Hoffmann-la Roche Inc.

Frederick M Konzelmann

Dennis D Keith

Harry A Albrecht

Yi Heng Chen

Manfred Weigele

Kin-Chun Thomas Luk

Jin-Jun Liu

Apostolos Dermatakis

Pamela Loreen Rossman

Naphthostyrils

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

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

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West Paterson, NJ, United States of America

Frederick M Konzelmann