6- and 1-Substituted-1-carbadethiapen-2-em-3-carboxylic acid
AssigneeMerck & Co., Inc.
InventorsBurton G. Christensen, David H. Shih
Life of this patent
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Abstract
Disclosed are 6- and 1-substituted-1-carbadethiapen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotics effect is indicated.
Claims4
A compound having the structure:
- ##STR147## and the pharmaceutically acceptable salts thereof;
- wherein R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen, and substituted and unsubstituted:
- alkyl having 1-6 carbon atoms, phenyl, phenylalkyl wherein the alkyl moiety has 1-6 carbon atoms, cycloalkyl and cycloalkylalkyl having 3 to 6 ring carbon atoms and 1-6 carbon atoms in the alkyl moiety;
- wherein the substituent or substituents on R.sup.1, R.sup.2 and R.sup.3 are selected from chloro, bromo, fluoro, hydroxyl, amino, mono-, di-, and trialkylamino (each alkyl having 1-6 carbon atoms), alkoxyl having 1-6 carbon atoms, cyano and carboxyl;
- wherein R.sup.3 is not hydrogen and R.sup.1 and R.sup.2 are not both hydrogen at the same time.
Dependencies are inferred from the claim text.