[EN] AURISTATIN COMPOUNDS AND CONJUGATES THEREOF<br/>[FR] COMPOSÉS AURISTATINE ET LEURS CONJUGUÉS
申请人:MERSANA THERAPEUTICS INC
公开号:WO2014093379A1
公开(公告)日:2014-06-19
An auristatin 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 an auristatin compound having a molecular weight ≤ 5 kDa. LD and Lp are distinct linkers connecting the auristatin compound and PBRM to the polymeric earner respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-auristatin 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auristatin化合物结合物。该结合物包括基于蛋白质的识别分子(PBRM)和聚合物载体,其被取代一个或多个-LD-D,其中,基于蛋白质的识别分子通过Lp与聚合物载体相连。每个D的出现都是独立的,具有分子量≤5 kDa的auristatin化合物。LD和Lp是连接auristatin化合物和PBRM到聚合物载体的不同连接物。还揭示了用于与PBRM结合形成聚合物-auristatin化合物-PBRM结合物的聚合物支架,以及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。