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US 5,288,709 AGranted
Erythromycin derivatives
AssigneeAbbott Laboratories
InventorsLeslie A. Freiberg, Larry L. Klein, Clinton M. Yeung, Carla M. Edwards, David J. Bacino
Life of this patent
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Abstract
New 9-deoxo-9,12-epoxy erythromycin derivatives are disclosed which have improved antibacterial properties. Compositions comprising the erythromycin derivatives and methods of treating mammalian patients with the erythromycin derivatives are also disclosed.
Claims5
A compound having the structure:
- ##STR4## wherein R.sub.1 is an oxo, oxime, hydroxy or amino group at the 11 position;
- R.sub.2 is hydrogen, an oxygen-containing group selected from the group consisting of hydroxy, oxime, C.sub.1 --to --C.sub.8 alkanoyloxy, C.sub.1 --to --C.sub.8 aminoalkoxy, aminocarbonyloxy and carbonate, or a nitrogen-containing group selected from the group consisting of amino, oxime, imine and carbamyl at the 4" position;
- and
- R.sub.3 is hydrogen or methyl;
- or a pharmaceutically acceptable salt thereof.
2 more elements
A compound selected from the group consisting of:
- (9S,11S)-9-Deoxo-12-deoxy-9,12-epoxyerythromycin A;
- (9S)-9-Deoxo-11,12-dideoxy 9,12-epoxy-11-oxoerythromycin A;
- (4"R,9S)-9-Deoxo-4",11,12-trideoxy -9,12-epoxy-11-oxo-4"-[[(phenylmethoxy)carbonyl]amino]erythromycin A;
- (4"R,9S)-4"-Amino-9-deoxo-4", 11,12-trideoxy-9,12-epoxy-11-oxoerythromycin A;
- (4"R,9S)-9-Deoxo-4",11,12-trideoxy-9,12-epoxy-4"-[[(dimethyamino)methylene] amino]-11-oxoerythromycin A;
- (4"R,9S)-4"-Acetylamino-9-deoxo-4",11,12-trideoxy-9,12-epoxy-11-oxoerythrom ycin A;
- (4"R,9S)-9-Deoxo-4",11,12-trideoxy-9,12-epoxy-4"-[(methylsulphonyl)amino]-1 1-oxoerythromycin A;
- (4"R,9S)-9-Deoxo-4",11,12-trideoxy-9,12-epoxy-11-oxo-4"-[(phenylmethyl)amin o]erythromycin A;
- (4"R,9S,11S)-4"-Amino-9-deoxo-4",12-dideoxy-9,12-epoxyerythromycin A;
- (4"S,9S)-4"-Amino-9-deoxo-4",11,12-trideoxy-9,12-epoxy-11-oxoerythromycin A;
- (4"S,9S,11S)-4"-Amino-9-deoxo-4",12-dideoxy-9,12-epoxyerythromycin A;
- (4"S,9S)-9-Deoxo-4",11,12-trideoxy-9,12-epoxy-4"-(methylsulfonyl)amino-11-o xoerythromycin A;
- (9S,11S)-4"-O-aminocarbonyl-9-deoxo-12-deoxy-9,12-epoxyerythromycin A;
- (9S)-9-Deoxo-11,12-dideoxy-9,12-epoxy-11-hydroxyiminoerythromycin;
- (9S,11S)-11-Amino-9-deoxo-11,12-deoxy-9,12-epoxyerythromycin A;
- (9S,11S)-11-Amino-9-deoxo-4",11,12-trideoxy-9,12-epoxyerythromycin A
- (4"R,9S,11S)-4",11-Diamino-9-deoxo-4",11,12-trideoxy-9,12-epoxyerythromycin A;
- (4"R,9S)-9-Deoxo-11,12-dideoxy-9,12-epoxy-11-oxoerythromycin A;
- (4"S,9S,11S)-4",11-Diamino-9-deoxo-4",11,12-trideoxy-9,12-epoxyerythromycin A;
- (9S,11S)-4"-O-Acetyl-9-deoxo-12-deoxy-9,12-epoxyerythromycin A;
- (9S)-4"-O-Aminocarbonyl-9-deoxo-11,12-dideoxy-9,12-epoxy-11-oxoerythromycin A;
- (4"S,9S)-4"-[(Aminocarbonyl)amino]-9-deoxo-4",11,12-trideoxy-9,12-epoxy-11- oxoerythromycin A;
- and pharmaceutically acceptable salts thereof.
20 more elements
A compound having the structure:
- ##STR5## wherein R.sub.2 is hydroxy, R.sub.3 is hydrogen and R.sub.1 is selected from the group consisting of oxo and hydroxy.
Dependencies are inferred from the claim text.