β-lactamase inhibitors

US8487093B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Timothy A. Blizzard · Middletown, US
• Helen Chen · Livingston, US
• Candido Gude · Staten Island, US
• Jeffrey D. Hermes · Hackettstown, US
• Jason Imbriglio · Piscataway, US
• Seongkon Kim · Holmdel, US
• Jane Yang Wu · Marlboro, US
• Christopher J. Mortko · Hoboken, US
• Ian Mangion · Cranford, US
• Nelo Rivera · Scotch Plains, US
• Rebecca T. Ruck · Jersey City, US
• Michael Shevlin · Plainfield, US

Key dates

• Filing date: Jan 15, 2009
• Grant date: Jul 16, 2013
• Expiry date: Nov 19, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D519/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.