CEPHALOSPORIN DERIVATIVES,THEIR MANUFACTURE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Acyl derivatives of the general formula in which A signifies a group of the general formulae -NHCO-, -NHCONHCO-, -NHCOCH=CH-, wherein R<6> represents hydrogen or lower alkyl; R<1> and R<2> in each case signify hydrogen or a protecting group, X signifies hydrogen, halogen, lower alkoxy. nitro or an additional group -OR<2>, n signifies the number 1 or 2, R<4> and R<5> both signify hydrogen or together signify an additional bond and Z signifies a direct bond or carbonyl (where R<4> and R<5> both represent hydrogen) or a group of the formula -O-B- (where R<4> and R<5> together represent an additional bond) in which B signifies straight-chain, branched or cyclic lower alkylene; and wherein further R<3> signifies a substituted bicyclic group of the general formulae in which R<7> and R<8> each individually represent hydrogen, lower alkyl or trifluoromethyl or (in formulae (a), (b), (e) and (f)) together represent alkylene with 3 or 4 carbon atoms and R', R'' and R''' each individually represent hydrogen, lower alkyl or lower cycloalkyl; whereby compounds of formula I in which R<4> and R<5> together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates, as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts. The compounds have antibiotic activity.