BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM Russian patent published in 2021 - IPC C07D471/04 C07D498/04 C07D487/04 A61K31/519 A61K31/5383 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound described by the formula (I), which can be used as an antagonist against the P2X₇ receptor. In the formula (I), Z¹ is N; Z² is N (R^5b); the dotted line is no bond; R^5b is a hydrogen atom, hydroxyalkyl or unsubstituted alkyl; the ring Q is unsubstituted 5-element nonaromatic heterocycle containing two nitrogen heteroatoms; Y¹ is O; R^2a is a group of the formula -(C(R^2a’) (R2^b’))_n-R¹; R^2b is a hydrogen atom; R¹ is 6-element aromatic carbocyclyl substituted with 1, 2 or 3 substituents selected from halogen, unsubstituted 6-element aromatic carbocyclyl, 6-element aromatic heterocyclyl containing one nitrogen atom substituted with two substituents selected from halogen; X is N(R^7a); R^7a is a hydrogen atom; R³ is phenyl substituted with 2 or 3 substituents selected from halogen, cyano, formyl, alkyl substituted with 1, 2 or 3 substituents selected from halogen, hydroxy and unsubstituted alkyloxy, unsubstituted alkyl, alkyloxy substituted with 1, 2 or 3 substituents selected from halogen, cyano, hydroxy, unsubstituted alkyloxy, unsubstituted alkylsulfonyl and hydroxy-cyclobutyl, unsubstituted alkyloxy, unsubstituted 5-element nonaromatic heterocyclyl containing one nitrogen atom and one oxygen atom, unsubstituted 6-element aromatic heterocyclyloxy, containing one nitrogen atom, and hydroxy-alkyl-cyclobutyloxy; pyridyl substituted with 1-3 substituents selected from halogen, unsubstituted alkyl, hydroxy-alkyl and unsubstituted alkyloxy; benzothiazolyl substituted with alkyl; or dihydroisobenzofuranyl substituted with alkyl; n is 0 and m is 0. The invention also relates to an inhibitor of the P2X₇ receptor, including a compound of the formula (I), and to a pharmaceutical composition having antagonistic activity against the P2X₇ receptor, including an effective amount of the compound of the formula (I).

EFFECT: obtaining an antagonist against the P2X₇ receptor.

12 cl, 53 tbl, 18 ex