7202244B2 (en) 2002-05-29 2007-04-10 Millennium Pharmaceuticals, Inc. Chk-1 inhibitors
AU2003245669A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
PL375263A1 (en) * 2002-07-02 2005-11-28 F.Hoffmann-La Roche Ag 2,5-substituted pyrimidine derivatives as ccr-3 receptor antagonists
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1400244A1 (en) 2002-09-17 2004-03-24 Warner-Lambert Company LLC New spirocondensed quinazolinones and their use as phosphodiesterase inhibitors
AU2003266607A1 (en) 2002-09-25 2004-04-19 Santen Pharmaceutical Co., Ltd. Therapeutic agent for rheumatism containing benzamide derivative as active ingredient
KR101050680B1 (ko) 2002-11-02 2011-07-21 사노피-아벤티스 도이칠란트 게엠베하 콜라게네이즈의 선택적인 억제를 위한 신규한피리미딘-4,6-디카복스아미드
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Jnk阻害剤
JP4847868B2 (ja) 2003-05-14 2011-12-28 ニューロジェネティック ファーマシューティカルズ、 インコーポレイテッド 化合物、及び、アミロイドベータの調節におけるその使用
JP2004339159A (ja) 2003-05-16 2004-12-02 Sankyo Co Ltd 4−オキソキノリン誘導体を含有する医薬組成物
DE10328999B4 (de) 2003-06-27 2006-08-31 Lanxess Deutschland Gmbh Verfahren zur Herstellung von Metallkomplexpigmenten mit niedriger Dispergierhärte
EP1781659B1 (en) 2003-07-16 2008-11-05 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
MXPA06000540A (es) 2003-07-16 2006-03-30 Janssen Pharmaceutica Nv Derivados de triazolopirimidinas como inhibidores de la glucogeno sintasa cinasa 3.
AU2004278413B2 (en) 2003-09-30 2008-07-31 Irm Llc Compounds and compositions as protein kinase inhibitors
NZ546058A (en) 2004-01-12 2010-09-30 Ym Biosciences Australia Pty Benzimidazole and other fused ring derivatives as selective janus kinase inhibitors
US20050176733A1 (en) 2004-01-20 2005-08-11 Millennium Pharmaceuticals, Inc. Chk-1 inhibitors
US7348346B2 (en) * 2004-03-08 2008-03-25 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
TW200616974A (en) 2004-07-01 2006-06-01 Astrazeneca Ab Chemical compounds
WO2006040568A1 (en) * 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
WO2006045010A2 (en) 2004-10-20 2006-04-27 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
EP1820795A4 (en) * 2004-12-07 2010-10-20 Toyama Chemical Co Ltd NEW ANTHRANILIC ACID DERIVATIVE OR SALT FROM IT
AU2005322855B2 (en) 2004-12-30 2012-09-20 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
US7563781B2 (en) 2005-01-14 2009-07-21 Janssen Pharmaceutica Nv Triazolopyrimidine derivatives
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
US20060247250A1 (en) * 2005-03-16 2006-11-02 Targegen, Inc. Pyrimidine inhibitors of kinases
HRP20110892T1 (hr) * 2005-12-13 2011-12-31 Schering Corporation Policiklični derivati indazola koji su inhibitori erk
TW200804349A (en) 2005-12-23 2008-01-16 Kalypsys Inc Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases
US20070155746A1 (en) 2005-12-23 2007-07-05 Kalypsys, Inc. Novel substituted pyridinyloxy and pyrimidinyloxy amides useful as inhibitors of protein kinases
AU2006332694A1 (en) * 2005-12-30 2007-07-12 Alantos Pharmaceuticals, Holding, Inc. Substituted bis-amide metalloprotease inhibitors
WO2007087443A2 (en) 2006-01-25 2007-08-02 Synta Pharmaceuticals Corp. Vinyl-phenyl derivatives for inflammation and immune-related uses
US20070275960A1 (en) 2006-01-25 2007-11-29 Synta Pharmaceuticals Corp. Phenyl and pyridyl compounds for inflammation and immune-related uses
US7951824B2 (en) 2006-02-17 2011-05-31 Hoffman-La Roche Inc. 4-aryl-pyridine-2-carboxyamide derivatives
CA2669695C (en) * 2006-11-13 2012-10-30 Synta Pharmaceuticals Corp. Tetrahydropyridinyl compounds for inflammation and immune-related uses
TW200916472A (en) * 2007-06-20 2009-04-16 Sirtris Pharmaceuticals Inc Sirtuin modulating compounds
EP2167497A2 (en) 2007-06-29 2010-03-31 Sunesis Pharmaceuticals, Inc. Heterocyclic compounds useful as raf kinase inhibitors
AR067354A1 (es) 2007-06-29 2009-10-07 Sunesis Pharmaceuticals Inc Compuestos utiles como inhibidores de la raf quinasa
WO2010078408A1 (en) 2008-12-30 2010-07-08 Biogen Idec Ma Inc. Heteroaryl compounds useful as raf kinase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005082367A1 (en) * 2004-02-18 2005-09-09 Devgen Nv Kinase inhibitors
WO2006065703A1 (en) * 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors

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