申请人:Nippon Kayaku Kabushiki Kaisha
公开号:EP2284209A1
公开(公告)日:2011-02-16
Disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein an amide bond is not used. The compound has chemical stability and adequate drug release rate in the living organism. Specifically disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein a substituent represented by formula (I) is bonded to a carboxy group of a block copolymer which is composed of a polyethylene glycol and a polymer having a carboxy group in a side chain, or a pharmacologically acceptable salt thereof.
[In the formula, A represents a monocyclic or fused aromatic group; G represents an optionally substituted (C1-C6) alkylene group; Y represents a hydrogen atom or a substituent; and E represents a residue of folic acid or a folic acid derivative.]
本发明公开了一种叶酸或叶酸衍生物的聚合物共轭物,其中未使用酰胺键。该化合物在生物体内具有化学稳定性和足够的药物释放率。具体公开了一种叶酸或叶酸衍生物的聚合物共轭物,其中由式(I)代表的取代基键合到嵌段共聚物的羧基上,嵌段共聚物由聚乙二醇和侧链中含有羧基的聚合物组成,或其药理学上可接受的盐。
[式中,A 代表单环或融合芳香基团;G 代表任选取代的(C1-C6)亚烷基;Y 代表氢原子或取代基;E 代表叶酸残基或叶酸衍生物。]