Invention Grant
- Patent Title: 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 (β)-HSD1
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Application No.: US15154254Application Date: 2016-05-13
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Publication No.: US09834549B2Publication Date: 2017-12-05
- Inventor: Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
- Applicant: The University Of Edinburgh
- Applicant Address: GB Edinburgh
- Assignee: THE UNIVERSITY OF EDINBURGH
- Current Assignee: THE UNIVERSITY OF EDINBURGH
- Current Assignee Address: GB Edinburgh
- Agency: Swanson & Bratschun, L.L.C.
- Main IPC: C07D409/14
- IPC: C07D409/14 ; C07D451/02 ; C07D451/04 ; C07D451/06
![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 (β)-HSD1](/abs-image/US/2017/12/05/US09834549B2/abs.jpg.150x150.jpg)
Abstract:
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.
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