James E. Bradner,Jun Qi,Minoru Tanaka,Justin M. Roberts
申请号：
US15778831
公开号：
US20180354973A1
申请日:
2016.11.23
申请国别(地区):
US
年份:
2018
代理人:
摘要：
The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V) and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases comprising the inventive compounds, as well as methods of using the inventive compounds.
