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US 9,309,507 B2Granted
Conjugated blood coagulation factor VIIa
AssigneePolytherics Limited
InventorWilliam Henry
Life of this patent
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Abstract
The present invention provides a biocompatible polymer conjugated to FVIIa via one or more cysteine residues, suitably via a linker across a reduced disulphide bond in FVIIa, and pharmaceutical compositions comprising such conjugated forms of FVIIa.
Claims25
A Factor VIIa-polyethylene glycol conjugate, wherein one or more polyethylene glycol groups are conjugated to FVIIa by a linker group bridging the sulphur atoms of two cysteine residues that formed a disulphide bond in FVIIa,
- wherein each polyethylene glycol group conjugated to FVIIa by a linker group bridging the sulphur atoms of two cysteine residues that formed a disulphide bond in FVIIa:
- wherein R1 is a substituent which is a direct bond, an alkylene group, or an optionally-substituted aryl or heteroaryl group;
- wherein the aryl group is selected from the group consisting of phenyl, benzoyl and naphthyl;
- wherein a suitable heteroaryl group is selected from the group consisting of pyridine, pyrrole, furan, pyran, imidazole, pyrazole, oxazole, pyridazine, pyrimidine and purine;
- wherein linkage to the polymer is by a hydrolytically labile bond, or by a nonlabile bond.
2 more elements
Dependencies are inferred from the claim text.