Shionogi Company Limited

Purdue Pharma L.p.

Glaxo Group Limited

Kenji Yamawaki

Toshiaki Aoki

Jun Sato

Masayuki Sano

Shinya Hisakawa

Hiroki Kusano

Katsuki Yokoo

Jiangchao Yao

Jianming Yu

Xiaoming Zhou

Yasuhiro Nishitani

Hideki Sugimoto

Yasushi Hasegawa

Neil David Pearson

Nobuyuki Tanaka

Israil Pendrak

Xiangmin Liao

Mikito Asai

Masatoshi Takeo

Yutaka Yokota

Yusuke Takeoka

Reema K Thalji

Reema Thalgi

The compounds of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.

2 substituted cephem compounds

The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R, R, R, Q, W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Benzimidazole-Type Piperidine Compound.

Substituted benzimidazole-type piperidine compounds and uses thereof

The invention relates to processes for the production of intermediates for preparing 2-alkyl cephem compounds useful as antimicrobial drugs. The invention provides a process which comprises oxidating a compound of the formula (I) or a salt thereof to give a compound of the formula (II) or a salt thereof wherein each symbol is as defined in the specification. 

Processes for production of intermediates for 2-alkyl cephem 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

The present disclosure describes Cephem compounds of the formula: wherein,

Cephalosporin 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

Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and a pharmaceutical composition comprising the same. The cephem compound has the formula (I): where W and U are as defined in the specification; Ris as defined in the specification; Rand Rare as defined in the specification, provided that Rand Rare not taken together to form an optionally substituted oxime group when Ris aminothiazole or aminothiadiazole optionally protected at the amino group; ring A is a benzene ring or a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms; Ris a hydrogen atom, &#x2014;OCHor &#x2014;NH&#x2014;CH(&#x2550;O); k is an integer from 0 to 2; Ris as defined in the specification; and D and E are as defined in accordance with a) or b) described in the specification.

Cephem derivative

Cephem compound having pseudo-catechol group

Growing community of inventors

Toyonaka, Japan

Kenji Yamawaki