C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 501/24 (2006.01) A61K 31/545 (2006.01) A61K 31/695 (2006.01) C07D 501/00 (2006.01) C07D 501/18 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2184971
The present invention relates to cephalosporin derivatives of the general formula I Image wherein R1 is a group selected from 2-, 3- and 4-hydroxyphenyl, 2- and 3- methoxyphenyl, 4-carboxyphenyl, 4-carbamoylphenyl, 3-trifluoro- methylphenyl, 2- and 3-fluorophenyl, 3-nitrophenyl, 3-fluoro-4- hyroxyphenyl, 2-fluoro-4-hydroxyphenyl, 3-fluoro-2-hydroxy- phenyl, 3-, 4-dihydroxyhenyl, benzyl, -CHR-phenyl, 3-hydroxy- benzyl, 4-aminobenzyl, 2-, 3- and 4-fluorobenzyl, 2-, 3- and 4- methoxybenzyl, 4-nitrobenzyl, 4-carboxybenzyl, 4-trifluoromethyl- benzyl, 1-naphthyl and 2-naphthyl, all hydroxy, amino, carboxy and carbamoyl substituents optionally being substituted, or is pyridinyl mono-substituted with halogen, pyrimidyl, pyrazinyl di-substituted with lower alkyl, pyridazinyl mono-substituted with halogen, piperidinyl in which the amino group may be substituted by an acyl group, thiadiazolyl, oxo-tetrahydrofuranyl, thiophenyl mono- substituted with lower alkoxycarbonyl or carbamoyl, tetrazolyl- lower alkyl, tetrahydrofuranyl-lower alkyl, thiophenyl-lower alkyl or benzimidazolyl-lower alkyl; and R is carboxy or esterified carboxy; readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts, as well as the their use and the process for manufacturing such compounds.
Hebeisen Paul
Heinze-Krauss Ingrid
Richter Hans
Runtz Valeri
Stalder Henri
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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