FIELD: organic chemistry; pharmaceuticals.
SUBSTANCE: compound of formula (II-I) having the properties of an inhibitor of GABA receptor function, a pharmaceutical composition based on it, a method of treating a disease of the central nervous system (CNS) associated with GABA function, and a method of inducing sedation and/or anesthesia with their use. In the general formula (II-I) t is 1; n is 0 or 1; R19 represents unsubstituted C2-C6-alkyl, unsubstituted C2-C6-alkenyl; R5 represents a hydrogen atom; R3 represents either a hydrogen atom or a C1-6 alkyl, optionally substituted with one or more C1-3 alkoxy; R6a and R6b each represent a hydrogen atom; R1 is a C1-6 alkyl, optionally substituted by one or more –OH, a 5-6 membered heterocyclyl containing 1-2 heteroatoms independently selected from N or O, and optionally substituted by one or more substituents independently selected from unsubstituted C1-6 alkyl, phenyl, optionally substituted with one or more halogens, or –S(O)2CH3, phenyl, optionally substituted with one or more unsubstituted C1-6 alkyls, 5-10 membered heteroaryl containing 1-4 atoms N and optionally substituted with one or more substituents independently selected from unsubstituted C1-6 alkyl, –CN or C1-6 alkoxy, or -N(RA1)2 where RA1 represents a hydrogen atom or phenyl, optionally substituted with one or several substituents independently selected from unsubstituted C1-6 alkyl or –CN; R2a, R2b, R4a, R4b, R7a, R7b, R11a, R11b, R12a, R12b or R17b each represents a hydrogen atom; each of R15a, R15b, R16a and R16b represents a hydrogen atom; and moreover
represents a single bond.
EFFECT: effective treatment of diseases of the central nervous system (CNS) associated with GABA function and inducing sedation and/or anesthesia.
31 cl, 50 ex
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