C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/242, 260/306
C07D 311/68 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01)
Patent
CA 1236458
ABSTRACT Compounds of formula (I): Image (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 ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl; r - 2 - one of R3 and R4 is hydrogen or Cl-4 alkyl and the other is C1-4 alkyl or R3 and R4 together are C2-5 polymethylene, either R5 is hydrogen, hydroxy, C1-6 alkoxy or Cl-7 acyloxy and R6 is hydrogen or R5 and R6 together are a bond; R7 is aryl or heteroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C1-6 alXyl, C1-6 alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, Cl-l2 carboxylic acyl, or amino or aminocarbonyl optionally substituted by one or two Cl-6 alkyl; R8 is hydrogen or Cl-6 alkyl; and X is oxygen or sulphur; the R8-N-CX-R7 group being trans to the R5 group when R5 is hydroxy, Cl-6 alkoxy or Cl-7 acyloxy; or a pharmaceutically acceptable salt or solvate thereof, have antihypertensive activity.
454467
Cassidy Frederick
Evans John M.
Beecham Group P.l.c.
Borden Ladner Gervais Llp
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