Patents by Inventor S. Wayne Mascarella

S. Wayne Mascarella 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).

  • Substituted 1,2,3,4-tetrahydroisoquinolines as kappa opioid antagonists
    Patent number: 11292783
    Abstract: Potent opioid receptor antagonists of formula (I) and their use as pharmacotherapies for treating depression, anxiety, schizophrenia, eating disorders, and addiction to cocaine, methamphetamine, nicotine, alcohol, and opiates are disclosed. More specifically, the disclosure provides potent and selective kappa opioid receptor antagonist compounds, pharmaceutical compositions of those compounds and uses of those compounds to ameliorate or treat addictions, eating disorders, etc.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: April 5, 2022
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Chad M. Kormos, Pauline W. Ondachi, Scott P. Runyon, Hernan A. Navarro, James B. Thomas, S. Wayne Mascarella
  • Tetrahydroisoquinoline Kappa Opioid Antagonists
    Publication number: 20190263781
    Abstract: Potent opioid receptor antagonists of formula (I) and their use as pharmacotherapies for treating depression, anxiety, schizophrenia, eating disorders, and addiction to cocaine, methamphetamine, nicotine, alcohol, and opiates are disclosed. More specifically, the disclosure provides potent and selective kappa opioid receptor antagonist compounds, pharmaceutical compositions of those compounds and uses of those compounds to ameliorate or treat addictions, eating disorders, etc.
    Type: Application
    Filed: September 15, 2017
    Publication date: August 29, 2019
    Applicant: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Chad M. Kormos, Pauline W. Ondachi, Scott P. Runyon, Hernan A. Navarro, James B. Thomas, S. Wayne Mascarella
  • Arylpiperazine opioid receptor antagonists
    Patent number: 9750738
    Abstract: Provided are opioid receptor antagonists represented by the formula (I): where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: September 5, 2017
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank Ivy Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
  • Hydroxybupropion analogues for treating drug dependence
    Patent number: 9527823
    Abstract: The invention provides hydroxybupropion analogs capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: December 27, 2016
    Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth University
    Inventors: Frank Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • 1-substituted 4-arylpiperazine as kappa opioid receptor antagonists
    Patent number: 9512105
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: December 6, 2016
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • ARYLPIPERAZINE OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20160095854
    Abstract: Provided are opioid receptor antagonists represented by the formula (I): where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
    Type: Application
    Filed: December 14, 2015
    Publication date: April 7, 2016
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. CARROLL, Juan P. CUEVA, James B. THOMAS, S. Wayne MASCARELLA, Scott P. RUNYON
  • Arylpiperazine opioid receptor antagonists
    Patent number: 9273027
    Abstract: Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: March 1, 2016
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
  • HYDROXYBUPROPION ANALOGUES FOR TREATING DRUG DEPENDENCE
    Publication number: 20150141416
    Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 21, 2015
    Inventors: Frank Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • 1-SUBSTITUTED 4-ARYLPIPERAZINE AS KAPPA OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20150005315
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 1, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • Hydroxybupropion analogues for treating drug dependence
    Patent number: 8906908
    Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 9, 2014
    Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth University
    Inventors: F. Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • KAPPA OPIOID RECEPTOR BINDING LIGANDS
    Publication number: 20130158072
    Abstract: Kappa opioid recep-tor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor, such as heroin or cocaine addictions.
    Type: Application
    Filed: January 19, 2010
    Publication date: June 20, 2013
    Applicant: Research Triangle Institute
    Inventors: Frank Ivy Carroll, James B. Thomas, S. Wayne Mascarella
  • ARYLPIPERAZINE OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20120295919
    Abstract: Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
    Type: Application
    Filed: October 12, 2010
    Publication date: November 22, 2012
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
  • Octahydroisoquinoline compounds as opioid receptor modulators
    Patent number: 7476679
    Abstract: Compounds which bind to opioid receptors are provided. In a preferred embodiment of the invention, the compounds are opioid receptor antagonists. The present invention also provides methods of treating conditions which are mediated by an opioid receptor.
    Type: Grant
    Filed: July 26, 2005
    Date of Patent: January 13, 2009
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Hernan A Navarro, S. Wayne Mascarella, James B. Thomas
  • Kappa opioid receptor ligands
    Patent number: 6974824
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors relative to nor-BNI, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Grant
    Filed: January 8, 2001
    Date of Patent: December 13, 2005
    Assignee: Research Triangle Institute
    Inventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
  • Opiate compounds, methods of making and methods of use
    Patent number: 6900228
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Grant
    Filed: March 9, 1999
    Date of Patent: May 31, 2005
    Assignee: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Novel opiate compounds, methods of making and methods of use
    Publication number: 20040146518
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Application
    Filed: December 23, 2003
    Publication date: July 29, 2004
    Applicant: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Novel opiate compounds, methods of making and methods of use
    Publication number: 20030158415
    Abstract: The present invention relates to a class of nitrogen-containing heterocyclic compounds which bind to opioid receptors. The inventive compounds can be used to treat a variety of disease states which involve the opioid receptors.
    Type: Application
    Filed: October 9, 2002
    Publication date: August 21, 2003
    Applicant: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Opiate compounds, methods of making and methods of use
    Patent number: 6593348
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: July 15, 2003
    Assignee: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Kappa opioid receptor ligands
    Patent number: 6559159
    Abstract: Structurally novel kappa opioid receptor antagonists are provided and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: May 6, 2003
    Assignee: Research Triangle Institute
    Inventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
  • Opiate compounds, methods of making and methods of use
    Patent number: 6552032
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: April 22, 2003
    Assignee: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella