| abstract |
Embedded image The present invention relates to a class of novel piperazine oxime derivatives having interesting NK-1 antagonist activity. The invention relates to compounds of general formula (1), wherein: X is CH 3, CF 3, OCH 3 , halogen, cyano and 5-CF 3 - 1 or 2 substituents from the group of tetrazole-1-yl Represents phenyl or pyridyl substituted with a group; Y is 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl wherein the group is optionally substituted with one or more halogen or alkyl (1-3C). or 3-indazolyl, 2-naphthyl, 3-benzo [b] thiophenyl, represents 2-benzofuranyl; n has a value of 0 to 3; m has a value of 0 to 2; R 1 is NH 2 , NH-alkyl (1-3C), dialkyl (1-3C) N, morpholino or morpholino substituted with one or two methyl and / or methoxymethyl groups, thiomorpholino, 1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH 3 - represents piperazinyl; R 2 is hydrogen, alkyl (1-4C) or phenyl, or R 2 is m is (CH 2 ) m being 1 and the carbon, nitrogen and oxygen atoms of the intermediate form an isoxazolyl or 4,5-dihydroisoxazolyl group; R 3 and R 4 are independently hydrogen or methyl Represent or alternatively, R 3 and R 4 are together oxygen. The present invention relates to the preparation of novel compounds and to pharmaceutical compositions comprising the compounds of formula (1) as active ingredients, and the use of these compounds in the treatment of disorders involving the neurokinin-1 receptor. |