THIA(DIA)ZOLES AS QUICK-DISSOCIATING ANTAGONISTS OF DOPAMINE 2 RECEPTOR Russian patent published in 2013 - IPC C07D417/12 A61K31/454 A61P25/18 C07D277/42 C07D285/12 

FIELD: biotechnologies.

SUBSTANCE: invention relates to derivatives of [1-(benzyl)piperydine-4-yl]-([1,3,4]thiadiazole- 2-yl)amine and [1-(benzyl)piperydine-4-yl]-(thiazole-2-yl)amine of the formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable salts, where R means hydrogen; R¹ means phenyl, substituted with 1, 2 or 3 substitutes, each of them is independently selected from a group containing halogen, cyano, C_1-4alkyl, perfluoroC_1-4alkyl and perfluoroC_1-4alkoxy; R² means hydrogen or C_1-4alkyl; R³ means hydrogen, trifluoromethyl or cyano; X means N or CR⁴, where R⁴ is trifluoromethyl. Also the invention relates to a pharmaceutical composition containing compounds of the formula as an active ingredient. The following derivatives are presented: derivatives of [1-(benzyl)piperydine-4-yl]-([1,3,4]thiadiazole-2-yl)amine and [1-(benzyl)piperydine-4-yl]-(thiazole-2-yl)amine of the formula (I) representing quick-dissociating antagonists of dopamine 2 receptors and used as medicinal agents for treatment or prevention of central nervous system.

EFFECT: improved properties of compounds.

7 cl, 22 ex