SPIROAZACYCLIC COMPOUNDS, METHOD FOR INHIBITION IF ACTIVITY OR ACTIVATION OF SEROTONIN 5-НТ2А RECEPTOR, METHOD FOR TREATMENT OF MORBID STATE ASSOCIATED WITH SEROTONIN 5-НТ2А RECEPTOR AND THEIR USING Russian patent published in 2008 - IPC C07D471/10 C07D498/10 A61K31/438 A61K31/537 A61P25/00 A61P9/00 

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes novel spiroazacyclic compounds of the general formula: wherein X means -CH₂, -CH₂O, -OCH₂ or oxygen atom (O); Y represents O; Z means -CH or nitrogen atom (N); R¹ means (C₁-C₆)-alkyl optionally substituted with morpholinyl, 1,3-dioxanyl, 1,4-dioxanyl, 1,3-dioxolanyl, 2-oxoimidazolidinyl, imidazolidinyl, 2-oxooxazolidinyl, oxazalidinyl or (C₃-C₆)-cycloalkyl, (C₂-C₈)-alkyl ester or benzyl ester; m is chosen from group comprising 0 or 1; R⁴ means hydrogen atom or benzyl optionally substituted with halogen atom or (C₁-C₄)-alkyl; R⁵ means hydrogen atom or benzyl optionally substituted with halogen atom, (C₁-C₄)-alkyl or (C₁-C₄)-alkoxy-group; R⁶ means hydrogen atom or benzyl optionally substituted with (C₁-C₄)-alkoxy-, cycloalkyl-(C₁-C₄-alkoxy)- or halogen-(C₁-C₄-alkoxy)-group; R² and R³ mean hydrogen atom and at least two radicals among R⁴, R⁵ and R⁶ mean optionally substituted benzyl. Also, invention relates to a method for inhibition of activity of serotonin 5-HT_2A receptors, a method for treatment of state mediated by serotonin 5-HT_2A receptors, and using spiroazacyclic compounds proposed.

EFFECT: improved method of treatment, valuable medicinal properties of compounds.

35 cl, 3 tbl, 2 dwg, 45 ex