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Spirocycles as inhibitors of 11-beta hydroxyl steroid dehydrogenase type 1 comprising compounds with carboxamide and diazaspiro[4.5]dec-7-yl moities
专利权人:
INCYTE CORPORATION
发明人:
YAO, WENQING,ZHUO, JINCONG,ZHANG, COLIN
申请号:
NZ58252408
公开号:
NZ582524A
申请日:
2008.06.20
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are four compounds: 5-{ 3-Fluoro-4-[(5S)-2-(cis-4-hydroxycyclohexyl)-1-oxo-2,7-diazaspiro[4.5]dec-7-yl]phenyl} -N,N-dimethylpyridine-2-carboxamide 5-{ 3-Fluoro-4-[(5S)-2-(cis-4-hydroxycyclohexyl)-1-oxo-2,7-diazaspiro[4.5]dec-7-yl]phenyl} -N-methylpyridine-2-carboxamide N-Ethyl-5-{ 3-fluoro-4-[(5S)-2-(cis-4-hydroxycyclohexyl)-1-oxo-2,7-diazaspiro[4.5]dec-7-yl]phenyl} pyridine-2-carboxamide 5-{ 3-Chloro-4-[(5S)-2-(cis-4-hydroxycyclohexyl)-1-oxo-2,7-diazaspiro[4.5]dec-7-yl]phenyl} -N-ethylpyridine-2-carboxamide and pharmaceutically acceptable salts thereof. The compounds are useful for: inhibiting activity of 11bHSD, the conversion of cortisone to cortisol in a cell, inhibiting the production of cortisol in a cell, and for treating obesity, diabetes, glucose intolerance, insulin resistance, hyperglycaemia (hyperglycemia), hypertension, hyperlipidaemia (hyperlipidemia), cognitive impairment, depression, dementia, glaucoma, cardiovascular disorders, osteoporosis, inflammation, metabolic syndrome, androgen excess or polycystic ovary syndrome (PCOS).
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