C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/104.1
C07D 501/36 (2006.01) C07C 59/21 (2006.01) C07D 237/24 (2006.01) C07D 487/04 (2006.01)
Patent
CA 1148939
ABSTRACT OF THE DISCLOSURE The invention relates to heterocyclyl derivatives of oxyimino- substituted cephalosporins of formula Image I wherein R represents an amino, aminocarbonyl or carboxy group; R1 represents a hydrogen atom or an amino-protecting group chosen from formyl, chloroacetyl, dichloroacetyl, tert-butoxycarbonyl, p-nitrobenzyloxycarbonyl and trityl; and R2 represents a hydrogen atom, a hydroxy-protecting group chosen from formyl, acetyl, chloroacetyl, dichloroacetyl, trifluoroacetyl, tetrahydrofuranyl, trityl, trimethylsilyl and dimethyl-tert-butyl-silyl or a branched or straight chain C1 - C4 alkyl group. The compounds display high antibacterial activity in animals and humans not only against Gram-positive and Gram-negative bacteria normally susceptible to cephalosporins such as staphylococci, streptococci, diplococci, Klebisiella, Escherichia coli, Proteus mirabilis, Salmonella, Shigella, Haemophilus and Neisseria, but also against the strong beta-lactamase producer Gram-negative micro-organisms, such as, for example, Klebsiella aerogenes 1082 E, Escherichia coli Tem, Enterobacter cloacae P 99, indole- positive Proteus and the like, as well as against Pseudomonas aeruginosa strains, which are normally resistant to most cephalosporins.
351677
Casabuona Ferruccio
Grasso Silvio
Nannini Giuliano
Perrone Ettore
Farmitalia Carlo Erba S.p.a.
Fetherstonhaugh & Co.
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