Stabilized polymeric thiol reagents
AssigneeNektar Therapeutics
InventorsAntoni Kozlowski, Samuel P. Mcmanus
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Abstract
Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 2, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.
Claims11
A polymer conjugate comprising the structure:
- POLY-[Y—S—S-A]x
- wherein:
- POLY is a water soluble polymer which is a polyethylene glycol;
- Y is a divalent linking group consisting of a saturated hydrocarbon backbone which is 4 to 6 carbon atoms in length and has substitutents selected from the hydrogen and methyl;
- S—S is a disulfide group attached to an sp3 hybridized carbon of Y;
- and
- A is a covalently linked residue of a pharmacologically active molecule;
- and
- x is 1 or 2.
A composition comprising, in a pharmaceutically acceptable carrier, a conjugate having the structure:
- POLY-[Y—S—S-A]x
- wherein:
- POLY is a water soluble polymer which is a polyethylene glycol;
- Y is a divalent linking group consisting of a saturated hydrocarbon backbone which is 4 to 6 carbon atoms in length and has substitutents selected from the hydrogen and methyl;
- S—S is a disulfide group attached to an sp3 hybridized carbon of Y;
- and
- A is a covalently linked residue of a pharmacologically active molecule, wherein said pharmacologically active molecule has a reactive thiol group in unconjugated form;
- and
- x is 1 or 2.
Dependencies are inferred from the claim text.