TETRAHYDROQUINOLINE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS Russian patent published in 2020 - IPC C07D215/48 C07D215/20 C07D221/04 C07D401/06 C07D401/12 C07D405/12 C07D417/12 C07D417/14 C07D471/10 C07D498/10 A61P13/12 A61P19/00 A61P29/00 A61P35/00 A61P37/00 A61P43/00 A61P9/06 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of general formula (I) possessing the property of a P2X7 receptor inhibitor, a based pharmaceutical composition and a method for preparing such a composition, to intermediate compounds, a method of treatment and use. In general formula (I), X is N or N-oxide; n equals 0 or 1; R¹ is selected from a group consisting of (1) hydrogen, (3) a hydroxyl group, (4) -NH₂ and (6) -S(O)mC_1-6 alkyl, where C_1-6 alkyl can be substituted with hydroxyl; where m equals 2; R² is selected from a group consisting of (1) hydrogen, (2) halogen, (3) C_1-6 alkyl and (4) -OC_1-6 alkyl; where C_1-6 alkyl or -OC_1-6 alkyl is unsubstituted or substituted with one or two substitutes independently selected from a group consisting of halogen, hydroxyl, -OC_1-6 alkyl, -CN, -NR^9aR^10a, -(C=O)-R^9a, -(C=O)-NR^9aR^10a and -S(O)m-R^9a, where m is independently 0, 1 or 2; R¹ can form with R² group =CH₂ or =O; or R¹ can form with R² 5–6-member ring which can contain from one to three heteroatoms independently selected from a group consisting of a nitrogen atom, an oxygen atom and a carbonyl group; where 5–6 member ring is unsubstituted or substituted with one C_1-6 alkyl; R³ is independently selected from a group consisting of (2) halogen and (3) C_1-6 alkyl; p is 0 or 1; R⁴ is selected from a group consisting of (1) hydrogen, (2) halogen and (3) a hydroxyl group; R⁵ denotes hydrogen or C_1-6 alkyl; R⁶ is (1) hydrogen; R⁵ can form saturated 5-member ring with R⁶; or can form with R^6a saturated or unsaturated 9–10-member bicyclic ring which can contain an oxygen atom; where saturated 5-member ring or a saturated or unsaturated bicyclic 9–10-member ring is optionally substituted with 1–3 substitutes selected from a group consisting of (2) halogen and (4) -OC_1-6-alkylphenyl; R^7a and R^7b are independently selected from a group consisting of (1) hydrogen, (4) C_1-6 alkyl and (5) -NR^9bR^10b; rest values of radicals are as specified in the claim.

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EFFECT: treating various P2X7 receptor-mediated disorders, such as autoimmune and inflammatory diseases; nervous and nervous-immune system diseases; diseases related and not related to central nervous system (CNS) neuroinflammation; diseases of cardiovascular, metabolic, gastrointestinal and urogenital systems, and so forth.

14 cl, 69 tbl, 354 ex