Dermatan disulfate, an inhibitor of thrombin generation and...

C - Chemistry – Metallurgy – 08 – B

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C08B 37/00 (2006.01) A61K 31/737 (2006.01) A61L 33/00 (2006.01) A61L 33/08 (2006.01) C08B 37/08 (2006.01)

Patent

CA 2279535

A method of inhibiting thrombin generation and complement activation is inhibited by using a dermatan disulfate having at least 2 sulfate groups per disaccharide obtained by chemical sulfation of native dermatan sulfate. The resulting dermatan disulfate having an average molecular weight from about 5000 to 35000 Daltons is characterized by high content (i) a high content of L-iduronic->4,6 di-O-sulfated-N-acetyl-D-galactosamine residues and (ii) a specific heparin cofactor II-mediated antithrombin activity, depending on average molecular weight, between about 25 to 125 u/mg.

L'invention porte sur un procédé inhibant la production de thrombine et l'activation du complément à l'aide de bisulfate de dermatan présentant au moins deux groupes sulfate par disaccharide et qu'on obtient par sulfatation chimique de sulfate de dermatan natif. Le bisulfate de dermatan résultant, d'un poids moléculaire moyen compris entre environ 5.000 et 35.000 dalton, se caractérise (i) par sa teneur élevée en résidus de L-iduronic->4,6 di-O-N-acétyl-D-galactosamine sulfatée, et (ii) par son activité antithrombique spécifique induite par le cofacteur II de l'héparine dépendant du poids moléculaire moyen (entre environ 25 et 125 u/mg).

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