Carbostyril derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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Details

544363, 544377, 544379, C07D21500, A61K 3147

Patent

active

045144010

ABSTRACT:
Novel carbostyril derivatives represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkyl group; R.sup.2 is a lower alkanoyl group, a lower alkoxycarbonyl group, a furoyl group, a lower alkane-sulfonyl group, a substituted benzoyl group, a substituted phenyl-lower alkenylcarbonyl group, a phenoxy-lower alkyl group, or a substituted phenylsulfonyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; and the substituted position of the side-chain of the formula, ##STR2## may be of 5-, 6-, 7- or 8-position in the carbostyril skeleton; and acid addition salts thereof.
The carbostyril derivatives of the general formula (1) of the present invention and acid addition salts thereof have myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity and hypotensive activity. They are useful as cardiotonics for curing various heart diseases such as congestive heart failure, mitralism, auricular fibrillation, auricular flutter, paroxysmal atrial tachycardia and the like.

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