Yamanouchi Pharmaceutical Company Ltd.

Yasuo Isomura

Noriki Ito

Makoto Takeuchi

Kazuo Kubo

Hiroshige Homma

Isao Souzu

Minoru Okada

Shuichi Sakamoto

Masafumi Kudou

Tetsushi Abe

Masuo Murakami

Toichi Takenaka

Toru Yoden

Yukiyasu Murakami

Tadao Kojima

Yoshinori Okamoto

Kazuharu Tamazawa

Hideki Arima

Kiyoshi Takanobu

Masahiko Hayakawa

Ken Ikeda

Eiji Kawaminami

Yasuhiro Yonetoku

Ryo Naito

Seijiro Akamatsu

Akira Suga

Takashi Fujikura

Isao Yanagisawa

Kunihiro Niigata

Yuzo Matsumoto

Masaki Yokota

Yasufumi Hirata

Masaaki Takeda

Yoshio Ishii

Masaharu Asano

Masahiro Iwata

Kazuhisa Takayama

Yoshiaki Shimada

Motonori Aoki

Noriya Yamamoto

Yoshisaburo Kaneko

Mamoru Hamada

Kousei Kawamuki

Akira Niwa

Noriko Nagaoka

Hiroaki Akane

Yasuhito Arakida

Tetshshi Abe

Shinichi Tsukamoto

Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same.

Quinuclidine derivatives and medicinal composition thereof

Azole derivative with leukotriene (LTs) antagonizing activity and

Naphthyridine derivatives and pharmaceutical compositions thereof

Triazolylated teritiary amine compound or salt thereof

A process is provided for producing diastereoisomer A or a pharmaceutically acceptable acid addition salt of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester which comprises subjecting a mixture of diastereoisomers A and B of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester to column chromatography using silica gel as a carrier and a mixture of ethyl acetate and acetic acid as an eluant, and then separating the acetate of diastereoisomer A from the eluate, or treating the acetate with a base, or further treating the resulting diastereoisomer A with a pharmaceutically acceptable acid.

Dihydropyridine-3, 5-dicarboxylic acid ester derivatives

Substituted tertiary amino compound or salt thereof

Crystal of monohydrate of heterocyclic bis(phosphonic acid) derivative

##STR1## A compound represented by general formula (I), a pharmaceutical composition containing same, a process for the production thereof, and an intermediate therefor. In formula (I) R.sup.1 represents lower alkyl which may be substituted by a substituent selected from the group consisting of mercapto, lower alkylthio, arylthio and lower acylthio; R.sup.2, R.sup.3 and R.sup.4 may be the same or different from one another and each represents lower alkyl; X represents oxygen or sulfur; and Y represents a single bond or lower alkylene. The compound (I) has a matrix metalloprotease inhibitory activity and is useful for preventing and treating diseases caused by the progress of connective tissue breakage.

Hydroxamic acid derivative

A dextro-rotatory optical isomer of diastereoisomer A of (.+-.)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl)ester 5-methyl ester is provided having the formula ##STR1## and wherein the melting point of the hydrochloride of the dextro-rotatory optical isomer is 223.degree. to 230.degree. C. (decomp.), or a pharmaceutically acceptable acid addition salt thereof.

Dihydropyridine-3,5-dicarboxylic acid ester derivatives

The diastereoisomer A of a dihydropyridine-3,5-dicarboxylic acid ester derivative is provided as well as its pharmaceutically acceptable acid addition salts. The invention further discloses a process for producing the compounds and their use as medicaments in imparting vasodilating activity.

(Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.

(Cycloalkylamino)methylenebis(phosphonic acid) and medicines contaiing

A novel heterocyclic bisphosphonic acid derivatives represented by the following general formula (I): ##STR1## in which .circle.Het means one of the following (A) and (B): ##STR2## wherein a dotted line in (A) means that two adjacent atoms are bonded by a single bond or a double bond, ##STR3## wherein R.sup.6 and R.sup.7 may be the same or different, each represents a hydrogen atom, a lower alkyl group, a halogen atom or a hydroxyl group,

Heterocyclic bisphosphonic acid derivatives

A novel heterocyclic bisphosphonic acid derivatives represented by the following general formula (I): ##STR1## in which, .circle.Het  means one of following (A) and (B): ##STR2## wherein a dotted line in (A) means that two adjacent atoms are bonded by a single bond or a double bond, ##STR3## wherein R.sup.6 and R.sup.7 may be the same or different, each represents a hydrogen atom, a lower alkyl group, a halogen atom or a hydroxyl group,

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Ibaraki, Japan

Yasuo Isomura