Toyama Chemical Co., Ltd.

Isamu Takakura

Isamu Saikawa

Shuntaro Takano

Takashi Yasuda

Kaishu Momonoi

Hiroyuki Imaizumi

Yutaka Kodama

Kiyoshi Tanaka

Hideo Taki

Hirokazu Ochiai

Chiaki Kutani

Kenshin Hayashi

Masaru Tai

Seietsu Kuroda

Bunei Nagahashi

Yasuo Watanabe

Masuru Tai

Shosaku Kato

Sadao Sotani

Sustained-release oral ointment

A 7.alpha.-methoxycephalosporin represented by the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents an organic group linked to the carbon atom through an oxygen or sulfur atom; R.sup.3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl or heterocyclic group, and a salt thereof. These compounds have a broad antibacterial spectrum, high resistance to .beta.-lactamase produced from bacteria, and an effective antibacterial activity against clinical isolates of bacteria.

7.alpha.-Methoxycephalosporins

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

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

A 7.alpha.-methoxycephalosporin represented by the general formula and a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents an organic group linked to the carbon atoms through an oxygen or sulfur atom; R.sup.3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl group. These compounds have a broad antibacterial spectrum and high resistance to .beta.-lactamase produced from bacteria, and are well absorbed in a living body.

7.alpha.-methoxycephalosporins and pharmaceutical composition comprising

Intermediate for cephalosporin type compound

Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinyl-carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and methods for producing the same.

Substituted

Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinylcarbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds.

7.alpha.-Methoxy-cephalosporins

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Toyama, Japan

Isamu Takakura