Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
申请人:Aicher Thomas Daniel
公开号:US20080214621A1
公开(公告)日:2008-09-04
The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention compositions containing these compounds for the treatment of metabolic syndrome, diabetes, hyperglycemia obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula I wherein G
1
is methylene or ethylene; L is —(C
1
-C
4
)alkylene-, —S—, —CH(OH)—, or —O—; R
0
is Formula II or Formula III and the other substituents are as defined in the claims.
本发明提供了I式化合物,其作为11-β羟基类固醇脱氢酶1的有效且选择性抑制剂。本发明还提供了一种制药组合物,其包括I式化合物或其药物盐以及药学上可接受的载体、稀释剂或赋形剂。此外,本发明还提供了含有这些化合物的组合物,用于治疗代谢综合征、糖尿病、高血糖、肥胖症、高血压、高脂血症、与高血糖相关的其他症状和相关疾病。其中,式中G1为亚甲基或乙烯基;L为—(C1-C4)烷基、—S—、—CH(OH)—或—O—;R0为II式或III式,其他取代基在权利要求中定义。