申请人:Mersana Therapeutics, Inc.
公开号:US20160022829A1
公开(公告)日:2016-01-28
A tubulysin compound conjugate is 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 a tubulysin compound having a molecular weight≦5 kDa. L
D
and L
P
are distinct linkers connecting the tubulysin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-tubulysin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
本文提供了一种管芽菌素化合物结合物。该结合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的出现独立地是分子量≦5 kDa的管芽菌素化合物。LD和LP是连接管芽菌素化合物和PBRM分别到聚合物载体的不同连接物。还公开了用于与PBRM结合形成聚合物-管芽菌素化合物-PBRM结合物的聚合物支架,包括结合物的组合物,其制备方法以及使用结合物或其组合物治疗各种疾病的方法。