3, 3 -DISUBSTITUTED- ( 8 - AZA - BICYCLO [3.2.1] OCT- 8 - YL) -[5- (1H - PYRAZOL - 4 -YL) -THIOPHEN-3 -YL] METHANONES AS INHIBITORS OF 11 (BETA) -HSD1

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.