Preparation of an activated polymer ester for protein conjugatio

Chemistry: natural resins or derivatives; peptides or proteins; – Proteins – i.e. – more than 100 amino acid residues – Lymphokines – e.g. – interferons – interlukins – etc.

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530405, 530409, 548520, 548545, 548547, C07D207404, C07K 308, C07K 1506, C07K 1526

Patent

active

052816982

ABSTRACT:
The present invention is a process for preparing an activated ester of polyethylene glycol or a polyoxyethylated polyol. After the activated ester is prepared, it can be reacted with a protein to form a polymer/protein conjugate. Conjugation with a polymer can reduce the protein's immunogenicity, increase its solubility, and increase its circulating in vivo half-life. Preferred proteins are IL-2, CSFs, and interferons.

REFERENCES:
patent: 4341707 (1982-07-01), Ogura et al.
patent: 4904584 (1990-02-01), Shaw
patent: 5235028 (1993-08-01), Barany et al.
Polymer Preprints, vol. 31, No. 2, Aug. 1990, pp. 173-174 and 213-214.

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