Patents by Inventor Valery Fokin

Valery Fokin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 10913726
    Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine 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). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.
    Type: Grant
    Filed: July 6, 2018
    Date of Patent: February 9, 2021
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Palmer Taylor, Zoran Radic, Karl Barry Sharpless, Valery Fokin, Rakesh Sit
  • Patent number: 10800749
    Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine 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). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: October 13, 2020
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Palmer Taylor, Zoran Radic, K. Barry Sharpless, Valery Fokin, Rakesh Sit
  • Publication number: 20190337911
    Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine 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). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.
    Type: Application
    Filed: July 11, 2019
    Publication date: November 7, 2019
    Inventors: Palmer TAYLOR, Zoran RADIC, Barry K. SHARPLESS, Valery FOKIN, Rakesh SIT
  • Patent number: 10308638
    Abstract: In alternative embodiments, provided are selective agonists having a high affinity for the alpha7 nicotinic acetylcholine receptor (?7 nAChR), assays for selectivity of nicotinic receptor subtype and ligand-gated ion channel subtype based on receptor occupation and response, behavioral assessments for reversing cognitive impairment after scopolamine treatment, enhancing memory retention over time, pharmaceutical compositions and formulations and devices comprising them, and methods for making and using them, including characterizing and efficiently assaying them for receptor subtype selectivity. In alternative embodiments, provided are substituted anti 1,2,3-triazoles compounds with high affinity, and selective binding, for the alpha7 nicotine acetylcholine receptor (?7 nAChR), as exemplified by 5-(1-(2-(Piperidin-1-yl)ethyl)-1H-1,2,3-triazol-4-yl)-1H-indole (“IND1”), 5-((quinuclid-3-yl)-1H-1,2,3-triazol-4-yl)-1H-indole (“IND8”) and 3-(4-hydroxyphenyl-1,2,3-triazol-1-yl) quinuclidine (“QND8”).
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: June 4, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Palmer Taylor, Gisela-Andrea Camacho-Hernandez, Karl Barry Sharpless, M. G. Finn, Valery Fokin
  • Publication number: 20190119237
    Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine 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). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.
    Type: Application
    Filed: July 6, 2018
    Publication date: April 25, 2019
    Inventors: Palmer TAYLOR, Zoran RADIC, Barry K. SHARPLESS, Valery FOKIN, Rakesh SIT
  • Patent number: 10172831
    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.
    Type: Grant
    Filed: October 15, 2014
    Date of Patent: January 8, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Palmer Taylor, Zoran Radic, Valery Fokin
  • Publication number: 20180244653
    Abstract: In alternative embodiments, provided are selective agonists having a high affinity for the alpha7 nicotinic acetylcholine receptor (?7 nAChR), assays for selectivity of nicotinic receptor subtype and ligand-gated ion channel subtype based on receptor occupation and response, behavioral assessments for reversing cognitive impairment after scopolamine treatment, enhancing memory retention over time, pharmaceutical compositions and formulations and devices comprising them, and methods for making and using them, including characterizing and efficiently assaying them for receptor subtype selectivity. In alternative embodiments, provided are substituted anti 1,2,3-triazoles compounds with high affinity, and selective binding, for the alpha7 nicotine acetylcholine receptor (?7 nAChR), as exemplified by 5-(1-(2-(Piperidin-1-yl)ethyl)-1H-1,2,3-triazol-4-yl)-1H-indole (“IND1”), 5-((quinuclid-3-yl)-1H-1,2,3-triazol-4-yl)-1H-indole (“IND8”) and 3-(4-hydroxyphenyl-1,2,3-triazol-1-yl) quinuclidine (“QND8”).
