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    Bicyclylaryl-aryl-amine compounds and their use
    2.
    发明授权
    Bicyclylaryl-aryl-amine compounds and their use 有权
    双环芳基 - 芳基胺化合物及其用途

    公开(公告)号：US08530468B2

    公开(公告)日：2013-09-10

    申请号：US12918266

    申请日：2009-02-19

    申请人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    IPC分类号： A61K31/497 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

    CPC分类号： C07D471/04

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation:

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些双环芳基 - 芳基胺化合物（本文称为BCAA化合物），其特别地抑制检测点激酶1（CHK1）激酶功能 。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射：

    BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE
    6.
    发明申请
    BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE 有权
    双氰胺 - 氨基化合物及其用途

    公开(公告)号：US20100331328A1

    公开(公告)日：2010-12-30

    申请号：US12918266

    申请日：2009-02-19

    申请人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/497 ,  A61P35/00 ,  C12N5/00 ,  C07D241/26 ,  A61K31/4965 ,  C07D413/12

    CPC分类号： C07D471/04

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation:

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些双环芳基 - 芳基胺化合物（本文称为BCAA化合物），其特别地抑制检测点激酶1（CHK1）激酶功能 。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射：

    PYRIMIDINE DERIVATIVES AS ZAP-70 INHIBITORS
    7.
    发明申请
    PYRIMIDINE DERIVATIVES AS ZAP-70 INHIBITORS 审中-公开
    吡嗪衍生物作为ZAP-70抑制剂

    公开(公告)号：US20120142667A1

    公开(公告)日：2012-06-07

    申请号：US13377550

    申请日：2010-06-10

    申请人： Nigel Ramsden ,  Jeremy Major ,  Adeline Morel ,  Mihiro Sunose ,  Nelly Piton

    发明人： Nigel Ramsden ,  Jeremy Major ,  Adeline Morel ,  Mihiro Sunose ,  Nelly Piton

    IPC分类号： A61K31/506 ,  C07D239/48 ,  A61P29/00 ,  C07D405/12 ,  A61P37/08 ,  A61P37/00 ,  A61K31/505 ,  C07D401/12

    CPC分类号： C07D239/48

    摘要： The invention relates to compounds of formula (I) wherein R1 to R5, X and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1至R 5，X和X 1至X 3具有如在说明书和权利要求书中引用的含义。 所述化合物可用作ZAP-70的抑制剂，用于治疗或预防免疫学，炎性，自身免疫性，过敏性疾病和免疫介导的疾病。 本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

    SULFONAMIDES AND SULFAMIDES AS ZAP-70 INHIBITORS
    9.
    发明申请
    SULFONAMIDES AND SULFAMIDES AS ZAP-70 INHIBITORS 审中-公开
    磺酰胺和磺酰胺作为ZAP-70抑制剂

    公开(公告)号：US20120165332A1

    公开(公告)日：2012-06-28

    申请号：US13379027

    申请日：2010-06-17

    申请人： Jeremy Major ,  Nelly Piton

    发明人： Jeremy Major ,  Nelly Piton

    IPC分类号： A61K31/5377 ,  C07D413/12 ,  A61P37/08 ,  C07D403/14 ,  A61P37/02 ,  A61P29/00 ,  A61K31/506 ,  C07D403/12

    CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D403/14

    摘要： The invention relates to compounds of formula (I) wherein R1 to R6 and T0 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

    摘要翻译： 本发明涉及式（I）化合物，其中R1至R6和T0具有在说明书和权利要求书中引用的含义。 所述化合物可用作ZAP-70的抑制剂，用于治疗或预防免疫学，炎性，自身免疫性，过敏性疾病和免疫介导的疾病。 本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。