Fujisawa Pharmaceutical Company, Ltd.

Osamu Nakaguti

Masashi Hashimoto

Takashi Kamiya

Teruo Kyoto Oku

Tsutomu Toyonaka Teraji

Yoshihisa Saito

Hidekazu Takeno

Hitoshi Nakamura

Keiji Hemmi

Yoshiharu Nakai

Norihiko Shimazaki

Takao Takaya

Hisashi Takasugi

Youichi Shiokawa

Tadaaki Komori

Yoshio Miyazaki

Yoshio Kawai

Ikuo Ueda

Masaaki Matsuo

Masakazu Kobayashi

Yoshinari Sato

Suminori Umio

Michie Nakatuka

Suita Saito

Teruo Oko

Diseases caused by platelet activating factor are prevented and treated by administration to a subject of a therapeutically effective amount of a piperazine compound of the formula: ##STR1## wherein R.sup.1 to R.sup.4 are as defined in the specification.

Piperazine compound as PAF-antagonist

The invention relates to a PAF-antagonist pharmaceutical composition comprising a compound of the formula: ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl or thiazolyl(lower)alkyl,

A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen,

Semicarbazide derivatives, processes for preparation thereof and

This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various groups at the fourth position of the azetidinone nucleus, which have antimicrobial activities against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammals including human beings and animals.

Azetidinone compounds and processes for preparation thereof

This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various group at the fourth position of the azetidinone nucleus, which have antimicrobial activity against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammals including human beings and animals.

2-Azetidinone compounds and processes for preparation thereof

New antimicrobial azetidinone derivatives and their salt of the formula: ##STR1## wherein R.sub.1 amino or acylamino, and A is selected from a variety of groups.

Azetidinone derivatives and process for preparation thereof

A process for producing a 2-cephem or 3-cephem derivative compound of the formula: ##STR1## wherein R.sub.1 represents a substituted or unsubstituted amino radical and R.sub.4 represents hydrogen or a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and the dotted line indicates the alternate bond structure providing 3-cephem or 2-cephem, which comprises:

Azetidinone 4-disulfides

This invention relates to a process for preparing an oxidized penam derivative of the formula: ##STR1## wherein R.sub.1 represents an amino or protected amino radical, and

Process for providing an oxidized penam

A compound of the formula ##STR1## wherein R.sup.1 is amino or substituted amino, R.sup.2 is carboxy or protected carboxy, R.sup.3 is lower alkyl and X is --S-- or ##STR2## or a pharmaceutically acceptable salt thereof is effective against various microorganisms.

2-Lower alkyl-2 or 3-cephem-4-carboxylic acid derivatives

This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various groups at the fourth position of the azetidinone nucleus, which have antimicrobial activities against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammal including human being and animals.

An oxoazetidine derivative compound of the formula: ##STR1## wherein R.sub.1 represents a substituted or unsubstituted amino radical and R.sub.3 represents a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and --SR.sub.2 is a residue of a thiophilic sulphur nucleophile.

Disulfide substituted oxazetidine derivatives

A process for preparing an azetidinone of the formula: ##STR1## which comprises reacting a C-unsubstituted methyleneamine of the formula: ##STR2## with R.sup.2 --CH.sub.2 COOH, its acid halide or anhydride, in the presence of boron trihalide and an organic base, wherein R.sup.1 is an organic residue bearing a carboxy group or its derivative and R.sup.2 is azido, substituted amino, halogen, acyloxy, alkoxy, aryloxy or aralkoxy.

Process for the preparation of 1,3-disubstituted-2-azetidinones from

Substituted phenylacetic acid compounds represented by the following general formula and preparation thereof: ##STR1## wherein R.sup.1 is hydrogen or protected carboxy,

Substituted phenylacetic acid compounds and process for preparation

A compound of the general formula: ##STR1## wherein R.sup.1 is amino or a conventional, pharmaceutically acceptable acylamino, R.sup.2 is carboxy or a conventionally protected carboxy, X is --S-- or ##STR2## R.sup.3 is lower alkyl and Y' is a residue of a strong nucleophile selected from the group consisting of azido, thiocyanato, lower alkyanoylthio and piperidinothiocarbonylthio.

Penam derivatives

New antimicrobial azetidinone derivatives and their salt of the formula: ##STR1## wherein R.sub.1 is amino or acylamino, and A is selected from a variety of groups.

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Osaka, Japan

Osamu Nakaguti