Cycloalkyl-substituerede glutaramidderivater, farmaceutiske præparater indeholdende disse forbindelser, forbindelserne til brug i lægemidler og deres anvendelse til fremstilling af lægemidler til behandling af hypertension, hjertesvigt eller
Compounds of the formula: Wherein A completes a 5 or 6 membered carbocyclic ring which may be saturated or monounsaturated; R is H or (C1-C4)alkyl; R and R are H, (C1-C6)alkyl, C3-C7 cycloalkyl, benzyl, or an alternative biolabile ester-forming group; Y is either a direct bond or an alkylene group o...
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Zusammenfassung: | Compounds of the formula: Wherein A completes a 5 or 6 membered carbocyclic ring which may be saturated or monounsaturated; R is H or (C1-C4)alkyl; R and R are H, (C1-C6)alkyl, C3-C7 cycloalkyl, benzyl, or an alternative biolabile ester-forming group; Y is either a direct bond or an alkylene group of from 1 to 6 carbon atoms; R is H, aryl, heterocyclyl, R CONR -, R NR CO-, R NR SO2- or R SO2NR -, with the proviso that Y is not a direct bond when R is H, aryl or heterocyclyl; wherein R is H, (C1-C6)alkyl or aryl(C1-C6)alkyl; R is (C1-C6)alkyl, aryl, aryl(C1-C6)alkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl or a group of the formula R R R C- wherein R is H, OH, (C1-C6)alkoxy, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, aryl(C1-C6)alkyl, (C2-C6)alkenyl, heterocyclyl, heterocyclyl(C1-C6)alkyl, R CONH-, R SO2NH- or (R )2N-; R and R are H or (C1-C6)alkyl; or R is H and R is amino(C1-C6)alkyl, imidazolylmethyl, aryl, aryl(C1-C6)alkyl, aryl(C1-C6)alkoxy(C1-C6)alkoxy, hydroxy(C1-C6)alkyl or methylthio(C1-C6)alkyl; or the two groups R and R form a 3 to 6 membered carbocyclic ring or a pyrrolidine or piperidine ring which may optionally be substituted by amino, (C2-C4)alkanoyl or aroyl; R is (C1-C6)alkyl, (C3-C7)cycloalkyl, aryl, aryl(C1-C6)alkyl, heterocyclyl or heterocyclyl(C1-C6)alkyl; each R is H, (C1-C6)alkyl, aryl(C1-C6)alkyl or the two groups R form a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C1-C4)alkyl-piperazinyl group; R is (C1-C6)alkyl, aryl, aryl(C1-C6)alkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl or a group of the formula R R R C- wherein R and R are as previously defined and R is (R )2NCO-, R OCH2- or R OCO, wherein R and R are as previously defined and R is (C1-C6)alkyl, (C3-C7)cycloalkyl or aryl(C1-C6)alkyl; and R is (C1-C6)alkyl, aryl, aryl(C1-C6)alkyl, heterocyclyl or heterocyclyl(C1-C6)alkyl; R is a group of the formula: wherein R is H, halo, 4-OH, 4-(C1-C6 alkoxy), 4-(C3-C7 cycloalkoxy) 4-(C2-C6 alkenyloxy), 4-[(C1-C6 alkoxy)carbonyloxy], 4-[(C3-C7 cycloalkoxy)carbonyloxy], or 3-(C1-C4 alkyl)SO2NH-; and R is H, C1-C4 alkyl, C1-C4 alkoxy, C2-C6 alkanoyl or halo; or R is a group of the formula: wherein said groups may optionally be substituted in the fused benzene ring by C1-C4 alkyl, C1-C4 alkoxy, OH, halo or CF3; are antihypertensive agents of utility in the treatment of hypertension, heart failure and renal insufficiency. |
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