公开(公告)号：EP2493910A1

公开(公告)日：2012-09-05

申请号：EP10774101.9

申请日：2010-10-29

申请人： Tranzyme Pharma, Inc.

发明人： HOVEYDA, Hamid ,  MARSAULT, Éric ,  THOMAS, Helmut ,  FRASER, Graeme ,  BEAUBIEN, Sylvie ,  MATHIEU, Axel ,  BEIGNET, Julien ,  BONIN, Marc-André ,  PHOENIX, Serge ,  DRUTZ, David ,  PETERSON, Mark ,  BEAUCHEMIN, Sophie ,  BRASSARD, Martin ,  VÉZINA, Martin

IPC分类号： C07K5/12 ,  A61K38/12 ,  A61P25/00 ,  A61P35/00 ,  A61P5/00 ,  A61P3/00 ,  A61P1/00 ,  A61P29/00 ,  A61P9/00

CPC分类号： C07K5/0808 ,  A61K38/00 ,  C07K5/0804 ,  C07K5/0812

摘要： The present invention provides novel conformationalIy- defined macrocyclic compounds of formula (I) that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, obesity and obesity- associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders.