Polymer-based prodrugs with molecular weights greater than 20,000 which comprise non-antigenic polymers

摘要

A water soluble prodrug of formula D-Y'-C(=Y)-[C(R1)(R2)]n-X-R3 is claimed wherein: D is a residue of biologically active moiety; X is an electron withdrawing group; Y and Y' are independently O or S; n is zero or a positive integer R1 and R2 are independently H, alkyl or optionally substituted aryl, aralkyl or heteroaryl; R3 is a substantially non-antigenic polymer, optionally substituted alkyl or cycloalkyl, carboxyalkyl, carboalkoxyalkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or -NR4R5 and R4 and R5 are independently H, alkyl or optionally substituted aryl, aralkyl, heteroaryl or jointly form a cyclic C5-C7 ring except that R1 and R2 are both not H when n is 1 and R3 is a substantially non-antigenic polymer.