[EN] DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS<br/>[FR] DÉRIVÉS DE DOLASTATINE 10 ET D'AURISTATINES
申请人:PF MEDICAMENT
公开号:WO2014174062A1
公开(公告)日:2014-10-30
The present invention concerns a compound of following formula (I) where: - R1 is H or OH, - R2 is a (C1-C6)alkyl, COOH, COO-((C1-C6)alkyl) or thiazolyl group, - R3 is H or a (C1-C6)alkyl group, and - R4 is: - an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or - a heterocycle-(C1-C8)alkyl group optionally substituted by one or more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.
本发明涉及以下式(I)的化合物,其中:- R1为H或OH,- R2为(C1-C6)烷基,COOH,COO-((C1-C6)烷基)或噻唑基,- R3为H或(C1-C6)烷基,- R4为:- 被OH和NR9R10基之一或多个基团取代的芳基-(C1-C8)烷基,或- 可选择地被(C1-C6)烷基,OH和NR12R13基团之一或多个基团取代的杂环-(C1-C8)烷基,或其药学上可接受的盐、水合物或溶剂化合物,以及其在特定用途中,特别是用于治疗癌症的用途,含有相同化合物的药物组合物以及其制备方法。