PYRROLO[1,2-A]PYRAZINE-CONTAINING LIGANDS OF THE 18 KDA TRANSLOCATOR PROTEIN WITH ANXIOLYTIC ACTIVITY Russian patent published in 2024 - IPC C07D487/04 C07D401/06 A61K31/4985 A61P25/00 A61P43/00 

FIELD: medicinal chemistry; pharmacology.

SUBSTANCE: invention relates to biologically active compounds of the 1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamides group with anxiolytic activity. The following is disclosed: 1-Phenylpyrrolo[1,2-a]pyrazine-3-carboxamide of general formula (1) and a method of treating diseases and conditions of the nervous system requiring the use of agents with anxiolytic activity, which consists in administering an effective amount of a compound of general formula (1). In the general formula (1), R¹ and R² may be propyl groups; or the NR¹R² fragment is an azepane group; or if R¹ is a benzyl group, then R² may be an ethyl or benzyl group; or if R¹ is a hydrogen atom, then R² may be a benzhydryl group, a 3,4-dimethoxyphenylethyl group, a 3,4,5-trimethoxybenzyl group, (S)-1-methoxy-1-oxo-3-phenylpropane-2-yl group, (S)-1,5-diethoxy-1,5-dioxopentan-2-yl group, (S)-1,4-diethoxy-1,4-dioxobutan-2-yl group, (S)-1 -methoxy-1-oxopropan-2-yl group, (S)-1-ethoxy-3-(1H-indol-3-yl)-1-oxopropan-2-yl group, (R)-1-ethoxy-3-(4-hydroxyphenyl)-1-oxopropan-2-yl group, (S)-1-carboxy-2-phenylethyl group.

EFFECT: use of the invention makes it possible to effectively treat diseases and conditions of the nervous system that require the use of medicinal products with anxiolytic activity.

6 cl, 4 dwg, 18 tbl, 16 ex