[EN] HYDROPHOBICALLY TAGGED SMALL MOLECULES AS INDUCERS OF PROTEIN DEGRADATION<br/>[FR] PETITES MOLÉCULES MARQUÉES DE FAÇON HYDROPHOBE EN TANT QU'INDUCTEURS DE LA DÉGRADATION DE PROTÉINE
申请人:DANA FARBER CANCER INST INC
公开号:WO2014063061A1
公开(公告)日:2014-04-24
Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.
提供了化学式(I)的双功能小分子,或其药用盐,其中M代表一个小有机分子,可以共价或非共价结合激酶,如Her3蛋白激酶;L1代表一个连接物;RH代表一个疏水基团。化合物化学式(I)的一个例子是化合物化学式(II)。还提供了包含化学式(I)或(II)的药物组合物,以及使用这些化合物治疗增殖性疾病的方法。