Shionogi Company Limited

Glaxo Group Limited

Masayuki Sano

Kenji Yamawaki

Jun Sato

Toshiaki Aoki

Yasushi Hasegawa

Neil David Pearson

Yasuhiro Nishitani

Israil Pendrak

Xiangmin Liao

Hideki Sugimoto

Katsuki Yokoo

Shinya Hisakawa

Hiroki Kusano

The present invention relates to cephalosporin antibacterial compounds of Formula (I): or corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.

Antibacterial compounds

The present invention provides a novel compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria. Specifically, the present invention provides a compound of the formula (I): wherein each symbol is as defined in the specification, or an amino-protected compound when the amino group is present on the ring in the 7-side chain, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.

Cephem compound having catechol or pseudo-catechol structure

A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom. 

Cephem derivative having catechol group

This invention provides Cephem compounds having the formula: or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, a pharmaceutical composition thereof, and a method for treating a bacterial infectious disease with the compound, the ester, the protected compound, the salt, or the solvate thereof, wherein the symbols in the formula are defined in the specification. The compounds exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and/or Gram positive bacteria, preferably beta-lactamase producing Gram negative bacteria, more preferably, multi-drug resistant microbials, in particular, Class B type metallo-beta-lactamase producing Gram negative bacteria, and still preferably extended-spectrum beta-lactamase (ESBL) producing bacteria. The compounds most preferably do not exhibit cross-resistance against known Cephem drugs or Carbapenem drugs.

Cephem compound having catechol group

Cephem compound having pseudo-catechol group

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Toyonaka, Japan

Masayuki Sano