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US 6,177,087 B1Granted
Non-antigenic amine derived polymers and polymer conjugates
AssigneeEnzon, Inc.
InventorsRichard B. Greenwald, Anthony Martinez, Annapurna Pendri
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Abstract
Substantially non-antigenic polymers containing pI and/or pH optimum modulating moieties are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed.
Claims13
A method of treatment comprising administering to a mammal in need thereof a therapeutically effective amount of a polymer conjugate comprising the formula:
- [R—B′—W—L1]z-(nucleolphile)
- wherein:
- (R) is a water soluble substantially non-antigenic polvmer residue:
- (B′) is a secondary or tertiary amine;
- when B′ is a tertiary amine, (W) is a spacer moietv selected from the group consisting of straight or branched C1-4alkyls, aralkyls, aryls, heteroarwl moieties, C(O)NHCH2CH2C(O) and CH2(O);
- when B′ is a secondary amine, (W) is selected from the group consisting of aralkyls, aryls, heteroaryl moieties, C(O)NHCH2CH2C(O) and CH2C(O);
- (nucleophile) is a member of the group consisting of proteins and chemotherapeutic agents;
- (L1) represents a covalent linkage between R—B′—W) and the nucleophile;
- and
- (z) represents the number of polymers attached to the nucleophile.
7 more elements
Dependencies are inferred from the claim text.