Centrally active and orally bioavailable uncharged bisoxime antidotes for organophosphate poisoning and methods for making and using them

US11820749B2 · kind B2 · utility

Assignees

• The Regents of the University of California · US
• Oak Ridge National Laboratory · US

Inventors

• Zoran Radic · San Diego, US
• Carlo Ballatore · San Diego, US
• Lukas Gorecki · Hradec, CZ
• Palmer Taylor · Village of La Jolla, US
• Andrey Kovalevsky · Oak Ridge, US
• Xiaolin Cheng · San Ramon, US

Key dates

• Filing date: May 21, 2020
• Grant date: Nov 21, 2023
• Expiry date: Nov 5, 2040

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D243/08
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

In alternative embodiments, provided are uncharged bis-oxime antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). In alternative embodiments, provided are pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi-chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound as provided herein.