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摘要：本发明公开了一种结构新颖的单分散六臂聚乙二醇修饰的阿伦磷酸钠的唑来膦酸盐的制备与应用，属于有机化学与医药化工领域。单分散六臂聚乙二醇与唑来膦酸和阿伦磷酸钠通过可在体内降解的化学键相连分别制备出一系列六臂聚乙二醇碳酸酯型阿伦磷酸钠的唑来膦酸盐。该方法通过调整单分散六臂聚乙二醇链的长度，可以合成出相应水溶性的阿伦磷酸钠的唑来膦酸盐，单分散六臂聚乙二醇链越长，水溶性就越好，水溶性的提高可以将其制备成水溶液的制剂，规避唑来膦酸和阿伦磷酸钠溶解代谢以及副作用的缺陷。本发明方法反应简单、条件温和、成本较低，便于工业化生产。
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Abstract： The invention discloses preparation and an application of a zoledronate coupled predrug of monodispersed hexahedral polyethylene glycol modified alendronate and belongs to the field of organic chemistry and medicinal chemical engineering. The monodispersed hexahedral polyethylene glycol and alendronateare connected through chemical bonds degraded in vivo to separately prepare a series of zoledronate of hexahedral polyethylene glycol carbonate alendronate. By adjusting the length of the monodispersed hexahedral polyethylene glycol chains, the method can synthesize corresponding water zoledronate of the soluble alendronate. The greater the lengths of the monodispersed hexahedral polyethylene glycol chains are, the better the water solubility is. The water solubility is improved, so that themonodispersed hexahedral polyethylene glycol can be prepared into a preparation of a water solution. Defects of dissolving metabolism and side effects of zoledronate and alendronate are avoided. The method is simple in reaction, mild in condition, relatively low in cost and convenient for industrial production.
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申请人： 湖南华腾制药有限公司
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Applicant： HUNAN HUATENG PHARMACEUTICAL CO LTD
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地址： 410205 湖南省长沙市高新开********(隐藏)
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发明(设计)人： 张安林 邓泽平 成佳 赵春晖
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Inventor： ZHANG ANLIN; DENG ZEPING; CHENG JIA; ZHAO CHUNHUI
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主分类号： C08G65/335(2006.01)I
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分类号： C08G65/335(2006.01)I C08G65/333(2006.01)I A61P19/10(2006.01)I
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