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1. WO1999028351 - PERSULFATED CHONDROITIN SULFATES, PROCESS FOR PRODUCING THE SAME, AND ANTICOAGULANTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

Publication Number WO/1999/028351
Publication Date 10.06.1999
International Application No. PCT/JP1998/000023
International Filing Date 08.01.1998
IPC
A61K 31/715 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
C08B 37/08 2006.1
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
08Chitin; Chondroitin sulfate; Hyaluronic acid; Derivatives thereof
CPC
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
C08B 37/0069
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
0063Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
0069Chondroitin-4-sulfate, i.e. chondroitin sulfate A; Dermatan sulfate, i.e. chondroitin sulfate B or beta-heparin; Chondroitin-6-sulfate, i.e. chondroitin sulfate C; Derivatives thereof
Applicants
  • SHIN NIPPON YAKUGYO CO., LTD. [JP]/[JP] (AllExceptUS)
  • IMANARI, Toshio [JP]/[JP] (UsOnly)
  • TOIDA, Toshihiko [JP]/[JP] (UsOnly)
  • LINHARDT, Robert, J. [US]/[US] (UsOnly)
Inventors
  • IMANARI, Toshio
  • TOIDA, Toshihiko
  • LINHARDT, Robert, J.
Agents
  • TANIGAWA, Hidejiro
Priority Data
9/34707102.12.1997JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) PERSULFATED CHONDROITIN SULFATES, PROCESS FOR PRODUCING THE SAME, AND ANTICOAGULANTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
(FR) SULFATES DE CHONDROITINE PERSULFATEE, PROCEDE DE PRODUCTION DE CES DERNIERS ET ANTICOAGULANTS CONTENANT CES DERNIERS COMME INGREDIENT ACTIF
Abstract
(EN) Novel compounds different from heparin and having a high anticoagulant activity. These compounds are persulfated chondroitin sulfates having at least 3.5, on average, O-sulfate groups per disaccharide repeating unit or pharmacologically acceptable salts thereof. These compounds can be produced by reacting a chondroitin sulfate salt with sulfur trioxide in an aprotic solvent at 30 to 50 °C by regulating the molar ratio of the free hydroxyl groups in the chondroitin sulfate salt to the sulfur trioxide of 1:10 to 1:20.
(FR) L'invention concerne de nouveaux composés différents de l'héparine, présentant une activité anticoagulante importante. Ces composés sont des sulfates de chondroïtine persulfatée comprenant en moyenne au moins 3,5 de groupes O-sulfate par unité disaccharidique répétée ou des sels pharmacologiquement acceptables de ces derniers. On peut produire ces composés en faisant réagir un sel de sulfate de chondroïtine avec du trioxyde de soufre dans un solvant aprotique à une température comprise entre 30 et 50 °C, le rapport molaire des groupes hydroxyle libres dans le sel de sulfate de chondroïtine et le trioxyde de soufre étant réglé entre 1:10 et 1:20.
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