DERIVATIVES OF N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDES AND THEREOF APPLICATION AS PDE10A INHIBITORS Russian patent published in 2015 - IPC C07D487/04 C07D519/00 A61K31/519 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to formula (I) compounds and their pharmaceutically acceptable salts. Invention compounds can be applied as PDE10A-inhibiting therapeutically active substances. In formula (I) R¹ represents phenyl or thienyl, where phenyl and thienyl are optionally substituted with 1 substituent, selected from the group, consisting of hydroxyl, halogen atom, lower alkoxy, lower halogenalkoxy, -OC(O)-lower alkyl, -OCH₂C(O)-lower alkoxy and phenyl; R² represents 5- or 6-membered monocyclic heteroaryl, which has from 1 to 3 heteroatoms, independently selected from N and O, where heteroaryl is optionally substituted with from 1 to 3 substituents, independently selected from the group, consisting of , halogen atom, nitro, lower alkyl, lower alkenyl, lower alkoxy, lower alkoxy -C(O)-, lower halogenalkyl, lower alkoxy - lower alkyl, C3-C6cycloalkyl, phenyl, 5-membered monocyclic heteroaryl, which has 2 heteroatoms, independently selected from N and O, and amino, substituted with 6-membered heteroaryl, which has 2 heteroatoms, selected from N, where two substituents R² together with heteroaryl, which they are bound to, can form 9-membered bicyclic ring; R⁸ represents hydrogen atom. Values of other radicals are given in invention formula. Invention also relates to formula (I') compounds, structural formula and values of radicals are given in invention formula. Invention also discloses pharmaceutical compositions and application of compounds for obtaining medication.

EFFECT: obtaining novel formula (I) compounds, possessing properties of PDE10A inhibitor.

15 cl, 176 ex