Carbostyril derivatives, process for producing the same and...

Details Carbostyril derivatives, process for producing the same and... Carbostyril derivatives, process for producing the same and...

C - Chemistry, Metallurgy

07

D

260/277.1, 260/2

C07D 215/48 (2006.01) C07C 205/57 (2006.01) C07D 401/00 (2006.01) C07D 413/06 (2006.01)

Patent

CA 1199915

ABSTRACT OF THE DISCLOSURE Novel carbostyril derivatives and their salts 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 and R3 may be the same or different and each are a lower alkyl group which may have hydroxy groups or halogen atoms as the substituents, or a phenyl-lower alkyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, or said phenyl-lower alkyl group may have a lower alkylenedioxy group as the substituent on the phenyl ring; further R and R3 may form, together with the adjacent nitogen atom, a 5- or 6-membered saturated heterocyclic ring which may have a lower alkyl group or a phenyl- lower alkyl group as the substituent; when said heterocyclic ring is a piperazinyl group, said piperazinyl ring may have a lower alkyl group or a phenyl-lower alkyl group as the substituent at 4-position in the piperazinyl ring, further said piperazinyl group may have, as the substituent at 4-position, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, a cycloalkyl- lower alkyl group, a lower alkanoyl group, a lower alkanoyl-lower alkyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a furoyl group, a lower alkylsulfonyl group, a substituted lower alkyl group, a phenoxy- lower alkyl group, a phenyl-lower alkyl group, a benzoyl group, a phenylsulfonyl group, a benzoyl-lower alkyl group, a phenyl-lower alkenylcarbonyl group, or a phenyl-lower alkanoyl group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond. Carbostyril deriva- tives of the present invention represented by the general formula (1) have myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity and hypotensive activity, thus they are useful as cardiotonic for curing various heart diseases such as congestive heart failure, mitral valvular disease, atrial fibrillation and flutter and parrxyamal atrial tachycardia.

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