公开(公告)号：US20050137135A1

公开(公告)日：2005-06-23

申请号：US11042562

申请日：2005-01-25

申请人： Simon Hinke ,  Susanne Manhart ,  Jan Ehses ,  Christopher McIntosh ,  Hans-Ulrich Demuth ,  Raymond Pederson

发明人： Simon Hinke ,  Susanne Manhart ,  Jan Ehses ,  Christopher McIntosh ,  Hans-Ulrich Demuth ,  Raymond Pederson

IPC分类号： A61K38/00 ,  A61P1/18 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07K7/08 ,  C07K14/00 ,  C07K14/47 ,  C07K14/605 ,  A61K38/10 ,  A61K38/14

CPC分类号： C07K14/605 ,  A61K38/00

摘要： The present invention relates to novel C-terminal truncated fragments and novel N-terminal modified analogues of gastric inhibitory polypeptide as well as various GIP analogues with a reduced peptide bond or alterations of the amino acids close to the dipeptidyl peptidase IV (DPIV)-specific cleavage site providing improved DPIV-resistance and prolonged half-life. Further the invention relates to novel analogs with different linkers between potential receptor binding sites of GIP. The compounds of the present invention and their pharmaceutically acceptable salts are useful in treating GIP-receptor mediated conditions, such as non-insulin dependent diabetes mellitus and obesity.

摘要翻译： 本发明涉及新型C末端截短的片段和胃抑制多肽的新型N-末端修饰类似物以及具有降低的肽键或接近二肽基肽酶IV（DPIV）特异性的氨基酸的改变的各种GIP类似物 切割位点提供改善的DPIV抗性和延长的半衰期。 此外，本发明涉及在GIP的潜在受体结合位点之间具有不同接头的新型类似物。 本发明的化合物及其药学上可接受的盐可用于治疗GIP受体介导的病症，例如非胰岛素依赖性糖尿病和肥胖症。