| 摘要 |
The present invention is directed to compositions of formula (I) 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 (0) or a positive integer, preferably from 1 to about 12; R1 and R2 are independently selected from the group consisting of H, C1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C1-6 alkyls; R3 is a substantially non-antigenic polymer, C1-12 straight or branched alkyl or substituted alkyl, C5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or (a); and R4 and R5 are independently selected from the group consisting of H, C1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C1-6 alkyls or jointly form a cyclic C5-C7 ring; except that R1 and R2 are both not H when n is I (one) when R3 is a substantially non-antigenic polymer. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.
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