Catalytic scavengers of organophosphates to potentiate butyrylcholinesterase (hBChE) as a catalytic bioscavenger and methods for making and using them

US10172831B2 · kind B2 · utility

Assignee

• The Regents of the University of California · US

Inventors

• Palmer Taylor · Village of La Jolla, US
• Zoran Radic · San Diego, US
• Valery Fokin · Oceanside, US

Key dates

• Filing date: Oct 15, 2014
• Grant date: Jan 8, 2019
• Expiry date: Oct 15, 2034

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12Y301/01008
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided are N-alkyl imidazole 2-aldoximes, including cationic imidazolium and uncharged tertiary imidazole aldoximes, and compositions and methods for making and using them, including methods for reactivating human butyrylcholinesterase (hBChE) or acetylcholinesterase (hAChE) inhibited by organophosphate (OP). By administration of a composition of the invention, the inactive or conjugated hBChE-OP or hAChE-OP is reactivated and the catalytic cycle of turnover and inactivation of the OP is completed; and in alternative embodiments, secondary mechanisms of reversible protection of hBChE and hAChE from irreversible inactivation by OPs and reactivation of tissue AChE also contribute to overall efficacy.