JP2013529199A5 - - Google Patents
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- JP2013529199A5 JP2013529199A5 JP2013510297A JP2013510297A JP2013529199A5 JP 2013529199 A5 JP2013529199 A5 JP 2013529199A5 JP 2013510297 A JP2013510297 A JP 2013510297A JP 2013510297 A JP2013510297 A JP 2013510297A JP 2013529199 A5 JP2013529199 A5 JP 2013529199A5
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- Prior art keywords
- aliphatic
- cancer
- composition
- compound according
- adenoma
- Prior art date
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| US (2) | US9096584B2 (https=) |
| EP (1) | EP2569284B1 (https=) |
| JP (1) | JP5856151B2 (https=) |
| CN (1) | CN102947272A (https=) |
| AU (1) | AU2011253021A1 (https=) |
| CA (1) | CA2798760A1 (https=) |
| MX (1) | MX2012013082A (https=) |
| NZ (1) | NZ603478A (https=) |
| WO (1) | WO2011143422A1 (https=) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170015566A (ko) | 2008-11-10 | 2017-02-08 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| ES2663222T3 (es) | 2008-12-19 | 2018-04-11 | Vertex Pharmaceuticals Incorporated | Derivados de pirazina útiles como inhibidores de la quinasa ATR |
| JP2013526539A (ja) | 2010-05-12 | 2013-06-24 | 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 | Ａｔｒキナーゼ阻害剤として有用なピラジン |
| JP2013526540A (ja) | 2010-05-12 | 2013-06-24 | 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 | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| US8969356B2 (en) | 2010-05-12 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| JP5856151B2 (ja) | 2010-05-12 | 2016-02-09 | 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 | Ａｔｒキナーゼ阻害剤として有用な２−アミノピリジン誘導体 |
| JP2013529200A (ja) | 2010-05-12 | 2013-07-18 | 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 | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| US9630956B2 (en) | 2010-05-12 | 2017-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| CN102718745A (zh) * | 2011-03-30 | 2012-10-10 | 中国科学院上海药物研究所 | 新型胺基吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途 |
| JP2014510151A (ja) | 2011-04-05 | 2014-04-24 | 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 | Ａｔｒキナーゼ（ｔｒａｋｉｎａｓｅ）阻害剤として有用なアミノピラジン化合物 |
| WO2012178124A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2723745A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| SG10201606774UA (en) * | 2011-09-30 | 2016-10-28 | Vertex Pharma | Processes for making compounds useful as inhibitors of atr kinase |
| WO2013049719A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013049859A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors |
| KR20140084112A (ko) | 2011-09-30 | 2014-07-04 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| WO2013071085A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US8841337B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US8841450B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071088A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CA2869309C (en) | 2012-04-05 | 2021-02-09 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| JP6280546B2 (ja) | 2012-06-26 | 2018-02-14 | デル マー ファーマシューティカルズ | ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法 |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| US8912198B2 (en) | 2012-10-16 | 2014-12-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| SI2941432T1 (en) | 2012-12-07 | 2018-07-31 | Vertex Pharmaceuticals Incorporated | 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR |
| ES2637170T3 (es) | 2013-01-02 | 2017-10-11 | H. Lundbeck A/S | Compuestos derivados de aminopiridina como inhibidores de LRRK2 |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | 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 | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| EP2983674A4 (en) | 2013-04-08 | 2017-05-10 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| JP6496731B2 (ja) * | 2013-11-27 | 2019-04-03 | シグナルケム・ライフサイエンシーズ・コーポレイションＳｉｇｎａｌｃｈｅｍ Ｌｉｆｅｓｃｉｅｎｃｅｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｔａｍファミリーキナーゼ阻害剤としてのアミノピリジン誘導体 |
| DK3077397T3 (da) | 2013-12-06 | 2019-12-16 | Vertex Pharma | 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf |
