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    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    4.
    发明公开
    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 有权
    2-氨基-6-氟-N-（5-氟-4-（4-（4-（氧杂环丁烷-3-基）哌嗪-1-基羰基）哌啶-1-基）吡啶-3-基）吡唑并[ 1,5ALPHA]吡咯烷-3-羧酰胺类ALS HEMMSTOFF DER ATR KINASE

    公开(公告)号：EP2941432A1

    公开(公告)日：2015-11-11

    申请号：EP13811716.3

    申请日：2013-12-06

    申请人： Vertex Pharmaceuticals Inc.

    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

    CPC分类号： C07D487/04 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10

    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 defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

    摘要翻译： 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，例如研究激酶在生物学和病理学现象中的用途; 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，其中变量如本文所定义。 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。

    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    7.
    发明公开
    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
    ALS ART-KINASEHEMMERNÜTZLICHEVERBINDUNGEN

    公开(公告)号：EP2723746A1

    公开(公告)日：2014-04-30

    申请号：EP12730138.0

    申请日：2012-06-22

    申请人： Vertex Pharmaceuticals Inc.

    发明人： STORCK, Pierre-Henri ,  CHARRIER, Jean-Damien ,  RUTHERFORD, Alistair ,  MORTIMORE, Michael, Paul ,  MACCORMICK, Somhairle ,  KNEGTEL, Ronald ,  DURRANT, Steven, John

    IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： The present invention relates to pyrrolopyrazines 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): wherein the variables are as defined herein.

    摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的吡咯并吡嗪化合物。 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，例如研究激酶在生物学和病理学现象中的用途; 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：其中变量如本文所定义。

    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    9.
    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：EP2723747A1

    公开(公告)日：2014-04-30

    申请号：EP12732758.3

    申请日：2012-06-22

    申请人： Vertex Pharmaceuticals Inc.

    发明人： EVERITT, Simon ,  MORTIMORE, Michael, Paul ,  CHARRIER, Jean-damien ,  MACCORMICK, Somhairle ,  STORCK, Pierre-henri ,  KNEGTEL, Ronald ,  PINDER, Joanne ,  DURRANT, Steven

    IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P35/00

    CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  A61N5/10

    摘要： The present invention relates to pyrrolopyrazines 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: wherein the variables are as defined herein.

    摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的吡咯并吡嗪类化合物。 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。 本发明化合物具有式I，其中变量如本文所定义。

    CRYSTAL STRUCTURE OF INTERLEUKIN-2 TYROSINE KINASE (ITK) AND BINDING POCKETS THEREOF
    10.
    发明公开
    CRYSTAL STRUCTURE OF INTERLEUKIN-2 TYROSINE KINASE (ITK) AND BINDING POCKETS THEREOF 审中-公开
    晶体结构的白细胞介素-2酪氨酸激酶（ICT）和IT结合位点

    公开(公告)号：EP1697508A2

    公开(公告)日：2006-09-06

    申请号：EP04813070.2

    申请日：2004-12-03

    申请人： Vertex Pharmaceuticals, Inc.

    发明人： CHEETHAM, Graham ,  BROWN, Kieron ,  KNEGTEL, Ronald ,  RENWICK, Suzanne ,  VIAL, Sarah

    IPC分类号： C12N9/12 ,  C07K14/71

    CPC分类号： C12N9/1205 ,  C07K2299/00 ,  G06F19/16

    摘要： The invention relates to molecules or molecular complexes which comprise binding pockets of ITK or its structural homologues. The invention relates to crystallizable compositions and crystals comprising ITK. The present invention also relates to a data storage medium encoded with the structural coordinates of molecules and molecular complexes which comprise the ITK or ITK-like ATP-binding pockets. The present invention also relates to a computer comprising such data storage material. The computer may generate a three-dimensional structure or graphical three-dimensional representation of such molecules or molecular complexes. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to ITK or homologues thereof.