THERAPEUTICALLY ACTIVE DERIVATIVES OF OXAZOLINE Russian patent published in 2018 - IPC C07D495/04 A61K31/519 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or its pharmaceutically acceptable salt, where Q is a group of formula (Qa), where the asterisk (*) shows the point of attachment to the remainder of the molecule; X is C-R⁶; Y is a linker group selected from -C(O)N(R⁷)-; Z is aryl, C_3-7 heterocycloalkyl or heteroaryl, wherein any one of these groups may be optionally substituted with one or two substituents independently selected from halogen, cyano, C_1-6alkyl, C_1-6alkoxy, difluoromethoxy, C_2-6alkylcarbonyl and C_2-6alkoxycarbonyl; A is hydrogen; R¹ is -NR^bR^c; R² is hydrogen or C_1-6 alkyl; and R³ is hydrogen; or R³ is C_1-6 alkyl; R⁴ is hydrogen or C_1-6 alkyl; and R⁵ is hydrogen; or R⁵ is C_1-6 alkyl; or R⁴ and R⁵, taken together with the carbon atom to which they are both attached, are C_3-7 cycloalkyl; R⁶ and R⁷ independently are hydrogen; R^b and R^c are independently hydrogen, wherein the aryl groups mentioned above are selected from phenyl and naphthyl; heterocycloalkyl groups mentioned above are selected from indolinyl; and the heteroaryl groups mentioned above are selected from thienyl and indolyl. Invention also relates to a pharmaceutical composition comprising compounds of formula (I) and a pharmaceutically acceptable carrier. (I), (Qa).

EFFECT: compounds have inhibitory activity when passing the test of mixed lymphocyte culture (MLC) reaction.

9 cl, 3 tbl, 21 ex