| PL3152212T3 (pl) | 2014-06-05 | 2020-06-15 | Vertex Pharmaceuticals Inc. | Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych |
| LT3157566T (lt) | 2014-06-17 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį |
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
| HK1258570A1 (zh) | 2015-09-30 | 2019-11-15 | Vertex Pharmaceuticals Inc. | 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法 |
| EP3936153B1 (en) | 2016-01-11 | 2024-08-21 | Celator Pharmaceuticals, Inc. | Inhibiting ataxia telangiectasia and rad3-related protein (atr) |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| AR110995A1 (es) | 2017-02-24 | 2019-05-22 | Bayer Ag | Combinación de inhibidores de quinasa atr con sal de radio-223 |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| WO2019025440A1 (en) | 2017-08-04 | 2019-02-07 | Bayer Pharma Aktiengesellschaft | COMBINATION OF ATR KINASE INHIBITORS AND PD-1 / PD-L1 INHIBITORS |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| CA3084863A1 (en) | 2017-12-08 | 2019-06-13 | Bayer Aktiengesellschaft | Predictive markers for atr kinase inhibitors |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| WO2020064971A1 (en) | 2018-09-26 | 2020-04-02 | Merck Patent Gmbh | Combination of a pd-1 antagonist, an atr inhibitor and a platinating agent for the treatment of cancer |
| EP3866785A1 (en) | 2018-10-15 | 2021-08-25 | Merck Patent GmbH | Combination therapy utilizing dna alkylating agents and atr inhibitors |
| EP3866805A1 (en) | 2018-10-16 | 2021-08-25 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| GB202108249D0 (en) * | 2021-06-09 | 2021-07-21 | Univ Of Sussex | Compounds |
Family Cites Families (140)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4309430A (en) | 1980-06-27 | 1982-01-05 | Merck & Co., Inc. | Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same |
| US5329012A (en) | 1987-10-29 | 1994-07-12 | The Research Foundation Of State University Of New York | Bis(acyloxmethyl)imidazole compounds |
| JP2597917B2 (ja) | 1990-04-26 | 1997-04-09 | 富士写真フイルム株式会社 | 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料 |
| JP2002241379A (ja) | 1997-03-21 | 2002-08-28 | Dainippon Pharmaceut Co Ltd | ３−オキサジアゾリルキノキサリン誘導体 |
| EP1097933A4 (en) | 1998-07-16 | 2001-11-07 | Shionogi & Co | PYRIMIDINE DERIVATIVES HAVING ANTI-TUMOR ACTIVITY |
| US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| EP1237880B1 (en) | 1999-12-17 | 2008-01-23 | Novartis Vaccines and Diagnostics, Inc. | Pyrazine based inhibitors of glycogen synthase kinase 3 |
| US6849660B1 (en) | 2000-08-01 | 2005-02-01 | Isis Pharmaceuticals, Inc. | Antimicrobial biaryl compounds |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| CA2446380A1 (en) | 2001-05-08 | 2002-11-14 | Yale University | Proteomimetic compounds and methods |
| SE0102439D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
| SE0102438D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
| US6992087B2 (en) | 2001-11-21 | 2006-01-31 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
| AU2002343557A1 (en) | 2001-11-21 | 2003-06-10 | Pharmacia And Upjohn Company | Substituted aryl 1,4-pyrazine derivatives |
| EP1472245A2 (en) | 2002-02-06 | 2004-11-03 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| ES2306859T3 (es) | 2002-03-13 | 2008-11-16 | Janssen Pharmaceutica Nv | Derivados de sulfonil como nuevos inhibidores de histona deacetilasa. |
| GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| EP1501514B1 (en) | 2002-05-03 | 2012-12-19 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| CA2482838A1 (en) | 2002-05-31 | 2003-12-11 | Eisai Co., Ltd. | Pyrazole compounds and pharmaceutical compositions containing the compound |
| US7015227B2 (en) | 2002-06-21 | 2006-03-21 | Cgi Pharmaceuticals, Inc. | Certain amino-substituted monocycles as kinase modulators |
| WO2004033431A2 (en) | 2002-10-04 | 2004-04-22 | Arena Pharmaceuticals, Inc. | Hydroxypyrazoles for use against metabolic-related disorders |
| SE0203752D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
| SE0203754D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
