PYRROLIDINE DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS Russian patent published in 2015 - IPC C07D401/06 C07D401/14 C07D403/14 C07D405/14 A61K31/44 A61P25/28 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula and its pharmaceutically active salts; R¹ represents hydrogen, halogen; n represents 1 or 2, if n represents 2, then R¹ can be different; R² represents C_2-7-alkyl or C_3-6-cycloalkyl; R³ represents the group wherein X represents CH; R⁵ represents hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, S(O)₂-lower alkyl, -C(O)-CH₂-CN, or represents -C(O)-C_3-6-cycloalkyl, wherein the cycloalkyl groups can be optionally substituted by a lower alkyl, -CH₂-O-lower alkyl, lower alkoxy, CF₃, halogen or cyano, or represents -C(O)-(4-6-merous heterocycloalkyl containing 1 heteroatom specified in O, N), or represents -C(O)-(6-merous heteroaryl containing 1-2 heteroatoms N), or represents 6-merous heteroaryl containing 1-2 heteroatoms N, or represents -C(O)-phenyl, wherein heterocycloalkyl, heteroaryl or phenyl groups are optionally substituted by halogen, lower alkyl, =O, lower alkyl substituted by a halogen, lower alkyl substituted by hydroxy, -C(O)-CH₂-N(di-lower alkyl), C(O)NH₂, -O-C(O)-lower alkyl, C(O)-lower alkyl, S(O)₂-lower alkyl or cyano; R⁴ represents phenyl substituted by a halogen. The invention also refers to the compound [(3S,4R)-4-(4-chloro-3-fluoro-phenyl)-1-(1-isopropyl-6-oxo-piperidin-3-carbonyl)-pyrrolidin-3-yl]-ethyl-carbamic acid 4-fluoro-phenyl ester; to a medicinal product possessing properties of an NK-3 receptor antagonist, containing one or more compounds of the inventions, and to the use of the compounds for preparing the medicinal product.

EFFECT: there are prepared new compounds, which possess the properties of the NK-3 receptor antagonist.

8 cl, 1 tbl, 126 ex