Cephem compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 501/59 (2006.01) A61K 31/545 (2006.01) A61K 31/546 (2006.01) C07D 501/00 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2335768

Cephem derivatives represented by general formula (I) and pharmaceutically acceptable salts thereof wherein (a) is a benzene ring, a pyridine ring, a pyrazine ring or a five-membered aromatic heterocycle (containing one oxygen or sulfur atom as the cycle-constituting atom); X and Y are each hydrogen, or alternatively CXY is C=N-OH; R1 is phenyl, thienyl or thiazolyl (which may be substituted with amino or halogeno); and R2, R3 and R4 are each hydrogen, halogeno, hydroxy C1-C6 alkyl, isothiuronium C1-C6 alkyl, amino C1-C6 alkyl or amino C1-C6 alkyl thio methyl, with the proviso that when (a) is a five- membered aromatic hetercycle, R4 is absent.

La présente invention se rapporte à des dérivés céphem représentés par la formule générale (I), ainsi qu'a leurs sels acceptables sur le plan pharmaceutique, formule dans laquelle (a) représente un cycle benzène, un cycle pyridine, un cycle pyrazine ou un hétérocycle aromatique à cinq chaînons (renfermant un atome d'oxygène ou de soufre tel que l'atome constituant le cycle); X et Y représentent chacun hydrogène, ou encore CXY représente C=N-OH; R¿1? représente phényle, thiényle ou thiazolyle (pouvant être substitué avec amino ou halogéno); et R¿2?, R¿3? et R¿4? représentent chacun hydrogène, halogène, hydroxy C¿1?-C¿2? alkyle, isothiuronium C¿1?-C¿6? aklyle thio méthyle, à condition que lorsque (a) constitue un hétérocycle aromtique à cinq chaînons, R¿4? est absent.

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