[EN] BI-PYRROLIDINYLVINL (CARBA) CEPHALOSPORINS<br/>[FR] BI-PYRROLIDINYLVINYL (CARBA) CEPHALOSPORINES
申请人:HOFFMANN LA ROCHE
公开号:WO2000032605A1
公开(公告)日:2000-06-08
The present invention relates to cephalosporin derivatives of general formula (I), wherein R is R4 -Ys-(CR5R6)m- or (formula a) R1, R2 are each independently hydrogen or lower alkyl; R3 is hydrogen, hydroxy-lower alkyl or carbamoylmethyl; Z is phenylene, heterocyclylen or naphthylene; R4 is halogen, phenyl, benzyl, naphthyl or heterocyclyl, the phenyl, benzyl, naphthyl or heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, lower alkoxy, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkoxycarbonyl or carbamoyl; Q is S or CH¿2?; Y is S, O, NH or CH2; M is 0 or 1; s is 0 or 1; R?5, R6¿ are each independently hydrogen or lower alkyl; X is CR8 or N; R7 is hydrogen, lower alkyl, lower cycloalkyl, formyl, acetyl or pivaloyl; R8 is hydrogen or halogen; and 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.