Patents by Inventor Rakesh SIT

Rakesh SIT 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).

  • Publication number: 20220079950
    Abstract: In alternative embodiments, the provided are therapeutic combinations comprising: 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 nervous system (CNS); and, a brain efflux transporter inhibitor, or an inhibitor of renal tubular secretion, wherein optionally the brain efflux transporter inhibitor or the inhibitor of renal tubular secretion comprises a P-glycoprotein inhibitor, an organic anion transporter (OAT) inhibitor and/or an organic cation (OCT) transporter inhibitor.
    Type: Application
    Filed: December 31, 2019
    Publication date: March 17, 2022
    Inventors: Palmer TAYLOR, Jeremiah MOMPER, Zoran RADIC, K. Barry SHARPLESS, Rakesh SIT
  • 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
  • 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
  • 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