PYRROLIDINE DERIVATIVES AS NK-3 ANTAGONISTS Russian patent published in 2016 - IPC C07D401/06 C07D401/14 C07D403/06 C07D413/10 A61K31/4025 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I, where R¹ is or phenyl, pyridinyl or pyridazinyl, where phenyl, pyridinyl, pyridazinyl can be substituted with cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or 2-oxo-piperidin-1-yl, X is NR or O, R is -C(O)-lower alkyl, -C(O)-cycloalkyl substituted with lower alkyl, cycloalkyl or phenyl, pyridinyl or pyridazinyl, where phenyl, pyridinyl, pyridazinyl can be substituted with lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl, substituted with halogen, R² represents hydrogen or lower alkyl, R³ represents hydrogen, halogen, R⁴ is hydrogen or lower alkyl, where R² and R⁴ simultaneously are not hydrogen or lower alkyl, R⁵ denotes lower alkyl, R⁶ - halogen, or their pharmaceutically acceptable acid-additive salts.

EFFECT: it has been found that present compounds are high potential NK-3 receptor antagonists for treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

18 cl, 36 ex