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US 2005/0147583 A1Published application
Hydrolytically degradable carbamate derivatives of poly(ethylene glycol)
AssigneeNektar Therapeutics AL, Corporation
InventorsMichael Bentley, Xuan Zhao
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Abstract
Poly(ethylene glycol) carbamate derivatives useful as water-soluble prodrugs are disclosed. These degradable poly(ethylene glycol) carbamate derivatives also have potential applications in controlled hydrolytic degradation of hydrogels. In such degradable hydrogels, drugs may be trapped in the gel and released by diffusion as the gel degrades, or they may be covalently bound through hydrolyzable carbamate linkages. Hydrolysis of these carbamate linkages releases the drug at a controllable rate as the gel degrades.
Claims30
1-7. (canceled)
A method of preparing a prodrug conjugate, said method comprising:
- a) providing a polymer having the structure:
- where
- POLY is a water soluble, non-peptidic polymer;
- L is a linking group;
- Ar is an aromatic group;
- and
- X is an activating group capable of reacting with an amino group of a biologically active agent to form a carbamate linkage, and
- b) reacting said polymer with a biologically active agent, H2N—Y, wherein H2N—Y is a biologically active agent comprising at least one amino group, under conditions effective to displace X from said polymer to thereby form a prodrug having the structure:
5 more elements
Dependencies are inferred from the claim text.