Novel sulfonamidomethylphosphonate inhibitors of beta-lactamase

C - Chemistry – Metallurgy – 07 – F

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C07F 9/6539 (2006.01) A61K 31/662 (2006.01) A61P 31/04 (2006.01) C07F 9/655 (2006.01) C07F 9/6553 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2652869

This invention provides novel .beta.-lactamase inhibitors of the aryl-and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of .beta.-lactamases and synergize the antibacterial effects of .beta.-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the .beta.-lactam antibiotics as a result of the presence of the .beta.-lactamases. Formula (I) or a pro-drug or pharmaceutically acceptable salt thereof, wherein: W represents: Formula (II).

La présente invention concerne de nouveaux inhibiteurs de .beta.-lactamases de la classe des monoesters d'aryl- et d'hétéroaryl-sulfonamidométhylphosphonate. Les composés inhibent trois classes de .beta.-lactamases et présentent des synergies avec les effets antibactériens des antibiotiques de type .beta.-lactame (par exemple imipenem et ceftazimdime) contre les micro-organismes qui sont habituellement résistants aux antibiotiques de type .beta.-lactame du fait de la présence de .beta.-lactamases. Formule (I) ou son promédicament ou son sel de qualité pharmaceutique, W représentant : Formule (II).

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