PYRIMIDINECYCLOHEXYL GLUCOCORTICOID RECEPTOR MODIFIERS Russian patent published in 2016 - IPC C07D239/56 C07D239/54 C07D401/06 C07D413/06 C07D417/06 A61K31/505 A61K31/513 A61P3/10 A61P3/04 A61P3/06 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel pyrimidinecyclohexyl compounds of formula I, its pharmaceutically acceptable salts and isomers which possess the properties of glucocorticoid receptor (GR). Invention also relates to a pharmaceutical composition. In formula I , dotted line is absent or is a bond; X is selected from a group consisting of O and S; R¹ is selected from a group consisting of phenyl and 5-6-member heteroaryl containing 1-3 heteroatoms, independently selected from N, O and S, optionally substituted by 1-3 groups R^1a; each R^1a independently selected from a group consisting of H, C_1-6 alkyl, C_1-6 alkoxy, halogen, C_1-6 haloalkyl, -NR^1bR^1c and -SO₂R^1b; R^1b and R^1c each independently selected from a group consisting of H and C_1-6 alkyl; R² is selected from a group consisting of H, C_1-6 alkyl, C_1-6 alkyl-OR^1b, C_1-6 alkyl-NR^1bR^1c and C_1-6 alkylene-heterocycloalkyl; R³ is selected from a group consisting of H and C_1-6 alkyl; Ar is phenyl, optionally substituted with 1-4 groups R⁴; each R⁴ independently selected from a group consisting of H, C_1-6 alkyl, C_1-6 alkoxy, halogen, C_1-6 haloalkyl C_1-6 haloalkoxy; L¹ is C_1-6 alkylene; subscript n is an integer from 0 to 3. Compounds can be used for treating a disease or condition by glucocorticoid receptor modulation.

EFFECT: disease or condition includes obesity and weight gain caused by neuroleptics.

17 cl, 7 tbl, 44 ex, 2 dwg