Patents by Inventor Pablo De Leon

Pablo De Leon 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: 20230265092
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit RNA polymerase I (Pol I). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) Pol I activity contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
    Type: Application
    Filed: September 15, 2021
    Publication date: August 24, 2023
    Inventors: Hester Hui Liu, James C. Barrow, Marikki K. Laiho, Rajesh Kumar Nv, Pablo de Leon, Tony Dorado, Asma Begum, Wenjun Fan, Gregory Stachelek
  • Publication number: 20230265091
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit RNA polymerase I (Pol I). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) Pol I activity contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
    Type: Application
    Filed: September 15, 2021
    Publication date: August 24, 2023
    Inventors: Hester Hui Liu, James C. Barrow, Marikki K. Laiho, Rajesh Kumar Nv, Pablo de Leon, Tony Dorado, Asma Begum, Wenjun Fan, Gregory Stachelek
  • Publication number: 20230257390
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit RNA polymerase I (Pol I). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) Pol I activity contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
    Type: Application
    Filed: September 15, 2021
    Publication date: August 17, 2023
    Inventors: Hester Hui Liu, James C. Barrow, Marikki K. Laiho, Rajesh Kumar Nv, Pablo de Leon, Tony Dorado, Asma Begum, Wenjun Fan, Gregory Stachelek
  • Publication number: 20210139479
    Abstract: This invention relates to compounds, pharmaceutical compositions and their use for treating neuropsychiatric and neurodegenerative disorders. In particular, the invention relates to inhibitors of catechol-O-methyltransferase and their use as therapeutics for central nervous system disease.
    Type: Application
    Filed: January 22, 2021
    Publication date: May 13, 2021
    Inventors: James Barrow, Glen Ernst, Dominique Swinnen, Florian Montel, Sabine Defays, Yifeng Huang, Pablo de Leon, Michael Steven Poslusney
  • Patent number: 10934283
    Abstract: Compounds that inhibit COMT enzyme and pharmaceutical compositions comprising the same are provided herein. Methods of treating various psychiatric and neurological disorders with the compounds and pharmaceutical compositions described herein are also provided.
    Type: Grant
    Filed: November 25, 2016
    Date of Patent: March 2, 2021
    Assignee: LIEBER INSTITUTE, INC.
    Inventors: James Barrow, Glen Ernst, Dominique Swinnen, Florian Montel, Sabine Defays, Yifang Huang, Pablo de León, Michael Steven Poslusney
  • Publication number: 20180305354
    Abstract: Compounds that inhibit COMT enzyme and pharmaceutical compositions comprising the same are provided herein. Methods of treating various psychiatric and neurological disorders with the compounds and pharmaceutical compositions described herein are also provided.
    Type: Application
    Filed: November 25, 2016
    Publication date: October 25, 2018
    Inventors: James Barrow, Glen Ernst, Dominique Swinnen, Florian Montel, Sabine Defays, Yifang Huang, Pablo de LEÓN, Michael Steven Poslusney
  • Patent number: 9663506
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Patent number: 9636337
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: May 2, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Patent number: 9624208
    Abstract: Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: April 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph E. Pero, Hannah D. G. F. Lehman, Michael J. Kelly, III, Lianyun Zhao, Michael A. Rossi, Dansu Li, Kevin F. Gilbert, Scott Wolkenberg, James Mulhearn, Mark E. Layton, Pablo de Leon
  • Publication number: 20160158217
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 18, 2016
    Publication date: June 9, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Publication number: 20160159744
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 18, 2016
    Publication date: June 9, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Patent number: 9273040
    Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: March 1, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
  • Publication number: 20150252034
    Abstract: Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 23, 2013
    Publication date: September 10, 2015
    Inventors: Joseph E. Pero, Hannah D.G.F. Lehman, Michael J. Kelly, III, Lianyun Zhao, Michael A. Rossi, Dansu Li, Kevin F. Gilbert, Scott Wolkenberg, James Mulhearn, Mark E. Layton, Pablo de Leon
  • Publication number: 20140309227
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Publication number: 20140303143
    Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
  • Publication number: 20120214847
    Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 26, 2010
    Publication date: August 23, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, James J. Perkins, Jesse J. Manikowski, Pablo de Leon, Robert S. Meissner
  • Publication number: 20120115885
    Abstract: The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: July 19, 2010
    Publication date: May 10, 2012
    Inventors: Pablo De Leon, Melissa Egbertson, Ivory D. Hills, Adam Wayne Johnson, Michelle Machacek