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    • 6. 发明申请
    • Polysaccharides derivatives with high antithrombotic activity in plasma
    • 血浆中具有高抗血栓活性的多糖衍生物
    • US20070042993A1
    • 2007-02-22
    • US10557584
    • 2004-07-07
    • Marco ManoniLiana SalsiniJacopo ChiniGiovanni Cipolletti
    • Marco ManoniLiana SalsiniJacopo ChiniGiovanni Cipolletti
    • A61K31/727C08B37/08
    • C08B37/0063C08B37/00C08B37/006C08B37/0075Y10S435/849
    • 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 6-0-sulphation, e) N-sulphation and an intermediate step of controlled depolimerization characterised by the fact that both 0-sulphations (0-sulphation and 60-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-Ila activity equal to or higher than 1 and to compositions comprising said products in combination with suitable and pharmaceutically acceptable excipients and/or diluent.
    • 本发明涉及一种用于制备源自N-乙酰基异烟芽孢杆菌的硫酸化葡糖胺聚糖的方法,其包括:a)由天然或重组细菌菌株,优选K5大肠杆菌制备的N-乙酰基异烟芽孢杆菌多糖的N-脱乙酰和N-硫酸化, b)用葡糖醛酸C5-差向异构酶进行酶促差向异构化,c)部分O-硫酸化,然后是部分O-脱硫,d)部分6-0-硫酸化,e)N-硫酸化和中间步骤, 事实上,0-硫酸化(O-硫酸化和60-硫酸化)都是部分的。 此外,本发明涉及根据显示抗Xa活性和等于或高于1的抗Ila活性之间的比例的方法获得的产品和包含所述产品的组合物与合适的和药学上可接受的赋形剂和/或 冲淡。