CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID-DEHYDROGENASE 1 Russian patent published in 2014 - IPC C07D413/10 C07D413/14 A61K31/5355 A61P19/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to a new compound of formula or its pharmaceutically acceptable salt, wherein R¹ represents (C₁-C₆)alkyl; an oxodihydropyridyl ring in the formula is optionally substituted by 1-3 groups optionally specified in fluorine, (C₁-C₆)alkyl, hydroxy(C₁-C₆)alkyl, (C₃-C₆)cycloalkyl, (C₄-C₇)cycloalkylalkyl, halo(C₁-C₆)alkyl and (C₁-C₆)alkoxy(C₁-C₆)alkoxy; R² represents (C₁-C₆)alkyl, phenyl, or tetrahydropyranyl optionally substituted by a group in the number of up to 1 independently specified in fluorine, hydroxy(C₁-C₆)alkyl and (C₃-C₆)cycloalkyl; R³ is specified in (C₁-C₆)alkyl optionally substituted by groups in the number of up to 3 independently specified in fluorine, cyano, R⁴, R⁴O-, (R⁴)₂N-, R⁴C(=O)NR⁴-, (R⁴)₂NC(=O)-, R⁴OC(=O)NR⁴-, R⁴S(=O)₂NR⁴- and oxadiazolyl optionally substituted by (C₁-C₆)alkyl; R⁴ independently represents H or (C₁-C₆)alkyl. Also, the invention refers to a method of treating an individual by using the above compound, a method of inhibiting 11β-HSD1, and a compound-based pharmaceutical composition.

EFFECT: there are prepared new compounds effective in treating the diseases related to 11β-HSD1 activity or expression.

15 cl, 6 tbl, 101 ex