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    COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
    2.
    发明申请
    COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
    化合物作为蛋白激酶抑制剂有用

    公开(公告)号：WO2008076392A3

    公开(公告)日：2008-08-07

    申请号：PCT/US2007025688

    申请日：2007-12-14

    Applicant: VERTEX PHARMA ,  CHARRIER JEAN DAMIEN ,  KAY DAVID ,  KNEGTEL RONALD

    Inventor： CHARRIER JEAN DAMIEN ,  KAY DAVID ,  KNEGTEL RONALD

    IPC: C07D475/12

    CPC classification number: C07D475/00

    Abstract: 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.

    Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 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
    4.
    发明申请
    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
    化合物作为ATR激酶的抑制剂有用

    公开(公告)号：WO2014089379A1

    公开(公告)日：2014-06-12

    申请号：PCT/US2013073457

    申请日：2013-12-06

    Applicant: VERTEX PHARMA

    Inventor： 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: C07D487/04 ,  A61K31/495 ,  A61P35/00

    CPC classification number: C07D487/04 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10

    Abstract: 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.

    Abstract translation: 本发明涉及可用作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化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型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，其中变量如本文所述。 此外，本发明的化合物具有式（I-A）或其药学上可接受的盐，其中变量如本文所定义。

    METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
    5.
    发明申请
    METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
    用于制备可用作蛋白激酶抑制剂的吡啶衍生物的方法

    公开(公告)号：WO2011038185A3

    公开(公告)日：2013-12-05

    申请号：PCT/US2010050132

    申请日：2010-09-24

    Applicant: VERTEX PHARMA ,  CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  KAY DAVID

    Inventor： CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  KAY DAVID

    IPC: C07D403/12

    CPC classification number: C07D487/14

    Abstract: 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 R10 is LG1 or -X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with -X1R1 to form the compound represented by Structural Formula (I).

    Abstract translation: 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为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。

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