发明名称 |
GLP-1 analogues and derivatives |
摘要 |
The invention relates to a GLP-1 analog which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1(7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ ID NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H31, and the Q residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogs and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration. |
申请公布号 |
US8815802(B2) |
申请公布日期 |
2014.08.26 |
申请号 |
US201013516312 |
申请日期 |
2010.12.16 |
申请人 |
Novo Nordisk A/S |
发明人 |
Kalthoff Christoph;Lau Jesper;Spetzler Jane;Garibay Patrick William;Kofoed Jacob;Linderoth Lars |
分类号 |
A61K38/26;A61P3/10;C07K14/605;A61K38/00;C07K14/65 |
主分类号 |
A61K38/26 |
代理机构 |
|
代理人 |
Bork Richard W. |
主权项 |
1. A GLP-1 analogue which comprises a histidine residue at a position corresponding to position 31 of GLP-1(7-37) (SEQ ID NO: 1), a glutamine residue at a position corresponding to position 34 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of ten additional amino acid modifications as compared to GLP-1(7-37) (SEQ ID NO: 1); wherein the histidine residue is designated H31, and the glutamine residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. |
地址 |
Bagsvaerd DK |