AMINOPYRAZINE COMPOUNDS WITH THE A2A ANTAGONIST PROPERTIES Russian patent published in 2020 - IPC C07D241/26 C07D413/04 C07D413/14 C07D403/04 C07D403/14 A61K31/497 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound or a pharmaceutically acceptable salt thereof, having a structure of formula A, where "Het" is a group of formula (given in the claim), where "R^a1" and R"^a2", each independently denotes: (a) -H or (b) lower alkyl, which is optionally substituted with 1–3 groups, which are: (i) halogen or (ii) lower alkoxy; (A) one of R¹ or R² is lower alkyl or -H, and the other is (a) a linear, branched, monocyclic or bicyclic alkyl group with up to 7 carbon atoms, which is optionally substituted with 1–3 substituents; (b) 9- or 10-member heteroaryl cycloalkyl condensed moiety containing 1 nitrogen heteroatom; (c) 6-member heterocycloalkyl containing 1 nitrogen heteroatom which is optionally substituted; (d) 9- or 10-member heterocycloalkylaryl condensed moiety containing 1 heteroatom selected from N and O, which is optionally substituted with -OH or halogen; (e) 9- or 10-member heteroaryl heterocycloalkyl condensed moiety containing 1 nitrogen heteroatom which is optionally substituted with -OH or halogen; (f) 9- or 10-member arylcycloalkyl condensed moiety which is optionally substituted; (B) R¹ and R², taken together, represent a group of formula -[(CR^B1R^B2)₂)_n]-, where "n" is integer from 3 to 5, and "R^B1" and "R"^B2", each independently represents: (a) hydrogen, (b) phenyl or (c) halogen; thereby forming a heterocycloalkyl group with the nitrogen atom to which they are bonded; or (C) R¹ and R², taken together, form 10-membered fused arylheterocycloalkyl fragment containing one nitrogen heteroatom, or 6-N-linked 6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine; and "R³" is: (a) -CN; (b) halogen, preferably -Cl; (c) lower alkyl, which is optionally substituted with one or two groups, which are: (i) -OH or (ii) halogen; where lower alkyl is a linear, branched or cycloalkyl moiety containing up to 6 carbon atoms; and lower alkoxy is RO-, where R is a linear, branched or cycloalkyl moiety containing up to 6 carbon atoms. Invention also relates to a compound or pharmaceutically acceptable salt thereof, having formula A-1, where R^A-1 is lower alkyl; "Het" is a group of formula (given in the claim; where "R^a1 " and "R^a2" are -H; and "R³" is: (a) halogen, preferably -Cl; (b) lower alkyl; where lower alkyl is a linear fragment containing up to 6 carbon atoms.

EFFECT: compounds are intended for use in therapy as an antagonist of A_2A-receptor, for treating a central nervous system (CNS) disorder.

10 cl, 4 tbl, 393 ex