The present invention provides a novel compound which has a broad antibacterial spectrum and particularly exhibits a high antibacterial activity on β-lactamase-producing gram-negative bacteria. Specifically provided are: a compound represented by formula (I)
wherein the meaning of each symbol is as defined in the description, an amino-group-protected form of a type of the compound which has the amino group on a ring in a position-7 side chain, or a pharmaceutically acceptable salt of the compound or the amino-group-protected form; and a pharmaceutical composition containing the compound, the amino-group-protected form or the pharmaceutically acceptable salt.
A compound of the formula:
wherein, W is —CH2
−
etc.; U is —S
−
etc.;
R
1
is substituted or unsubstituted carbocyclyl etc.;
R
2A
and R
2B
is a) or b) described in the specification;
R
3
is a hydrogen atom etc.; R
11
is carboxylate anion (—COO
−
) etc.;
L is substituted or unsubstituted lower alkylene etc.,
E is a substituted or unsubstituted divalent group containing quaternary ammonium ion;
G is a single bond etc.;
D is —C(═O)—C(═O)—NR
6
— etc.;
R
10
1) to 3) described in 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.
The present invention relates to 2-substituted cephem compounds of Formula (I) having a quaternary ammonium group on the 3-side chain, preferably together with a cathechol group, or pharmaceutically acceptable salts thereof, which exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and/or Gram positive bacteria, corresponding pharmaceutical compositions, methods of making, treatment methods for bacterial infections or uses thereof.
NOVEL CEPHEM COMPOUND HAVING CATECHOL OR PSEUDO-CATECHOL STRUCTURE
申请人:Nishitani Yasuhiro
公开号:US20140088302A1
公开(公告)日:2014-03-27
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.
PROCESSES FOR PRODUCTION OF INTERMEDIATES FOR 2-ALKYL CEPHEM COMPOUNDS
申请人:SHIONOGI & CO., LTD.
公开号:US20150291619A1
公开(公告)日:2015-10-15
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.