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.
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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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