68672-65-1Relevant articles and documents
Cephalosporin compounds
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, (2008/06/13)
The present invention relates to new cephalosporin compounds of the formula(I), pharmaceutically acceptable non-toxic salts thereof, and physiologically hydrolyzable esters and solvates thereof, which have potent and broad antibacterial activities STR1 wherein R1 is a C1?4 alkyl, C3?4 alkenyl, C3?4 alkynyl group, or --C(Ra)(Rb)CO2 H1 wherein Ra and Rb are the same or different, and each is a hydrogen atom or a C1?4 alkyl group, or Ra and Rb form a C3?7 cycloalkyl group with the carbon atom to which they are linked; R2 is a C1?4 alkyl, C3?4 alkenyl or C3?4 cycloalkyl group, a substituted or unsubstituted amino group, or a substituted or unsubstituted phenyl group; R3 is hydrogen or a C1?4 alkyl group; and Q is N or CH. The invention further relates to a process for preparing said compounds, and to pharamaceutical compositions containing said compounds.
(6R,7R)-7-[(Z)-2-(2-Aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4-carboxylate and salts thereof
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, (2008/06/13)
Cephalosporin antibiotics of the general formula STR1 (wherein Ra and Rb, which may be the same or different, each represent a C1-4 alkyl group or Ra and Rb together with the carbon atom to which they are attached form a C3-7 cycloalkylidene group; and R4 represents hydrogen or a 3- or 4-carbamoyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms. A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimono) acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4 carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of such antibiotics.
Cephalosporanic acid derivatives
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, (2008/06/13)
Novel syn isomers of 7-amino-thiazolyl-acetamido-3-acetoxymethyl-cephalosporanic acid derivatives of the formula STR1 wherein R1 is selected from the group consisting of --CN, --CONH2 and --COOR1 ', R1 ' is selected from the group consisting of alkyl of 1 to 3 carbon atoms, hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, R' and R" are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms with the STR2 group in the syn position with the proviso that when R1 is --COOR1 ' and R1 ' is hydrogen, A is hydrogen and when R1 is --COOR1 ' and R1 ' is an alkali metal, alkaline earth metal, magnesium, ammonium or an organic amine, A is an alkali metal, alkaline earth metal, magnesium ammonium or an organic amine having antibiotic properties and novel intermediates and processes.