Cephalosporin antibiotics
AssigneeMicrocide Pharmaceuticals, Inc.
InventorsIn-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
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Abstract
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounde of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
Claims9
A compound of the formula:
- ##STR13## wherein Pg.sub.1 is hydrogen or a first protecting group and wherein Pg.sub.2 is a second protecting group selected from the group consisting of triphenylmethy, (p-anisyl)diphenylmethyl, tetrahydropyranyl, 2-methoxy-2-propyl, t-butyldimethylsilyl, trimethylsilyloxyethyl, trimethylsilyloxyethoxycarbonyl, trichloroethyl, trichloroethoxycarbonyl, phenylsulfonylethyl, phenylsulfonylethoxycarbonyl, carboethoxyethoxycarbonyl, cyanoethoxycarbonyl, methoxymethyl, 2-methoxyethoxymethyl, 1-methoxy-1-methylethyl, p-methoxybenzyl, benzyl, 2,4-dimethoxybenzyl, 2,4,6-trimethoxybenzyl, p-methoxybenzyloxycarbonyl, benzyloxycarbonyl, 2,4-dimethoxybenzyloxycarbonyl, 2,4,6-trimethoxybenzyloxycarbonyl, p-nitrophenyl, o-nitrophenyl, p-nitrobenzoyl, and t-butyloxycarbonyl.
A compound of the formula:
- ##STR14## wherein Pg.sub.1 is hydrogen or a first protecting group selected from the group consisting of hydrogen, triphenylmethyl, (p-anisyl)diphenylmethyl, t-butyloxycarbonyl, N-trichloroethoxycarbonyl, formyl, acetyl, trimethylsilylethoxycarbonyl, benzyloxycarbonyl, benzyl, p-methoxybenzyl, 2,4-dimethoxybenzyl, 2,4,6-trimethoxybenzyl, pivaloyl, tetrahydropyranyl, t-butyl, methoxymethyl, p-toluenesulfonyl, benzoyl, trifluoroacetyl, benzenesulfenyl, methanesulfonyl, benzenesulfonylethyl, cyanoethyl, carboethoxyethyl, and 2-methoxy-2-propyl, and wherein Pg.sub.2 is a second protecting group.
Dependencies are inferred from the claim text.