DERIVATIVES OF (3-METHYLPYRROLIDIN-3-YL)-METHYL PYRIDINYL ETHER AND THEIR USE AS ANTAGONISTS OF RECEPTOR NK-3 Russian patent published in 2017 - IPC C07D401/12 C07D401/14 C07D405/14 C07D413/14 A61K31/4439 A61P25/00 

Abstract RU 2625798 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of the general formula

Wherein A is taken from groups (a), (b) or (c): (a) or (b) or is cycloalkyl possibly substituted with a lower alkyl (c); Ar1 is phenyl or a six-membered heteroaryl containing one or two nitrogen atoms; X1 is N or CH; X2 is N-R1 or O; R1 is S(O)2-lower alkyl, C(O)-cycloalkyl, substituted with a lower alkyl, or is C(O)-lower alkyl, lower alkyl, cyano group, cycloalkyl or a six-membered heteroaryl containing one or two nitrogen atoms substituted with a lower alkyl, cyano group, C(O)-lower alkyl, halogen, lower alkyl substituted with halogen or lower alkoxy group, or is a phenyl substituted with a cyano group or halogen. R2 is a lower alkyl, halogen, pyrazolyl, 3-methyl-[1,2,4]oxazolyl, 5-methyl-[1,2,4]oxadiazol-3-yl, pyridyl substituted with a cyano group or is a phenyl substituted with a halogen or is a cyano group, lower alkoxy group or is piperidine-2-on. The invention may also relate to pharmaceutically active salts of the coumpound of the formula I.

EFFECT: compounds are prospective antagonists of the NK-3 receptor for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety syndrome and attention deficit/hyperactivity disorder.

12 cl, 1 tbl, 27 ex

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RU 2 625 798 C2

Authors

Nettekofen Mattias

Ratni Khasan

Vifian Valter

Dates

2017-07-19Published

2011-07-04Filed