申请人:Vertex Pharmaceuticals Incorporated
公开号:EP3311816A1
公开(公告)日:2018-04-25
The present invention relates to compounds useful as inhibitors of ATR protein kinase for use in the treatment of a cancer having a defect in the ATM signaling pathway. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of this invention and combination therapies thereof; use of said compounds in the treatment of various diseases, disorders, and conditions; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.
The compounds of this invention have formula I:
wherein the variables are as defined herein. Preferably, the compound is VE-822.
本发明涉及作为 ATR 蛋白激酶抑制剂用于治疗 ATM 信号通路缺陷癌症的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物及其联合疗法;所述化合物在治疗各种疾病、失调和病症中的用途;制备本发明化合物的工艺;制备本发明化合物的中间体;以及在体外应用中使用本发明化合物的方法,例如研究生物和病理现象中的激酶;研究由此类激酶介导的细胞内信号转导通路;以及比较评估新的激酶抑制剂。
本发明的化合物具有式 I:
其中变量如本文所定义。优选地,本发明化合物为 VE-822。