Novel carbapenem compounds

Details Novel carbapenem compounds Novel carbapenem compounds

C - Chemistry, Metallurgy

07

D

C07D 477/24 (2006.01) A61K 31/407 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/5377 (2006.01) A61P 31/04 (2006.01) C07D 477/10 (2006.01) C07D 477/14 (2006.01)

Patent

CA 2465336

The present invention is directed to a compound or its pharmaceutically acceptable salt represented by the following formula, Image It is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and causes serious clinical problems, and Haemophilus influenzae which has acquired resistance against the existing .beta.-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as .beta.- lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae. The compounds of the present invention have excellent oral absorbability.

La présente invention concerne de nouveaux composés carbapenem représentés par la formule générale (1) suivante ou des sels de ceux-ci répondant aux normes pharmaceutiques:(1). Dans cette formule le cycle E représente un cycle de benzène ou un cycle thiophène, R1 représente alkyle, etc., A représente alkylène, etc., R0 représente hydrogène, carbamoyl, carboxyle, etc., R représente hydrogène, etc. et Y représente hydrogène, alkyle, etc.. Ces composés sont destinés à fournir des médicaments beta -lactame possédant une excellente activité antimicrobienne contre les virus de la grippe qui ont développé une vaste résistance aux médicaments beta -lactame existants du fait de mutations de protéines de fixation de la pénicilline contenues dans des souches gram positif et dans des souche gram négatif sur une large gamme, en particulier streptococcus pneumoniae résistant à la pénicilline (PRSP), etc..

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