IMIDAZOLONE AND IMIDAZOLIDINONE DERIVATIVES AS 11B-HSD1 INHIBITORS FOR DIABETES Russian patent published in 2012 - IPC C07D233/02 C07D233/06 C07D233/10 C07D233/28 C07D471/10 A61K31/4166 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula in which R¹ denotes a) adamantyl, hydroxyadamantyl or trifluoromethylphenyl; R² denotes hydrogen, methyl, ethyl or cyclopropyl; one of R³ and R⁴ denotes alkyl, cycloalkyl, haloalkyl or is absent, and the other denotes a) hydrogen, alkyl, pyridinyl, cycloalkyl, cycloalkylalkyl or haloalkyl; b) phenyl or phenyl substituted with one to three substitutes independently selected from fluorine, chlorine, bromine, haloalkyl and alkoxy group; c) phenylalkyl, where the phenylalkyl is optionally substituted with one to three halogens; e) naphthyl or tetrahydronaphthyl; f) phenylalkoxyalkyl; g) hydroxyalkyl; or h) pyridinyloxyalkyl or pyridinyloxyalkyl substituted with an cyano group; or R³ and R⁴ together with a carbon atom with which they are bonded form a cycloalkane or piperdine, where the cycloalkyl and piperidine are optionally substituted with one to three substitutes independently selected from aryl and arylalkyl; one of R⁵ and R⁶ denotes hydrogen, isopropyl, isobutyl or haloalkyl, and the other denotes hydrogen or is absent; and to pharmaceutically acceptable salts thereof, under the condition that 1,3-dihydro-4-phenyl-1-(3-(trifluoromethyl)phenyl)-2H-imidazol-2-one is excluded, and if one of R³ and R⁴ denotes methyl, ethyl, n-propyl or n-butyl, and the other denotes hydrogen or is absent, then R² denote hydrogen or methyl. The invention also relates to a pharmaceutical composition.

EFFECT: obtaining novel biologically active compounds, having 11-beta-hydroxysteroid dehydrogenase 1 (11-beta-HSDI) inhibiting activity.

15 cl, 257 ex