公开(公告)号：US20130217871A1

公开(公告)日：2013-08-22

申请号：US13809203

申请日：2011-07-11

申请人： Helmut Knoller ,  Dominik Heckmann ,  Frank Hacket ,  Norbert Zander ,  Saswata Lahiri ,  Nitin Gupta ,  Vivek Kumar ,  Mukesh Madan Mudgal

发明人： Helmut Knoller ,  Dominik Heckmann ,  Frank Hacket ,  Norbert Zander ,  Saswata Lahiri ,  Nitin Gupta ,  Vivek Kumar ,  Mukesh Madan Mudgal

IPC分类号： C08B31/00

CPC分类号： C08B31/00 ,  A61K47/61

摘要： 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.

摘要翻译： 本发明涉及羟基烷基淀粉共轭物及其制备方法，包含羟烷基淀粉衍生物和细胞毒性剂的羟烷基淀粉缀合物，细胞毒性剂包含至少一个伯羟基，其中羟烷基淀粉通过所述初级 羟基对细胞毒性剂。 根据本发明的缀合物具有根据下式HAS'（ - LM）n的结构，其中M是细胞毒性剂的残基，L是连接部分，HAS'是羟烷基淀粉衍生物的残基，以及 n大于或等于1，其中羟烷基淀粉衍生物的平均分子量（MW）高于肾阈值，摩尔取代度（MS）在0.6至1.5的范围内。