申请人:Andrulis Research Corporation
公开号:EP0137900A1
公开(公告)日:1985-04-24
Bis-platinum complexes having the formula
wherein A is a ligand having two pairs of platinum-coordinating acidic groups which are each independently a carboxylate, phenolate, sulfonate or phosphonate group, each said pair being capable of coordinating with a platinum ion to form a 5-10 membered chelate ring; Z is a water-solubilizing group; n is 0 or a positive integer, with the proviso that n is 0 only when at least one of said platinum-coordinating acidic groups is sulfonate or phosphonate or when at least one platinum ion is a Pt(IV) ion; and R1, R2, R3, R4, R. and R6 are each independently H or a C1-20 alkyl, aryl, aralkyl, or alkaryl group, or together form one or more C1-30 alkylene, cycloalkylene, arylene, aralkylene or alkarylene groups; or a pharmaceutically acceptable salt thereof, are useful as readily water-soluble antitumor agents.
双铂配合物,其式如下
其中 A 是配体,具有两对铂配位酸性基团,这两对酸性基团各自独立地为羧酸基、苯酚基、磺酸基或膦酸基,每对酸性基团都能与铂离子配位形成一个 5-10 分子的螯合环;Z 是水溶性基团; n 是 0 或正整数,但只有当至少一个铂配位酸性基团是磺酸盐或膦酸盐时,或至少一个铂离子是 Pt(IV) 离子时,n 才为 0;以及 R1、R2、R3、R4、R.和 R6 各自独立地为 H 或 C1-20 烷基、芳基、烷基或烷芳基,或共同形成一个或多个 C1-30 烷基、环烷基、芳基、烷基或烷芳基;或其药学上可接受的盐,可用作易溶于水的抗肿瘤剂。