The Green Cross Corporation

Asahi Glass Company, Limited

Yoshihisa Inoue

Kazumasa Yokoyama

Chikara Fukaya

Taizo Ono

Tadakazu Suyama

Yoshio Arakawa

Youichiro Naito

Yoshio Tsuda

Norifumi Nakamura

Hajime Ebisu

Takashi Okazoe

Yoshitomi Morizawa

Arata Yasuda

Atsuyuki Ashimori

Jun Sasaki

Naomichi Ishida

Kazuhiro Maeda

Takehiro Okada

Masahiro Eda

Teruaki Imada

Fumio Mori

Feng Wang

Ruriko Ikegawa

Tomohiro Yoshida

Shinichiro Ono

Keigo Kosaka

Shuzhong Wang

Koichi Yamauchi

Tomoko Ito

Quinolin-2-yl benzoic acid compounds which are useful as intermediates of quinoline compounds having angiotensin II antagonist activity prepared by decarboxylating 2-(carboxyphenyl)-4-quinolinecarboxylic acid compounds in which a carboxyl group bonded to a phenyl group may be esterified, while a carboxyl group bonded to a quinoline ring is not esterified, and both rings may have one or more substituents inert to the decarboxylation reaction.

Process for producing 2-(carboxyphenyl)-4-quinolinecarboxylic acid

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

A quinoline compound represented by the formula (1) or a salt thereof: ##STR1## wherein the definition of each substituents are described in the specification, which have angiotensin II antagonism and hypotensive action and are useful as an agent for the prevention and treatment of cardiovascular system diseases such as hypertension, heart failure and the like.

Quinoline compounds

An isoindazole compound of the formula (1) or a salt thereof; a method for the production thereof; and pharmaceutical use of the compound and a salt thereof, particularly as an angiotensin II antagonist and as an agent for the prophylaxis and treatment of circulatory diseases (particularly hypertension and heart failure); ##STR1## wherein Q is a heterocyclic derivative of the formula (2) or (3) ##STR2## wherein other symbols of the above formulas are as defined in the Specification. The compound and its salt show superior angiotensin II antagonism and are low toxic. Accordingly, they are useful as angiotensin II antagonists for the treatment or prophylaxis of angiotensin II-mediated diseases such as circulatory diseases of hypertension (e.g. essential hypertension, renal hypertension) and heart failure.

Isoindazole compound

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

A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 or 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.

Perfluoro-1-azatricyclic amine compounds useful as blood substitutes or

Perfluoro-1-azatricyclic amines as blood substitutes

A perfluoroether compound having the following formula is useful as a thermostable, inert solvent and inter alia as an oxygen carrier in an artificial blood or infusion fluid. ##STR1## wherein Rf.sub.1 and Rf.sub.2 are different from each other and are selected from the group of a C.sub.1 or C.sub.3 perfluoroalkyl group which may be interrupted by an oxygen atom, and a C.sub.5 -C.sub.7 perfluorocycloalkyl group, and n and n' are zero or an integer of 1; one of Rf.sub.1 and Rf.sub.2 being the C.sub.5 -C.sub.7 perfluorocycloalkyl group and the total number of carbon atoms being 9-11 inclusive.

Perfluoro ether compound containing perfluorocycloalkyl moiety

A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 to 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.

Perfluoro-1-azatricyclic amine compounds useful as oxygen carriers in

Perfluoro-1-azatricyclic amine compound

A perfluorotricyclic amine compound which is usable as an oxygen carrier in an artificial blood, represented by the general formula ##STR1## wherein R denotes a perfluoroalkyl group having 1-4 carbon atoms; the ring A denotes a five- or six-membered ring, the ring B denotes a five-, six- or seven-membered ring, the ring C denotes a five- or six-membered ring any one of the rings A, B and C optionary being substituted by one or more lower perfluoroalkyl group in addition to the above-mentioned substituent R; and further f, g, h, i, j and k denote integers appropriately selected to construct the above-mentioned size of rings A, B, and C; is prepared by reacting the corresponding perhydrotricyclic amine with fluorine.

Perfluorotricyclic amines as oxygen carriers

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Kyoto, Japan

Yoshihisa Inoue