发明名称 Substituted phenyl sulfonamides as selective B3 agonists for the treatment of diabetes and obesity.
摘要 <p>Substituted phenylsulphonamides having the formula: &lt;CHEM&gt; where the variables are as defined in Claim 1; are selective beta-3 adrenergic receptor agonists with very little 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 very potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to reduce triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to reduce gut motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenylsulphonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for reduction of triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.</p>
申请公布号 EP0611003(A1) 申请公布日期 1994.08.17
申请号 EP19940200303 申请日期 1994.02.03
申请人 MERCK & CO. INC. 发明人 FISHER, MICHAEL H.;PARMEE, EMMA R.;MATHVINK, ROBERT J.;WEBER, ANN E.;OK, HYUN O.
分类号 A61K31/18;A61K31/335;A61K31/34;A61K31/343;A61K31/38;A61K31/381;A61K31/40;A61K31/403;A61K31/415;A61K31/42;A61K31/423;A61K31/425;A61K31/428;A61K31/433;A61K31/44;A61K31/4406;A61K31/4433;A61K31/47;A61K31/496;A61K31/505;A61K31/63;A61K31/635;A61P3/04;A61P3/08;A61P3/10;C07C311/02;C07C311/10;C07C311/13;C07C311/14;C07C311/21;C07C311/29;C07C311/44;C07C311/46;C07C311/47;C07D209/02;C07D209/08;C07D209/12;C07D209/34;C07D213/65;C07D213/71;C07D213/73;C07D213/75;C07D215/36;C07D233/54;C07D239/34;C07D261/20;C07D277/64;C07D277/74;C07D285/10;C07D285/14;C07D307/78;C07D307/79;C07D307/82;C07D311/08;C07D317/62;C07D319/18;C07D333/34;C07D333/54;C07D333/62;C07D401/12;C07D405/12;C07D409/04;C07D409/12;C07D413/12;C07D417/12;(IPC1-7):C07C311/21;C07D213/30;C07D213/38 主分类号 A61K31/18
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