Patents by Inventor Gideon Shapiro

Gideon Shapiro 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).

  • TREATMENT OF AUTISM SPECTRUM DISORDERS, OBSESSIVE-COMPULSIVE DISORDER AND ANXIETY DISORDERS
    Publication number: 20190298725
    Abstract: Disclosed are methods for treating NMDA receptor-mediated disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. NMDA receptor-mediated disorders include autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders.
    Type: Application
    Filed: November 21, 2017
    Publication date: October 3, 2019
    Inventors: Gideon Shapiro, Dorothy G. Flood
  • Pyrrolopyrimidine derivatives as NR2B NMDA receptor antagonists
    Patent number: 10420768
    Abstract: Disclosed are chemical entities of formula I: wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: September 24, 2019
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20190218194
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: December 12, 2018
    Publication date: July 18, 2019
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
    Patent number: 10294230
    Abstract: Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: May 21, 2019
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20190135819
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Application
    Filed: October 2, 2018
    Publication date: May 9, 2019
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20190100496
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: September 7, 2018
    Publication date: April 4, 2019
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20190077795
    Abstract: Provided herein are various compounds, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: August 10, 2018
    Publication date: March 14, 2019
    Applicant: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Kerren Kalai Swinger, Gideon Shapiro, Paula Ann Boriack-Sjodin
  • PRMT1 inhibitors and uses thereof
    Patent number: 10227307
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: March 12, 2019
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
  • 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists
    Patent number: 10221182
    Abstract: Disclosed are chemical entities of Formula (I): wherein X, Y, Z, R1, R3, R4 and R5 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: March 5, 2019
    Assignee: RUGEN HOLDINGS (CAYMAN) LIMITED
    Inventor: Gideon Shapiro
  • PRMT1 Inhibitors and Uses Thereof
    Publication number: 20190022064
    Abstract: Described herein are compounds of Formula (I-a) and (I-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Application
    Filed: July 23, 2018
    Publication date: January 24, 2019
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Kevin Wayne Kuntz
  • 3,3-DIFLUOROPIPERIDINE CARBAMATE HETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
    Publication number: 20180346476
    Abstract: Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Application
    Filed: August 10, 2018
    Publication date: December 6, 2018
    Inventor: Gideon Shapiro
  • CARM1 inhibitors and uses thereof
    Patent number: 10118931
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: November 6, 2018
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • PYRROLOPYRIMIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS
    Publication number: 20180303834
    Abstract: Disclosed are chemical entities of formula I: wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.
    Type: Application
    Filed: April 24, 2018
    Publication date: October 25, 2018
    Inventor: Gideon Shapiro
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20180289671
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: January 26, 2018
    Publication date: October 11, 2018
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20180290982
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 22, 2018
    Publication date: October 11, 2018
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20180282343
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Application
    Filed: December 8, 2017
    Publication date: October 4, 2018
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Treatment of Cognitive Disorders with (R)-7-Chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-Carboxamide and Pharmaceutically Acceptable Salts Thereof
    Publication number: 20180271844
    Abstract: (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide has been found to have procognitive effects in humans at unexpectedly low doses. Thus, (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof can be used at unexpectedly low doses to improve cognition.
    Type: Application
    Filed: October 27, 2017
    Publication date: September 27, 2018
    Inventors: Richard Chesworth, Gerhard Koenig, Gideon Shapiro
  • TREATMENT OF ANXIETY DISORDERS AND AUTISM SPECTRUM DISORDERS
    Publication number: 20180271869
    Abstract: Disclosed are methods for treating autism spectrum disorders and/or anxiety disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. Anxiety disorders include agoraphobia (with or without panic disorder), generalized anxiety disorder (GAD), social anxiety disorder (SAD), panic disorder (PD), post-traumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD).
    Type: Application
    Filed: September 22, 2015
    Publication date: September 27, 2018
    Inventors: Jie Liu, Todd A. Verdoorn, Gideon Shapiro, Gang Chen
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 10081603
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: September 25, 2018
    Assignee: Epizyme Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • PRMT1 INHIBITORS AND USES THEREOF
    Publication number: 20180265478
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Application
    Filed: December 21, 2017
    Publication date: September 20, 2018
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin