摘要:
Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making betalactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.
摘要:
Cephalosporin compounds represented by the general formula ##STR1## in which R.sup.1 is a hydrogen atom or a protective group for the amino group,R.sup.2 is a hydrogen atom or a protective group for the hydroxyl group,R.sup.3 is a hydrogen atom, a salt-forming cation or a protective group for the carboxyl group, andR.sup.4 is a hydrogen atom, a halogen atom or a lower alkyl group,and their pharmacologically acceptable salts, process for their production and use of the same compounds as medicaments, particularly as antibiotic agents.
摘要:
Disclosed is a novel cephem compound which is either one of a cis- or trans-isomer or a mixture of the cis-and trans-isomers, represented by the following general formula (I) and a pharmacologically acceptable salt thereof: ##STR1## wherein all of the substituents are as defined hereinbefore. Also disclosed are a process for producing the above compound and its use as an anti-bacterial agent comprising the same.
摘要:
Disclosed 2-(syn)-hydroxyimino-acetamide derivatives of the formula: ##STR1## wherein Y is hydrogen, hydroxyl, an acyloxy, carbamoyloxy, a quaternary ammonium or a nitrogen-containing heterocyclic ring-substituted thio group; or pharmaceutically acceptable salts or esters thereof are useful as antibacterial agents. Also disclosed are processes for producing them.
摘要:
This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, or lower acyl, R.sup.3 is hydrogen, or lower alkanoyloxy, andR.sup.4 is hydrogen, 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl, 1-(ethoxycarbonyloxy)ethyl,1-(pivaloyloxy)ethyl, 1-(cyclohexylacetoxy)ethyl, or 1-(cyclohexyloxycarbonyloxy) ethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art. The acids (R.sup.4 is hydrogen) are useful as intermediates for making the esters.
摘要:
This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl or acyl, R.sup.3 is hydrogen, lower alkyl, lower alkoxy, lower alkanoyloxy, andR.sup.4 is hydrogen, pivaloyloxymethyl, acetoxymethyl, 1-acetoxyethyl, 5-methyl-2-oxo-1, 3-dioxolen-4-ylmethyl or 4-glycyloxybenzoyloxymethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art.
摘要:
The invention relates to novel halovinyl cephem derivatives of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is a group of the formula:R.sup.4 --A--CONH--in which R.sup.4 is cyano(lower)alkenylthio or a group of the formula: ##STR2## in which R.sup.6 is hydrogen, amino or a protected amino group, andA is carbonyl, lower alkylene, hydroxy(lower)alkylene or a group of the formula: ##STR3## in which R.sup.5 is hydrogen, carboxy(lower)alkyl or protected carboxy(lower)alkyl;R.sup.2 is carboxy or a protected carboxy group; andX is halogen, and pharmaceutically acceptable salts thereof.
摘要:
A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is acetoxy or (1-methyl-1H-tetrazol-5-yl)thio, andR.sup.3 is carboxy; orR.sup.2 is a group of the formula: ##STR2## R.sup.3 is --COO.sup.- and Y is hydrogen, hydroxymethyl or carbamoyl; andn is an integer of 2 or 3,or a pharmaceutically acceptable salt thereof and processes for their preparation are disclosed. Said cephalosporin compound is useful as an antimicrobial agent.