| 摘要 |
Disclosed herein is an adamantlyl derivative of formula (I), wherein A1 is formyl or alkyl substituted with cyano, sulfanylidene, or sulfo; and the other substituents are as defined within the specification; processes for their preparation, compositions comprising said compounds and uses thereof. Said compounds are useful as inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1 enzyme and are therefore useful in the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, onset of cognitive decline, dementia, steroid-induced actue psychosis, depression, anxiety or a condition that involves excessive glucocorticoid action. Examples of preferred compounds include: · E-4-[2-(4-chlorophenoxy)-2-methyl-propionylamino]-adamantane-1-carbaldehyde; · E-{ 4-[2-(4-chlorophenoxy)-2-methyl-propionylamino]-adamantan-1-yl} -acetonitrile; · N-{ (E)-5-[(thioacetyl)methyl]-2-adamantyl} -2-(4-chlorophenoxy)-2-methylpropanamide; · N-{ (E)-5 -[(sulfonic acid)methyl] -2-adamantyl} -2-(4-chlorophenoxy)-2-methylpropanamide; · ((E)-4-{ [2-(4-chlorophenoxy)-2-methylpropanoyl] amino} -1-adamantyl)acetic acid; · 2-(4-chlorophenoxy)-N-[(E)-5-(hydroxymethyl)-2-adamantyl]-2-methylpropanamide; and · E-4-[2-(2-chloro-4-fluorophenoxy)-2-methyl-propionylamino]-adamantane-carbonitrile.
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