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–אזא–ביציקלו[1.2.3]אוקט–8–איל)–[5–(h1–פיראזול–4–איל)–תיופנ–3–איל]מתאנונים דו–מותמרים בעמדה 3 כמעכבי 11(ביטא)–1hsd
专利权人:
THE UNIVERSITY OF EDINBURGH
发明人:
申请号:
IL22241712
公开号:
IL222417A
申请日:
2012.10.14
申请国别(地区):
IL
年份:
2016
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 11&bgr;-hydroxysteroid dehydrogenase type 1 (11&bgr;-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&bgr;-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11&bgr;-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.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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