NOVEL COMPOUND, MANUFACTURE AND MEDICINAL COMPOSITION

摘要

Compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) wherein: either one of R1 and R2 is hydrogen and the other is selected from the class of C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto C2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino or ethenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl(NOH) or -C(C1-6 alkyl)NNH2 or, when Y is oxygen, one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by C2-7 alkanoyl; one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R2 and R3 together are C2-5 polymethylene; R5 is hydroxy, C1-6 alkoxy or C1-7 acyloxy; R6 is hydrogen or C1-6 alkyl; R7 is NR8R9 wherein R8 and R9 are independently C1-6 alkyl, R8 is hydrogen and R9 is C1-6 alkyl or R8 and R9 together are C4-5 polymethylene; or R6 and R8 together are -(CH2)n-wherein n is 2 or 3, and R9 is hydrogen or C1-6 alkyl; or R7 is CH2R10 wherein R10 is hydrogen or C1-5 alkyl optionally substituted by halo, hydroxy or C1-6 alkoxy; or R6 and R10 are --(CH2)m- wherein m is 2 or 3; X is oxygen or sulphur; and Y is oxygen, CH2 or NH; the R6-CH-CX-R7 group being trans to the R5 group; having blood pressure lowering activity, a process for their preparation and their use as pharmaceuticals.