Yamanouchi Pharmaceutical Company Ltd.

Tetsuya Maeda

Noriaki Nagano

Masaru Iwanami

Yoshinobu Nagano

Masaharu Fujimoto

Atsuki Yamazaki

Tadao Shibanuma

Masuo Murakami

Kiyoshi Murase

Ichiro Isaka

Kazaharu Tamazawa

Masaki Yokota

Toru Yoden

Masato Satoh

Ryuichiro Hara

Tokuo Koide

Norio Kawahara

Hideki Anan

Toshio Okazaki

Ei-ichi Nakai

Katsuhiko Hamaguchi

Masauki Komiya

Masato Sato

A cephalosporin compound represented by the general formula: ##STR1## This compound exhibits a high antimicrobial activity.

Cephalosporin derivatives

A 7-[2-(2-amino-4-thiazolyl)-2-(hydroxyimino)-acetamido]-3-(1,3-dithiolan-2- yl)-3-cephem-4-carboxylic acid derivative is provided which can be represented by the general formula: ##STR1## wherein A represents a hydrogen atom, a 1-acetoxyethyl group, a 1-cyclohexylacetoxyethyl group or a pivaloyloxy-methyl group.

Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.

1,3-Dithietane-2-carboxylic acid penicillin and cephalosporin derivatives

The invention relates to novel 7.alpha.-methoxycephalosporin derivatives having at the 7.beta.-position an amido group acylated by a 1,3-dithietane carboxylic acid residue and to 7.beta.-isothiazolylthioacetamido-7.alpha.-methoxycephalosporins having antibacterial activity by themselves and, as the case may be, capable of being converted into the aforesaid 7.alpha.-methoxycephalosporin derivatives. The compounds of this invention exhibit excellent antibacterial activity and are particularly effective against gram negative bacteria.

Process for the preparation of

The invention relates to novel 7.alpha.-methoxycephalosporin derivatives having at the 7.beta.-position an amido group acylated by a 1,3-dithietane carboxylic acid residue and to 7.beta.-isothiazolylthioacetamido-7.alpha.-methoxycephalosporins having antibacterial activity by themselves and, as the case may be, capable of being converted into the aforesaid 7.alpha.-methoxycaphalosporin derivatives. The compounds of this invention exhibit excellent antibacterial activity and are particularly effective against gram negative bacteria.

7.alpha.-Methoxy-7.beta.-(1,3-dithietane-2-carboxamido)cephalosporanic

1,3-Dithietane-2-carboxylic acids and the preparation thereof

Novel 7.alpha.-methoxy-7.beta.-heterocyclic thioacetamido-3-heterocyclic thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acid derivatives and pharmaceutically acceptable salts thereof. These compounds show high antibiotic activities against various microorganisms including gram positive and negative bacteria.

7.alpha.-METHOXY-CEPHALOSPORANIC ACID DERIVATIVES

A novel cephalosporin derivative having at the 3-position of the cephem ring a heterocyclic thiomethyl group having a carboxy group or a sulfo group and at the 7-position of the cephem ring, an .alpha.-heterocyclic acylaminophenylacetamide group. The compounds of this invention have excellent antibacterial activity against Pseudomonas and Proteus strains of bacteria.

Cephalosporin derivatives having at the 3-position of the cephem ring a

Novel 7-(.alpha.-hydroxy-substituted pyridylcarboxamido-.alpha.-phenylacetamido)-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acid derivatives are disclosed. The compounds of this invention have high water solubility and show excellent antibacterial activities against various strains of Pseudomonas and Proteus.

Derivatives of 7-(.alpha.-hydroxy-substituted pyridyl carboxamido-.alpha. p

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Urawa, Japan

Tetsuya Maeda