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11. 发明申请

WO2005085236A2 CASPASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： CASPASE抑制剂及其用途
公开(公告)号：WO2005085236A2
公开(公告)日：2005-09-15
申请号：PCT/US2005/006540
申请日：2005-02-28
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven , MORTIMORE, Michael , O'DONNELL, Michael , RUTHERFORD, Alistair , RAMAYA, Sharn , STUDLEY, John, R. , TRUDEAU, Martin , LOOKER, Adam
发明人： CHARRIER, Jean-Damien , DURRANT, Steven , MORTIMORE, Michael , O'DONNELL, Michael , RUTHERFORD, Alistair , RAMAYA, Sharn , STUDLEY, John, R. , TRUDEAU, Martin , LOOKER, Adam
IPC分类号： C07D405/00
CPC分类号： C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
摘要翻译：本发明提供了式（I）化合物：其中变量如本文所定义。本发明还提供了制备式（I）化合物及其中间体的方法，包含这些化合物的药物组合物，以及使用该化合物和组合物的方法。

12. 发明申请

WO2007120760A3 THIOPHENE-CARBOXAMIDES USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
公开(公告)号：WO2007120760A3
公开(公告)日：2007-10-25
申请号：PCT/US2007/009018
申请日：2007-04-12
申请人： VERTEX PHARMACEUTICALS INCORPORATED , BRENCHLEY, Guy , CHARRIER, Jean-Damien , DURRANT, Steven , KNEGTEL, Ron , RAMAYA, Sharn , SADIQ, Shazia
发明人： BRENCHLEY, Guy , CHARRIER, Jean-Damien , DURRANT, Steven , KNEGTEL, Ron , RAMAYA, Sharn , SADIQ, Shazia
IPC分类号： C07D409/04 , A61K31/4178 , A61P35/00
摘要： The present invention relates to compounds of Formula I useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

13. 发明申请

WO2007027528A3 3,5-DISUBSTITUTED PYRID-2-ONES USEFUL AS INHIBITORS OF TEC FAMILY OF NON-.RECEPTOR TYROSINE KINASES 审中-公开
公开(公告)号：WO2007027528A3
公开(公告)日：2007-03-08
申请号：PCT/US2006/033282
申请日：2006-08-25
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , RAMAYA, Sharn , DURRANT, Steven , JIMENEZ, Juan-Miguel , GOLEC, Julian, M.C. , MORTIMORE, Michael
发明人： CHARRIER, Jean-Damien , RAMAYA, Sharn , DURRANT, Steven , JIMENEZ, Juan-Miguel , GOLEC, Julian, M.C. , MORTIMORE, Michael
IPC分类号： C07D401/14 , C07D401/04 , A61K31/444 , A61P37/00 , A61P35/00 , C07D213/64
摘要： The present invention relates to pyrid-2-one compounds of formula (I) wherein V is (A), (B), (C) or (D) useful as inhibitors of protein kinase. These compounds and pharmaceutically acceptable compositions thereof are useful for treating or preventing autoimmune, inflammatory, proliferative, hyperproliferative or immunologically-mediated diseases.

14. 发明申请

WO2011036566A1 METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：用于制备作为蛋白激酶抑制剂有用的吡啶衍生物的方法
公开(公告)号：WO2011036566A1
公开(公告)日：2011-03-31
申请号：PCT/IB2010/002655
申请日：2010-09-24
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-damien , DURRANT, Steven , O'DONNELL, Michael
发明人： CHARRIER, Jean-damien , DURRANT, Steven , O'DONNELL, Michael
IPC分类号： C07D475/00 , C07D475/10 , C07D487/04
CPC分类号： C07D475/00 , C07D475/10 , C07D487/04
摘要： A method of preparing a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the steps of: a) reacting a compound represented by Structural Formula (A) with FTNR 1 R 7 under suitable conditions to form a compound represented by Structural Formula (B); and b) i) when R 12 is -NO 2 , and R 11 is -OR 14 : 1) cyclizing the compound represented by Structural Formula (B) under suitable cyclisation conditions to form a compound represented by Structural Formula (II); and 2) optionally reacting the compound represented by Structural Formula (II) with R 9 -LG 2, wherein LG 2 is a suitable leaving group, to form the compound represented by Structural Formula (I), wherein R 8 is R 9 ; or ii) when R 12 is halogen, and R 11 is -NHR 13 : 1) cyclizing the compound represented by Structural Formula (B) under suitable cyclisation conditions to form the compound represented by Structural Formula (I); and 2) optionally, when R 13 is - H, reacting the compound produced from step b), ii), 1) with R 9 -LG 2 , wherein LG 2 is a suitable leaving group, to form the compound represented by Structural Formula (I) wherein R 8 is R 9 .
摘要翻译：一种制备由结构式（I）表示的化合物或其药学上可接受的盐的方法，其中结构式（I）的变量如说明书和权利要求书中所述，包括以下步骤：a）使表示的化合物通过结构式（A）与FTNR1R7在合适的条件下形成由结构式（B）表示的化合物; 和b）i）当R 12为-NO 2且R 11为-OR 14：1时）在合适的环化条件下使结构式（B）表示的化合物环化以形成由结构式（II）表示的化合物; 和2）任选地使结构式（II）表示的化合物与其中LG2是合适的离去基团的R9-LG2反应以形成由结构式（I）表示的化合物，其中R8是R9; 或ii）当R 12为卤素且R 11为-NHR 13时：1）在合适的环化条件下使结构式（B）表示的化合物环化，形成由结构式（I）表示的化合物; 和2）任选地，当R 13是-H时，使由步骤b），ii），1）产生的化合物与R9-LG2反应，其中LG2是合适的离去基团，以形成由结构式（I）表示的化合物，其中 R8是R9。

