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    • 4. 发明申请
    • LOW MOLECULAR POLYSACCHARIDES HAVING ANTITHROMBOTIC ACTIVITY
    • 具有抗血栓活性的低分子多糖
    • WO2005058976A3
    • 2005-08-04
    • PCT/IB2004004128
    • 2004-12-15
    • GLYCORES 2000 SRLORESTE PASQUA ANNAZOPPETTI GIORGIO
    • ORESTE PASQUA ANNAZOPPETTI GIORGIO
    • A61K31/726A61K31/727A61K31/737C08B37/00C08B37/10
    • C08B37/0063
    • depolymerized-LMWepiK5-N,O-sulfates obtainable starting from a LMWepiK5-N-sulfate prepared by nitrous depolymerization of an epiK5-N-sulfate or by C5-epimerization of a LMW-K5-N-sulfate obtained by nitrous depolymerization of a K5-N-sulfate. A process consists of submitting the starting depolymerized-LMW-epiK5-N-sulfate to four steps: an O-oversulfation, a partial 0-desulfation, a 6-0-sulfation and a N-sulfation. The depolymerized­LMWepiK5-N,O-sulfates present a di- or trisulfated 2,5-anhydromannitol unit at the reducing end of the majority of its chains, have a content of iduronic acid of 40-60%, a sulfation degree of from 2.3 to 2.9 and a mean molecular weight of from about 1,500 to about 12,000. They exhibit a good antithrombotic activity with a low pro-hemorrhagic risk.
    • 解聚的LMWepiK5-N,O-硫酸盐,可从通过epiK5-N-硫酸盐的亚硝解聚制备的LMWepiK5-N-硫酸盐或通过K5的亚硝解聚得到的LMW-K5-N-硫酸盐的C5差向异构体 -N-硫酸盐。 一个过程包括将起始解聚的LMW-epiK5-N-硫酸盐提交到四个步骤:O-过硫酸盐,部分O-脱硫,6-0-硫酸化和N-硫酸化。 解聚的MWepiK5-N,O-硫酸盐在其大部分链的还原末端呈现二硫酸化或三硫酸化的2,5-脱水甘露糖醇单元,其具有40-60%的艾杜糖醛酸含量,硫酸化度为2.3至 2.9,平均分子量为约1,500至约12,000。 它们具有良好的抗血栓形成活性,具有低的出血性风险。