公开(公告)号：US08466127B2

公开(公告)日：2013-06-18

申请号：US12999520

申请日：2009-06-16

申请人： Fuqiang Hu ,  Yongzhong Du ,  Hong Yuan ,  Pan Meng

发明人： Fuqiang Hu ,  Yongzhong Du ,  Hong Yuan ,  Pan Meng

IPC分类号： A61K31/722 ,  A61K31/704 ,  A61K31/337 ,  A61K31/522 ,  C08B37/08 ,  A61P31/12 ,  A61P35/00

CPC分类号： C08G65/33317 ,  C08B37/003 ,  C08G65/331 ,  C08G65/3318 ,  C08G2650/26 ,  C08L5/08 ,  C08L2203/02 ,  C08L2205/05

摘要： The present invention provides a PEGylated and fatty acid grafted chitosan oligosaccharide comprising a structural unit represented by the following Formula (I) and a structural unit represented by the following Formula (II) and synthesize method, wherein the chitosan oligosaccharide has a molecular weight of less than 200,000 Da, and a degree of deacetylation of 70%-100%, and part of free amino groups of chitosan oligosaccharide chain are replaced by a fatty acid or PEG, where n refers to degree of polymerization of the PEG, and R is an alkyl group having 11-21 carbon atoms. The grafting ratio of fatty acids is 1%-50%, and the grafting ratio of PEG is 0.05%-50%. The present invention also comprise a pharmaceutical composition comprising the PEGylated and fatty acid grafted chitosan oligosaccharide as a carrier, and use of the PEGylated and fatty acid grafted chitosan oligosaccharide in preparation of a pharmaceutical composition.

摘要翻译： 本发明提供一种聚乙二醇化和脂肪酸接枝的壳聚糖寡糖，其包含由下式（I）表示的结构单元和由下式（II）表示的结构单元和合成方法，其中壳聚糖寡糖的分子量较小 超过200,000Da，脱乙酰度为70％-100％，壳聚糖寡糖链的部分游离氨基被脂肪酸或PEG代替，其中n表示PEG的聚合度，R为 具有11-21个碳原子的烷基。 脂肪酸的接枝率为1％〜50％，PEG的接枝率为0.05％〜50％。 本发明还包含含有聚乙二醇化和脂肪酸接枝的壳聚糖寡糖作为载体的药物组合物，以及聚乙二醇化和脂肪酸接枝的壳聚糖寡糖在制备药物组合物中的用途。

公开(公告)号：US20110118200A1

公开(公告)日：2011-05-19

申请号：US12999520

申请日：2009-06-16

申请人： Fuqiang Hu ,  Yongzhong Du ,  Hong Yuan ,  Pan Meng

发明人： Fuqiang Hu ,  Yongzhong Du ,  Hong Yuan ,  Pan Meng

IPC分类号： A61K31/704 ,  C08B37/08 ,  C12P19/26 ,  A61K31/407 ,  A61P31/14 ,  A61P35/00 ,  A61K31/337 ,  A61K31/4745 ,  A61K31/711 ,  A61K31/713 ,  A61K31/675 ,  A61K31/522

CPC分类号： C08G65/33317 ,  C08B37/003 ,  C08G65/331 ,  C08G65/3318 ,  C08G2650/26 ,  C08L5/08 ,  C08L2203/02 ,  C08L2205/05

摘要： The present invention provides a PEGylated and fatty acid grafted chitosan oligosaccharide comprising a structural unit represented by the following Formula (I) and a structural unit represented by the following Formula (II) and synthesize method, wherein the chitosan oligosaccharide has a molecular weight of less than 200,000 Da, and a degree of deacetylation of 70%-100%, and part of free amino groups of chitosan oligosaccharide chain are replaced by a fatty acid or PEG, where n refers to degree of polymerization of the PEG, and R is an alkyl group having 11-21 carbon atoms. The grafting ratio of fatty acids is 1%-50%, and the grafting ratio of PEG is 0.05%-50%. The present invention also comprise a pharmaceutical composition comprising the PEGylated and fatty acid grafted chitosan oligosaccharide as a carrier, and use of the PEGylated and fatty acid grafted chitosan oligosaccharide in preparation of a pharmaceutical composition.

摘要翻译： 本发明提供一种聚乙二醇化和脂肪酸接枝的壳聚糖寡糖，其包含由下式（I）表示的结构单元和由下式（II）表示的结构单元和合成方法，其中壳聚糖寡糖的分子量较小 超过200,000Da，脱乙酰度为70％-100％，壳聚糖寡糖链的部分游离氨基被脂肪酸或PEG代替，其中n表示PEG的聚合度，R为 具有11-21个碳原子的烷基。 脂肪酸的接枝率为1％〜50％，PEG的接枝率为0.05％〜50％。 本发明还包含含有聚乙二醇化和脂肪酸接枝的壳聚糖寡糖作为载体的药物组合物，以及聚乙二醇化和脂肪酸接枝的壳聚糖寡糖在制备药物组合物中的用途。