15. 发明申请

WO2010008459A1 PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：蛋白激酶抑制剂
公开(公告)号：WO2010008459A1
公开(公告)日：2010-01-21
申请号：PCT/US2009/003723
申请日：2009-06-23
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven
发明人： CHARRIER, Jean-Damien , DURRANT, Steven
IPC分类号： C07D487/04 , A61K31/519 , A61K35/00
CPC分类号： C07D487/04
摘要： In one aspect, the invention provides compounds of Formula (I) or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
摘要翻译：一方面，本发明提供式（I）的化合物或其药学上可接受的盐。另一方面，本发明提供了治疗由蛋白激酶介导的疾病或病症的方法，其包括施用治疗有效量的本发明化合物。

16. 发明申请

WO2006065946A1 PYRID-2-ONES USEFUL AS INHIBITORS OF TEC FAMILY PROTEIN KINASES FOR THE TREATMENT OF INFLAMMATORY, PROLIFERATIVE AND IMMUNOLOGICALLY-MEDIATED DISEASES 审中-公开
标题翻译： PYRID-2-ONES作为TEC家族蛋白激酶的抑制剂用于治疗炎症，增殖和免疫介导的疾病
公开(公告)号：WO2006065946A1
公开(公告)日：2006-06-22
申请号：PCT/US2005/045336
申请日：2005-12-15
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven , RAMAYA, Sharn , JIMENEZ, Juan-Miguel , RUTHERFORD, Alistair
发明人： CHARRIER, Jean-Damien , DURRANT, Steven , RAMAYA, Sharn , JIMENEZ, Juan-Miguel , RUTHERFORD, Alistair
IPC分类号： C07D213/22 , C07D213/64 , C07D213/75 , C07D401/14 , C07D409/14 , C07D407/14 , C07D417/14 , A61K31/4427 , A61K31/444 , A61K31/4412 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D401/14 , C07D213/22 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/85 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： This invention describes compounds of Formula (I), or a pharmaceutically accepted salt thereof, wherein each R 3 and R 4 is independently H, halogen or C 1-4 aliphatic optionally substituted with halogen, C 1-2 aliphatic, OCH 3 , NO 2 , NH 2 , CN, NHCH 3 , SCH 3 , or N(CH) 2 . R 2 is a 3-8membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R 2 is optionally substituted with J R ; each X 1 and X 2 is independently -C(O)-, -NR-, or -SO 2 - wherein one of X 1 or X 2 is -NR- and other of X 1 or X 2 is -C(O)- or -SO 2 -; R1 and R are as described herein; These compounds are effective as inhibitors of Tec family (e.g., Tec, Btk, Itk/Emt/Tsk, Bmx, Txk/Rlk) protein kinases. These compounds and pharmaceutically acceptable compositions thereof are useful for treating or preventing a variety of diseases, disorders or conditions, including, but not limited to, an autoimmune, inflammatory, proliferative, or hyperproliferative disease or an immunologically-mediated disease.
摘要翻译：本发明描述了式（I）化合物或其药学上可接受的盐，其中每个R 3和R 4独立地是H，卤素或C 1〜 4脂族，任选被卤素取代，C 1-2脂族基，OCH 3，NO 2，NH 2， CN，NHCH 3，SCH 3或N（CH）2。 R 2是具有0-3个独立地选自氮，氧或硫的杂原子的3-8元饱和，部分不饱和或完全不饱和的单环，或8-12元饱和的，部分不饱和的，或具有0-5个独立地选自氮，氧或硫的杂原子的完全不饱和的双环体系; R 2任选被J取代; 每个X 1和X 2独立地是-C（O） - ， - NR - 或-SO 2 - ，其中X < SUP> 1或X 2是-NR-，X 1或X 2中的另一个是-C（O） - 或-SO 2 - ; R1和R如本文所述; 这些化合物作为Tec家族（例如，Tec，Btk，Itk / Emt / Tsk，Bmx，Txk / Rlk）蛋白激酶的抑制剂是有效的。这些化合物及其药学上可接受的组合物可用于治疗或预防各种疾病，病症或病症，包括但不限于自身免疫性，炎性，增殖性或过度增殖性疾病或免疫介导的疾病。

