Vinyl-pyrrolidinone cephalosporins with basic substituents

Details Vinyl-pyrrolidinone cephalosporins with basic substituents Vinyl-pyrrolidinone cephalosporins with basic substituents

C - Chemistry, Metallurgy

07

D

C07D 501/56 (2006.01) A61K 31/546 (2006.01) A61P 31/04 (2006.01) C07D 417/12 (2006.01) C07D 501/06 (2006.01)

Patent

CA 2224438

The present invention relates to cephalosporin derivatives of the general formula (see formula I) wherein X is CH or N; R1 is hydrogen or cyclopentyl; R2 is a group of formula (see formula II) R3 is hydrogen, an alkalimetal ion or a tertiary ammonium group; R4 is hydrogen, an amino protecting group, pyrrolidin-2- ylmethyl, azetidin-3-ylmethyl, iminomethyl, 1- carbamimidoyl; R5 is hydrogen, dialkylcarbamoyl, .omega.-hydroxyalkyl, .omega.- aminoalkyl, pyridinium-1-ylmethyl, 1-hydroxy-3- aminomethyl-propyl or (hydroxy)-(pyrrolidin-2- yl)methyl; R6 is hydrogen, trifluoromethyl or hydroxy; and R7 is alkyl, .omega.-hydroxy-alkyl, cycloalkyl, 3-pyrrolidinyl, 3- azetidinyl, iminomethyl or 1-carbamimidoyl; as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts; the invention is further concerned with the manufacture of compounds of formula I; with their use as pharmaceutically active substances, particularly for the treatment and prophylaxis of infectious diseases, and with pharmaceutical preparations containing a compound of formula I for the treatment and prophylaxis of infectious diseases.

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