4-thia-1-aza-bicyclo[4,2,0]oct-2-ene derivatives

Details 4-thia-1-aza-bicyclo[4,2,0]oct-2-ene derivatives 4-thia-1-aza-bicyclo[4,2,0]oct-2-ene derivatives

1992-03-20

1995-01-31

Rizzo, Nicholas S.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540221, 540222, 540225, 540214, C07D41712, A61K 3154

Patent

active

053858972

ABSTRACT:
A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R.sub.b --NH--, Ra is an organic radical, Ri and Rj are individually selected from the group consisting of hydrogen, aliphatic hydrocarbon, aromatic hydrocarbon and heterocycle or taken together with the nitrogen atom to which they are attached form an optionally substituted ring, Rb is selected from the group consisting of carbocyclic aryl and heterocyclic aryl, both optionally substituted, R.sub.1A is selected from the group consisting of ##STR3## R.sub.A ' and R.sub.B ' are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, Z.sub.A is selected from the group consisting of a simple bond, --O-- and optionally oxidize sulfur, R.sub.3A is selected from the group consisting of optionally substituted carbocyclic aryl and heterocyclic aryl, optionally substitute quaternary ammonium, acetyl, carbamoyl, alkoxycarbonyl, alkyl and haloalkyl of 1 to 4 carbon atoms, --CN and azido, R.sub.4 is selected from the group consisting of hydrogen and methoxy, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, magnesium, --NH.sub.4, an organic amine and esterified carboxy or --COOA is --COO.sup..crclbar., n.sub.2 is an integer from 0 to 2 and their non-toxic, pharmaceutical acceptable acid addition salts having excellent antibiotic activity.

REFERENCES:
patent: 4476124 (1984-10-01), Heymes et al.
patent: 4908359 (1990-03-01), Costerousse et al.

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