Southern Methodist University

Alamx, LLC

Lakshminarayana Vogeti

John D Buynak

The invention provides compounds of formula (I): wherein: R-Rand A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &#x3b2;-lactamase enzymes, for enhancing the activity of &#x3b2;-lactam antibiotics, and for treating &#x3b2;-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).

7-alkylidene-3-substituted-3-cephem-4-carboxylates as beta-lactamase inhibitors

The invention provides compounds of formula (I):wherein: R-Rand A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &#x3b2;-lactamase enzymes, for enhancing the activity of &#x3b2;-lactam antibiotics, and for treating &#x3b2;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), wherein Rand Rare each independently hydrogen, (C-C)alkyl, (C-C)alkenyl, (C-C)alkenyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkanoyl, (C-C)alkanoyloxy, (C-C)alkoxycarbonyl, aryl, heterocycle, halo, cyano, nitro, &#x2014;COOR, &#x2014;C(&#x2550;O)NRR, &#x2014;OC(&#x2550;O)NRR, NRR, or &#x2014;S(O)R; Ris hydrogen, halo, aryl, heteroaryl, &#x2014;S(O)R, or &#x2014;CH&#x2550;CHC(&#x2550;O)NRR; Ris hydrogen; A is thio, sulfinyl, or sulfonyl; and intermediates useful for the synthesis of compounds of formula (I).

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Dallas, TX, United States of America

Lakshminarayana Vogeti