To obtain the subject new derivatives comprising specific vinylpyrrolidinone cephalosporin derivatives and useful for treatment and prevention, etc., of diseases due to gram-positive bacteria, especially sensitive and resistant staphylococcus, Pneumococcus and enteric coccus.
The new vinylpyrrolidinone cephalosporin derivatives are represented by formula I [R1 is a halogen, a (substituted)lower alkyl, a (substituted)phenyl, a (substituted)benzyl, a (substituted)heterocyclic group, etc.; R2 is H, OH, a lower alkyl-Qr (Q is an alkylene, CO or SO2; (r) is 0 or 1), an aryl-Qr, etc.; R3 is OH, a lower alkoxy, OM (M is an alkali metal), etc.; R4 and R5 are each H, a lower alkyl or phenyl; X is S, O, NH or CH2; (n) is 0, 1 or 2; (m) and (s) are each 0 or 1] and useful as a medicine, etc., for treatment and prevention of infectious diseases. The compound is obtained by treating a compound having formula II (Rf is H or trimethylsilyl; Rg is H, benzhydryl, etc.) with a carboxylic acid of formula III (Y is OH or its reactive derivative).
HEINZE-KRAUSS INGRID
RICHTER HANS G F