Hydrolytically degradable carbamate derivatives of poly (ethylene glycol)
AssigneeShearwater Corporation
InventorsMichael David Bentley, Xuan Zhao
Life of this patent
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Abstract
Poly(ethylene glycol) carbamate derivatives useful as water-soluble pro-drugs 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 either 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 amine drug at a controllable rate as the gel degrades.
Claims18
A compound having the formula:
- wherein:
- POLY is a water soluble, non-peptidic polymer;
- L is a hydrolytically stable linking group;
- Ar is an aromatic group;
- and
- X is activating group capable of reacting with a moiety of a biologically active agent to form a carbamate linkage.
A compound having the formula:
- wherein:
- L is —O— or —NHCO—;
- POLY is poly(ethylene glycol) having a capping group selected from the group consisting of—OH, alkoxy, and
- wherein L is as described.
A compound having the formula:
- wherein:
- POLY is a poly(ethylene glycol) having a molecular weight of from about 200 to about 100,000 Daltons;
- L is a hydrolytically stable linking group;
- Ar is an aromatic group;
- and
- X is activating group capable of reacting with a moiety of a biologically active agent to form a carbamate linkage.
A compound having the formula:
- wherein:
- POLY is a water soluble, non-peptidic polymer selected from the group consisting of poly(alkylene oxides), copolymers of ethylene glycol and propylene glycol, poly(oxyethylated polyols), poly(vinyl alcohol), carbohydrate-based polymers, and random or block copolymers and terpolymers based on monomers of the these polymers;
- L is a hydrolytically stable linking group;
- Ar is an aromatic group;
- and
- X is activating group capable of reacting with a moiety of a biologically active agent to form a carbamate linkage.
Dependencies are inferred from the claim text.