Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
申请人:Aicher Thomas Daniel
公开号:US20080207691A1
公开(公告)日:2008-08-28
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 provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru
0
is (II), or (III) G
1
is methylene or ethylene; L is a divalent linking group selected from —(C
1
-C
4
) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.
本发明提供了式I的化合物,其作为11-β羟基类固醇脱氢酶1的有效和选择性抑制剂。本发明进一步提供了一种药物组合物,其包括式I的化合物或其药用盐,以及药用可接受的载体、稀释剂或赋形剂。此外,本发明还提供了包含式I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(I)中,Ru0是(II)或(III),G1是亚甲基或乙烯基;L是选择自—(C1-C4)烷基-、—S—、—CH(OH)—或—O—的二价连接基;A是亚甲基、—S—、—O—或—NH—;其他取代基如权利要求所定义。