Erythromycin derivatives

Details Erythromycin derivatives Erythromycin derivatives

1991-05-03

1993-06-08

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 72, 536 74, A61K 3170, C07H 1708

Patent

active

052179605

ABSTRACT:
Antibacterial compounds are disclosed having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is --NR.sup.4 R.sup.6, where R.sup.4 and R.sup.6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R.sup.4 and R.sup.6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R.sup.2 is selected from the group consisting of hydrogen, --OH and, when R.sup.3 is methylene, oxygen so as to form an epoxide; and R.sup.3 is selected from the group consisting of --CH.sub.2 OH, --NR.sup.4 R.sup.6, --(CH.sub.2).sub.n NR.sup.4 R.sup.6 and, when R.sup.2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R.sup.4 and R.sup.6 are as previously defined, with the proviso that when R.sup.2 is --OH, R.sup.3 may not be --NR.sup.4 R.sup.6 ; or R.sup.2 and R.sup.3 together are.dbd.CH.sub.2. Also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.

REFERENCES:
patent: 3652537 (1972-03-01), Massey et al.
patent: 4826820 (1989-05-01), Brain
Mauske et al, J. Org. Che., 48:5138 (1983).

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