| abstract |
FIELD: medicine, pharmaceutics. n SUBSTANCE: invention relates to new derivatives of piperidine of formula I: , in which: R 1 and R 2 are selected from group, including alkyl, halogenalkyl, alkyl substituted with one or more hydroxy groups, -CN, alkynyl, -N(R 6 ) 2 , - N(R 6 )-S(O 2 )-alkyl, -N(R 6 )-C(O)-N(R 9 ) 2 , -alkylene-CN, -cycloalkylene-CN, -alkylene-O-alkyl, -C(O)-alkyl, -C(=N-OR 5 )-alkyl, -C(O)-O-alkyl, -alkylene-C(O)-alkyl, -alkylene-C(O)-O-alkyl, -alkylene-C(O)-N(R 9 ) 2 and group , , , , n provided that at least one of R 1 and R 2 stands for -CN or group , , , , n W stands for =C(R 8 )- or =N-; X stands for -C(O)- or -S(O 2 )-; Y is selected from group, including -CH 2 -, -O- and -N(R 6 )-C(O)-, provided that: (a) atom of nitrogen of group -N(R 6 )-C(O)- is linked with X, and (b) if R 1 and/or R 2 stands for and Y stands for -O-, then X does not stand for -S(O 2 )-; Z stands for -C(R 7 ) 2 -, -N(R 6 )-, or -O-; R 3 is selected from group, including H and non-substituted alkyl; R 4 stands for H; R 5 stands for H or alkyl; R 6 is selected from group, including H, alkyl, cycloalkyl and aryl; each R 7 independently stands for H or alkyl; or each R 7 together with circular atom of carbon, to which they are linked, as indicated, forms cycloalkylene ring; R 8 is selected from group including H, alkyl, alkyl substituted with one or large number of hydroxygroups, -N(R 6 ) 2 , -N(R 6 )-S(O 2 )- alkyl, -N(R 6 )-S(O 2 )-aryl, -N(R 6 )-C(O)-alkyl, -N(R 6 )-C(O)-aryl, alkylene-O-alkyl and -CN; R 9 is selected from group including H, alkyl and aryl, or each R 9 jointly with atom of nitrogen, to which, as indicated, they are linked, forms heterocycloalkyl ring; Ar 1 stands for non-substituted phenyl; Ar 2 stands for phenyll substituted with 0-3 substituents, selected from group including halogenalkyl; n equals 0, 1 or 2; and m equals 1, 2 or 3, and to their pharmaceutically acceptance salts and hydrates. n EFFECT: production of new biologically active compounds, having properties of antagonist of neurokinin receptor NK 1. n 35 cl, 60 ex |