Smithkline Corporation

Smithkline Beecham Corporation

David A Berges

John J Taggart

Randall K Johnson

George L Dunn

Robert Philip Hertzberg

William D Kingsbury

The present invention provides water soluble camptothecin analogs of Formula I: ##STR1## which are particularly useful as antineoplastic agents; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.

Water soluble camptothecin analogs

The present invention provides a method of treating viral infections by using antiviral substituted indolizino�1,2-b!quinolinone compounds, antiviral substituted indolizino�1,2-b!quinolinone compounds, and pharmaceutical compositions thereof.

Substituted indolizino�1,2-b!quinolinones

The present invention provides a water soluble camptothecin analog of Formula I: ##STR1## which is particularly useful as an antineoplastic agent; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.

Novel cephalosporins with improved antibacterial and pharmacokinetic properties are disclosed. These compounds have a 2-alkoxyimino-2-(2-amino-4-thiazolyl)-acetamido group at position 7 and a sulfaminoalkyltetrazolythio group at position 3.

7-[2-Alkoxyimino-2-(amino-thiazole)acetami

The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.

7-Acyl-3-(substituted tetrazolyl thiomethyl)cephalosporins

7-Acylamino-3-(substituted tetrazolyl thiomethyl) cephalosporins

The compounds of this invention are phosphonoalkyl and esterified phosphonoalkyl substituted tetrazole thiols useful for preparing antibacterially active 7-acylamino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted tetrazolylthiomethyl)cephalosporins.

Phosphonoalkyl and esterified phosphonoalkyl substituted tetrazole thiols

Novel cephalosporins having various acyl substituents at the 7-position and a carboxymethylaminoethyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.

7-Acylamino-3-[1-[2-(carboxymethylamino)ethyl]tetrazol-5-ylthio

The compounds of this invention are 7-amino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted tetrazolylthiomethyl)cephalosporins useful as intermediates for preparing antibacterially active 7-acylamino cephalosporins.

7-Amino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted

The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.

Sulfaminoalkyl substituted tetrazole thiol intermediates for preparing

Novel cephalosporins having various acyl substituents at the 7-position and a sulfamidoethyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.

1-(2-Sulfamidoethyl)-1,4-dihydro-5H-tetrazole-5-thione

Novel cephalosporins having various acyl substituents at the 7-position and a carboxymethylthio substituted triazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.

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Wayne, PA, United States of America

David A Berges