申请人:Nippon Kayaku Kabushiki Kaisha
公开号:EP2431403A1
公开(公告)日:2012-03-21
A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.
Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, R8 and R9 each independently are hydrogen atom or (C1-C6) alkyl which may have a substituent, R10 is hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX-CY represents CH-CH or C=C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups].
我们需要一种生理活性物质的聚合物共轭物,它能使药物释放不受生物酶的影响,并可望具有较高的治疗效果。
本发明提供了一种生理活性物质的聚合物共轭物,它包括聚乙二醇分子和具有两个或两个以上羧基的聚合物的嵌段共聚物,其中通式(I)或通式(II)所代表的取代基通过酰胺键与嵌段共聚物的至少一个侧链羧基相连[式中,R8 和 R9 各自独立地为氢原子或可具有取代基的(C1-C6)烷基、R10 是氢原子、可能具有取代基的 (C1-C40) 烷基、可能具有取代基的 (C1-C40) 芳烷基、可能具有取代基的芳香基、具有受保护羧基的氨基酸残基或可能具有取代基的糖残基,CX-CY 代表 CH-CH 或 C=C(双键),A 代表通过从具有一个或多个羟基的生理活性物质中去除一个或多个羟基而得到的残基]。