Carbostyril derivative

C - Chemistry – Metallurgy – 07 – D

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260/266.3

C07D 401/06 (2006.01) C07D 215/227 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01)

Patent

CA 1205807

ABSTRACT OF THE DISCLOSURE Novel carbostyril derivatives represented by the general formula (1), Image (1) [wherein R1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl- lower alkyl group; R2 is a lower alkanoyl group, a lower alkoxycarbonyl group, a furoyl group, a lower alkane- sulfonyl group, a benzoyl group (which may have 1 to 3 substitutents selected from the group consisting of a lower alkyl group, a lower alkoxy group, a halogen atom, a cyano group, an amino group and a nitro group on the phenyl ring, or may have a lower alkylenedioxy group as the substituent on the phenyl ring), a phenyl-lower alkenylcarbonyl group (which may have 1 to 3 lower alkenyl- carbonyl groups as the substituents on the phenyl ring), a phenoxy-lower alkyl group, or a phenylsulfonyl group (which may have a lower alkyl group as the substituent on the phenyl ring); 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, Image may be of 5-, 6-, 7- or 8-position in the carbostyril skeleton], and acid addition salt thereof. The carbostyril derivatives of the general formula (1) of the present invention and acid addition salt thereof have myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity and hypotensive activity, thus 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. Specifical- ly, carbostyril derivatives and salts thereof of the general formula (1) have excellent effects in positive inotropic activity, coronary blood flow increasing activity and hypotensive activity, while they are charac- terized that as they have less toxicities to the heart such as have very weak heart beat increasing activity.

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