Benzoxazolinone compounds with selective activity in voltage-gated sodium channels

US9624208B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Joseph E. Pero · Harleysville, US
• Hannah D. G. F. Lehman · Boyertown, US
• Michael J. Kelly, III · Paoli, US
• Lianyun Zhao · Burlington, US
• Michael A. Rossi · Limerick, US
• Dansu Li · New York, US
• Kevin F. Gilbert · Barto, US
• Scott Wolkenberg · Whitemarsh, US
• James Mulhearn · Cheltenham, US
• Mark E. Layton · Harleysville, US
• Pablo de Leon · Philadelphia, US

Key dates

• Filing date: Oct 23, 2013
• Grant date: Apr 18, 2017
• Expiry date: Oct 23, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.