17. 发明申请

WO2011038185A2 METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：用于制备作为蛋白激酶抑制剂有用的吡啶衍生物的方法
公开(公告)号：WO2011038185A2
公开(公告)日：2011-03-31
申请号：PCT/US2010/050132
申请日：2010-09-24
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven , KAY, David
发明人： CHARRIER, Jean-Damien , DURRANT, Steven , KAY, David
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： A method of preparing a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula (A) under suitable reductive cyclisation conditions to form a compound represented by Structural Formula (B) wherein R 10 is LG 1 or -X 1 R 1 , and -LG 1 is a suitable leaving group; and b) optionally, when R 10 of Structural Formula (B) is LG 1 , further comprising the step of replacing the -LG 1 of Structural Formula (B) with -X 1 R 1 to form the compound represented by Structural Formula (I).
摘要翻译：一种制备由结构式（I）表示的化合物或其药学上可接受的盐的方法，其中结构式（I）的变量如说明书和权利要求书中所述，包括以下步骤：a）使代表的化合物通过结构式（A）在合适的还原环化条件下形成由结构式（B）表示的化合物，其中R 10是LG1或-X1R1，-LG1是合适的离去基团; 和b）任选地，当结构式（B）的R 10是LG 1时，还包括用-X1R1替代结构式（B）的-LG1以形成由结构式（I）表示的化合物的步骤。

18. 发明申请

WO2007027594A1 3,5-DISUBSTITUTED PYRID-2-ONES USEFUL AS INHIBITORS OF TEC FAMILY OF NON-RECEPTOR TYROSINE KINASES 审中-公开
标题翻译：作为非受体酪氨酸激酶TEC家族的抑制剂的3,5-取代的吡啶-2-酮
公开(公告)号：WO2007027594A1
公开(公告)日：2007-03-08
申请号：PCT/US2006/033510
申请日：2006-08-29
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , RAMAYA, Sham , DURRANT, Steven
发明人： CHARRIER, Jean-Damien , RAMAYA, Sham , DURRANT, Steven
IPC分类号： C07D401/04 , A61K31/4418 , A61P35/00 , A61P37/00
CPC分类号： C07D401/04 , C07D401/12
摘要： The present invention relates to pyrid-2-one compounds of formula (I) useful as inhibitors of Tec family (e.g. Tec, Btk, Itk/emt/Tsk, Bmx, Txk/Rlk) protein kinases. These compounds and pharmaceutically acceptable compositions thereof are useful for treating or preventing autoimmune, inflammatory, proliferative, hyperproliferative or immunologically-mediated diseases, wherein R2' is a ring; Q is 5-membered heteroaryl containing 1-4 nitrogen atoms, wherin one of the nitrogen atoms is NH; each Q is optionally substituted with 0-3 JQ and is optionally fused to ring Q1; each R3 and R4 is as described herein (Formula I).
摘要翻译：本发明涉及可用作Tec家族（例如Tec，Btk，Itk / emt / Tsk，Bmx，Txk / Rlk）蛋白激酶抑制剂的式（I）的吡啶-2-酮化合物。这些化合物及其药学上可接受的组合物可用于治疗或预防自身免疫，炎症，增殖，过度增殖或免疫介导的疾病，其中R2'是环; Q是含有1-4个氮原子的5元杂芳基，其中一个氮原子是NH; 每个Q任选被0-3JQ取代，并且任选地与环Q1稠合; 每个R 3和R 4如本文所述（式I）。

19. 发明申请

WO2007015931A3 CASPASE INHIBITOR PRODRUGS 审中-公开
公开(公告)号：WO2007015931A3
公开(公告)日：2007-02-08
申请号：PCT/US2006/028174
申请日：2006-07-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED , DURRANT, Steven , CHARRIER, Jean-Damien , STUDLEY, John
发明人： DURRANT, Steven , CHARRIER, Jean-Damien , STUDLEY, John
IPC分类号： C07D498/04 , A61K31/429
摘要： This invention relates to prodrugs of caspase inhibitors comprising of a furo [3, 2-d] oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.

20. 发明申请

WO2014089379A9 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
公开(公告)号：WO2014089379A9
公开(公告)日：2014-06-12
申请号：PCT/US2013/073457
申请日：2013-12-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： AHMAD, Nadia , BOYALL, Dean , CHARRIER, Jean-Damien , DAVIS, Chris , DAVIS, Rebecca , DURRANT, Steven , ETXEBARRIA I JARDI, Gorka , FRAYSSE, Damien , JIMENEZ, Juan-Miguel , KAY, David , KNEGTEL, Ronald , MIDDLETON, Donald , ODONNELL, Michael , PANESAR, Maninder , PIERARD, Francoise , PINDER, Joanne , SHAW, David , STORCK, Pierre-Henri , STUDLEY, John , TWIN, Heather
IPC分类号： C07D487/04 , A61K31/495 , A61P35/00
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I) or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula (I-A) or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

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