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    5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-(TRIFLUOROMETHYL)-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF
    4.
    发明申请
    5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-(TRIFLUOROMETHYL)-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF 有权
    5 - [[4 - [[MORPHOLIN-2-YL]甲基氨基] -5-（三氟甲基）-2-吡啶基]氨基]吡嗪-2-羰基酮及其治疗方法

    公开(公告)号：US20150126471A1

    公开(公告)日：2015-05-07

    申请号：US14396338

    申请日：2013-05-14

    Applicant: Cancer Research Technology Limited

    Inventor： Ian Collins ,  Thomas Peter Matthews ,  Tatiana Faria Da Fonseca Mchardy ,  James Osborne ,  Michael Lainchbury ,  Michael Ian Walton ,  Michelle Dawn Garrett

    IPC: C07D413/14 ,  A61K31/4745 ,  A61K9/00 ,  A61K31/7068 ,  A61K31/5377 ,  A61K45/06

    CPC classification number: C07D413/14 ,  A61K9/0053 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/7068 ,  A61K45/06 ,  C07D401/12

    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as “TFM 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 a thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; (e) ionising radiation; (f) an inhibitor of a mitosis regulator or a mitotic checkpoint regulator; (g) an inhibitor of a DNA damage signal transducer; or (h) an inhibitor of a DNA damage repair enzyme.

    Abstract translation: 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及5 - [[4 - [[吗啉-2-基]甲基氨基] -5-（三氟甲基）-2-吡啶基]氨基]吡嗪-2-甲腈化合物（本文称为“TFM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）抗代谢物或胸苷酸合酶（TS）抑制剂; （d）微管靶向剂; （e）电离辐射; （f）有丝分裂调节剂或有丝分裂检查点调节剂的抑制剂; （g）DNA损伤信号传感器的抑制剂; 或（h）DNA损伤修复酶的抑制剂。

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