发明公开
- 专利标题: N-TERMINALLY MODIFIED GLP-1 RECEPTOR MODULATORS
- 专利标题(中): N末端修饰的GLP-1受体调节剂
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申请号: EP06760391.0申请日: 2006-05-26
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公开(公告)号: EP1883652A2公开(公告)日: 2008-02-06
- 发明人: EWING, William R. , MAPELLI, Claudio , RIEXINGER, Douglas, James , LEE, Ving, G. , SULSKY, Richard, B. , ZHU, Yeheng
- 申请人: Bristol-Myers Squibb Company
- 申请人地址: P.O. Box 4000, Route 206 and Province Line Road Princeton, NJ 08543-4000 US
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 当前专利权人地址: P.O. Box 4000, Route 206 and Province Line Road Princeton, NJ 08543-4000 US
- 代理机构: Reitstötter - Kinzebach
- 优先权: US684805P 20050526
- 国际公布: WO2006127948 20061130
- 主分类号: C07K14/605
- IPC分类号: C07K14/605
摘要:
The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
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