C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/6553 (2006.01) A61K 31/67 (2006.01) A61K 31/675 (2006.01) A61P 31/04 (2006.01) C07F 9/6539 (2006.01) C07F 9/6541 (2006.01) C07F 9/6558 (2006.01) C07F 9/6561 (2006.01)
Patent
CA 2652995
This invention provides novel .beta.-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. 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 pharmaceutically acceptable salt thereof.
La présente invention concerne de nouveaux inhibiteurs de la .beta.-lactamase de la classe des monoesters d'aryl- et d'hétéroaryl-sulfonamidométhylphosphonate ayant des cations à base d'azote ou des groupes ammonium quaternaire. Les composés inhibent trois classes de .beta.-lactamases et ont un effet synergique avec les effets antibactériens des antibiotiques de type .beta.-lactame (par exemple, l'imipénème et le ceftazidime) contre ceux des micro-organismes normalement résistants aux antibiotiques de type .beta.-lactame à la suite de la présence de .beta.-lactamases.
Chen Helen
Dininno Frank
Dykstra Kevin
Gaudette Frederic
Georgopapadakou Nafsika
Mbm Intellectual Property Law Llp
Merck & Co. Inc.
Methylgene Inc.
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