Fujisawa Pharmaceutical Company, Ltd.

Takao Takaya

Hisashi Takasugi

Takashi Masugi

Toshiyuki Chiba

Kohji Kawabata

Hiromu Kochi

Hideaki Yamanaka

Kiyoshi Tsuji

Masayoshi Murata

Yoshikazu Inoue

Nobuyoshi Yasuda

Zenzaburo Tozuka

Kazuo Sakane

Kenzi Miyai

Akiteru Yoshioka

Takashi Kamiya

Kiyotaka Ito

Atsushi Kuno

Ikuo Ueda

Takashi Ogino

Masakazu Kobayashi

Hideo Tsutsumi

Keiji Matsuda

Tadashi Kitaguchi

Hiroyoshi Sakai

Yoshie Sugiyama

Tsutomu Toyonaka Teraji

Shigetaka Nishino

Masashi Hashimoto

Teruo Kyoto Oku

Keiji Hemmi

Youichi Shiokawa

Osamu Nakaguti

Tadaaki Komori

Yoshihisa Saito

Shintaro Nishimura

Kazuhiro Maeda

Kimio Esumi

Yoshie Sakamoto

Kenji Miyai

Akito Tanaka

Fumio Shimojo

Fumiyuki Shirai

Yousuke Katsura

Teruaki Matuo

Hitoshi Nakamura

Yoshiko Inamoto

Keiji Takai

Nobuyuki Yasuda

Hideaki Yamanada

Kiyosha Tsuji

Yasunobu Inaba

The present invention relates to new cephem compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same and anti-bacterial methods of using the same. The subject cephem compounds comprise a thiadiazine ring bonded to the cephem through an iminoacetamido chain and a pyarzolium ring bonded to the cephem through a methylene chain.

Cephem compounds and processes for preparation thereof

A compound of the formula: ##STR1## in which R.sup.2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl,

7-acylamino-3-substituted cephalosporanic acid derivatives

Intermediates of the following formula are disclosed: ##STR1## wherein R.sup.1 is aryl; R.sup.2 is carboxy or protected carboxy; Z.dbd.CH.dbd.CH.sub.2, CH.sub.2 --X.sup.2, --CH.sub.2 --P.sup.+ (R.sup.7).sub.3 .X.sup.3 or CH .dbd.P(R.sup.7).sub.3 wherein X.sup.2 and X.sup.3 are each halogen and R.sup.7 is aryl. The compounds are useful as intermediates for cephalosporins.

Cephalosporin intermediates

The invention relates to compounds of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,

Cephem compounds

The invention relates to cephem compounds characterized by a substituted 2-pyrazolimethyl group and a 7-(aminothiazolyl) (hydroxyimino)-acetamido group and certain derivatives thereof, to pharmaceutical compositions comprising the same and to use for treatment of infectious diseases.

The invention relates to intermediate compounds of the formula: ##STR1## wherein R.sup.3 is a lower alkyl, hydroxy(lower)alkyl or a protected hydroxy(lower)alkyl,

Intermediates for cephem compounds

The invention relates to a compound of antibacterial activity of the formula: ##STR1## in which R.sup.1 is aminothiazolyl which may have halogen, aminothiadiazolyl, aminooxadiazolyl, aminopyridyl, aminopyrimidinyl, acyl aminothiazolyl which may have halogen, di(lower)alkylaminomethyleneaminothiadiazolyl, di(loweralkylaminomethyleneaminooxadiazolyl, or acylaminopyridyl,

7-acylamino-3-vinylcephalosporanic acid derivatives

The invention relates to a compound, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 and R.sup.4 are each amino or a protected amino group,

The compound of the formula: ##STR1## wherein R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, and R.sup.6 is amino or protected amino, or its reactive derivative at the carboxy group effective for transforming the carboxy group into a reactive N-acylating group, or a salt thereof.

Syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and

The benzazole compounds of this invention can be represented by the following formula [I]: ##STR1## wherein R.sup.1 is aryl or a heterocyclic group, each of which may have suitable substitutent(s),

Benzazole compounds and pharmaceutical composition comprising the same

A compound of the formula ##STR1## in which R.sup.1 is a group of the formula: ##STR2## wherein R.sup.4 is lower alkyl and R.sup.5 is amino or a protected amino group, R.sup.2 lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl, R.sup.3 is carboxy or a protected carboxy group, and A is lower alkylene which may have a substituent selected from the groups consisting of amino, a protected amino group, hydroxy, oxo and a group of the formula:

The invention relates to a pharmaceutical composition as a therapeutic agent for ischemic disease comprising a compound of the formula ##STR1## wherein R.sup.1 is carbamoyl substituted with morpholino (lower) alkyl, thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl; and

N-containing heterocyclic compounds, and composition comprising the same

The invention relates to a cephem compound of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino, R.sup.2 is hydrogen, phenyl, pyridyl which may have a lower alkyl group, or cyano, and R.sup.3 is carboxy or protected carboxy, or a salt thereof.

A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, aryl, ar(lower)alkyl or a heterocyclic group, each of which may have suitable substituent(s),

Amino-pyridinyl and pyrimidinyl intermediates have been synthesized.

7-acylamino-3-vinylcephalosporanic acid derivatives and processes for

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Kawanishi, Japan

Takao Takaya