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US 5,614,549 AGranted
High molecular weight polymer-based prodrugs
AssigneeEnzon, Inc.
InventorsRichard B. Greenwald, Annapurna Pendri
Life of this patent
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Abstract
Water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active nucleophile; M is X or Q; x is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y'; Y and Y' are oxygen or sulfur; R is a polyalkylene oxide; and Z is OH, C.sub.1-4 alkyl moieties or ##STR2## are disclosed.
Claims10
A composition of the formula:
- ##STR26## wherein:
- R.sub.1 is C.sub.6 H.sub.5 or (CH.sub.3).sub.3 CO;
- R.sub.2 is H or CH.sub.3 CO;
- and
- R.sub.3 is aryl, aralkyl or heteroaryl.
2 more elements
A taxane-based composition, comprising the formula:
- ##STR27## wherein:
- R.sub.1 is C.sub.6 H.sub.5 (CH.sub.3).sub.3 CO;
- R.sub.2 is H or CH.sub.3 CO;
- R.sub.3 is aryl, aralkyl or heteroaryl;
- M is X or Q;
- X is an electron withdrawing group;
- Q is a moiety containing a free electron pair positioned five or six atoms from Y',
- Y and Y' are independently O or S;
- R is a polyalkylene oxide;
- and
- Z is one of OH, a C.sub.1-4 alkyl moiety or ##STR28## wherein D is a biologically active nucleophile.
8 more elements
Dependencies are inferred from the claim text.