Novel .beta.-lactam compounds and process for producing the...

C - Chemistry – Metallurgy – 07 – D

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C07D 519/00 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01) A61K 31/55 (2006.01) C07D 477/20 (2006.01)

Patent

CA 2331586

Novel .beta.-lactam compounds represented by general formula (1), wherein R1 represents lower alkyl or hydroxylated lower alkyl; R2 represents H or lower alkyl; X represents O or S; R3 represents H, a metal or a protective group; and W represents a 6- or 7-membered heterocycle containing nitrogen optionally substituted at carbon atom(s). These .beta.-lactam compounds exert an excellent antibacterial activity on gram-positive bacteria, in particular, methicillin resistant Staphylococcus aureus and methicillin resistant coagulase negative Staphylococcus aureus.

L'invention concerne de nouveaux composés beta -lactam représentés par la formule (1). Dans cette formule, R<1> représente alkyle inférieur ou alkyle inférieur hydroxylé; R<2> représente H ou alkyle inférieur; X représente O ou S; R<3> représente H, un métal ou un groupe protecteur; et W représente un hétérocycle à 6 ou 9 éléments contenant de l'azote éventuellement substitué, au niveau des atomes de carbone. Ces composés beta -lactam exercent une excellente activité antibactérienne sur les bactéries gram positif, en particulier sur le staphylocoque doré résistant à la méthicilline et sur le staphylocoque doré à coagulase négative résistant à la méthicilline.

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