发明授权
US09365564B2 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
有权
3,3-二取代 - (8-氮杂 - 双环[3.2.1]辛-8-基) - [5-(1H-吡唑-4-基) - 噻吩-3-基] - 甲酮作为11 &bgr;) - HSD1
- 专利标题: 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
- 专利标题(中): 3,3-二取代 - (8-氮杂 - 双环[3.2.1]辛-8-基) - [5-(1H-吡唑-4-基) - 噻吩-3-基] - 甲酮作为11 &bgr;) - HSD1
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申请号: US13642963申请日: 2011-03-10
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公开(公告)号: US09365564B2公开(公告)日: 2016-06-14
- 发明人: Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
- 申请人: Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
- 申请人地址: GB Edinburgh
- 专利权人: The University Of Edinburgh
- 当前专利权人: The University Of Edinburgh
- 当前专利权人地址: GB Edinburgh
- 代理机构: Swanson & Bratschun, L.L.C.
- 国际申请: PCT/GB2011/000345 WO 20110310
- 国际公布: WO2011/135276 WO 20111103
- 主分类号: C07D451/06
- IPC分类号: C07D451/06 ; C07D451/02 ; C07D409/14 ; C07D451/04
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.
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