186347-31-9Relevant articles and documents
(4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE
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Page/Page column 77, (2011/04/19)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)- [5-(1 H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-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 1 1 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-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.
Phenylacetamides as selective α-1A adrenergic receptor antagonists
Patane, Michael A.,DiPardo, Robert M.,Newton, Randall C.,Price, RoseAnn P.,Broten, Theodore P.,Chang, Raymond S.L.,Ransom, Richard W.,Di Salvo, Jerry,Nagarathnam, Dhanapalan,Forray, Carlos,Gluchowski, Charles,Bock, Mark G.
, p. 1621 - 1624 (2007/10/03)
A novel class of potent and selective α-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known α-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described. (C) 2000 Elsevier Science Ltd. All rights reserved.
ALPHA 1A ADRENERGIC RECEPTOR ANTAGONISTS
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, (2008/06/13)
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