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Title: Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them

Abstract

Described herein are oxime compounds capable of inactivating OP-based AChE inhibitors, crossing the blood brain barrier (BBB), and/or reactivation of OP-inhibited acetylcholinesterase (AChE) and related methods, systems and compositions for inactivation of one or more OP-based AChE inhibitors, therapeutic and/or prophylactic treatment of an individual, and/or decomposition of OP-based AChE inhibitors for decontamination.

Inventors:
; ; ; ; ; ; ; ;
Issue Date:
Research Org.:
Lawrence Livermore National Laboratory (LLNL), Livermore, CA (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1860113
Patent Number(s):
11186548
Application Number:
16/198,627
Assignee:
Lawrence Livermore National Security, LLC (Livermore, CA)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
DOE Contract Number:  
AC52-07NA27344
Resource Type:
Patent
Resource Relation:
Patent File Date: 11/21/2018
Country of Publication:
United States
Language:
English

Citation Formats

Valdez, Carlos A., Be, Nicholas A., Malfatti, Michael A., Enright, Heather Ann, Bennion, Brian J., Carpenter, Timothy S., Hok, Saphon, Lao, Hio Leong, and Nguyen, Tuan H. Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them. United States: N. p., 2021. Web.
Valdez, Carlos A., Be, Nicholas A., Malfatti, Michael A., Enright, Heather Ann, Bennion, Brian J., Carpenter, Timothy S., Hok, Saphon, Lao, Hio Leong, & Nguyen, Tuan H. Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them. United States.
Valdez, Carlos A., Be, Nicholas A., Malfatti, Michael A., Enright, Heather Ann, Bennion, Brian J., Carpenter, Timothy S., Hok, Saphon, Lao, Hio Leong, and Nguyen, Tuan H. Tue . "Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them". United States. https://www.osti.gov/servlets/purl/1860113.
@article{osti_1860113,
title = {Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them},
author = {Valdez, Carlos A. and Be, Nicholas A. and Malfatti, Michael A. and Enright, Heather Ann and Bennion, Brian J. and Carpenter, Timothy S. and Hok, Saphon and Lao, Hio Leong and Nguyen, Tuan H.},
abstractNote = {Described herein are oxime compounds capable of inactivating OP-based AChE inhibitors, crossing the blood brain barrier (BBB), and/or reactivation of OP-inhibited acetylcholinesterase (AChE) and related methods, systems and compositions for inactivation of one or more OP-based AChE inhibitors, therapeutic and/or prophylactic treatment of an individual, and/or decomposition of OP-based AChE inhibitors for decontamination.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2021},
month = {11}
}

Works referenced in this record:

Blood-brain barrier active efflux transporters: ATP-binding cassette gene family
journal, January 2005


The biodistribution and pharmacokinetics of the oxime acetylcholinesterase reactivator RS194B in guinea pigs
journal, November 2017


Oximes For Treatment Of Peripheral And Central Nervous System Exposure To Acetyl Cholinesterase Inhibitors
patent-application, February 2013


Syrian gas attack reinforces need for better anti-sarin drugs
journal, October 2013


Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A Review
journal, February 2015


A Quantitative Analysis and Chemical Approach for the Reduction of Nonspecific Binding Proteins on Affinity Resins
journal, October 2003


A new and rapid colorimetric determination of acetylcholinesterase activity
journal, July 1961


A Method to Predict Blood-Brain Barrier Permeability of Drug-Like Compounds Using Molecular Dynamics Simulations
journal, August 2014


Decontamination of Chemical Warfare Agents [English]
journal, May 2010


Chemical approaches for detection and destruction of nerve agents
journal, January 2013


Blood Brain Barrier-Penetrating Oximes for Cholistenerases Reactivation
patent-application, February 2014


Compounds for Reactivation of Acetylcholinesterase and Related Compositions Methods and Systems
patent-application, November 2017


Nonquaternary Reactivators for Organophosphate-Inhibited Cholinesterases
journal, December 2011


Report on 640 Victims of the Tokyo Subway Sarin Attack
journal, August 1996


A Novel Design of Artificial Membrane for Improving the PAMPA Model
journal, January 2008


Design, synthesis, and characterization of novel, nonquaternary reactivators of GF-inhibited human acetylcholinesterase
journal, April 2014


The Tokyo subway sarin attack—lessons learned
journal, September 2005


Predicting a Drug’s Membrane Permeability: A Computational Model Validated With in Vitro Permeability Assay Data
journal, May 2017


Isoxazole Derivatives Useful As Antibacterial Agents
patent-application, January 2014


Decontamination of chemical warfare agents
journal, December 1992