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    Glucagon-Like Peptide-1 derivatives and their pharmaceutical use
    2.
    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：US08895694B2

    公开(公告)日：2014-11-25

    申请号：US12676451

    申请日：2008-09-05

    申请人： Jane Spetzler ,  Lauge Schäffer ,  Jesper Lau ,  Thomas Kruse ,  Patrick William Garibay ,  Steffen Reedtz-Runge ,  Henning Thøgersen ,  Ingrid Pettersson

    发明人： Jane Spetzler ,  Lauge Schäffer ,  Jesper Lau ,  Thomas Kruse ,  Patrick William Garibay ,  Steffen Reedtz-Runge ,  Henning Thøgersen ,  Ingrid Pettersson

    IPC分类号： A61K38/00 ,  A61K39/00 ,  C07K14/605

    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.

    摘要翻译： 本发明涉及长效的胰高血糖素样肽-1（GLP-1）衍生物及其治疗用途。 本发明的GLP-1衍生物包含具有总共2-12个氨基酸修饰的修饰的GLP-1（7-37）序列，包括Glu22和Arg26，并用白蛋白结合残基衍生或在18位聚乙二醇化， 20,23,30,31,34,36,37或39.这些化合物可用于治疗或预防2型糖尿病和相关疾病。 该化合物是有效的，稳定的，具有长的半衰期，与白蛋白结合的高亲和力，和/或与GLP-1受体（GLP-1R）细胞外结构域结合的高亲和力，所有这些都是 对于实现长效，稳定和活性的GLP-1衍生物的总体目标的潜在相关性，具有每周一次行政的潜力。

    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE
    4.
    发明申请
    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE 有权
    GLUCAGON-LIKE PEPTIDE-1衍生物及其药物用途

    公开(公告)号：US20110082079A1

    公开(公告)日：2011-04-07

    申请号：US12676451

    申请日：2008-09-05

    申请人： Jane Spetzler ,  Lauge Schäffer ,  Jesper Lau ,  Thomas Kruse ,  Patrick William Garibay ,  Steffen Runge ,  Henning Thøgersen ,  Ingrid Petersson

    发明人： Jane Spetzler ,  Lauge Schäffer ,  Jesper Lau ,  Thomas Kruse ,  Patrick William Garibay ,  Steffen Runge ,  Henning Thøgersen ,  Ingrid Petersson

    IPC分类号： A61K38/22 ,  C07K14/575 ,  A61P3/10 ,  A61P9/12 ,  A61P3/04 ,  A61P9/10 ,  A61P1/00 ,  A61P1/04

    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.

    摘要翻译： 本发明涉及长效的胰高血糖素样肽-1（GLP-1）衍生物及其治疗用途。 本发明的GLP-1衍生物包含具有总共2-12个氨基酸修饰的修饰的GLP-1（7-37）序列，包括Glu22和Arg26，并用白蛋白结合残基衍生或在18位聚乙二醇化， 20,23,30,31,34,36,37或39.这些化合物可用于治疗或预防2型糖尿病和相关疾病。 该化合物是有效的，稳定的，具有长的半衰期，与白蛋白结合的高亲和力，和/或与GLP-1受体（GLP-1R）细胞外结构域结合的高亲和力，所有这些都是 对于实现长效，稳定和活性的GLP-1衍生物的总体目标的潜在相关性，具有每周一次行政的潜力。

    FGF21 derivatives with albumin binder A-B-C-D-E- and their use
    6.
    发明授权
    FGF21 derivatives with albumin binder A-B-C-D-E- and their use 有权
    具有白蛋白结合剂A-B-C-D-E-的FGF21衍生物及其用途

    公开(公告)号：US09480753B2

    公开(公告)日：2016-11-01

    申请号：US12692227

    申请日：2010-01-22

    申请人： Tina Møller Tagmose ,  Patrick William Garibay ,  Bírgítte Andersen ,  Henning Thøgersen ,  Birgit Wieczorek

    发明人： Tina Møller Tagmose ,  Patrick William Garibay ,  Bírgítte Andersen ,  Henning Thøgersen ,  Birgit Wieczorek

    IPC分类号： A01N43/64 ,  A61K31/41 ,  A01N43/36 ,  A61K31/40 ,  A01N37/00 ,  A61K31/19 ,  A61K47/48 ,  C07K14/50 ,  A61K38/00

    CPC分类号： A61K47/48046 ,  A61K38/00 ,  A61K47/543 ,  A61K47/60 ,  A61K47/643 ,  C07K14/50

    摘要： The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B-C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.

    摘要翻译： 本发明涉及成纤维细胞生长因子21（FGF21），更具体地涉及具有共价连接的式A-B-C-D-E-的白蛋白结合物的FGF21化合物的衍生物。 本发明还涉及新型FGF21类似物，以及这些FGF21衍生物和类似物的药物用途，特别是用于治疗糖尿病，血脂异常，肥胖症，心血管疾病，代谢综合征和/或非酒精性脂肪肝病（ NAFLD）。 本发明的衍生物是延长的，例如。 能够维持较长时间的低血糖水平，能够增加FGF21的体内半衰期，和/或导致FGF21的较低清除率。 本发明的衍生物优选还具有改善的氧化稳定性。