Kanebo, Limited

Goro Tsukamoto

Keizo Ito

Fumio Sakamoto

Shoji Ikeda

Koichiro Yoshino

Takashi Nose

Masahiro Taguchi

Hiroshi Ohtaka

Hirosato Kondo

Isamu Utsumi

Tominori Morita

Toshihiko Kohno

Yoshimasa Inoue

Tsuneo Kawashima

Ryuichi Iemura

Yoshihiro Kawahata

Katsumi Dezawa

Hajime Kagaya

Toshikazu Fukuda

Koji Iuchi

Toshio Uno

Toshiro Kanazawa

Toshio Satoh

Shigeru Yamabe

Mitsuo Okazaki

Mikio Sotomura

Masanori Takamatsu

Koichi Yokota

Akira Yamashita

Norihiko Seko

Yoichiro Hamada

Keiso Ito

Yasushi Takebe

Masaru Moriyama

Toshimi Okuno

Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.

Quinolinecarboxylic acid derivative starting compounds

Quinolinecarboxylic acid derivatives and antibacterial agent containing

Novel benzylpiperazine compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, which has excellent hypolipidemic activity without undesirable side effect, and a pharmaceutical composition containing the compound as an active ingredient suitable for the prophylaxis and treatment of hyperlipidemia.

Benzylpiperazine compound and pharmaceutical composition as

A 1-benzhydryl-4-cinnamylpiperazine derivative represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a methoxy group, and R.sup.2 represents a hydrogen or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof. The compound (I) is prepared by selectively reducing the corresponding 1-benzhydryl-4-cinnamoylpiperazine derivative and optionally converting the product into its acid addition salt. The compound (I) is useful for treatment of cerebrovascular disease in a human.

Novel 1-benzhydryl-4-cinnamylpiperazine derivatives, and pharmaceutical

Novel compounds of the formula: ##STR1## wherein R is ethyl, 2-fluoroethyl or cyclopropyl, and X is hydrogen atom or fluorine atom, and a pharmaceutically acceptable salt thereof, which have excellent antimicrobial activities in vivo and hence are useful as an antimicrobial agent, and an antimicrobial composition containing said compound as an active ingredient, and processes for the preparation of the compounds.

Quinolinecarboxylic acid compounds and antimicrobial agent containing

Novel N-phenyl-trans-4-guanidinomethylcyclohexanecarboxamide compounds of the formula: ##STR1## wherein R is hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which have excellent anti-ulcer activities and hence are useful as an anti-ulcer drug, and a pharmaceutical composition useful for the treatment and prophylaxis of peptic ulcers which comprises as an active ingredient the compound as set forth above in admixture with a conventional pharmaceutically acceptable carrier or diluent.

Novel guanidinomethylcyclohexanecarboxylic acid compounds and anti-ulcer

A 1-benzyl-4-benzhydrylpiperazine derivative represented by the following general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a methoxy group, and

1-(2,3,4-tri-methoxybenzyl)-4[bis(4-fluorophenyl)methyl] piperazines are

Novel 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)-thiazoles of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, 2,2,2-trifluoroethyl, a group of the formula: --CH.sub.2 COOR.sup.2 R.sup.2 is C.sub.1-8 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, or phenyl-C.sub.1-2 alkyl), or a group of the formula: --(CH.sub.2).sub.n --A--R.sup.3 (A is oxygen or sulfur, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and n is 1, 2 or 3), a process for the preparation of the compounds, and a pharmaceutical composition useful as a platelet aggregation inhibitor which comprises as an active ingredient the above 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)thiazole compound in admixture with a conventional pharmaceutically acceptable carrier or diluent.

Novel 4,5-Bis (4-methoxyphenyl)-2-(pyrrol-2-yl) thiazoles and

An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4. The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.

Novel ethyl benzylphosphinate derivatives, process for production

Novel benzimidazole derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R.sup.2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof, which have potent antihistaminic activity with less toxicity and hence are useful as an antihistaminics, and a process for the preparation of the compounds, and a pharmaceutical composition useful as antihistaminics containing the compound as an essential active ingredient.

1-substituted-2-(piperazinyl or homopiperazinyl)-benzimidazole compounds

4-Chloro-4-methyl-5-methylene-1,3-dioxolane-2-one

1-Ethyl-6,8-difluoro-1,4-dihydro-7-(1-imidazolyl)-4-oxoquinoline-3-carboxyl ic acid derivative of the formula: ##STR1## wherein R is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, which have excellent anti-microbial activities and are useful as an anti-microbial agent for the treatment of infectious diseases in warm-blooded animals including human beings, and an anti-microbial composition containing said compound as an active ingredient.

Antimicrobial

A novel quinolinecarboxylic acid derivative of the formula ##STR1## or a pharmaceutically acceptable salt thereof. These compounds are useful as antibacterial agents, and are prepared by a process which comprises reacting a compound of the formula ##STR2## with a compound of the formula ##STR3##

Quinolinecarboxylic acid derivative, and antibacterial agent containing

A 1,1-dioxopenicillanic acid ester represented by formula (I) ##STR1## wherein R represents a methyl or phenyl group. The ester of formula (I) may be prepared by reacting 1,1-dioxopenicillanic acid or its salt with a compound represented by formula (III) ##STR2## wherein R is as defined above, and X represents a halogen atom, or by oxidizing a compound of formula (V) ##STR3## wherein R is as defined above. The ester of the formula (I) is useful as a .beta.-lactamase inhibitor and may be used in association with a .beta.-lactam antibiotic.

Ester of 1,1-dioxopenicillanic acid, and use thereof as .beta.-lactamase

A phosphonic acid ester of the formula ##STR1## exhibits calcium-antagonistic, coronary vasodilating and hypotensive activities. Pharmaceutical compositions containing the same are useful for the prophylaxis and treatment of circulatory organ diseases such as angina pectoris, hypertension and the like.

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Toyonaka, Japan

Goro Tsukamoto