公开(公告)号：US20180036294A1

公开(公告)日：2018-02-08

申请号：US15553593

申请日：2016-02-26

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng WANG ,  Yujun ZHAO ,  Bing ZHOU ,  Angelo AGUILAR

IPC分类号： A61K31/437 ,  C07D487/14 ,  C07D231/38 ,  C07D471/04 ,  C07D261/06 ,  A61K31/519 ,  C07D487/04

CPC分类号： A61K31/437 ,  A61K31/519 ,  C07D231/38 ,  C07D261/06 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14

摘要： The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.