SUBSTITUTED 3-SULPHONYL-[1,2,3]TRIAZOLO[1,5-a]PYRIMIDINES-ANTAGONISTS OF SEROTONIN 5-HT RECEPTORS, METHOD OF PRODUCING SAID COMPOUNDS AND USE Russian patent published in 2010 - IPC C07D487/04 C07D495/14 A61K31/519 A61P25/28 

FIELD: pharmacology.

SUBSTANCE: present invention relates to antagonists of serotonin 5-HT₅ receptors with general formula 1 and their pharmaceutically acceptable salts and/or hydrates, particularly to substituted 3-sulphonyl-[1,2,3]triazolo[1,5-a]quinazolines and 3-sulphonyl-thieno[2,3-e][1,2,3]triazolo [1,5-a]pyrimidines, as active compounds for pharmaceutical compositions and medicinal agents, and methods of producing said compounds. In general formula 1 , Ar is a phenyl which is unsubstituted or substituted with halogen or at least one lower alkyl; R¹ is a hydrogen atom or optionally substituted amine group, or optionally substituted 5-6 member azaheterocyclyl, bonded by a nitrogen atom to a carbon atom of a triazolopyrimidine ring with 1-2 heteroatoms selected from nitrogen, oxygen or sulphur, and optionally annulated with a benzene ring; where the substitutes are selected from hydrogen, optionally substituted C₁-C₅alkyl, optionally substituted C₃-C₈cycloalkyl, alkoxy group, acyl, saturated or unsaturated optionally annulated 5-7 member heterocyclyl, where heteroatoms are selected from nitrogen, oxygen or sulphur, optionally substituted phenyl; R² and R³ together with carbon atoms to which they are bonded form an optionally substituted benzene or thiophene ring, where substitutes are selected from C₁-C₅alkyl or halogen atom.

EFFECT: invention also relates to pharmaceutical compositions and medicinal agents, a method of treating or preventing development of CNS diseases mediated by action of serotonin 5-HT₅ receptors, for example Alzheimer's disease.

20 cl, 6 dwg, 4 tbl, 8 ex