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1. WO1996005212 - WATER-SOLUBLE POLYENE CONJUGATE

Publication Number WO/1996/005212
Publication Date 22.02.1996
International Application No. PCT/US1995/010522
International Filing Date 16.08.1995
Chapter 2 Demand Filed 07.03.1996
IPC
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C08B 37/00 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/-C08B35/110; Derivatives thereof
C08B 37/02 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/-C08B35/110; Derivatives thereof
02Dextran; Derivatives thereof
CPC
A61K 47/61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
61the organic macromolecular compound being a polysaccharide or a derivative thereof
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C08B 37/0021
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
0006Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
0009alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
0021Dextran, i.e. (alpha-1,4)-D-glucan; Derivatives thereof, e.g. Sephadex, i.e. crosslinked dextran
C08B 37/006
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
006Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
Applicants
  • HELFGOTT & KARAS, P.C. [US]/[US] (MW)
  • YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM [IL]/[IL]
Inventors
  • LINDEN, Galina
  • DOMB, Abraham, J.
  • POLACHECK, Itzhack
  • BENITA, Shimon
Agents
  • KARAS, Aaron, B.
Priority Data
08/291,29216.08.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) WATER-SOLUBLE POLYENE CONJUGATE
(FR) CONJUGUE DE POLYENE HYDROSOLUBLE
Abstract
(EN)
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 polysaccharide conjugates of the polyene Nystatin.
(FR)
L'invention concerne un procédé d'obtention d'un conjugué polysaccharide d'un antibiotique polyène. Le procédé consiste: (a) à activer le polysaccharide pour obtenir un dialdéhyde après oxydation par du periodate; (b) à purifier le dialdéhyde par retrait des anions et des sous-produits perturbateurs; (c) à accoupler le polyène au dialdéhyde par formation des bases de Schiff afin de former le conjugué; et (d) à purifier le conjugué. Selon un mode de réalisation préféré, le conjugué obtenu en (c) subit sous l'effet d'un agent réducteur une réduction produisant un conjugué d'amine avant sa purification. L'invention concerne par ailleurs des conjugués polysaccharide d'imine et d'amine du polyène Nystatine.
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