    Type: Application
    Filed: March 24, 2016
    Publication date: August 30, 2018
    Inventors: Palmer TAYLOR, John YAMAUCHI, Todd T. TALLEY, Kuntarat ARUNRUNGVICHIAN, Opa VAJRAGUPTA, Valery FOKIN
  • Patent number: 9896547
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(—R2-A)n-; each A is SO2, C(?O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Grant
    Filed: April 11, 2017
    Date of Patent: February 20, 2018
    Assignee: The Scripps Research Institute
    Inventors: Jiajia Dong, Valery Fokin, Larisa Krasnova, Luke R. Kwisnek, James S. Oakdale, K. Barry Sharpless
  • Publication number: 20170218127
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(—R2-A)n-; each A is SO2, C(?O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Application
    Filed: April 11, 2017
    Publication date: August 3, 2017
    Inventors: Jiajia Dong, Valery Fokin, Larisa Krasnova, Luke R. Kwisnek, James S. Oakdale, K. Barry Sharpless
  • Patent number: 9624344
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(?O) or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: April 18, 2017
    Assignee: The Scripps Research Institute
    Inventors: Jiajia Dong, Valery Fokin, Larisa Krasnova, Luke R. Kwisnek, James S. Oakdale, K. Barry Sharpless
  • Publication number: 20170002148
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(?O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Application
    Filed: September 19, 2016
    Publication date: January 5, 2017
    Inventors: Jiajia Dong, Valery Fokin, Larisa Krasnova, Luke R. Kwisnek, James S. Oakdale, K. Barry Sharpless
  • Patent number: 9447243
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(?O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: September 20, 2016
    Assignee: The Scripps Research Institute
    Inventors: Jiajia Dong, Valery Fokin, Larisa Krasnova, Luke R. Kwisnek, James S. Oakdale, K. Barry Sharpless
  • Publication number: 20160256438
    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.
    Type: Application
    Filed: October 15, 2014
    Publication date: September 8, 2016
    Inventors: Palmer TAYLOR, Zoran RADIC, Valery FOKIN
  • Publication number: 20160244435
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to imidazole, thiazole, and furan derivatives and their use as therapeutic agents.
    Type: Application
    Filed: June 20, 2014
    Publication date: August 25, 2016
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Lars Eckmann, Yukiko Miyamoto, Valery Fokin, Karl Barry Sharpless
  • Publication number: 20160214946
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Ru ion to form a 1,4-disubstituted 1,2,3-triazole.
    Type: Application
    Filed: March 30, 2016
    Publication date: July 28, 2016
    Applicant: The Scripps Research Institute
    Inventors: K. Barry SHARPLESS, Valery FOKIN, Vsevold A. ROSTOVTSEV, Luke GREEN, Fahmi HIMO
  • Patent number: 9302997
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Cu(I) ion to form a 1,4-disubstituted 1,2,3-triazole, wherein the source of Cu(I) ion comprises Cu(II) and a metal capable of reducing Cu(II) to Cu(I). In some embodiments, the metal capable of reducing Cu(II) to Cu(I) is selected from the group consisting of Al, Be, Co, Cr, Fe, Mg, Mn, Ni, and Zn.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: April 5, 2016
    Assignee: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Valery Fokin, Vsevold A. Rostovtsev, Luke Green, Fahmi Himo
  • Publication number: 20150361060
    Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine 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). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.
    Type: Application
    Filed: February 15, 2014
    Publication date: December 17, 2015
    Applicant: The Regents of the University of California
    Inventors: Palmer TAYLOR, Zoran RADIC, Barry K. SHARPLESS, Valery FOKIN, Rakesh SIT
  • Publication number: 20150315340
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(?O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Application
    Filed: December 3, 2013
    Publication date: November 5, 2015
    Inventors: Jiajia Dong, Valery Fokin, Larisa Krasnova, Luke R. Kwisnek, James S. Oakdale, K. Barry Sharpless
  • Publication number: 20150232432
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Cu(I) ion to form a 1,4-disubstituted 1,2,3-triazole, wherein the source of Cu(I) ion comprises Cu(II) and a metal capable of reducing Cu(II) to Cu(I). In some embodiments, the metal capable of reducing Cu(II) to Cu(I) is selected from the group consisting of Al, Be, Co, Cr, Fe, Mg, Mn, Ni, and Zn.
    Type: Application
    Filed: May 6, 2015
    Publication date: August 20, 2015
    Applicant: The Scripps Research Institute
    Inventors: K. Barry SHARPLESS, Valery FOKIN, Vsevold A. ROSTOVTSEV, Luke GREEN, Fahmi HIMO
  • Patent number: 9040716
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion in human blood plasma to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt, Cu(II) ion in the presence of a reducing agent, or copper metal.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: May 26, 2015
    Assignee: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Valery Fokin, Vsevold A. Rostovtsev, Luke Green, Fahmi Himo