DERIVATIVES OF BENZIMIDAZOLIDINONE AS AGENTS FOR MUSCARINIC RECEPTORS Russian patent published in 2006 - IPC C07D417/06 C07D413/06 C07D401/06 A61K31/445 A61K31/423 A61K31/428 A61P25/18 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a compound of the formula (I): or its pharmaceutically acceptable salt wherein X is chosen from the group consisting of carbon (C), oxygen (O), nitrogen (N) and sulfur (S) atoms; Z represents nitrogen atom (N); Y is chosen from the group consisting of =O, =S or their tautomers; SPU means a spacer element providing distance d between Z and N atom wherein -SPU- represents bi-radical -(CR⁶R⁷)_n- wherein n means 1, 2, 3, 4 or 5; N atom in common with R¹ and R² forms heterocyclic ring wherein indicated heterocyclic ring is chosen from the group consisting of piperidine and 8-azabicyclo[3.2.1]octane and wherein heterocyclic ring is substituted with one or more substitutes R⁴ chosen from the group consisting of hydrogen atom, (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl, (C₁-C₈)-alkoxy-group, (C₁-C₈)-alkylidene, (C₂-C₈)-alkenyl, (C₂-C₈)-alkynyl, (C₁-C₆)-alkyloxyimino-group each of them is substituted optionally with a substitute R⁵ and wherein at least with one of indicated substitutes R⁴ is represented by R^4' chosen from the group consisting of (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl, (C₁-C₈)-alkoxy-group and (C₁-C₈)-alkylidene wherein each of them is substituted optionally with a substitute R⁵ wherein R⁵ is chosen from the group consisting of hydrogen, halogen atom, hydroxy-group, (C₁-C₈)-alkyl, (C₁-C₈)-alkoxy-group, (C₃-C₈)-cycloalkyl, (C₂-C₈)-alkenyl and (C₂-C₈)-alkynyl; R^X can absent or can be chosen from the group consisting of hydrogen atom and optionally substituted (C₁-C₈)-alkyl; R³ can be represented in 0-4-fold range and chosen from the group consisting of halogen atom, optionally substituted (C₁-C₈)-alkyl and (C₁-C₈)-alkoxy-group; each R⁶ and R⁷ is chosen optionally and independently among the group consisting of hydrogen atom, hydroxy-group and optionally substituted (C-C₈)-alkyl. Also, invention relates to a pharmaceutical composition possessing the selective activity with respect to M and/or M₄-subtypes of muscarinic receptors and antagonism with respect to D₂-dopamine receptors and comprising compound of the formula (I) by claim 1 in common with pharmaceutically acceptable carriers or excipients. Also, invention relates to a method for enhancing activity of cholinergic receptor comprising interaction of cholinergic receptor and system comprising cholinergic receptor with the effective amount of at least one compound of the formula (I) by claim 1. Also, invention relates to using the compound according to any claim among 1-11 or its pharmaceutically acceptable salt, or pharmaceutical composition containing any base for preparing a medicinal preparation used in prophylaxis aim or treatment of psychosis or for attenuation of symptoms associated with psychosis.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

27 cl, 3 ex