Benzoxazolinone compounds with selective activity in voltage-gated sodium channels

US9273040B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Mark E. Layton · Harleysville, US
• Joseph E. Pero · Harleysville, US
• Hannah Fiji · Boyertown, US
• Michael J. Kelly, III · Paoli, US
• Pablo de Leon · Philadelphia, US
• Michael A. Rossi · Limerick, US
• Kevin F. Gilbert · Barto, US
• Anthony J. Roecker · Harleysville, US
• Zhijian Zhao · Wilmington, US
• Swati I P. Mercer · Philadelphia, US
• Scott Wolkenberg · Whitemarsh, US
• James Mulhearn · Cheltenham, US
• Lianyun Zhao · Burlington, US
• Dansu Li · New York, US

Key dates

• Filing date: Oct 26, 2012
• Grant date: Mar 1, 2016
• Expiry date: Oct 26, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D493/10
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of 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.