The Green Cross Corporation

Yoshitomi Pharmaceutical Industries, Ltd.

Atsuyuki Ashimori

Yoshihisa Inoue

Masahiro Eda

Teruaki Imada

Kazumasa Yokoyama

Chikara Fukaya

Taizo Ono

Kazuhiro Maeda

Takehiro Okada

Norifumi Nakamura

Hajime Ebisu

Fumio Mori

Masahide Nakajima

Feng Wang

Tomohiro Yoshida

Ruriko Ikegawa

Fumihiko Akahoshi

Takuya Yoshimura

Shinichiro Ono

Keigo Kosaka

Hiroshi Sakashita

Hajime Fukuyama

Mizuo Miyazaki

Hideki Okunishi

Heterocyclic amide compounds and medicinal uses thereof

Heterocyclic amide compounds and pharmaceutical use of the same

A novel carboxylic acid compound having a condensed ring; which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.

Carboxylic acid compound having condensed ring, salt thereof and

Dihydropyridine derivatives represented by formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6, which may be the same or different, each represents an alkyl group, a cycloalkyl group or an alkoxyalkyl group; R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a nitro group, a halogenated alkyl group, an alkylsulfonyl group, a halogenated alkoxy group, an alkylsulfinyl group, an alkyl group, a cycloalkyl group, an alkxoy group, a cyano group, an alkoxycarbonyl group or an alkylthio group (provided that R.sub.4 and R.sub.5 are not hydrogen atoms at the same time); X represents a vinylene group or an azomethine group; A and B are each an alkylene group or an alkenylene group; R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an aryl group, or a heterocyclic group (provided that R.sub.7 and R.sub.8 may combine with the adjacent nitrogen atom to form a heterocyclic ring), and acid addition salts of the dihydropyridine derivatives of formula (I).

Dihydropyridine derivatives

Dihydropyridine derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.

Dihydropyridine derivatives and pharmaceutical composition thereof

There is provided a dihydropyridine derivative having the formula ##STR1## wherein R'.sub.1 denotes methyl, chlorine, bromine, fluorine, trifluoromethyl, nitro, cyano or methoxy, R.sub.7 denotes benzyl; and the dihydropyridine links to the 2-, 3-, or 4-position of the pyridine. The compound has an activity as a Ca-antagonist, and is useful for treating vascular disorders such as coronary artery disease, celebral artery disease, hypertension and the like.

Certain 1,4-dihydro-2,6-dilower-alkyl-4-(mono-substituted pyridyl)

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Hirakata, Japan

Atsuyuki Ashimori