4-amino derivatives of 2-oxo-1-azetidinesulfonic acid salts
AssigneeE. R. Squibb & Sons, Inc.
InventorsUwe D. Treuner, Theodor Denzel, Hermann Breuer
Life of this patent
Estimating the term…
Abstract
.beta.-Lactams having a sulfonic acid salt substituent in the 1-position, an acylamino substituent in the 3-position and an --NR.sub.2 R.sub.3 substituent in the 4-position wherein R.sub.2 and R.sub.3 are the same or different and each is ##STR1## or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached are ##STR2## R.sub.4 is alkyl, aryl or arylalkyl; and R.sub.5 and R.sub.6 are the same or different and each is hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, carboxyl or a carboxyl salt; have antibacterial activity.
Claims10
A pharmaceutically acceptable salt, including inner salt, of a .beta.-lactam having the formula ##STR51## wherein R is hydrogen or methoxy;
- R.sub.1 is an acyl group derived from a carboxylic acid;
- R.sub.2 and R.sub.3 are the same or different and each is ##STR52## or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached are ##STR53## R.sub.4 is alkyl, aryl or arylalkyl;
- R.sub.5 and R.sub.6 are the same or different and each is hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, carboxyl or a pharmaceutically acceptable carboxyl salt;
- and wherein the terms "alkyl" and "alkoxy" refer to groups having 1 to 10 carbon atoms and the term "aryl" refers to phenyl and phenyl substituted with 1, 2 or 3 amino, halogen, hydroxyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms groups.
A .beta.-lactam having the structural formula ##STR58## wherein R.sub.2 and R.sub.3 are the same or different and each is ##STR59## or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached are ##STR60## R.sub.4 is alkyl, aryl, or arylalkyl;
- and R.sub.5 and R.sub.6 are the same or different and each is hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, carboxyl or a pharmaceutically acceptable carboxyl salt;
- wherein the terms "alkyl" and "alkoxy" refer to groups having 1 to 10 carbon atoms and the term "aryl" refers to phenyl and phenyl substituted with 1, 2 or 3 amino, halogen, hydroxyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms groups.
Dependencies are inferred from the claim text.