| CA2517720A1 (en) | 2003-03-11 | 2004-09-23 | Pfizer Products Inc. | Pyrazine compounds as transforming growth factor (tgf) inhibitors |
| JP2006520794A (ja) | 2003-03-21 | 2006-09-14 | スミスクライン ビーチャム コーポレーション | 化合物 |
| WO2004084824A2 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
| GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| US20060252741A1 (en) | 2003-05-15 | 2006-11-09 | Colandrea Vincent J | 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists |
| AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| US7807696B2 (en) | 2003-10-07 | 2010-10-05 | The Feinstein Institute For Medical Research | Isoxazole and isothiazole compounds useful in the treatment of inflammation |
| EP1715867A4 (en) | 2004-02-12 | 2009-04-15 | Merck & Co Inc | BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5 |
| WO2005123672A2 (en) | 2004-06-14 | 2005-12-29 | Takeda San Diego, Inc. | Kinase inhibitors |
| JP4116670B2 (ja) | 2004-06-28 | 2008-07-09 | インサイト コーポレイション | ケモカイン受容体の調節剤としての３−アミノシクロペンタンカルボキサミド |
| MX2007001126A (es) | 2004-07-27 | 2007-09-25 | Sgx Pharmaceuticals Inc | Moduladores de heterociclo cinasa de anillo fusionado. |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| WO2006053342A2 (en) | 2004-11-12 | 2006-05-18 | Osi Pharmaceuticals, Inc. | Integrin antagonists useful as anticancer agents |
| EP1814883A1 (en) | 2004-11-22 | 2007-08-08 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
| GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
| WO2006071548A2 (en) | 2004-12-27 | 2006-07-06 | Alcon, Inc. | Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases |
| GB0500492D0 (en) | 2005-01-11 | 2005-02-16 | Cyclacel Ltd | Compound |
| US7622583B2 (en) | 2005-01-14 | 2009-11-24 | Chemocentryx, Inc. | Heteroaryl sulfonamides and CCR2 |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| CA2598456A1 (en) | 2005-02-16 | 2006-08-24 | Schering Corporation | Heterocyclic substituted piperazines with cxcr3 antagonist activity |
| JP5033119B2 (ja) | 2005-04-25 | 2012-09-26 | 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 ハフツング | キナーゼ阻害剤としての新規アザ複素環化合物 |
| WO2006124874A2 (en) * | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| CN101258142A (zh) * | 2005-08-02 | 2008-09-03 | 莱西肯医药有限公司 | 作为蛋白激酶抑制剂的2-氨基芳基吡啶 |
| WO2007015632A1 (en) | 2005-08-04 | 2007-02-08 | Cgk Co., Ltd. | Atm and atr inhibitor |
| TW200736260A (en) | 2005-11-10 | 2007-10-01 | Smithkline Beecham Corp | Inhibitors of Akt activity |
| WO2007063012A1 (en) | 2005-12-01 | 2007-06-07 | F. Hoffmann-La Roche Ag | Heteroaryl substituted piperidine derivatives as l-cpt1 inhibitors |
| EP1970377A4 (en) | 2005-12-09 | 2013-02-27 | Meiji Seika Kaisha | LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THIS AS AN ACTIVE SUBSTANCE |
| EP1962853A1 (en) | 2005-12-22 | 2008-09-03 | Alcon Research, Ltd. | (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions |
| PE20070978A1 (es) * | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| ITMI20060311A1 (it) | 2006-02-21 | 2007-08-22 | Btsr Int Spa | Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione |
| GB0603684D0 (en) | 2006-02-23 | 2006-04-05 | Novartis Ag | Organic compounds |
| WO2007096764A2 (en) | 2006-02-27 | 2007-08-30 | Glenmark Pharmaceuticals S.A. | Bicyclic heteroaryl derivatives as cannabinoid receptor modulators |
| TW200800203A (en) | 2006-03-08 | 2008-01-01 | Astrazeneca Ab | New use |
| ES2336625T3 (es) * | 2006-03-22 | 2010-04-14 | Vertex Pharmaceuticals Incorporated | Inhibidores de la proteina quinasa c-met para el tratamiento de trastornos proliferativos. |
| CN101454314A (zh) | 2006-03-31 | 2009-06-10 | 先灵公司 | 激酶抑制剂 |
| JP2009541323A (ja) | 2006-06-22 | 2009-11-26 | マリンクロット インコーポレイテッド | 拡張された共役を有するピラジン誘導体およびその使用 |
| CA2654358A1 (en) | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
| EP1900727A1 (en) * | 2006-08-30 | 2008-03-19 | Cellzome Ag | Aminopyridine derivatives as kinase inhibitors |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k lipid kinase inhibitors |
| GB0619342D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
