Kanebo, Limited

Keizo Ito

Goro Tsukamoto

Hiroshi Ohtaka

Koichiro Yoshino

Takashi Nose

Ryuichi Iemura

Tominori Morita

Koichi Yokota

Tsuneo Kawashima

Toshihiko Kohno

Akira Yamashita

Toshikazu Fukuda

Toshiro Kanazawa

Kenji Yoshida

Masahiro Taguchi

Takayuki Sukamoto

Katsumi Dezawa

Kenji Suzuki

Hajime Kagaya

Manabu Hori

Noriko Yamamoto

Masaru Moriyama

Norihiko Seko

Yoichiro Hamada

Hideaki Hara

Sigeru Tajima

Koichi Shimohara

A neuroprotecting drug comprises as an essential active ingredient ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl]pyrrol-1-yl acetate, which is useful with high safety for the prophylaxis and treatment of brain dysfunction induced by hypoxia due to the disturbance of cerebral circulation such as cerebral hemorrhage or cerebral infarction in human being.

Neuroprotective drug

A quinazoline derivative represented by the following formula (I) ##STR1## or its pharmacologically acceptable acid addition salt and processes for production thereof. The quinazoline compound is used as a cerebral dysfunction remedying agent.

Quinazoline derivative, processes for its production, and cerebral

Novel piperazine compounds of the formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is methoxy group and another is hydrogen atom, or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-peptic ulcer activities with potent activity for promoting the action of the defensive factor, and hence are useful as an anti-ulcer agent for the prophylaxis and treatment of peptic ulcers.

Piperazine compounds and anti-ulcer composition containing the same

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

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

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.

Phosphonic acid ester, pharmaceutical compositions containing the same

Novel benzimidazole derivatives of the formula: ##STR1## wherein R.sup.1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and n is 2 or 3, or pharmaceutically acceptable acid addition salts thereof, which have excellent antihistaminic activities and are useful as antiallergics for various allergic diseases, and a process for the preparation thereof, and an antihistaminic composition containing the compound as an active ingredient.

Benzimidazole derivatives, process for the preparation thereof and

2-Substituted benzimidazole compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl or lower alkoxy, and R.sub.2 is hydrogen or lower alkyl with the proviso that R.sub.1 and R.sub.2 do not stand for hydrogen simultaneously and, when R.sub.1 is hydrogen, R.sub.2 cannot mean a methyl group at 6th position on the pyridin-2-yl group or methyl an isobutyl group on the phenyl group; are useful as anti-inflammatory agents and/or analgesics.

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Osaka, Japan

Keizo Ito