WEBSTER, SCOTT PETER,SECKL, JONATHAN ROBERT,WALKER, BRIAN ROBERT,WARD, PETER,PALLIN, THOMAS DAVID,DYKE, HAZEL JOAN,PERRIOR, TREVOR ROBERT
申请号：
CA2796297
公开号：
CA2796297C
申请日:
2011.03.10
申请国别(地区):
CA
年份:
2017
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 (I) that, inter alia, inhibit 11 ß-hydroxysteroid dehydrogenase type 1 (11 ß-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 11 ß-hydroxysteroid dehydrogenase type 1； to treat disorders that are ameliorated by the inhibition of 11 ß-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.
