336882-79-2Relevant 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 70-71, (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.
4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same
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Referential example 2, (2010/01/31)
Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1and R2are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4and R5each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9or —OCOR10(in which R6, R9and R10each independently represents a hydrogen atom, a lower alkyl group, or the like, R7and R8are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.