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.
化合物公式为(I)的化合物,包括其药学上可接受的盐和前药:是11β-H
SD1酶的选择性
抑制剂。它们抑制11β-H
SD1介导的
可的松和其他11-
酮基-糖
皮质激素转化为
皮质醇和其他11β-羟基-糖
皮质激素的过程。因此,11β-H
SD1
抑制剂减少了目标组织中
皮质醇的含量,从而调节了
皮质醇的效应。调节
皮质醇可能对控制非
胰岛素依赖性糖尿病(NID
DM)、高血糖、肥胖症、
胰岛素抵抗、血脂异常、高脂血症、高血压、X综合征和与体内过多
皮质醇有关的其他症状有效。