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    METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
    2.
    发明公开
    METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
    PROCESS FOR PRODUCING嘧啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：EP2480553A2

    公开(公告)日：2012-08-01

    申请号：EP10819504.1

    申请日：2010-09-24

    申请人： Vertex Pharmaceuticals Incorporated

    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).

    THIOPHENE-CARBOXAMIDES USEFUL AS INHIBITORS OF PROTEIN KINASES
    3.
    发明公开
    THIOPHENE-CARBOXAMIDES USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
    噻吩甲酰胺用作蛋白激酶抑制剂

    公开(公告)号：EP2027116A2

    公开(公告)日：2009-02-25

    申请号：EP07795219.0

    申请日：2007-05-23

    申请人： VERTEX PHARMACEUTICALS INCORPORATED

    发明人： BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ronald ,  RAMAYA, Sharn

    IPC分类号： C07D409/04

    CPC分类号： C07D409/04

    摘要： The present invention relates to compounds 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.

    摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。 本发明还提供了制备本发明化合物的方法。

    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    10.
    发明公开
    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
    用作ATR激酶抑制剂的化合物

    公开(公告)号：EP2970288A1

    公开(公告)日：2016-01-20

    申请号：EP13812337.7

    申请日：2013-12-06

    申请人： Vertex Pharmaceuticals Incorporated

    发明人： CHARRIER, Jean-Damien ,  DAVIS, Chris ,  DURRANT, Steven ,  FRAYSSE, Damien ,  JIMENEZ, Juan-Miguel ,  KAY, Dave ,  KNEGTEL, Ronald ,  O'DONNELL, Michael ,  PIERARD, Francoise ,  PINDER,Joanne ,  STORCK, Pierre-Henri ,  TWIN, Heather

    IPC分类号： C07D487/04 ,  A61K31/437 ,  A61P35/00

    CPC分类号： C07D487/04 ,  A61K31/437 ,  C07D491/107 ,  C07D519/00

    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 R
    1 , R
    2 , R
    3 , and R
    4 are as defined herein.

    摘要翻译： 本发明涉及用作ATR蛋白激酶抑制剂的化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用这些化合物的方法，例如生物学和病理学现象中的激酶研究; 这种激酶介导的细胞内信号转导途径的研究; 和新的激酶抑制剂的比较评估。 本发明的化合物具有式（I）; 或其药学上可接受的盐，其中变量R 1，R 2，R 3和R 4如本文所定义。