发明申请
US20050070720A1 11-Beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
失效
用于治疗糖尿病，肥胖和血脂异常的11-β-羟基类固醇脱氢酶1抑制剂
- 专利标题： 11-Beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
- 专利标题（中）： 用于治疗糖尿病，肥胖和血脂异常的11-β-羟基类固醇脱氢酶1抑制剂
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申请号： US10502967申请日： 2003-01-28
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公开(公告)号： US20050070720A1公开(公告)日： 2005-03-31
- 发明人: James Balkovec , Rolf Thieringer , Steven Mundt , Anne Hermanowski-Vosatka , Donald Graham , Gool Patel , Susan Aster , Sherman Waddell , Steven Olson , Milana Maletic
- 申请人： James Balkovec , Rolf Thieringer , Steven Mundt , Anne Hermanowski-Vosatka , Donald Graham , Gool Patel , Susan Aster , Sherman Waddell , Steven Olson , Milana Maletic
- 国际申请： PCT/US03/02558 WO 20030128
- 主分类号： A61K31/4196
- IPC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
摘要：
Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-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.