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).

  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20230416263
    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: November 23, 2022
    Publication date: December 28, 2023
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Carm1 inhibitors and uses thereof
    Patent number: 11834455
    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: March 18, 2020
    Date of Patent: December 5, 2023
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
    Patent number: 11752155
    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: Grant
    Filed: March 17, 2021
    Date of Patent: September 12, 2023
    Assignee: Rugen Holdings (Cayman) Limited
    Inventors: Gideon Shapiro, Dorothy G. Flood
  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20230279020
    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: March 18, 2020
    Publication date: September 7, 2023
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • 3-(2-(Aminoethyl)-Indol-4-ol Derivatives, Methods of Preparation Thereof, and the Use as 5-HT2 Receptor Modulators
    Publication number: 20230140635
    Abstract: A compound of Formula I, which possesses 5-HT2A and/or 5-HT2C selective receptor activity, but lacks at lease some of the undesirable characteristics of 5-HT2B-agonist related activities, is disclosed. Methods of preparing said compounds are also described. The compound of Formula I may be useful in the treatment of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.
    Type: Application
    Filed: March 12, 2021
    Publication date: May 4, 2023
    Inventors: Alan Kozikowski, Gideon Shapiro, Werner Tueckmantel, John McCorvy
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 11512053
    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: August 27, 2020
    Date of Patent: November 29, 2022
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • 3,3-DIFLUOROPIPERIDINE CARBAMATE HETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
    Publication number: 20220024937
    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: October 1, 2021
    Publication date: January 27, 2022
    Inventor: Gideon Shapiro
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 11185531
    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 26, 2020
    Date of Patent: November 30, 2021
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
    Patent number: 11136328
    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: March 5, 2020
    Date of Patent: October 5, 2021
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • TREATMENT OF AUTISM SPECTRUM DISORDERS, OBSESSIVE-COMPULSIVE DISORDER AND ANXIETY DISORDERS
    Publication number: 20210220365
    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: March 17, 2021
    Publication date: July 22, 2021
    Inventors: Gideon Shapiro, Dorothy G. Flood
  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20210155631
    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: March 18, 2020
    Publication date: May 27, 2021
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
    Patent number: 11000526
    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: Grant
    Filed: November 21, 2017
    Date of Patent: May 11, 2021
    Assignee: Rugen Holdings (Cayman) Limited
    Inventors: Gideon Shapiro, Dorothy G. Flood
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20210078951
    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: August 27, 2020
    Publication date: March 18, 2021
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 10800743
    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: September 7, 2018
    Date of Patent: October 13, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • 3,3-DIFLUOROPIPERIDINE CARBAMATE HETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
    Publication number: 20200299300
    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: March 5, 2020
    Publication date: September 24, 2020
    Inventor: Gideon Shapiro
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20200289469
    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: February 26, 2020
    Publication date: September 17, 2020
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 10632103
    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: January 26, 2018
    Date of Patent: April 28, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • CARM1 inhibitors and uses thereof
    Patent number: 10633389
    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: October 2, 2018
    Date of Patent: April 28, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
    Patent number: 10584127
    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: May 31, 2016
    Date of Patent: March 10, 2020
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • Crystalline Form of (R)-7-Chloro-N-(Quinuclidin-3-YL)benzo[B]thiophene-2-Carboxamide Hydrochloride Monohydrate
    Publication number: 20190315736
    Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.
    Type: Application
    Filed: October 26, 2018
    Publication date: October 17, 2019
    Inventors: Patricia Oliver-Shaffer, Gideon Shapiro, Richard Chesworth, Muneki Kishida, Takayuki Ishige