Conjugates of biologically active substances

Details Conjugates of biologically active substances Conjugates of biologically active substances

1998-06-04

2000-01-04

Peselev, Elli

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 25, 530395, 536 64, 536 186, 5361231, A61K 3702, A61K 3736, C07K 1300

Patent

active

060110082

ABSTRACT:
A method for producing a water-soluble polysaccharide conjugate of an oxidation-sensitive substance is described. The method comprises the following steps: (a) activating the polysaccharide to a dialdehyde by periodate oxidation; (b) purifying the dialdehyde from interfering anions and by-products; and (c) coupling the substance to the purified dialdehyde by Schiff base formation to form the conjugate. Optionally, the conjugate of step (c) is reduced to an amine conjugate by a reducing substance. The product conjugate may then be further purified from various reaction byproducts. The disclosed method results in the substance substantially retaining its biological activity. Also described are imine and amine polysaccaride conjugates of various drugs and polypeptides.

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