Water-Soluble polyene conjugate

US5567685A · kind A · utility

Assignee

• YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD. · IL

Inventors

• Galina Linden · Rishon LeZion, IL
• Abraham J. Domb · Beer Sheva, IL
• Itzhack Polacheck · Jerusalem, IL
• Shimon Benita · Mevaseret Tsiyon, IL

Key dates

• Filing date: Aug 16, 1994
• Grant date: Oct 22, 1996
• Expiry date: Aug 16, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C08B37/0021
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A method for producing a substantially stable water-soluble polysaccharide conjugate of a polyene antibiotic 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; (c) coupling the polyene to the purified dialdehyde by Schiff base formation to form the conjugate; and (d) purifying the conjugate. In a preferred embodiment, the conjugate of step (c) is reduced to an amine conjugate by a reducing agent prior to purification. Also described are imine and amine polysaccaride conjugates of the polyene Nystatin.