| EP2450350A1 (en) | 2006-10-04 | 2012-05-09 | F. Hoffmann-La Roche AG | 3-Pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as HDL-cholesterol raising agents |
| WO2008060907A2 (en) | 2006-11-10 | 2008-05-22 | Bristol-Myers Squibb Company | Pyrrolo-pyridine kinase inhibitors |
| EP2125808A2 (en) | 2006-12-15 | 2009-12-02 | Bayer Schering Pharma Aktiengesellschaft | 3-h-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| EP2125781A2 (en) | 2006-12-20 | 2009-12-02 | Amgen Inc. | Substituted heterocycles and methods of use |
| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
| GB0625659D0 (en) * | 2006-12-21 | 2007-01-31 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| AU2008219166B2 (en) | 2007-02-16 | 2013-05-16 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors |
| MX2009009304A (es) | 2007-03-01 | 2009-11-18 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso. |
| MY146638A (en) | 2007-04-10 | 2012-09-14 | Bayer Cropscience Ag | Insecticidal aryl isoxazoline derivatives |
| PE20090288A1 (es) | 2007-05-10 | 2009-04-03 | Smithkline Beecham Corp | Derivados de quinoxalina como inhibidores de la pi3 quinasa |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
| EP2157090A4 (en) | 2007-06-21 | 2011-09-07 | Taisho Pharmaceutical Co Ltd | PYRAZINAMIDE COMPOUND |
| CN101784269A (zh) | 2007-06-26 | 2010-07-21 | 莱西肯医药有限公司 | 治疗由5-羟色胺介导的疾病和病症的方法 |
| WO2009005638A2 (en) * | 2007-06-27 | 2009-01-08 | Merck & Co., Inc. | Pyridyl and pyrimidinyl derivatives as histone deacetylase inhibitors |
| GB0713259D0 (en) | 2007-07-09 | 2007-08-15 | Astrazeneca Ab | Pyrazine derivatives 954 |
| RS54303B1 (sr) | 2007-07-19 | 2016-02-29 | Lundbeck, H., A/S | 5-člani heterociklični amidi i srodna jedinjenja |
| JP5241834B2 (ja) | 2007-07-19 | 2013-07-17 | メルク・シャープ・アンド・ドーム・コーポレーション | プロテインキナーゼ阻害剤としての複素環アミド化合物 |
| BRPI0815042A2 (pt) | 2007-08-01 | 2015-02-10 | Pfizer | Compostos de pirazol |
| WO2009024825A1 (en) | 2007-08-21 | 2009-02-26 | Astrazeneca Ab | 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors |
| WO2009037247A1 (en) | 2007-09-17 | 2009-03-26 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
| ATE523508T1 (de) | 2007-10-25 | 2011-09-15 | Astrazeneca Ab | Für die behandlung von zellproliferativen erkrankungen geeignete pyridin- und pyrazinderivate |
| CA2709784A1 (en) * | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| WO2009099982A1 (en) * | 2008-02-04 | 2009-08-13 | Osi Pharmaceuticals, Inc. | 2-aminopyridine kinase inhibitors |
| CA2716223A1 (en) | 2008-02-25 | 2009-09-03 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
| JP5368485B2 (ja) | 2008-02-25 | 2013-12-18 | エフ．ホフマン−ラ ロシュ アーゲー | ピロロピラジンキナーゼインヒビター |
| AU2009218609A1 (en) | 2008-02-25 | 2009-09-03 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
| ATE522536T1 (de) | 2008-02-25 | 2011-09-15 | Hoffmann La Roche | Pyrrolopyrazin-kinasehemmer |
| TW200940537A (en) * | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
| JP2011513332A (ja) * | 2008-02-29 | 2011-04-28 | アレイ バイオファーマ、インコーポレイテッド | 癌の治療のためのｒａｆ阻害剤としてのｎ−（６−アミノピリジン−３−イル）−３−（スルホンアミド）ベンズアミド誘導体 |
| US8110576B2 (en) | 2008-06-10 | 2012-02-07 | Plexxikon Inc. | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications |
| GB0814364D0 (en) | 2008-08-05 | 2008-09-10 | Eisai London Res Lab Ltd | Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase |
| JP2012506381A (ja) | 2008-10-21 | 2012-03-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | ｃ−ＭＥＴタンパク質キナーゼ阻害剤 |
| KR20170015566A (ko) | 2008-11-10 | 2017-02-08 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| CA2744498C (en) | 2008-11-25 | 2017-10-24 | University Of Rochester | Mlk inhibitors and methods of use |
| KR101361858B1 (ko) | 2008-12-05 | 2014-02-12 | 에프. 호프만-라 로슈 아게 | 피롤로피라지닐 우레아 키나아제 저해제 |
| ES2663222T3 (es) | 2008-12-19 | 2018-04-11 | Vertex Pharmaceuticals Incorporated | Derivados de pirazina útiles como inhibidores de la quinasa ATR |
| CA2740193A1 (en) | 2008-12-23 | 2010-07-01 | Abbott Laboratories | Anti-viral compounds |
| KR20110132564A (ko) | 2009-02-11 | 2011-12-08 | 선오비온 파마슈티컬스 인코포레이티드 | 히스타민 ｈ3 역 작용제 및 길항제, 및 이의 사용 방법 |
