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    • 1. 发明申请
    • N-GLYCOSYLATED INSULIN ANALOGUES
    • N-糖苷类胰蛋白酶类似物
    • US20140235537A1
    • 2014-08-21
    • US14237369
    • 2012-08-03
    • Michael MeehlNatarajan SethuramanSandra Rios
    • Michael MeehlNatarajan SethuramanSandra Rios
    • C07K14/62
    • C07K14/62A61K38/00A61K38/28
    • Compositions and formulations comprising N-glycosylated insulin analogues are described. In particular embodiments, the glycosylated insulin analogues are produced in vivo and comprise one or more the N-linked N-glycans selected from high mannose or fucosylated or non-fucosylated hybrid, paucimannose, or complex N-glycans. In other embodiments, the N-glycan comprising the high mannose or fucosylated or non-fucosylated hybrid, paucimannose, or complex N-glycan is attached to the insulin analogue in vitro. Examples of N-glycans include but are not limited to a molecule having a structure selected from N-glycans in the group consisting of Man(1—9)GlcNAc2; or selected from N-glycans in the group consisting of GlcNAc(1—4)Man3GlcNAc2; or selected from N-glycans in the group consisting of Gal(j. 4)GlcNAc(1—4)Man3GlcNAe2; or selected from N-glycans in the group consisting of NANA({umlaut over (ι)}_4)Gal(1—4)GlcN Ac(1—4)Man3 GlcN Ac2—
    • 描述了包含N-糖基化胰岛素类似物的组合物和制剂。 在具体实施方案中,糖基化胰岛素类似物在体内产生,并且包含一种或多种选自高甘露糖或岩藻糖基化或非岩藻糖基化杂合物,低聚西南糖或复合N-聚糖的N-连接的N-聚糖。 在其它实施方案中,包含高甘露糖或岩藻糖基化或非岩藻糖基化的杂交体,低聚甘露糖或复合N-聚糖的N-聚糖在体外与胰岛素类似物连接。 N-聚糖的实例包括但不限于具有选自Man(1-9)GlcNAc2组中的N-聚糖的结构的分子; 或选自由GlcNAc(1-4)Man 3 GlcNAc 2组成的组中的N-聚糖; 或选自由Gal(j.4)GlcNAc(1-4)Man3GlcNAe2组成的组中的N-聚糖; 或选自NANA({umlaut over(ι)} _4)Gal(1-4)GlcN Ac(1-4)Man3 GlcN Ac2-