申请人:Yale University
公开号:US20160022642A1
公开(公告)日:2016-01-28
The present description includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In certain embodiments, the description includes a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. The target protein contemplated within the description comprises an androgen receptor. Compounds of the present description may be used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.
本描述包括作为目标蛋白质降解剂的化合物,其中降解与目标蛋白质的类别或其定位无关。在某些实施例中,描述包括一种化合物,其中蛋白质降解基团与连接剂共价结合,该化合物的ClogP等于或高于1.5。描述中考虑的目标蛋白质包括雄激素受体。本描述的化合物可用于治疗蛋白质降解是可行治疗方法的疾病状态,如癌症或任何一种氧化应激疾病状态。