Activated polyethylene glycol esters
AssigneePharmacia Corporation
InventorFoe S. Tjoeng
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Abstract
The present invention relates to the preparation of polyethylene glycol carbonate active esters useful for the PEGylation of biological active and pharmaceutically useful peptides and proteins. The invention involves the use of activated carbonate and oxalate esters in the formation of polyethylene glycol mixed carbonate active esters that then react with a linker or directly with a target peptide or protein.
Claims19
A method of producing an activated ester of polyethylene glycol (PEG), comprising the step of activating PEG with N,N′-disuccinimidyl oxalate or 1,1′-bis[6-(trifluoromethyl)benzotriazolyl] oxalate under the appropriate conditions.
A method of conjugating an activated ester of polyethylene glycol (PEG) and a biologically active nucleophile, comprising the steps:
- (a) activating PEG with N,N′-disuccinimidyl oxalate;
- (b) providing the biologically active nucleophile;
- and
- (c) reacting the PEG active ester and the biologically active nucleophile under appropriate conditions.
A method of conjugating a PEG-linker and a biologically active nucleophile, comprising the steps:
- (a) activating PEG with N,N′-disuccinimidyl oxalate;
- (b) providing a linker;
- (c) reacting the PEG active ester with the linker;
- and
- (d) reacting the resulting PEG-linker with a biologically active nucleophile under appropriate conditions.
A method of conjugating an activated ester of polyethylene glycol (PEG) and a biologically active nucleophile, comprising the steps:
- (a) activating PEG with 1,1′-bis[6-(trifluoromethyl)benzotriazolyl] oxalate;
- (b) providing the biologically active nucleophile;
- and
- (c) reacting the PEG active ester and the biologically active nucleophile under appropriate conditions.
A method of conjugating a PEG-linker and a biologically active nucleophile, comprising the steps:
- (a) activating PEG with 1,1′-bis[6-(trifluoromethyl)benzotriazolyl] oxalate;
- (b) providing a linker;
- (c) reacting the PEG active ester with the linker;
- and
- (d) reacting the resulting PEG-linker with a biologically active nucleophile under appropriate conditions.
Dependencies are inferred from the claim text.