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    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE
    1.
    发明授权
    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE 有权
    胰高血糖素样肽-1衍生物及其药物用途

    公开(公告)号：EP2190872B1

    公开(公告)日：2018-03-14

    申请号：EP08803724.7

    申请日：2008-09-05

    申请人： Novo Nordisk A/S

    发明人： SPETZLER, Jane ,  SCHÄFFER, Lauge ,  LAU, Jesper ,  KRUSE, Thomas ,  GARIBAY, Patrick William ,  RUNGE, Steffen ,  THØGERSEN, Henning ,  PETTERSSON, Ingrid

    IPC分类号： C07K14/605 ,  A61K38/26

    CPC分类号： C07K14/605 ,  A61K38/26

    摘要： The invention relates to protracted Glucagon-Like Peptide- 1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.

    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE
    6.
    发明公开
    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE 有权
    胰高血糖素样肽-1衍生物及其药物用途

    公开(公告)号：EP2190872A1

    公开(公告)日：2010-06-02

    申请号：EP08803724.7

    申请日：2008-09-05

    申请人： Novo Nordisk A/S

    发明人： SPETZLER, Jane ,  SCHÄFFER, Lauge ,  LAU, Jesper ,  KRUSE, Thomas ,  GARIBAY, Patrick William ,  RUNGE, Steffen ,  THØGERSEN, Henning

    IPC分类号： C07K14/605 ,  A61K38/26

    CPC分类号： C07K14/605 ,  A61K38/26

    摘要： The invention relates to protracted Glucagon-Like Peptide- 1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.