Conjugates of hydroxyalkyl starch and an active substance, prepared by chemical ligation via thiazolidine
申请人:Fresenius Kabi Deutschland GmbH
公开号:EP1762250A1
公开(公告)日:2007-03-14
The present invention relates to a method for preparing conjugates of an active substance and hydroxyalkyl starch and to conjugates of an active substance and hydroxyalkyl starch, preferably hydroxyethyl starch, wherein the conjugates are prepared by covalently linking the hydroxyalkyl starch and the active substance by a chemical residue having a structure according to formula (I)
or formula (I')
or formula (I")
wherein R1, R2, R2', R3, R3' and R4 are independently selected from the group consisting of hydrogen, an optionally suitably substituted, linear, cyclic and/or branched alkyl, aryl, heteroaryl, aralkyl, and heteroaralkyl group, preferably hydrogen.
本发明涉及一种制备活性物质和羟基烷基淀粉共轭物的方法,以及制备的活性物质和羟基烷基淀粉共轭物,优选羟乙基淀粉。共轭物是通过化学残基(具有公式(I)、公式(I')或公式(I")结构)共价连接羟基烷基淀粉和活性物质而制备的,其中R1、R2、R2'、R3、R3'和R4独立地选自氢、可选适当取代的线性、环状和/或支链烷基、芳基、杂芳基、芳基烷基和杂芳基烷基群,优选氢。