发明名称 Aliphatic prodrug linker
摘要 A polymeric prodrug is described which comprises at least one polymer attached via at least one permanent bond to a bicine linker. The bicine linker is attached via a temporary linkage to an amine containing biologically active moiety. The amine containing biologically active moiety—such as a drug—can be released by cleaving the temporary linkage.
申请公布号 US8980242(B2) 申请公布日期 2015.03.17
申请号 US200611993645 申请日期 2006.06.21
申请人 Ascendis Pharma GmbH 发明人 Vetter Dirk;Rau Harald;Wegge Thomas;Hersel Ulrich
分类号 A61K31/74;A61K47/48 主分类号 A61K31/74
代理机构 Frommer Lawrence & Haug LLP 代理人 Frommer Lawrence & Haug LLP
主权项 1. A polymeric prodrug comprising: at least one polymer attached via at least one permanent bond to a bicine linker, the bicine linker being attached via a temporary linkage to an amine containing biologically active moiety; wherein the prodrug has the following structure:and wherein: T is D;D is a residue of an amine containing biologically active moiety;X is a spacer moiety;R2 and R3 are independently selected from the group consisting of hydrogen, acyl groups, and protecting groups for hydroxyl groups;R4 to R12 are independently selected from the group consisting of hydrogen, X—R1, substituted and non-substituted linear, branched and cyclical C1 to C8 alkyls and heteroalkyls, aryls, substituted aryls, substituted and nonsubstituted heteroaryls, cyano, nitro, halogen, carboxy, and carboxamide; andR1 is a polymer.
地址 Hellerup DK