Cephalosporin antibiotics

Details Cephalosporin antibiotics Cephalosporin antibiotics

C - Chemistry, Metallurgy

07

D

167/187, 260/104

C07D 501/24 (2006.01) A61K 31/545 (2006.01) C07D 277/20 (2006.01) C07D 277/38 (2006.01)

Patent

CA 1282406

ABSTRACT "CEPHALOSPORIN ANTIBIOTICS" Compounds of general formula (I) (I) Image (where R1 is a carboxyl group, a group COO? or a blocked carboxyl group; R2 is an amino or protected amino group; and R is hydrogen or a group of the formula CH2X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR3, where R3 is hydrogen, a C1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR4, where R4 is a C1-4 alkyl group optionally substituted by halogen or a C1-4 alkoxy group; or a pyridinium, 3-carbamoyl- pyridinium or 4-carbamoyl-pyridinium group; b is -S- or -SO- (.alpha.- or .beta.-); and the dotted line bridqing the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R 1 is other than COO?)are disclosed. Process for their preparation and pharmaceutical compositions containinG them are also dis- closed. These compounds exhibit broad spectrum antibiotic activity.

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