The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.
本公开提供了由式(I)表示的融合1,4-二氮杂环烷,并其药用盐和溶剂合物,其中A、E、R1、R2、R3、R4、R5和Ar如规范中所定义。本公开还涉及使用具有式(I)的化合物来治疗对BET
溴结构域蛋白抑制敏感的疾病、症状或紊乱,如癌症。