Last Updated: May 14, 2026

Claims for Patent: 7,795,243

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Summary for Patent: 7,795,243

Title:	Penem prodrugs
Abstract:	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.
Inventor(s):	Katherine E. Brighty, Anthony Marfat, Dale G. McLeod, John P. O'Donnell
Assignee:	Pfizer Corp SRL, Pfizer Inc
Application Number:	US11/769,849
Patent Claims:	1. A compound of the formula: 2. The compound of claim 1, which is (2-ethyl-1-oxobutoxy)methyl (5R,6S)-6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-4-thia-1-azabicydo[3.2.0]hept-2-ene-2-carboxylate. 3. The compound of claim 1, which is (2-ethyl-1-oxobutoxy)methyl (5R,6S)-6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate in the crystalline form having an X-ray powder diffraction pattern substantially the same as that represented in FIGS. 3 and 5. 4. A pharmaceutical composition comprising the compound of claim 2 formulated for oral administration in admixture with one or more excipients. 5. A pharmaceutical composition comprising about 800 mg to about 2.5 g of the compound of claim 2, formulated for oral administration with one or more excipients. 6. A method of treating bacterial infection comprising orally administering a therapeutically effective amount of the compound of claim 2 to a human in need thereof. 7. A method of treating bacterial infection comprising orally administering a therapeutically effective amount of about 500 mg to about 2.5 g BID or TID of the compound of claim 2 to a human in need thereof. 8. A method of treating bacterial infection comprising orally administering a therapeutically effective amount of about 800 mg to about 1 g BID of the compound of claim 2 to a human in need thereof. 9. A method of treating bacterial infection comprising orally administering a therapeutically effective amount of about 7 mg/kg to about 25 mg/kg BID of the compound of claim 2 to a human in need thereof. 10. A method of treating bacterial infection comprising orally administering a therapeutically effective amount of about 17 mg/kg to about 45 mg/kg BID of the compound of claim 2 to a human in need thereof.

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