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polysaccharidderivate with antithrombotischer effect in plasma

机译:血浆中具有抗血栓形成作用的多糖衍生物

摘要

The present invention relates to a process for the preparation of sulphated glycosaminoglycans derived from N acetylheparosan which comprises: a) N-deacetylation and N-sulphation of the N-acetylheparosan polysaccharide prepared from natural or recombinant bacterial strain, preferably K5 E. coli, b) enzymatic epimerization with the glucuronyl C5-epimerase enzyme, c) partial O-sulphation followed by a partial O-desulphation, d) partial 6-O-sulphation, e) N-sulphation and an intermediate step of controlled depolimerization characterised by the fact that both O-sulphations (O-sulphation and 6O-sulphation) are partial. Furthermore the invention relates to the products obtained according to the process which show a ratio between the anti-Xa activity and anti-IIa activity equal to or higher than 1 and to compositions comprising said products in combination with suitable and pharmaceutically acceptable excipients and/or diluent.
机译:本发明涉及一种衍生自N-乙酰肝素聚糖的硫酸化糖胺聚糖的制备方法,该方法包括:a)由天然或重组细菌菌株,优选K5大肠杆菌,b。制备的N-乙酰肝素多糖的N-脱乙酰化和N-硫酸化。 )用葡糖醛酸酰基C5-表异构酶进行酶促差向异构化,c)部分O-硫酸化,然后进行部分O-脱硫,d)部分6-O-硫酸化,e)N-硫酸化和受控脱聚的中间步骤这两个O硫酸化(O硫酸化和6O硫酸化)都是部分的。此外,本发明涉及根据该方法获得的显示出抗Xa活性和抗IIa活性之比等于或高于1的产物,并且涉及包含所述产物与合适的和药学上可接受的赋形剂和/或组合物的组合物。冲淡。

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