公开(公告)号：EP0946558A1

公开(公告)日：1999-10-06

申请号：EP97947251.0

申请日：1997-12-18

申请人： Lek Tovarna Farmacevtskih in Kemicnih Izdelkov, D.D.

发明人： COPAR, Anton ,  SOLMAJER, Tomaz ,  ANZIC, Borut ,  KUZMAN, Tadeja ,  MESAR, Tomaz ,  KOCJAN, Darko

IPC分类号： A61K31 ,  A61P31 ,  C07D477 ,  C07D495

CPC分类号： C07D477/00 ,  C07D495/14

摘要： Disclosed are novel ethylidene derivatives of tricyclic carbapenems of formula (I), wherein the ring marked C and X have the meaning as in the description, in the form of pure diastereoisomers and in the form of pure geometric isomers. Novel ethylidene derivatives of tricyclic carbapenems of formula (I) are used as inhibitors of the action of the enzyme β-lactamase and/or as antibiotics in human and veterinary medicine. Also disclosed are pharmaceutical formulations for the treatment of bacterial infections of human and animal organisms comprising as an active ingredient a therapeutically effective amount of an ethylidene derivative of tricyclic carbapenems of formula (I) in the form of an acid, a pharmaceutically acceptable salt or ester thereof and optionally in a combination with a β-lactam antibiotic, and usual pharmaceutically acceptable carriers and auxiliary substances. Also disclosed is a process for the preparation of novel ethylidene derivatives of tricyclic carbapenems of formula (I).