3,7-disubstituted-3-cephem-4-carboxylic acid compounds and...

C - Chemistry – Metallurgy – 07 – D

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C07D 501/20 (2006.01) A61K 31/545 (2006.01) C07D 277/20 (2006.01) C07D 277/34 (2006.01) C07D 277/40 (2006.01) C07D 277/46 (2006.01) C07D 277/48 (2006.01) C07D 277/52 (2006.01)

Patent

CA 1218054

ABSTRACT OF THE DISCLOSURE New 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and their process of preparation are provided of formula (I) Image (I) and tautomers thereof, wherein R1 is amino, lower alkylamino, a protected amino, a protected lower alkylamino, hydroxy or lower alkoxy, R2 is hydrogen, acyloxy, pyridinium or a hetero- cyclic-thio group which may have suitable substituent(s), R3 is carboxy or its derivative, A is carbonyl, hydroxy(lower) alkylene or a protected hydroxy(lower)alkylene and R4 is hydro- gen or halogen, or R2 and R3 are linked together to represent a group of the formula: -COO-, wherein R3 is -COO- when R2 is pyridinium, provided that R2 is not acetoxy or 1-methyl-1H-te- trazol-5-ylthio when the group of the formula: Image is 2-hydroxy-2-(2-amino-1,3-thiazol-4-yl)acetyl or 2-hydroxy- 2-[2-(2,2,2-trichloroethoxy)carbonylamino-1,3-thiazol-4-yl] acetyl, as well as pharmaceutically acceptable salts, the new compounds have an antimicrobial activity and are active against a number of pathogenic microorganisms.

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