abstract |
Compounds of formula (I):n wherein:n one of X and Y is CO and the other is NH; R, is C 1-6 alkoxy or C 1-6 alkylthio; R 2 is hydrogen, trifluoromethyl, C 1-6 alkylthio, C 1-7 acyl, C,7 acylamino, C 1-6 alkylsulphonyl, C,. e alkysulphinyl, halogen, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3 . s cycloalkyl C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl groups any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C 1-6 alkoxy or nitro groups, or N-disubstituted by C 2-6 polymethylene; R 3 is amino, aminocarbonyl or aminosulphonyl N-substituted by one or two C 3-8 cycloalkyl, C 3-8 cycloalkyl C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl groups any of which phenyl moieties may be substituted by or more halogen, trifluoromethyl, C 1-6 alkoxy or nitro groups, or N-disubstituted by C 1-6 alkyl and one of the foregoing list of N-substituents or C 4-5 polymethylene; R 6 is C 1-7 alkyl, -(CH 2 ).R 7 ,s being 0 to 2 and R 7 being C 3-8 cycloalkyl, -(CH 2 ) t R 8 , t being 1 or 2 and R s being thienyl or phenyl optionally substituted by one or two substituents selected from C 1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy and C 1-4 alkyl optionally substituted by hydroxy, C 1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolysable acyloxy; Z is CH 2 or oxygen; p and q are independently 0 to 2 when X is CH 2 and are both 1 when Z is oxygen, having dopamine antagonist activity, a process for their prepartion and their use as pharmaceuticals. |