The present invention relates to a conjugate of an active substance and hydroxyalkyl starch, wherein the active substance and the hydroxyalkyl starch are linked by a chemical moiety, having a structure according to formula (I)wherein Y is a heteroatom, selected from the group consisting of O and S, and X is selected from the group consisting of SH andsaid conjugate having a structure according to formula (IV)wherein HAS' is the residue of the hydroxyalkyl starch or derivative thereof which was linked to the thioester group, and wherein AS' is the residue of the active substance or a derivative thereof which was linked to the alpha-X beta-amino group,or a structure according to formula (V)wherein HAS' is the residue of the hydroxyalkyl starch or derivative thereof which was linked to the alpha-X beta-amino group, and wherein AS' is the residue of the active substance or a derivative thereof which was linked to the thioester group,and wherein the group -(C=Y) is derived from the thioester group -(C=Y)-S-R' and the group HN-CH-CH2-X is derived from the alpha-X beta amino group.
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机译:活性物质与羟烷基淀粉的缀合物本发明涉及一种活性物质与羟烷基淀粉的缀合物,其中该活性物质与羟烷基淀粉通过化学部分连接,具有根据式(I)的结构 <图像文件=“ IMGA0001.GIF” he =“ 29” imgContent =“ chem” imgFormat =“ GIF” wi =“ 98” /> Chemistry>其中Y是杂原子,选自O和S,并且X选自SH和 <图像文件=“ IMGA0002.GIF” he =“ 19” imgContent =“ chem” imgFormat =“ GIF” wi =“ 28” /> Chemistry>所述缀合物具有根据式(IV)的结构 <图像文件=“ IMGA0003.GIF” he =“ 30” imgContent =“ chem” imgFormat =“ GIF” wi =“ 107” /> Chemistry>其中HAS'是与硫酯基连接的羟烷基淀粉或其衍生物的残基,并且其中AS'是与α-Xβ-氨基连接的活性物质或其衍生物的残基,或根据式(V)的结构 <图像文件=“ IMGA0004.GIF” he =“ 30” imgContent =“ chem” imgFormat =“ GIF” wi =“ 107” /> Chemistry>其中HAS'是连接到α-Xβ-氨基的羟烷基淀粉或其衍生物的残基,其中AS'是连接到硫酯基的活性物质或其衍生物的残基,其中基团-(C = Y)衍生自硫酯基团-(C = Y)-SR',基团HN-CH-CH 2 Sub> -X衍生自α-X β氨基。
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