CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF Russian patent published in 2018 - IPC C07D401/12 C07D401/06 C07D471/04 C07D413/06 C07D417/12 C07D403/06 C07D405/06 A61K31/4709 A61K31/4725 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, specifically to a heterocyclic compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein each R¹ and R^1a is independently selected from the group consisting of H, methyl, CONHC(CH₃)₃, OH, CO₂H, CO₂CH₃, CO₂CH₂CH₃, CH₂OH, CN, OCH₃ and phenyl; or R¹ represents CH₂CO₂H; or any two R¹ on the same carbon atom when taken together may form a group of the formula =O; Ar is a heteroaryl group selected from the group consisting of:

,

where each R⁷ is independently selected from the group consisting of halogen, OH, CN, C₁-C₃ alkyl, C₁-C₃ alkoxy, C₃cycloalkyl, heterocycloalkyl selected from piperidine which may be substituted with one carboxyl group; C₆aryl, which may be substituted by one halogen atom; heteroaryl, selected from the group consisting of thiophene, furan, which may be substituted with C₁-C₃alkyl, and pyridine; wherein R⁸ is selected from the group consisting of H, C₁-C₂alkyl, C₁alkoxy, C₃cycloalkyl and SO₂R⁹; wherein R⁹ is C₆aryl; e is an integer selected from a group consisting of 0, 1 and 2; f is an integer selected from a group consisting of 0 and 1; A is -CR^aR^b-; B is CH₂; wherein each R^a and R^b is independently selected from the group consisting of H, OH, CN, CF₃, C₁-C₃alkyl, C₆aryl, heteroaryl selected from thiophene; and wherein R^a and R^b are different; W¹ and W² are selected such that one is N and the other is (CR¹₂); bond from the carbonyl carbon is joined to W¹ or W², which is N; D is O or (CR¹₂); a is an integer selected from a group consisting of 0, 1 and 2; b is an integer selected from a group consisting of 0 and 1; c is equal to 1. Invention also relates to the pharmaceutical composition based on compound with formula (I) and use of compound with formula (I). .

EFFECT: novel heterocyclic compounds having the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).

12 cl, 1 tbl, 268 ex