5-(Pyridin-2-yl-Amino)-Pyrazine-2-Carbonitrile Compounds and Their Therapeutic Use
申请人:Cancer Research Technology Limited
公开号:US20150225372A1
公开(公告)日:2015-08-13
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, 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 thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
本发明涉及治疗化合物领域。更具体地,本发明涉及某些吡啶基氨基吡嗪碳腈化合物,其在其他作用中抑制检查点激酶1(CHK1)激酶功能。本发明还涉及包含这些化合物的制药组合物,以及这些化合物和组合物的使用,无论是体外还是体内,来抑制CHK1激酶功能,并用于治疗由CHK1介导的疾病和病况,通过抑制CHK1激酶功能而改善,等等,包括增殖性疾病如癌症等,可选择与另一药剂联合使用,例如:(a)DNA拓扑异构酶I或II抑制剂;(b)DNA损伤剂;(c)抗代谢物或胸腺嘧啶酸合酶(TS)抑制剂;(d)微管靶向剂;和(e)电离辐射。