Cephem compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 501/24 (2006.01) A61K 31/545 (2006.01) C07D 501/00 (2006.01) C07D 501/18 (2006.01) C07D 519/06 (2006.01)

Patent

CA 2276097

Cephem compounds of general formula (I), wherein formula (a) represents benzene, pyridine, pyrazine or a five-membered aromatic heterocycle (containing oxygen or sulfur as the ring atom), provided when is a five- membered aromatic heterocycle, R4 is absent; X and Y each represents hydrogen, CXY represents C=N-OR5 (wherein R5 represents hydrogen, halo-C1-6 alkyl or C3- 7 cycloalkyl); R1 represents phenyl, furyl, thienyl, thiazolyl (which may be substituted by amino), tetrazolyl or thiadiazolyl; and R2, R3 and R4 each represents hydrogen, halogen, hydroxyl, nitro, C1-6 alkoxyl, trifluoromethyl, isothiuronium-C1-6 alkyl, amino-C1-6 alkyl, halo-C1-6 alkyl, morpholino, piperidino or piperazinyl.

Composés du céphème, de formule générale (I), dans laquelle (a) représente benzène, pyridine, pyrazine ou un hétérocycle aromatique à cinq éléments (l'atome du noyau étant l'oxygène ou le soufre), à condition que quand (a) est un hétérocycle aromatique à cinq éléments, R¿4? soit absent; X et Y représentent hydrogène; CXY représente C=N-OR¿5? (où R¿5? représente hydrogène, haloalkyle C¿1?-C¿6? ou cycloalkyle C¿3?-C¿7?); R¿1? représente phényle, furyle, thiényle, thiazolyle (qui peut être substitué par amino), tétrazolyle ou thiadiazolyle; et R¿2?, R¿3? et R¿4? représentent chacun hydrogène, halogène, hydroxyle, nitro, alcoxy C¿1?-C¿6?, trifluorométhyle, isothiuroniumalkyle C¿1?-C¿6?, aminoalkyle C¿1?-C¿6?, alkyle, haloalkyle C¿1?-C¿6?, morpholino, pipéridino ou pipérazinyle.

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