7-alkylidene-3-substituted-3-cephem-4-carboxylates as...

C - Chemistry – Metallurgy – 07 – D

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C07D 501/00 (2006.01) A61K 31/546 (2006.01) A61K 31/549 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2454413

The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting .beta.-lactamase enzymes, for enhancing the activity of .beta.-lactam antibiotics, and for treating .beta.- lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), and intermediates useful for the synthesis of compounds of formula (I).

L'invention se rapporte à des composés représentés par la formule (I) dans laquelle R¿1?-R¿4? et A possèdent n'importe laquelle des valeurs définies dans le descriptif, et à leurs sels pharmaceutiquement acceptables, utiles dans l'inhibition des enzymes de beta-lactamase, dans l'amélioration de l'activité des antibiotiques de .beta.-lactame, et dans le traitement des infections bactériennes résistant à la .beta.-lactame chez un mammifère. L'invention concerne aussi des compositions pharmaceutiques, des procédés de préparation des composés de la formule (I), et des produits intermédiaires utiles dans la synthèse des composés de la formule (I).

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