Vinylpyrrolidinon cephalosporin derivatives

Details Vinylpyrrolidinon cephalosporin derivatives Vinylpyrrolidinon cephalosporin derivatives

C - Chemistry, Metallurgy

07

D

C07D 501/24 (2006.01) A61K 31/545 (2006.01) A61K 31/55 (2006.01) A61K 31/675 (2006.01) A61K 31/695 (2006.01) C07D 501/00 (2006.01) C07F 7/10 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2220188

The present invention relates to cephalosporin derivatives of the general formula Image where R1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted phenyl, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkyl- carboxy, carbamoyl or lower alkylcarbamoyl; R4, R5 independently are hydrogen, lower alkyl or phenyl; X is S, O, NH or CH2; n is 0, 1 or 2; m is 0 or 1; s is 0 or 1; R2 is hydrogen, hydroxy, -CH2-CONHR6, lower alkyl-Q r, cycloalkyl-Q r, lower alkoxy, lower alkenyl, cycloalkenyl-Q r, lower alkynyl, aralkyl-Q r, aryl-Q r, aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Q r, the lower alkyl, cyclo- alkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring may be substituted with at least one group selected from carboxy, amino, nitro, cyano, -SO2NHR6, optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, -CONR6R7, -CH2CONR6R7, -N(R7)COOR8, R7CO-, R7OCO-, R7COO-, -C(R7R9)C02R8, -C(R7R9)CONR7R10, wherein R6 is hydrogen, lower alkyl, cycloalkyl or aryl; R7 and R9 are independently hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; and R10 is hydrogen, .omega.-hydroxy-alkyl, phenyl, naphthyl or heterocyclyl, the phenyl, naphthyl or heterocyclyl being unsubstituted or substituted with at least one of the groups of optionally protected hydroxy, halogen, optionally substituted lower alkyl or .omega.-hydroxyalkyl, optionally substituted lower alkoxy and/or cyano, or R7 and R10 form together group of Image formula Q is -CHR-, -CO- or -SO2-; r is 0 or 1; R is hydrogen or lower alkyl; and R3 is hydroxy, -O-, lower-alkoxy, or -OM and M represents an alkali metal; 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, as well as the preparation of such compounds, their use for the treatment of infectious diseases and pharmaceutical preparations containing such compounds.

Affiliated with

Also associated with

Rating

Vinylpyrrolidinon cephalosporin derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Vinylpyrrolidinon cephalosporin derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Vinylpyrrolidinon cephalosporin derivatives will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-2087408