C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 499/00 (2006.01) A61K 31/43 (2006.01) A61P 31/04 (2006.01)
Patent
CA 2494953
Prodrugs of 6-.szlig.-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a betalactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
L'invention concerne des promédicaments de sulfone de l'acide 6-.beta.-hydroxyméthylpénicillanique ayant la structure (I), dans laquelle R désigne H ou un méthyle et des solvates de ceux-ci. L'invention concerne en outre des compositions pharmaceutiques comprenant un promédicament selon l'invention, ou un solvate de celui-ci, à titre facultatif, un antibiotique béta-lactame, et au moins un excipient pharmaceutiquement acceptable. L'invention concerne également un procédé d'accroissement de l'efficacité thérapeutique d'un antibiotique béta-lactame chez un mammifère, par administration d'une quantité efficace d'antibiotique béta-lactame et d'une quantité, accroissant l'efficacité, d'un promédicament selon l'invention, ou d'un solvate de celui-ci. Par ailleurs, l'invention concerne un procédé de traitement d'une infection bactérienne chez un mammifère, par administration à un mammifère en demande, d'une quantité thérapeutiquement efficace d'une composition selon l'invention.
Marfat Anthony
Mcleod Dale Gordon
Pfizer Products Inc.
Sim & Mcburney
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