| abstract |
Compounds of formula (I): <IMAGE> (I) wherein: one of X and Y is CO and the other is NH; R1 is C1-6 alkoxy or C1-6 alkylthio; R2 is hydrogen, trifluoromethyl, C1-6 alkylthio, C1-7 acyl, C1-7 acylamino, C1-6 alkylsulphonyl, C1-6 alkylsulphinyl, halogen, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two groups selected from C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-4 alkyl, phenyl or phenyl C1-4 alkyl groups any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C1-6 alkoxy or nitro groups, or N-disubstituted by C2-5 polymethylene; R3 is amino, aminocarbonyl or aminosulphonyl N-substituted by one or two C3-8 cycloalkyl, C3-8 cycloalkyl C1-4 alkyl, phenyl or phenyl C1-4 alkyl groups any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C1-6 alkoxy or nitro groups, or N-disubstituted by C1-6 alkyl and one of the foregoing list of N-substituents or C4-5 polymethylene; R6 is C1-7 alkyl, -(CH2)sR7, s being 0 to 2 and R7 being C3-8 cycloalkyl, -(CH2)t R8, t being 1 or 2 and R8 being thienyl or phenyl optionally substituted by one or two substituents selected from C1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy and C1-4 alkyl optionally substituted by hydroxy, C1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; Z is CH2 or oxygen; p and q are independently 0 to 2 when X is CH2 and are both 1 when Z is oxygen, having dopamine antagonist activity, a process for their preparation and their use as pharmaceuticals. |