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US 4,359,472 AGranted
Bis-hydroxymethyl carbonate bridged antibacterial agents
AssigneePfizer Inc.
InventorErnest S. Hamanaka
Life of this patent
Estimating the term…
Abstract
Antibacterial agents in which a penicillin and a beta-lactamase inhibitor are linked by means of a bis-hydroxymethyl carbonate bridge are of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 is hydrogen, hydroxy, certain acyloxy or certain alkoxycarbonyloxy groups, a method for their use, pharmaceutical compositions thereof, and intermediates useful in their production.
Claims19
A compound of the formula:
- ##STR25## or a pharmaceutically acceptable acid addition salt thereof wherein:
- R.sup.1 is hydrogen, hydroxy, formyloxy, alkanoyloxy having from two to seven carbon atoms, alkoxycarbonyloxy having from two to seven carbon atoms or R.sup.2 C.sub.6 H.sub.4 COO where R.sup.2 is hydrogen, alkyl having from one to four carbon atoms, alkoxy having from one to four carbon atoms, F, Cl, Br, I or CN.
A compound of the formula:
- ##STR26## wherein R.sup.1 is hydrogen, hydroxy, formyloxy, alkanoyloxy having from two to seven carbon atoms, alkoxycarbonyloxy having from two to seven carbon atoms or R.sup.2 C.sub.6 H.sub.4 COO where R.sup.2 is hydrogen, alkyl having from one to four carbon atoms, alkoxy having from one to four carbon atoms, F, Cl, Br, I or CN;
- and Q is azido, benzyloxycarbonylamino, 4-nitrobenzyloxycarbonylamino or 1-methyl-2-methoxycarbonylvinylamino.
A compound of the formula:
- ##STR27## wherein X is Cl, Br or I.
A compound of the formula:
- ##STR28## wherein R.sup.1 is hydrogen, hydroxy, formyloxy, alkanoyloxy having from two to seven carbon atoms, alkoxycarbonyloxy having from two to seven carbon atoms or R.sup.2 C.sub.6 H.sub.4 COO where R.sup.2 is hydrogen, alkyl having from one to four carbon atoms, alkoxy having from one to four carbon atoms, F, Cl, Br, I or CN;
- Q is azido, benzyloxycarbonylamino, 4-nitrobenzyloxycarbonylamino or 1-methyl-2-methoxycarbonylvinylamino;
- and
- X is Cl, Br or I.
1 more element
Dependencies are inferred from the claim text.