COLLINS, IAN,MATTHEWS, THOMAS PETER,FARIA DA FONSECA MCHARDY, TATIANA,OSBORNE, JAMES,LAINCHBURY, MICHAEL,WALTON, MICHAEL IAN,GARRETT, MICHELLE DAWN
申请号：
IN9221DEN2014
公开号：
IN9221DEN2014A
申请日:
2014.11.04
申请国别(地区):
IN
年份:
2015
代理人:
摘要：
The present invention pertains gen erally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4- [[morpholin-2 -yljmethylamino] -5- (trifluoro - methyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as 'TFM com pounds') which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present in vention also pertains to pharmaceutical composi tions 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 in hibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., op tionally in combination with another agent, for ex ample, (a) a DNA topoisomerase I or II inhibitor； (b) a DNA damaging agent； (c) an antimetabolite or a thymidylate synthase (TS) inhibitor； (d) a mi crotubule 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.
