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

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.

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A - human necessities
A01 - agriculture
A21 - baking
A22 - butchering
A23 - foods or foodstuffs
A24 - tobacco
A41 - wearing apparel
A42 - headwear
A43 - footwear
A44 - haberdashery
A45 - hand or travelling articles
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A47 - furniture
A61 - medical or veterinary science
A62 - life-saving
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A99 - subject matter not otherwise provided for in this section
B - performing operations
B01 - physical or chemical processes or apparatus in general
B02 - crushing, pulverising, or disintegrating
B03 - separation of solid materials using liquids or using pneumatic tables or jigs
B04 - centrifugal apparatus or machines for carrying-out physical or chemical processes
B05 - spraying or atomising in general
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B68 - saddlery
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D01 - natural or man-made threads or fibres
D02 - yarns
D03 - weaving
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D05 - sewing
D06 - treatment of textiles or the like
D07 - ropes
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F03 - machines or engines for liquids
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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:: 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.

Issue Date:: Tue Nov 30 00:00:00 EST 2021

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

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A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
A61K31/55 - having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
A61P25/00 - Drugs for disorders of the nervous system

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07D - HETEROCYCLIC COMPOUNDS
C07D223/16 - Benzazepines

Show less

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.

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                    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.

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                    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.

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@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         = {Tue Nov 30 00:00:00 EST 2021},

  month        = {Tue Nov 30 00:00:00 EST 2021}

}

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Chemical approaches for detection and destruction of nerve agents
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Similar Records

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

Citation Formats

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

Structure of HI-6•Sarin-Acetylcholinesterase Determined by X-Ray Crystallography and Molecular Dynamics Simulation: Reactivator Mechanism and Design journal, June 2009

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

Compounds for reactivation of acetylcholinesterase and related compositions methods and systems patent, March 2020

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

A Novel Method for the Preparation of Optically Active Dipeptide. Chemo- and Stereoselective Reduction of 2-Hydroxyimino Amides with Samarium Diiodide. journal, January 1992

Decontamination of chemical warfare agents journal, December 1992

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

Structure of HI-6•Sarin-Acetylcholinesterase Determined by X-Ray Crystallography and Molecular Dynamics Simulation: Reactivator Mechanism and Design
journal, June 2009

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

Compounds for reactivation of acetylcholinesterase and related compositions methods and systems
patent, March 2020

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

A Novel Method for the Preparation of Optically Active Dipeptide. Chemo- and Stereoselective Reduction of 2-Hydroxyimino Amides with Samarium Diiodide.
journal, January 1992

Decontamination of chemical warfare agents
journal, December 1992