申请人:Oreste Anna Pasqua
公开号:US20070155694A1
公开(公告)日:2007-07-05
Novel depolymerized-LMWepiK5-N,O-sulfates obtainable starting from a LMW-epiK5-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: a O-oversulfation, a partila O-desulfation, a 6-O-sulfation and a N-sulfation. The new depolymerized-LMWepiK5-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.
由通过硝基降解epiK5-N-硫酸盐或通过硝基降解K5-N-硫酸盐获得的LMW-epiK5-N-硫酸盐制备的Novel depolymerized-LMWepiK5-N,O-硫酸盐,或通过C5-表异构化得到的LMW-K5-N-硫酸盐。该过程包括将起始的去聚合-LMW-epiK5-N-硫酸盐提交给四个步骤:O-过度硫酸化,部分O-脱硫酸化,6-O-硫酸化和N-硫酸化。新的去聚合-LMWepiK5-N,O-硫酸盐在其大部分链的还原端具有二硫酸化或三硫酸化的2,5-脱水甘露糖单元,具有40-60%的异硫酸酸含量,2.3至2.9的硫酸化程度和约1,500至约12,000的平均分子量。它们表现出良好的抗血栓形成活性,低的促出血风险。