Toyama Chemical Co., Ltd.

Kaishu Momonoi

Isamu Saikawa

Shuntaro Takano

Seietsu Kuroda

Takashi Yasuda

Yutaka Kodama

Miwako Komatsu

Okuta Takashima

Chosaku Yoshida

Isamu Takakura

Kiyoshi Tanaka

Chiaki Kutani

Kenshin Hayashi

Joji Nakano

Bunei Nagahashi

Satoshi Ono

Yasuo Watanabe

Hirokazu Ochiai

Isao Watanabe

Toru Hiraiwa

Shinzaburo Minami

Hirohiko Fukuda

Yoshiharu Murotani

Katsuyuki Nagumo

Hiroyasu Takagi

Toshio Hayashi

Osamu Yoshino

Tetsuo Yamafuji

Hisaaki Chaki

Nobuhisa Taya

Kyoko Kasuya

This invention relates to a process for producing a compound represented by formula (6a) or (6b): ##STR1## wherein R.sup.2 represents a hydrogen atom or a hydroxyl-protecting group and R.sup.4 and R.sup.5, which may be the same or different, represents lower alkyl groups, using a compound represented by formula (2a) or (2b) obtained by preferential crystallization: ##STR2## and also to a compound represented by the following formula (7) which is an intermediate useful for producing the compound of formula (6a) or (6b): ##STR3## wherein R.sup.1 represents a group represented by formula (8): ##STR4## wherein R.sup.2 and R.sup.3 is as defined above and R.sup.3 represents a hydrogen atom, a group or a carboxyl protecting group represented by formula (9): ##STR5## or a group represented by formula (10): ##STR6## wherein R.sup.2 is as defined above.

Benzo[b]thiophen-5-yl derivative and process for producing the same

A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents an protected or unprotected carboxyl group or a carboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

Penam derivatives and salts thereof, process for producing the same and

A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents a protected or unprotected carboxy group or a craboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

Penam derivatives and salts thereof, and antibacterial agent comprising

This invention relates to a novel 1,4-dihydropyridine derivative of the formula ##STR1## wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.

Pyridyl ester containing 1,4-dihydropyridine derivatives and salts

This invention relates to a 1,4-dihydropyridine derivative of the formula ##STR1## wherein Y represents an oxygen or sulfur atom or a vinylene group, Z represents an oxygen or sulfur atom or an alkylene group, R.sup.2 represents an imidazolyl or pyridyl group and the remaining substituents are herein defined. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity.

Vasodilating and platelet aggregation inhibiting 1,4 dihydropyridines

Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.

Cephalosporins

This disclosure relates to a novel process for producing 7-(substituted)amino-3-substituted thiomethyl cephem carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

Process for producing 7-(substituted)amino-3-substituted thiomethyl

Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable anti-bacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.

Novel penicillins

This disclosure relates to a novel process for producing 7-(substituted)-amino-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

Process for producing 7-(substituted)amino-3-substituted

The N,N-dimethylacetamide adduct of 7-[D(-)-.alpha.-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-.alpha.-(4-hyd roxyphenyl)acetamido]-3-[5-(1-methyl-1,2,3,4-tetrazolyl)thiomethyl]-.DELTA. .sup.3 -cephem-4-carboxylic acid, a process for the production thereof, and a process for producing said acid and a pharmaceutically acceptable salt thereof through said adduct.

Process for producing

Intermediate for cephalosporin type compound

Novel penicillins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable antibacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.

Novel penicillins and cephalosporins and process for producing same

Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable antibacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.

Growing community of inventors

Shinminato, Japan

Kaishu Momonoi