Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-11-10
1989-02-28
Schwartz, Richard A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514220, 514221, 5142345, 514303, 514338, 514367, 514373, 514387, 514395, 514400, 540496, 540506, 540507, 544139, 546118, 546271, 548161, 548179, 548180, 548305, 548329, 548330, 548342, A61K 31415, C07D41306
Patent
active
048086053
ABSTRACT:
Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof. The compounds of formual I have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias, high blood pressure and cardiac insufficiency.
REFERENCES:
patent: 3914216 (1975-10-01), Bauer et al.
patent: 4680310 (1987-07-01), Hengartner et al.
Chem. Abstracts 90(15):121465x (1979) (Furnefeld, E., et al., J. Org. Chem. 1979, 44(5), 835-839).
Branca Quirico
Jaunin Roland
Maki Hans P.
Marti Franzi
Ramuz Henri
Boxer Matthew
Hoffmann-La Roche Inc.
Leon Bernard S.
Saxe Jon S.
Schwartz Richard A.
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