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    • 13. 发明申请
    • GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE
    • GLUCAGON-LIKE PEPTIDE-1衍生物及其药物用途
    • US20150025003A1
    • 2015-01-22
    • US14506052
    • 2014-10-03
    • Novo Nordisk A/S
    • Jane SpetzlerLauge SchaefferJesper LauThomas KrusePatrick W. GaribaySteffen Reedtz-RungeHenning ThoegersenIngrid Pettersson
    • C07K14/605A61K38/26
    • C07K14/605A61K38/26
    • 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.
    • 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。
    • 20. 发明授权
    • Glucagon-like peptide-1 derivatives and their pharmaceutical use
    • 胰高血糖素样肽-1衍生物及其药物用途
    • US09409966B2
    • 2016-08-09
    • US14506052
    • 2014-10-03
    • Novo Nordisk A/S
    • Jane SpetzlerLauge SchaefferJesper LauThomas KrusePatrick W. GaribaySteffen Reedtz-RungeHenning ThoegersenIngrid Pettersson
    • C07K14/605A61K38/26
    • C07K14/605A61K38/26
    • 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.
    • 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。