Patent ID: 6156747
Filing Date: 2000-12-05
Classification: A61P,C07D

Abstract:
A compound of formula ##STR44## a N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, whereinn is zero, 1, 2, 3, 4, 5, or 6;p is zero, 1, 2 or 3;q is zero, 1, 2 or 3;r is zero, 1, 2 or 3;R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or a radical of formula: ##STR45## wherein R.sup.9, R.sup.10, R.sup.11 and R.sup.12 each independently are hydrogen, halo, trihalomethyl, or C.sub.1-6 alkyl;m is zero, 1, 2, or 3;R.sup.13, R.sup.14, R.sup.15 and R.sup.16 each independently are hydrogen or C.sub.1-6 alkyl; orR.sup.15 and R.sup.16 taken together may form a bivalent radical C.sub.4-5 alkanediyl;R.sup.17 is hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl;C.sub.1-6 alkyloxycarbonyl; aryl; di(aryl)methyl; C.sub.1-6 alkyl substituted with hydroxy,C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl;each R.sup.3 independently is halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl;each R.sup.4 independently is halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl;each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl;X is CR.sup.6 R.sup.7 ; whereinR.sup.6 and R.sup.7 each independently are hydrogen, hydroxy, C.sub.1-6 alkyl, trihalomethyl, C.sub.1-6 alkyloxy or R.sup.6 and R.sup.7 taken together may form methylene; mono- or di(cyano)methylene; a bivalent radical of formula --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 --, --O--(CH.sub.2).sub.2 --O--, --O--(CH.sub.2).sub.3 --O--; or, together with the carbon atom to which they are attached, a carbonyl;R.sup.8 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl, arylcarbonyl, arylC.sub.1-6 alkylcarbonyl, C.sub.1-6 alkylsulfonyl, arylsulfonyl or arylC.sub.1-6 alkylsulfonyl;each ##STR46## independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is phenyl; or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C.sub.1-6 alkyl and trihalomethyl.