abstract |
A compound of formula (I) or a pharmaceutically acceptable salt thereof:n wherein:n one of R, and F 2 is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl or R, and R 2 together are C 2 - 5 polymethylene; either R 3 is hydrogen, hydroxy, C 1-6 alkoxy or C 1-7 acyloxy and R4 is hydrogen or R 3 and R 4 together are a bond; R s is hydrogen; C 1-6 alkyl optionally substituted by up to three halo atoms, by hydroxy, C 1-6 alkoxy, C 1- 6 alkoxycarbonyl, carboxy, or amino optionally substituted by one or two independent C 1-6 alkyl groups or disubstituted by C 4 . 5 polymethylene; C 2 - 6 alkenyl; amino optionally substituted by a C 1-6 alkyl or C 1-6 alkenyl group or by a C 1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C 1-6 alkyl, C 1-6 alkoxy or halogen; or aryl or heteroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, C 1-12 carboxylic acyl, or amino or aminocarbonyl optionally substituted by one or two C 1-6 alkyl groups; or (when X is 0), R s is selected from the class of carboxy, C 1- 6 alkoxycarbonyl, or aminocarbonyl optionally substituted by one or two C 1-6 alkyl groups; and R 6 is hydrogen or C 1-6 alkyl; or R s and R 6 together are -CH 2 -(CH 2 ) -Z-(CH2)m-wherein m and n are 0 to 2 such that m + n is 1 or 2 and Z is CH 2 , O, S or NR wherein R is hydrogen, C 1-9 alkyl, 2-7 alkanoyl, phenyl C 1-4 -alkyl, naphthylcarbonyl, phenylcarbonyl or benzyl-carbonyl optionally substituted in the phenyl or naphthyl ring by one or two of C 1-6 alkyl, C 1-6 alkoxy or halogen; or R is heteroarylcarbonyl; or halogen, or aryl or heteroaryl, either being optionally substituted by one or more groups or atoms X is oxygen or sulphur; or R s , R 6 , X and N together are tetrahydroisoquinolinone or tetrahydroisoquinolin- thione optionally substituted in the phenyl ring as defined for R above; the nitrogen-containing group in the 4-position being trans to the R 3 group when R 3 is hydroxy, C 1-6 alkoxy or C 1-7 acyloxy; having pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals. |