Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]
x
, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp
3
hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.
本发明揭示了一种
水溶性聚合物共轭物,其包括结构POLY-[Y—S—S-A]x,其中POLY是一种
水溶性聚合物;Y是一个碳氢基的间隔基团,x为1至25,S—S是连接到Y的sp3杂化碳的二
硫键基团;而A是一种药理活性分子的共价连接残基。最好的情况下,
水溶性聚合物是一种P
EG聚合物。本发明还揭示了制备这种共轭物有用的聚合物试剂,以及其形成和使用的方法。