公开(公告)号：EP0906310A1

公开(公告)日：1999-04-07

申请号：EP97929769.0

申请日：1997-06-03

申请人： MERCK & CO., INC.

发明人： BIFTU, Tesfaye ,  FENG, Danqing, Dennis ,  FISHER, Michael, H. ,  KUO, Chan-Hwa ,  LIANG, Gui-Bai ,  WEBER, Ann, E. ,  NAYLOR, Elizabeth, M.

IPC分类号： A61K31 ,  A61P3 ,  A61P25 ,  A61P43 ,  C07D213 ,  C07D409 ,  C07D413

CPC分类号： C07D213/40 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

摘要： Oxadiazole substituted benzenesulfonamides are selective β3 adrenergic receptor agonists with very little β1 and β2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.