ARYL-ISOXAZOL-4-YL-IMIDAZO[1,2-a]PYRIDINE SUITABLE FOR TREATING ALZHEIMER'S DISEASE THROUGH GABA RECEPTORS Russian patent published in 2011 - IPC C07D471/04 A61K31/437 A61P25/28 

FIELD: chemistry.

SUBSTANCE: in general formula I R¹ denotes hydrogen atom, a halogen atom, hydroxy, lower alkyl, benzyloxy or -O-(CH₂)-(CO)-(5-member heteroaryl with 2 heteroatoms selected from N, O), substituted with phenyl or lower alkyl; R² denotes a hydrogen atom, a halogen atom, lower alkyl, lower alkynyl, amino, -NHC(O)R^a or -(CO)-R^a; R³ denotes a hydrogen atom, a halogen atom, cyano, lower alkyl, lower alkynyl, amino, -NHC(O)-R^a, -(CO)-R^a, 4- or 5-member heterocycloalkyl substituted with a =O group or a 5-member heteroaryl with 1-2 heteroatoms selected from N; R⁴ denotes a hydrogen atom or a 5-member heteroaryl with 2 heteroatoms selected from N; R⁵ denotes lower alkyl or C₃-C₇cycloalkyl; R^a denotes lower alkoxy, -(CH₂)_n-(6-member heteroaryl with 1 heteroatom selected from N), phenyl C₃-C₇-cycloalkyl or NR'R", where each of R' and R" independently denotes a hydrogen atom, lower alkyl, substituted hydroxy, lower alkynyl, -(CH₂)_n-C₃-C₇-cycloalkyl, -(CH₂)_n-(6-member heterocycloalkyl with 1-2 heteroatoms selected from O, N) or -(CH₂)_n-(5- or 6-member heteroaryl with 1 heteroatom selected from N, O); n assumes values from 0 to 3. The invention also relates to a medicinal agent containing one or more compounds of formula I and use of the disclosed compounds to prepare the medicinal agent.

EFFECT: high activity and selectivity towards GABA A receptor subunit α5.

18 cl, 72 ex