公开(公告)号：EP2459226A2

公开(公告)日：2012-06-06

申请号：EP10739386.0

申请日：2010-07-26

申请人： Lipoxen Technologies Limited ,  Baxter International Inc ,  Baxter Healthcare SA

发明人： JAIN, Sanjay ,  GREGORIADIS, Gregory ,  DWIVEDI, Archana ,  NATH, Srijit ,  SIEKMANN, Juergen ,  HAIDER, Stefan ,  ROTTENSTEINER, Hanspeter ,  TURECEK, Peter

IPC分类号： A61K47/48

CPC分类号： A61K47/6455 ,  A61K47/60 ,  A61K47/61 ,  A61K47/65

摘要： A water soluble polymer, in particular polysialic acid (PSA) or a modified PSA (mPSA), is conjugated to an oxidized carbohydrate moiety of a glycoprotein other than a blood coagulation protein or to a ganglioside or drug delivery system by contacting the oxidized carbohydrate moiety with the water soluble polymer, wherein said water soluble polymer contains an aminooxy group and an oxime linkage is formed between the oxidized carbohydrate moiety and the aminooxy group on the water soluble polymer or wherein said water soluble polymer contains a hydrazide group and a hydrazone linkage is formed between the oxidized carbohydrate moiety and the hydrazide group on the water soluble polymer. Conjugates of aminooxy- or hydrazide-water soluble polymer, such as PSA and mPSA, are thus obtained in which the PSA or mPSA is attached via a carbohydrate moiety.

公开(公告)号：EP2459226B1

公开(公告)日：2016-06-29

申请号：EP10739386.0

申请日：2010-07-26

申请人： Lipoxen Technologies Limited ,  Baxalta Incorporated ,  Baxalta GmbH

发明人： JAIN, Sanjay ,  GREGORIADIS, Gregory ,  DWIVEDI, Archana ,  NATH, Srijit ,  SIEKMANN, Juergen ,  HAIDER, Stefan ,  ROTTENSTEINER, Hanspeter ,  TURECEK, Peter

IPC分类号： A61K47/48

CPC分类号： A61K47/6455 ,  A61K47/60 ,  A61K47/61 ,  A61K47/65

摘要： A water soluble polymer, in particular polysialic acid (PSA) or a modified PSA (mPSA), is conjugated to an oxidized carbohydrate moiety of a glycoprotein other than a blood coagulation protein or to a ganglioside or drug delivery system by contacting the oxidized carbohydrate moiety with the water soluble polymer, wherein said water soluble polymer contains an aminooxy group and an oxime linkage is formed between the oxidized carbohydrate moiety and the aminooxy group on the water soluble polymer or wherein said water soluble polymer contains a hydrazide group and a hydrazone linkage is formed between the oxidized carbohydrate moiety and the hydrazide group on the water soluble polymer. Conjugates of aminooxy- or hydrazide-water soluble polymer, such as PSA and mPSA, are thus obtained in which the PSA or mPSA is attached via a carbohydrate moiety.

摘要翻译： 将水溶性聚合物，特别是聚唾液酸（PSA）或修饰的PSA（mPSA）与不同于凝血蛋白的糖蛋白的氧化碳水化合物部分缀合或通过使氧化的碳水化合物部分接触而与神经节苷脂或药物递送系统 其中所述水溶性聚合物含有氨基氧基，并且在水溶性聚合物上的氧化碳水化合物部分和氨基氧基之间形成肟键，或者其中所述水溶性聚合物含有酰肼基，腙键是 形成在水溶性聚合物上的氧化碳水化合物部分和酰肼基团之间。 因此得到氨基氧基或酰肼 - 水溶性聚合物如PSA和mPSA的结合物，其中PSA或mPSA通过碳水化合物部分连接。