CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION
申请人:Knoller Helmut
公开号:US20130217871A1
公开(公告)日:2013-08-22
The present invention relates to hydroxyalkyl starch conjugates and a method for preparing the same, the hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one primary hydroxyl group, wherein the hydroxyalkyl starch is linked via said primary hydroxyl group to the cytotoxic agent. The conjugates according to the present invention have a structure according to the following formula HAS′(-L-M)
n
wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS′ is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold and a molar substitution (MS) in the range of from 0.6 to 1.5.
本发明涉及羟基烷基淀粉共轭物及其制备方法,所述羟基烷基淀粉共轭物包括羟基烷基淀粉衍生物和细胞毒素药物,所述细胞毒素药物包括至少一个主要羟基基团,其中羟基烷基淀粉通过所述主要羟基基团与细胞毒素药物连接。本发明的共轭物具有以下式子的结构:HAS'(-L-M)n,其中M是细胞毒素药物的残基,L是连接基团,HAS'是羟基烷基淀粉衍生物的残基,n大于等于1,且羟基烷基淀粉衍生物具有平均分子量(MW)高于肾小球阈值且摩尔取代(MS)在0.6至1.5范围内。