SUBSTITUTED 8-SULPHONYL-2,3,4,5-TETRAHYDRO-1H-GAMMA-CARBOLINES, LIGANDS, PHARMACEUTICAL COMPOSITION, SYNTHESIS METHOD AND USE THEREOF Russian patent published in 2010 - IPC C07D471/04 A61K31/437 A61P25/18 A61P25/22 A61P25/28 A61P25/24 

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted 8-sulphonyl-2,3,4,5-tetrahydro-1H-γ-carbolines of general formula 1 or pharmaceutically acceptable salts thereof, which are ligands with a wider range of simultaneous activity towards alpha adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepiniphrine receptors and serotonin receptors. In compounds of general formula 1 R1 is an amino group substitute selected from hydrogen; C₁-C₃alkyl optionally substituted with phenyl; C₁-C₄alkyloxycarbonyl; R2 is a cyclic system substitute selected from hydrogen, C₁-C₃alkyl optionally substituted with phenyl, pyridin-(3- or 4-yl), (6-methylpyridin-3-yl); C₁-C₃alkenyl substituted with phenyl; or optionally substituted phenylsulphonyl; R3 is an optionally halogen-substituted phenyl, six member aromatic azaheterocycle, mono- or di-C₁-C₃alkylamino group, phenylamino group which is optionally substituted with halogen atoms on the phenyl ring, or a substituted six member azaheterocycle containing an additional nitrogen atom, substituted with C₁-C₃alkyl.

EFFECT: compounds can be used in treating and preventing diseases and pathological conditions of the central nervous system, such as anxiety disorders, cognitive disorders, neurodegenerative diseases and depression.

18 cl, 2 dwg, 6 tbl, 23 ex