Semi-synthetic sulphaminoheparosansulphates having high...

A - Human Necessities – 61 – K

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A61K 31/737 (2006.01) A61K 31/727 (2006.01) A61P 35/04 (2006.01) C08B 37/00 (2006.01) A61K 31/726 (2006.01)

Patent

CA 2264929

Sulphaminoheparosansulphates obtainable from the Escherichia coli K5 polysaccharide by deacetilation and the subsequent sulfation with the sulphuric anhydride/trimethylamine adduct carried out at 0°C, for times ranging from 0.25 to 2 hours and using a reactant/polysaccharide ratio (SO3 equivalents/available OH groups equivalents) equal to 5 have been found having high anti-metastatic activity and low anticoagulant activity.

Cette invention concerne des sulfaminohéparosansulfates, lesquels peuvent être obtenus par déacétylation à partir du polysaccharide K5 d'Escherichia coli, puis par sulfatation avec un produit d'addition sulfurique de type anhydride /triméthylamine à une température de 0 DEG C. Ce processus se fait sur une durée de 0,25 à 2 heures, et selon un rapport réactif/polysaccharide (équivalents de SO3/équivalents de groupes OH disponibles) égal à 5. Ces sulfaminohéparosansulfates possèdent une activité anti-métastatique élevée, et une faible activité anticoagulante.

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