发明名称 Thiazole benzenesulfonamides as beta<sub>3</sub> agonists for the treatment of diabetes and obesity
摘要 Thiazole substituted benzenesulfonamides are beta 3 adrenergic receptor agonists with very litte beta 1 and beta 2 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 decreasing gut motility are also disclosed.
申请公布号 AU6038498(A) 申请公布日期 1998.08.18
申请号 AU19980060384 申请日期 1998.01.23
申请人 MERCK & CO., INC. 发明人 ROBERT J. MATHVINK;EMMA R. PARMEE;SAMUEL TOLMAN;ANN E. WEBER
分类号 A61K31/4439;A61K31/4709;A61P1/00;A61P3/06;A61P3/10;A61P25/24;A61P25/28;A61P43/00;C07D417/12;C07D417/14 主分类号 A61K31/4439
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