Carbostyril derivative

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

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Details

5142352, 514312, 544 586, 544128, 544331, 544332, 546153, 546157, 546158, A61K 3147, A61K 31505, C07D40112, C07D40312

Patent

active

054017408

ABSTRACT:
The novel carbostyril derivative represented by the general formula (1) ##STR1## [in the formula, A, R.sup.1, R.sup.2 and the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton have the same definitions as above] has an excellent platelet aggregation inhibitory activity, a phosphodiesterase inhibitory activity, a venticular contraction activity (a positive contraction activity), an anti-ulcer activity, an anti-inflammatory activity, a cerebral blood flow increasing activity, a thrombus dissociation activity, a thromboxane A.sub.2 antagonism activity, etc. The carbostyril derivative of the present invention is characterized in that it exhibits the above activities for a long time, is low in toxicity (particularly low in toxicity to hearts of cardiovascular hyperplasia, myocardipathy, etc.), and is low in circulation activities such as heart rate increasing activity, blood pressure decreasing activity and the like. Also, the carbostyril derivative of the present invention has advantages in that it is easily absorbed by the intestinal tract and easily migrates into blood. Therefore, the carbostyril derivative of the present invention can be used most suitably as a preventive and remedy for thrombi such as apoplexia, cerebral infarction, myocardial infarction and the like, a cerebral circulation improving agent, an anti-inflammatory agent, an anti-asthmatic agent, a cardiotonic agent and a phosphodiesterase inhibitory agent.

REFERENCES:
patent: 4070470 (1978-01-01), Nakagawa et al.
patent: 4298739 (1981-11-01), Nishi et al.
patent: 4435404 (1984-03-01), Nishi et al.
patent: 4482560 (1984-11-01), Banno et al.
patent: 5008274 (1991-04-01), Nishi et al.

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