发明公开
- 专利标题: GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE
- 专利标题(中): 胰高血糖素样肽-1衍生物及其药物用途
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申请号: EP08803724.7申请日: 2008-09-05
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公开(公告)号: EP2190872A1公开(公告)日: 2010-06-02
- 发明人: SPETZLER, Jane , SCHÄFFER, Lauge , LAU, Jesper , KRUSE, Thomas , GARIBAY, Patrick William , RUNGE, Steffen , THØGERSEN, Henning
- 申请人: Novo Nordisk A/S
- 申请人地址: Novo Allé 2880 Bagsværd DK
- 专利权人: Novo Nordisk A/S
- 当前专利权人: Novo Nordisk A/S
- 当前专利权人地址: Novo Allé 2880 Bagsværd DK
- 优先权: EP07115746 20070905; EP08101008 20080128
- 国际公布: WO2009030738 20090312
- 主分类号: C07K14/605
- IPC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.
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