Antibiotics
AssigneeBeecham Group Limited
InventorsRoger J. Ponsford, Thomas T. Howarth
Life of this patent
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Abstract
The compounds of the formula (II): ##STR1## and salts and esters theereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.
Claims65
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises a synergistically effective amount of an in vivo hydrolyzable ester of a compound of the formula ##STR32## or a pharmaceutically acceptable salt thereof wherein R.sub.4 is hydrogen, R.sub.5 is hydrogen or alkyl of 1 to 4 carbon atoms and R.sub.6 is phenyl unsubstituted or substituted by a substituent selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms and hydroxyl, ##STR33## or a pharmaceutically acceptable salt thereof wherein each of R.sub.8 to R.sub.11 is independently hydrogen or methyl and R.sub.12 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl unsubstituted or substituted by a substituent selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms and hydroxyl, or ##STR34## or a pharmaceutically acceptable salt thereof wherein each of R.sub.8 to R.sub.11 is independently hydrogen or methyl and R.sub.12 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl unsubstituted or substituted by a substituent selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms, alkoxyl of 1 to 4 carbon atoms and hydroxyl, an antibacterially effective amount of amoxycillin or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier.
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises a synergistically effective amount of benzyl diallylaminodeoxyclavulanate and an antibacterially effective amount of amoxycillin or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier.
A method of treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof a synergistically effective amount of an in vivo hydrolyzable ester of a compound of the formula ##STR40## or a pharmaceutically acceptable salt thereof wherein R.sub.4 is hydrogen, R.sub.5 is hydrogen or alkyl of 1 to 4 carbon atoms and R.sub.6 is phenyl unsubstituted or substituted by a substituent selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms and hydroxyl, ##STR41## or a pharmaceutically acceptable salt thereof wherein each of R.sub.8 to R.sub.11 is independently hydrogen or methyl and R.sub.12 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl unsubstituted or substituted by a substituent selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms and hydroxyl, or ##STR42## or a pharmaceutically acceptable salt thereof wherein each of R.sub.8 to R.sub.11 is independently hydrogen or methyl and R.sub.12 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl unsubstituted or substituted by a substituent selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms, alkoxyl of 1 to 4 carbon atoms and hydroxyl, an antibacterially effective amount of amoxycillin or a pharmaceutically acceptable salt thereof.
A method of treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof a synergistically effective amount of benzyl diallylaminodeoxyclavulanate, and an antibacterially effective amount of amoxycillin or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.