High molecular weight polymer-based prodrugs

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United States of America Patent

PATENT NO 5965566
SERIAL NO

08914927

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention is directed compositions of the formula: ##STR1## 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; wherein: R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls; wherein: R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted allyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## wherein: R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.

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Patent Owner(s)

  • ENZON, INC.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Greenwald, Richard B Somerset, NJ 79 4892
Pendri, Annapurna Matawan, NJ 50 2186
Zhao, Hong Piscataway, NJ 281 3784

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