FIELD: pharmaceuticals.
SUBSTANCE: invention relates to compounds of formula (I), pharmaceutically acceptable salts and esters. Compounds of formula (I) have affinity and selectivity for GABA A α5 receptor. In formula X is N or CH; R1, R2 - C1-C7-alkyl, phenyl substituted by 1 halogen, wherein one of substituents R1 and R2 is an alkyl group; R3 - haloC1-C7-alkyl, nitro, -C(O) R4, -C(O) NR5R6; R4 - C1-C7-alkyl, hydroxy, C1-C7-alkoxy; R5 - hydrogen, C1-C7-alkyl, haloC1-C7 alkyl hydroxyC1-C7-alkyl, -(CH2)n-C3-C8 cycloalkyl, - (CH2)n- (4-6 membered heterocycloalkyl with 1 heteroatom selected from O), wherein heterocycloalkyl is optionally substituted with one C1-C7-alkyl group; n is an integer ranging from 0 to 1; R6 - hydrogen, C1-C7-alkyl; or R5 and R6 together with nitrogen to which they are attached form a bicyclic 7-membered heterocycloalkyl with additional heteroatom selected from O, 6-membered heterocycloalkyl with additional heteroatom selected from O, S, wherein heterocycloalkyl is optionally substituted by one or more oxo groups. Invention also relates to a pharmaceutical composition comprising a compound of invention in an effective amount, to a method for treating or preventing diseases associated with GABA A α5 receptor, use of compounds for preparation of medicaments and use of compounds for treating or preventing diseases associated with GABA A α5 receptor.
EFFECT: technical result is obtaining novel compounds having affinity and selectivity for GABA A α5 receptor.
23 cl, 1 tbl, 53 ex
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Authors
Dates
2016-06-27—Published
2011-12-07—Filed