| US20120065247A1 (en) | 2009-03-27 | 2012-03-15 | Discoverybiomed, Inc. | Modulating ires-mediated translation |
| CA2767091A1 (en) | 2009-07-15 | 2011-01-20 | Abbott Laboratories | Pyrrolopyrazine inhibitors of kinases |
| DE102009043260A1 (de) * | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
| HUE027946T2 (en) * | 2010-01-18 | 2016-11-28 | Medicines For Malaria Venture Mmv | New anti-malaria drugs |
| US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| EP2556060A1 (en) | 2010-04-08 | 2013-02-13 | Ah Usa 42 Llc | Substituted 3,5- diphenyl-isoxazoline derivatives as insecticides and acaricides |
| ES2602475T3 (es) | 2010-04-15 | 2017-02-21 | Tracon Pharmaceuticals, Inc. | Potenciación de la actividad anticáncer por terapia de combinación con inhibidores de la vía BER |
| JP5856151B2 (ja) | 2010-05-12 | 2016-02-09 | 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 | Ａｔｒキナーゼ阻害剤として有用な２−アミノピリジン誘導体 |
| US9630956B2 (en) | 2010-05-12 | 2017-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| JP2013529200A (ja) | 2010-05-12 | 2013-07-18 | 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 | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| JP2013526539A (ja) | 2010-05-12 | 2013-06-24 | 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 | Ａｔｒキナーゼ阻害剤として有用なピラジン |
| JP2013526540A (ja) | 2010-05-12 | 2013-06-24 | 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 | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| US8969356B2 (en) | 2010-05-12 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CN102906095A (zh) | 2010-05-20 | 2013-01-30 | 弗·哈夫曼-拉罗切有限公司 | 作为syk和jak抑制剂的吡咯并吡嗪衍生物 |
| CA2799904A1 (en) | 2010-05-20 | 2011-11-24 | F. Hoffmann-La Roche Ag | Pyrrolo [2, 3 - b] pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors |
| CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| CN102311396B (zh) | 2010-07-05 | 2015-01-07 | 暨南大学 | 一种吡嗪类衍生物和其制备方法及在制药中的应用 |
| EP2407478A1 (en) | 2010-07-14 | 2012-01-18 | GENETADI Biotech, S.L. | New cyclotetrapeptides with pro-angiogenic properties |
| AR085607A1 (es) * | 2011-03-04 | 2013-10-16 | Lexicon Pharmaceuticals Inc | Inhibidores de la mst1 quinasa y metodos para su utilizacion |
| US8962623B2 (en) * | 2011-03-04 | 2015-02-24 | Locus Pharmaceuticals, Inc. | Aminopyrazine compounds |
| JP2014510151A (ja) | 2011-04-05 | 2014-04-24 | 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 | Ａｔｒキナーゼ（ｔｒａｋｉｎａｓｅ）阻害剤として有用なアミノピラジン化合物 |
| CA2836417A1 (en) | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Azaindole derivatives as tyrosine kinase inhibitors |
| EP2723745A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| WO2012178124A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| SG10201606774UA (en) | 2011-09-30 | 2016-10-28 | Vertex Pharma | Processes for making compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013049859A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors |
| KR20140084112A (ko) | 2011-09-30 | 2014-07-04 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| WO2013049719A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071088A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8841450B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071085A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8841337B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
-
2011
- 2011-05-12 JP JP2013510297A patent/JP5856151B2/ja not_active Expired - Fee Related
- 2011-05-12 WO PCT/US2011/036242 patent/WO2011143422A1/en not_active Ceased
- 2011-05-12 MX MX2012013082A patent/MX2012013082A/es not_active Application Discontinuation
- 2011-05-12 CN CN2011800296664A patent/CN102947272A/zh active Pending
- 2011-05-12 CA CA2798760A patent/CA2798760A1/en not_active Abandoned
- 2011-05-12 US US13/106,178 patent/US9096584B2/en active Active
- 2011-05-12 NZ NZ603478A patent/NZ603478A/en not_active IP Right Cessation
- 2011-05-12 AU AU2011253021A patent/AU2011253021A1/en not_active Abandoned
- 2011-05-12 EP EP11721403.1A patent/EP2569284B1/en not_active Not-in-force
-
2014
- 2014-12-08 US US14/562,965 patent/US20150239874A1/en not_active Abandoned
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