DIHYDROOXAZOLE-2-AMINE DERIVATIVES Russian patent published in 2016 - IPC C07D263/28 C07D263/16 C07D413/12 C07D413/14 A61K31/4725 A61K31/4427 A61K31/506 A61K31/497 A61K31/421 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I), in which R1 is hydrogen or lower alkyl; R² represents hydrogen or represents heteroaryl, selected from a pyridinyl, containing as a substitute cyano group; R³ represents hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy group, lower alkoxy group, substituted with halogen, cyano group, S-lower alkyl, S(O)-lower alkyl, S(O)₂-lower alkyl, C(O)-lower alkyl or C_3-6-cycloalkyl; R⁴ is hydrogen or lower alkyl; 6-member aromatic ring, possibly containing (N), is a phenyl or pyridinyl, in which N atom can be in different positions; X is a bond or -CH(CF₃)-; Ar denotes aryl or heteroaryl, selected from phenyl, naphthyl, quinolinyl, pyridinyl, pyrimidinyl, pyrazinyl, possibly containing one or more as a substitute R³. Invention also relates to a pharmaceutical composition having high affinity for trace amine receptors (TAAR1), containing as an active ingredient a compound of formula (I) and a pharmaceutically acceptable carrier.

EFFECT: dihydrooxazole-2-amine derivatives, having high affinity for trace amine receptors (TAAR1), used as therapeutically active substance.

14 cl, 1 tbl, 75 ex

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