Pfizer Corporation

Dale G McLeod

Anthony Marfat

John Paul Mathias

Thomas V Magee

Simon Bailey

Sandra Marina Monaghan

Alan J Henderson

Blanda L C Stammen

Elisabeth C L Gautier

Katherine E Brighty

John P O'Donnell

Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.

Penem prodrugs

Prodrugs of 6-&#x3b2;-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 a pharmaceutically acceptable excipient. 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 beta-lactam 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.

Beta-lactamase inhibitor prodrug

The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

Nicotinamide derivatives useful as PDE4 inhibitors

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Ledyard, CT, United States of America

Dale G McLeod