会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明申请
    • BIVALENT BROMODOMAIN INHIBITORS AND USES THEREOF
    • 双活性BROMODOMAIN抑制剂及其用途
    • WO2017091673A8
    • 2017-06-01
    • PCT/US2016/063502
    • 2016-11-23
    • DANA-FARBER CANCER INSTITUTE, INC.
    • QI, JunTANAKA, MinoruROBERTS, Justin, M.BRADNER, James E.
    • A61K31/5025C07D487/04
    • 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 BDl and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.
    • 本发明提供了BET溴结构域的二价抑制剂,例如式(I),(II),(III),(IV),(V)和(VI)的化合物。 一些含溴结构域蛋白(例如BRD4)具有包含多于一个溴结构域结合位点的串联溴结构域一级结构(例如,BRD4包含BD1和BD2)。 本文提供的BET溴结构域的二价抑制剂可以通过有利的多价相互作用靶向溴结构域,因此可以治疗与含溴结构域的蛋白质相关的疾病或病症。 本发明还提供了包含本发明化合物的药物组合物和试剂盒,以及使用本发明化合物的方法。