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Substituted 8-sulphonyl-2,3,4,5-tetrahydro-1h-gamma-carbolines, ligands, pharmaceutical composition, synthesis method and use thereof. RU patent 2404180.

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

IPC classes for russian patent Substituted 8-sulphonyl-2,3,4,5-tetrahydro-1h-gamma-carbolines, ligands, pharmaceutical composition, synthesis method and use thereof. RU patent 2404180. (RU 2404180):

C07D471/04 - Ortho-condensed systems

A61P25/28 - for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

A61P25/24 - Antidepressants

A61P25/22 - Anxiolytics

A61P25/18 - Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

A61K31/437 -

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