Novel carbapenem derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 519/00 (2006.01) A61K 31/429 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/4709 (2006.01) A61K 31/4725 (2006.01) A61K 31/496 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61K 31/541 (2006.01) A61P 31/04 (2006.01) C07D 477/10 (2006.01) C07D 477/14 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2429675

It is intended to provide carbapenem derivatives which have a potent antibacterial power on MRSA, PRSP, Haemophilus influenzaeand .beta.-lactamase- producing bacteria and a high stability to DHP-1. The above compounds involve compounds represented by the following general formulae (I) and (II) and pharmaceutically acceptable salts thereof, wherein R1 represents H or methyl; R2 and R3 represent each H, halogeno, optionally substituted alkyl, cycloalkyl, optionally substituted alkylcarbonyl, carbamoyl, optionally substituted aryl, optionally substituted alkylthio, morpholinyl, alkylsulfonyl or formyl; n is from 0 to 4; and Hy represents an optionally substituted, monocyclic or bicyclic heterocyclic group.

L'invention concerne des dérivés de cabapenem présentant une puissante activité antimicrobienne sur les virus MRSA, PRSP, Haemophilus influenzae et les bactéries de production de .beta.-lactamase ainsi qu'une grande stabilité au DHP-1. Ces composés sont représentés par les formules générales (I) et (II) ou des sels pharmaceutiquement acceptables de ces composés. Dans ces formules, R1 représente H ou méthyle; R2 et R3 représentent chacun H, halogéno, alkyle éventuellement substitué, cycloalkyle, alkylcarbonyle éventuellement substitué, carbamoyle, aryle éventuellement substitué, alkylthio éventuellement substitué, morpholinyle, alkylsulfonyle ou formyle; n est compris entre 0 et 4; et Hy représente un groupe monocyclique, bicyclique ou hétérocyclique éventuellement substitué.

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