Antihypertensive substituted imidazole derivatives
AssigneeFarmos Group Ltd.
InventorsArto J. Karjalainen, Kauko O. A. Kurkela
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Abstract
The invention provides novel compounds of the formula: ##STR1## wherein the various substituents are defined herein below. Processes for the preparation of these compounds are described, as are novel pharmaceutical compositions comprising at least one of the compounds of their salts. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antihypertensive agents. Furthermore, some of the compounds have proved to possess antithrombotic and diuretic activity. Antimycotic and antifungal properties have also been found.
Claims12
A substituted imidazole of the formula:
- ##STR61## or a non-toxic pharmaceutically acceptable addition salt thereof, wherein R.sub.1 is H, alkyl of 1 to 4 carbon atoms or --CH.sub.2 OH;
- R.sub.2 is H or --CH.sub.3 ;
- R.sub.3 is --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, ##STR62## --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3, or --CH.sub.2 CH.dbd.CH.sub.2, and R.sub.4 is H or OH;
- or R.sub.3 and R.sub.4 together represent .dbd.CH.sub.2, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, ##STR63## or .dbd.CH--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 ;
- R.sub.5 R.sub.6 and R.sub.7 which can be the same or different are H, --CH.sub.3, --CH.sub.2 CH.sub.3, halogen, OH or --OCH.sub.3, at least one of R.sub.5, R.sub.6 and R.sub.7 being other than hydrogen, or R.sub.5 is hydrogen and R.sub.6 and R.sub.7 together form an --O--CH.sub.2 --O--bridge between two adjacent carbon atoms in the phenyl group.
A pharmaceutical composition useful for producing an anti-hypertensive effect comprising an effective amount of a substituted imidazole of the formula:
- ##STR64## or a non-toxic pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is H, alkyl of 1 to 4 carbon atoms or --CH.sub.2 OH;
- R.sub.2 is H or --CH.sub.3 ;
- R.sub.3 is --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, ##STR65## --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3, or --CH.sub.2 CH.dbd.CH.sub.2, and R.sub.4 is H or OH;
- or R.sub.3 and R.sub.4 together represent .dbd.CH.sub.2, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, ##STR66## or .dbd.CH--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 ;
- R.sub.5 R.sub.6 and R.sub.7 which can be the same or different are H, --CH.sub.3, --CH.sub.2 CH.sub.3, halogen, OH or --OCH.sub.3, at least one of R.sub.5, R.sub.6 and R.sub.7 being other than hydrogen, or R.sub.5 is hydrogen and R.sub.6 and R.sub.7 together form an --O--CH.sub.2 --O--bridge between two adjacent carbon atoms in the phenyl group, and a compatible, pharmaceutically acceptable carrier therefor.
Dependencies are inferred from the claim text.