Otsuka Pharmaceutical Company, Limited

Takafumi Fujioka

Shuji Teramoto

Michiaki Tominaga

Kazuyuki Nakagawa

Yoichi Yabuuchi

Kazuo Banno

Hidenori Ogawa

Hiroshi Shimizu

Kazumi Kondo

Michinori Tanaka

Fujio Tabusa

Masaaki Osaki

Shigeharu Tamada

Yasuo Oshiro

Kazuyoshi Nagami

Yung-hsiung Yang

Atsushi Abiko

Michiaki Tominago

The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity. Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.

Peripheral vasodilating agent containing piperidine derivative as active

Peripheral vasodilating agents containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity, said piperidine derivative or pharmaceutically acceptable salt thereof being represented by the general formula (1) ##STR1## wherein R, R.sup.1 and R.sup.2 are as defined herein.

Antiarrhythmic agent

Peripheral vasodilators

A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R.sup.2 is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula --A--NR.sup.3 R.sup.4 (wherein A is a lower alkylene group, R.sup.3 and R.sup.4 are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation, an agent for platelet aggregate dissociation, an ameliorant of cerebral circulation and a phosphodiesterase inhibitor.

Agent for treating thrombosis and phosphodiesterase inhibitor

A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R.sup.2 is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula --A--NR.sup.3 R.sup.4 (wherein A is a lower alkylene group, R.sup.3 and R.sup.4 are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation and as an agent for platelet aggregate dissociation.

Method for prophylaxis and treatment of heart diseases using a carbostyril derivative-of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

Cardiotonic carbostyril agents for treating heart ailments

Novel carbostyril derivatives and salts thereof having useful pharmacological activities such as myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity, hypotensive activity, activity for inhibiting vasoconstriction induced by norepinephrine, and anti-inflammatory effect in one hand, while they do not possess activity for increasing heart beat at all substantially as well as show quite low toxicity and low side-effects in central nervous system activities.

Carbostyril derivatives and salts thereof

Method for the treatment of congestive heart failure or paroxymal frequent heart pulse using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of -A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

Method of treating congestive heart failure using carbostyril derivatives

Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

Cardiotonics

Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cyclocalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoyalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition of prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

Carbostyril derivatives and salts thereof having excellent positive inotropic activity, increasing activity of coronary blood flow, as well as hypotensive activity in one hand, and also they do not have substantially increasing activity of heart beat as their characteristic property, as well as they have less side-effects in the central nervous system, such as they have less vomiting effect, decreasing effect in motor function and tremor effect.

Growing community of inventors

Tokushima, Japan

Takafumi Fujioka