申请人:Mersana Therapeutics, Inc.
公开号:US20160220696A1
公开(公告)日:2016-08-04
Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L
D
-D, the protein based recognition-molecule being connected to the polymeric carrier by L
P
. Each occurrence of D is independently an Auristatin compound. L
D
and L
P
are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
本文提供了Auristatin化合物及其共轭物。该共轭物包括一种基于蛋白质的识别分子(PBRM)和一种聚合物载体,该聚合物载体被取代了一个或多个-LD-D,其中,基于蛋白质的识别分子通过LP连接到聚合物载体上。每个D的出现都是独立的Auristatin化合物。LD和LP是连接治疗剂和PBRM到聚合物载体的连接物。还公开了用于与PBRM共轭形成聚合物-药物-PBRM共轭物的聚合物支架,以及包含共轭物的组合物,其制备方法以及使用共轭物或其组合物治疗各种疾病的方法。