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

C - Chemistry – Metallurgy – 07 – D

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C07D 477/20 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61P 31/04 (2006.01) C07D 207/20 (2006.01) C07D 417/04 (2006.01) C07D 477/06 (2006.01)

Patent

CA 2427812

The present invention is directed to a .beta.-lactam compound of the formula [1]; (see formula 1) wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, -C(R3)=NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.

L'invention concerne des composés de beta -lactame représentés par la formule générale (I), des sels pharmaceutiquement acceptables et des esters non toxiques de ces derniers, formule dans laquelle R1 représente un alkyle inférieur, R2 représente H ou un alkyle inférieure, X représente O, S ou NH, m et n sont chacun compris entre 0 et 4, Y1 représente halogéno etc., et Y2 représente H, un alkyle éventuellement substitué, etc. Ces composés présentent une activité antibactérienne excellente contre des bactéries à gram positif, notamment Staphylococcus aureus résistant à la méthicilline et Staphylococcus aureus à coagulase négative résistant à la méthicilline.

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