[EN] TUBULYSIN COMPOUNDS AND CONJUGATES THEREOF<br/>[FR] COMPOSÉS DE TUBULYSINE ET LEURS CONJUGUÉS
申请人:MERSANA THERAPEUTICS INC
公开号:WO2014160360A1
公开(公告)日:2014-10-02
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 -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by Lp. Each occurrence of D is independently a tubulysin compound having a molecular weight < 5 kDa. LD and Lp 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.
本文提供了一种管状霉素化合物结合物。该结合物包括基于蛋白质的识别分子(PBRM)和与一个或多个-LD-D取代的聚合物载体,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的出现独立地是具有分子量<5 kDa的管状霉素化合物。LD和Lp是连接管状霉素化合物和PBRM到聚合物载体的不同连接物。还公开了用于与PBRM结合形成本文所述聚合物-管状霉素化合物-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。