Hoffmann-La Roche Inc.

Harry A Albrecht

Dennis D Keith

Manfred Weigele

Frederick M Konzelmann

Ka-kong Chan

Chung-Chen Wei

Pamela Loreen Rossman

John T Plati

Rudolf L Then

Frederick M Konzelman

Roxana Yang

There are presented antibacterial cephalosporine having broad antimicrobial activity, having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group: R.sub.1 represents a substituted piperazinyl group of formula ##STR2## or a substituted pyrrolidinylamino group of formula ##STR3## or a substituted pyrrolidinylmethylamino group of formula ##STR4## where the piperazinyl or pyrrolidinyl group may be optionally substituted with one or more lower alkyl groups, and where Q represents a substituted quinolinyl or naphthyridinyl group: R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group: and m is 0, 1 or 2, but preferably 0; as well as the corresponding readily hydrolyzable esters. pharmaceutically acceptable salts and hydrates of these compounds.

Antibacterial cephalosporin compounds

There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group; R.sub.1 is a substituted piperazinium group of the formula ##STR2## in which Q represents a substituted quinolinyl or naphthyridinyl group and the piperazine nucleus may be optionally substituted with one or more lower alkyl groups; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group; and m is 0, 1 or 2, preferably 0; as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds.

There are presented anti-bacterial cephalosporins having broad antimicrobial activity of the formula ##STR1## wherein R.sub.1 is an antibiotically active quinolonyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, amino, lower alkylthio and amido; R.sub.3 is selected from the group consisting of hydrogen, and acyl group, and m is 0, 1 or 2 and the readily hydrolysable esters or salts of these compounds and hydrates of the compounds of formula I or of their esters or salts.

Anti-bacterial cephalosporin compounds

Compounds of the formula ##STR1## wherein A is ##STR2## in which R.sub.1 is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxy-carbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 and R.sub.4, are each hydrogen, lower alkyl, lower alkoxy, aryl, aryloxy or aralkyl, as well as the pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents for combatting infections in mammals.

Isothiazolyl beta-lactam antibacterial agents

Compounds of the formula ##STR1## wherein A is one of the following: ##STR2## in which R.sub.1, is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl and R.sub.4 and R.sub.4 ' are hydrogen, lower alkyl, lower alkoxy, acyl or aralkyl, as well as pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents.

.beta.-lactam antibacterial agents

A novel family of .beta.-lactam antibacterials, synthetic methods and intermediates useful in the production of such antibacterials, and the use of such compounds as antibacterials are disclosed. The novel compounds have the formula ##STR1## wherein, Z.sup.1 is a group --OR.sup.1, --NR.sup.3 R.sup.4, or --SR.sup.5 ;

1-(N-phosphinylcarbamoyl) .beta.-lactam antibacterial agents

N.sup.1 -(1,2-dihydro-2-oxo-4-pyrimidinyl)sulfanilamides, bearing a lower alkyl, cycloalkyl or cycloalkyl-lower alkyl substituent in the 1-position, prepared by reaction of the corresponding 1-substituted-1,2-dihydro-2-oxo-4-aminopyrimidine and N-acylated sulfanilyl chloride with subsequent hydrolysis, are described. The end products are useful as antibacterial agents.

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Towaco, NJ, United States of America

Harry A Albrecht