Otsuka Pharmaceutical Company, Limited

Yoshio Shu

Takao Nishi

Katsumi Tamura

Yasuo Koga

Makoto Komatsu

Minoru Okada

Tetsuyuki Uno

Carbostyril derivatives

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.

Carbostyril derivative

Carbostyril compounds or salts thereof of the formula ##STR1## wherein A is a C.sub.1 -C.sub.6 alkylene group; R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl group which may have, as a substituent, a group selected from the group consisting of C.sub.1 -C.sub.6 alkoxycarbonyl groups, a carboxy group, C.sub.2 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl groups, amino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylamino-C.sub.1 -C.sub.6 alkyl groups and hydroxy-C.sub.1 -C.sub.6 alkyl groups, a C.sub.3 -C.sub.8 cycloalkyl group, a tetrahydropyranyl-C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.3 alkylenedioxy group-substituted C.sub.1 -C.sub.6 alkyl group, a phenyl-C.sub.1 -C.sub.6 alkyl group having, as a substituent on the phenyl ring, 1 to 3 groups selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and a hydroxyl group, or a piperidinyl-C.sub.1 -C.sub.6 alkyl group having a C.sub.1 -C.sub.6 alkyl group as a substituent; R.sup.2 is a 5-membered or 6-membered saturated or unsaturated heterocyclic-C.sub.1 -C.sub.6 alkyl group, said heterocyclic being selected from the group consisting of pyrrolidinyl, morpholino, piperidinyl, thiomorpholino, imidazolyl, 1,2,4-triazolyl, furyl, piperazinyl, pyridyl, tetrahydropyranyl and 1,3-oxathiolranyl groups which may have, as a substituent thereon 1 to 3 groups selected from the group consisting of hydroxy-C.sub. 1 -C.sub.6 alkyl groups, C.sub.2 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl groups, a hydroxyl group, C.sub.1 -C.sub.6 alkyl groups, amino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylamino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkoxy groups, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkoxy groups, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl groups, a thio group and C.sub.1 -C.sub.6 alkylamido groups; the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton being a single bond or a double bond and pharmaceutical compositions containing the compound as the active ingredient.

Growing community of inventors

Tokyo, Japan

Yoshio Shu