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发明授权
CN104302635B 5-[[4-[[吗啉-2-基]甲基氨基]-5-(三氟甲基)-2-吡啶基]氨基]吡嗪-2-腈及其治疗应用 有权

5-[[4-[[吗啉-2-基]甲基氨基]-5-(三氟甲基)-2-吡啶基]氨基]吡嗪-2-腈及其治疗应用
摘要：
本发明总体上涉及治疗化合物的领域。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-腈化合物(在此称作“TFM化合物”)，其，除其他外，抑制细胞周期检测点激酶1(CHK1)激酶功能。本发明还涉及包含这样的化合物的药物组合物，和这样的化合物与组合物在体外和体内以抑制CHK1激酶功能的应用，以及在由CHK1介导的、通过抑制CHK1激酶功能改善等的疾病和病况的治疗中的应用，包括增殖性病况如癌症等，可选地与其他药剂组合，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成酶(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测点调节剂的抑制剂；(g)DNA损伤信号转导剂的抑制剂；和(h)DNA损伤修复酶的抑制剂。
摘要（英）：

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.

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