Scott Peter Webster;Thomas David Pallin;Jonathan Robert Seckl;Hazel Joan Dyke;Brian Robert Walker;Trevor Robert Perrior;Peter Ward
发明人:
Scott Peter Webster,Jonathan Robert Seckl,Brian Robert Walker,Peter Ward,Thomas David Pallin,Hazel Joan Dyke,Trevor Robert Perrior
申请号：
US13642963
公开号：
US20130123268A1
申请日:
2011.03.10
申请国别(地区):
US
年份:
2013
代理人:
摘要：
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1； to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1； to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease； to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease； etc.
