NUCLEOPHILIC CATALYSTS FOR OXIME LINKAGE
    1.
    发明公开
    NUCLEOPHILIC CATALYSTS FOR OXIME LINKAGE 审中-公开
    NUKLEOPHILE KATALYSATORENFÜROXIM-VERBINDUNG

    公开(公告)号:EP2598172A1

    公开(公告)日:2013-06-05

    申请号:EP11741727.9

    申请日:2011-07-29

    IPC分类号: A61K47/48

    CPC分类号: A61K47/61 A61K47/60

    摘要: The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.

    摘要翻译: 本发明涉及将水溶性聚合物与治疗性蛋白质的氧化碳水化合物部分缀合的材料和方法,包括在允许缀合的条件下使氧化的碳水化合物部分与活化的水溶性聚合物接触。 更具体地说,本发明涉及上述材料和方法,其中水溶性聚合物含有活性氨基氧基,其中在水溶性聚合物上的氧化碳水化合物部分和活性氨基氧基之间形成肟或腙键,其中 共轭在亲核催化剂存在下进行。

    NUCLEOPHILIC CATALYSTS FOR OXIME LINKAGE
    4.
    发明公开
    NUCLEOPHILIC CATALYSTS FOR OXIME LINKAGE 审中-公开
    亲核催化剂上肟CONNECTION

    公开(公告)号:EP2849795A1

    公开(公告)日:2015-03-25

    申请号:EP13728026.9

    申请日:2013-05-16

    IPC分类号: A61K47/48

    CPC分类号: A61K47/61 A61K47/60

    摘要: The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.

    BLOOD COAGULATION PROTEIN CONJUGATES
    7.
    发明公开
    BLOOD COAGULATION PROTEIN CONJUGATES 有权
    血液凝固蛋白缀合物

    公开(公告)号:EP2459224A2

    公开(公告)日:2012-06-06

    申请号:EP10738119.6

    申请日:2010-07-26

    IPC分类号: A61K47/48

    摘要: The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a blood coagulation protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer. In one embodiment of the invention the conjugation is carried out in the presence of the nucleophilic catalyst aniline. In addition the generated oxime linkage can be stabilized by reduction with NaCNBH
    3 to form an alkoxyamine linkage.

    摘要翻译: 本发明涉及使水溶性聚合物与血液凝固蛋白的氧化碳水化合物部分缀合的材料和方法,包括使氧化碳水化合物部分与活化的水溶性聚合物在允许缀合的条件下接触。 更具体地说,本发明涉及上述材料和方法,其中水溶性聚合物含有活性氨氧基,并且其中在水溶性聚合物上的氧化碳水化合物部分和活性氨氧基之间形成肟键。 在本发明的一个实施方案中,缀合在亲核催化剂苯胺存在下进行。 另外,生成的肟键可以通过用NaCNBH 3还原形成烷氧基胺键来稳定。