Research Corporation Technologies, Inc.

Southern Methodist University

Akireddy Srinivasa Rao

John D Buynak

Venkata Ramana Doppalapudi

Greg C Adam

Compounds of formula I: wherein R, R, R, Rand n 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 novel intermediates useful for the synthesis of compounds of formula I.

Penicillanic acid derivative compounds and methods of making

2 &bgr;-substituted-6-alkylidene penicillanic acid derivatives as &bgr;-lactamase inhibitors

A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.

Process for the preparation of &agr;-oxolactams

Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n 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 novel intermediates useful for the synthesis of compounds of formula I.

2.beta.-substituted-6-alkylidene penicillanic acid derivatives as

The present invention relates to the use of 7-alkylidene derivatives of cephalosporin esters, such as sulfides, sulfoxides, and sulfones, as inhibitors of human leukocyte elastase. These materials are therefore useful as anti-inflammatory and anti-degenerative agents.

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Waukegan, IL, United States of America

Akireddy Srinivasa Rao