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    Glucagon/GLP-1 receptor co-agonists
    1.
    发明公开
    Glucagon/GLP-1 receptor co-agonists 审中-公开
    胰高血糖素激素/ GLP-1-受体激动剂

    公开(公告)号：EP2487184A1

    公开(公告)日：2012-08-15

    申请号：EP11196006.8

    申请日：2008-02-13

    申请人： Indiana University Research and Technology Corporation

    发明人： Day, Jonathan ,  Patterson, James ,  Chabenne, Joseph ,  Dimarchi, Maria ,  Smiley, David ,  Dimarchi, Richard D.

    IPC分类号： C07K14/605 ,  A61K38/26

    CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K38/26 ,  A61K47/60 ,  C07K16/00 ,  C07K2317/52 ,  C07K2319/30

    摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. These modified glucagon co-agonist analogs may be combined with other anti-diabetic or anti-obesity compounds and used to control hyperglycemia, or to induce weight loss or prevent weight gain. In one embodiment the modified glucagon peptides comprise lactam bridges or substitution of the terminal carboxylic acid with an amide group. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, substitution of carboxy terminal amino acids, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR). Use of a glucagon/GLP-1 co-agonist for administration in combination with an anti-diabetic agent or anti-obesity agent.

    摘要翻译： 公开了相对于天然胰高血糖素在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。 这些修饰的胰高血糖素共激动剂类似物可以与其它抗糖尿病或抗肥胖化合物组合，并用于控制高血糖症，或诱导体重减轻或防止体重增加。 在一个实施方案中，修饰的胰高血糖素肽包含内酰胺桥或末端羧酸与酰胺基团的取代。 这些高效胰高血糖素类似物的溶解度和稳定性可以通过聚乙二醇化，多肽羧基末端氨基酸的取代或加入选自SEQ ID NO：26（GPSSGAPPPS ），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）。 胰高血糖素/ GLP-1共同激动剂与抗糖尿病剂或抗肥胖剂联合给药的用途。