SUBSTITUTED THIAZOLES OR OXAZOLES AS P2X7 RECEPTOR ANTAGONISTS Russian patent published in 2019 - IPC C07D413/14 C07D413/06 C07D417/06 C07D417/14 C07D263/32 C07D277/28 A61K31/454 A61K31/506 A61K31/5377 A61P1/00 A61P13/00 A61P21/00 A61P25/00 A61P27/00 A61P29/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, including any stereochemically isomeric form thereof, where n equals 1 or 2; Y is oxygen or sulphur; each of R¹ and R² is independently selected from a group consisting of hydrogen, deuterium, C1-C4alkyl optionally substituted with hydroxy or halogen, such as hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, C3-C6cycloalkyl optionally substituted with hydroxy or halogen, or C1-C4alkyloxy; each of R³ and R⁴ is independently selected from a group consisting of hydrogen, halogen, C1-C4alkyl, C1-C4alkyloxy, NR⁹R¹⁰, where R⁹ and R¹⁰ independently represent hydrogen or C1-C4alkyl, or 1,2-thiazolidine-1,1-dione; or two groups R³ or group R³ and R⁴ together form a six-member heterocyclic ring containing a nitrogen atom; R⁵ is selected from hydrogen, halogen or represents a heterocyclic ring selected from pyrimidin-2-yl, pyridin-2-yl or pyrazin-2-yl optionally substituted with halogen, C1-C4alkyl; R⁷ is hydrogen or C1-C4alkyl; radical of formula (a) is optionally substituted azetidine, piperidine, morpholine, oxazepane or 1,2,3,4-tetrahydroisoquinoline ring, where each of R⁶ is independently selected from a group consisting of hydrogen, halogen, C3-C6 spirocycloalkyl, phenyl, pyrazolyl, phenoxy or benzyloxy, where the phenyl or pyrazolyl group is optionally substituted with halogen, C1-C4alkyl, fluoromethyl, difluoromethyl, trifluoromethyl.

, (a).

EFFECT: compounds of formula (I) have P2X7 receptor antagonist properties.

15 cl, 1 dwg, 2 tbl, 26 ex