Carbapenem derivatives, utilization thereof and intermediate...

C - Chemistry – Metallurgy – 07 – D

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C07D 477/20 (2006.01) A61K 31/40 (2006.01)

Patent

CA 2330641

Carbapenem compounds represented by general formula (I) wherein R1 represents a modifying group hydrolyzable in vivo; R2 and R3 may be the same or different and each represents lower alkyl; and R represents a group represented by formula (B) or formula (C) (wherein R4 and R5 may be the same or different and each represents hydrogen or lower alkyl; and R6 represents C1-10 alkyl). When administered orally, the compounds (I) are excellent in the absorbability via the digestive tract and exhibit sufficient antibacterial effects over a broad scope of bacterial species. Thus, they are highly useful as preventives/remedies for infectious diseases, in particular, microbisms.

L'invention concerne des composés de carbapenem correspondant à la formule générale (I) dans laquelle R?1¿ représente un groupe modificateur hydrolysable in vivo; R?2¿ et R?3¿ peuvent être identiques ou différents et représentent chacun un alkyle inférieur; et R représente un groupe qui correspond à la formule (B) ou à la formule (C) (dans laquelle R?4¿ et R?5¿ peuvent être identiques ou différents et représentent chacun hydrogène ou alkyle inférieur; et R?6¿ représente un alkyle C¿1-10?). Administrés par voie orale, les composés (I) manifestent une excellente capacité d'absorption dans le tract digestif et d'excellents effets antibactériens vis-à-vis d'un large spectre d'espèces bactériennes. Ils sont, par conséquent, d'une grande utilité en tant que substances préventives ou médicaments lors de maladies infectieuses, notamment de microbismes.

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