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    • 10. 发明申请
    • CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION
    • 包含羟基烷基淀粉和细胞毒素的方法及其制备方法
    • US20130178437A1
    • 2013-07-11
    • US13809069
    • 2011-07-11
    • Helmut KnollerDominik HeckmannFrank HacketNorbert Zander
    • Helmut KnollerDominik HeckmannFrank HacketNorbert Zander
    • C07H15/24
    • C07H15/24A61K47/61
    • The present invention relates to hydroxyalkyl starch (HAS) conjugates and to a method for preparing the hydroxyalkyl starch (HAS) conjugates, the hydroxyalkyl starch (HAS) conjugates comprising a hydroxyalkyl starch derivative and a cytotoxic agent, said conjugate having a structure according the following formula HAS′(-M)n wherein M is a residue of a cytotoxic agent, the cytotoxic agent comprising a carbonyl group, HAS′ is a residue of the hydroxyalkyl starch derivative comprising at least one functional group X, n is greater than or equal to 1, and wherein the cytotoxic agent is linked via the carbonyl function present in the cytotoxic agent to the functional group X comprised in the hydroxyalkyl starch derivative, wherein the linkage via the carbonyl function is a cleavable linkage, which is capable of being cleaved in vivo so as to release the cytotoxic agent.
    • 本发明涉及羟烷基淀粉(HAS)缀合物和制备羟烷基淀粉(HAS)偶联物的方法,包含羟烷基淀粉衍生物和细胞毒性剂的羟烷基淀粉(HAS)缀合物,所述缀合物具有下列结构: 式(M)n其中M是细胞毒性剂的残基,细胞毒性剂包含羰基,HAS'是包含至少一个官能团X的羟烷基淀粉衍生物的残基,n大于或等于 至1,并且其中细胞毒性剂通过存在于细胞毒性剂中的羰基官能团连接到包含在羟烷基淀粉衍生物中的官能团X,其中通过羰基官能团的键可切割键,其能够被切割 以释放细胞毒性剂。