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US 5,122,614 AGranted
Active carbonates of polyalkylene oxides for modification of polypeptides
AssigneeEnzon, Inc.
InventorShmuel Zalipsky
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Abstract
Poly(ethylene glycol)-N-succinimide carbonate and its preparation are disclosed. Polyethylene glycol (PEG) is converted into its N-succinimide carbonate derivative. This form of the polymer reacts readily with amino groups of proteins in aqueous buffers. The modified proteins have PEG-chains grafted onto the polypeptide backbone by means of stable, hydrolysis-resistant urethane (carbamate) linkages.
Claims6
A compound having the structure:
- ##STR8## wherein R.sub.1 is H--, H.sub.3 C--, or an oxycarbonyl-N-dicarboximide group;
- wherein each R.sub.2, R.sub.3, and R.sub.4 is an alkyl group which may be straight or branched, and wherein each R.sub.2, R.sub.3, and R.sub.4 may be independently the same as, or different from, the others of R.sub.2, R.sub.3, and R.sub.4 ;
- wherein R.sub.5 is an N-dicarboximide group;
- and
- wherein a is an integer between 1 and 1000 and each of b and c is an integer between 0 and 1000, and the sum of a, b, and c is between 10 and 1000.
2 more elements
Dependencies are inferred from the claim text.