Stable oxapenem-3-carboxylic acids

C - Chemistry – Metallurgy – 07 – D

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C07D 503/10 (2006.01) A61K 31/42 (2006.01) C07D 205/08 (2006.01) C07D 205/09 (2006.01) C07D 403/12 (2006.01) C07D 503/00 (2006.01)

Patent

CA 1339450

Compounds of the structural formulae (see fig.I) or (see fig.II) and their pharmaceutically acceptable salts, esters and amide derivatives, in which R1 and R2, independently of one another, denote hydrogen or pharmaceutically acceptable groups which have 1 to 10 carbon atoms and are bonded to the remaining part of the molecule via carbon-carbon single bonds, and in which R3, R4 and R5, independently of one another, denote pharmaceutically acceptable groups which have 1 to 10 carbon atoms and are bonded to the remaining part of the molecule via carbon-carbon single bonds, are useful antibiotics. The trisubstitution by three groups R3, R4 and R5, which are bonded via carbon-carbon single bonds, results in a noticeable increase in the hydrolysis stability and thus also in the antibacterial action of oxa-penemcarboxylic acids.

573432

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