发明名称 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FORTHE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA
摘要 Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11.beta.-HSD1 enzyme. They inhibit the 11.beta.-HSD1-mediated conversion of cortisone and other 11-keto- glucocorticoids to cortisol and other 11.beta.-hydroxy-glucocorticoids. The 11.beta.-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body.
申请公布号 CA2474168(A1) 申请公布日期 2003.08.14
申请号 CA20032474168 申请日期 2003.01.28
申请人 MERCK & CO., INC. 发明人 THIERINGER, ROLF;MALETIC, MILANA;OLSON, STEVEN H.;BALKOVEC, JAMES M.;WADDELL, SHERMAN T.;PATEL, GOOL F.;ASTER, SUSAN D.;GRAHAM, DONALD W.;MUNDT, STEVEN S.;HERMANOWSKI-VOSATKA, ANNE
分类号 A61K31/4196;A61K31/437;A61K31/438;A61K31/439;A61K31/4439;A61K31/55;A61K31/551;A61K31/554;A61K45/00;A61K45/06;A61P1/18;A61P3/04;A61P3/06;A61P3/10;A61P5/50;A61P9/10;A61P13/12;A61P25/00;A61P27/02;A61P43/00;C07D249/08;C07D249/12;C07D249/14;C07D401/12;C07D405/04;C07D405/06;C07D405/12;C07D405/14;C07D409/04;C07D409/06;C07D471/04;C07D471/08;C07D487/04;C07D487/08;C07D491/14;C07D491/147;C07D491/20;C07D513/04;(IPC1-7):C07D249/16;A61K31/419 主分类号 A61K31/4196
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