Patents Assigned to Epizyme, Inc.
  • Patent number: 11951109
    Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: November 15, 2021
    Date of Patent: April 9, 2024
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah Kathleen Knutson, Danielle Johnston Blackwell
  • Patent number: 11952572
    Abstract: The present disclosure provides methods and pharmaceutical compositions for treating or slowing the progression of cancer, i.e., pancreatic cancer or esophageal cancer, by administering to a human subject in need thereof a therapeutically effective amount of an inhibitor of the histone methyltransferase, SETD2.
    Type: Grant
    Filed: August 14, 2018
    Date of Patent: April 9, 2024
    Assignee: Epizyme, Inc.
    Inventors: Alexandra Rose Grassian, Michael Thomenius, Jennifer Anne Totman
  • Patent number: 11951108
    Abstract: The disclosure relates to a method for treatment of cancer comprising administering to a subject in need thereof a first agent in a therapeutically effective amount and a second agent in a therapeutically effective amount. Preferably, the first agent comprises an EZH2 inhibitor, e.g., tazemetostat or a pharmaceutically acceptable salt thereof. In certain embodiments, the methods of the disclosure are used to treat breast cancer, ovarian cancer, or both.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: April 9, 2024
    Assignee: EPIZYME, INC.
    Inventor: Maria Alejandra Raimondi
  • 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
  • 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
  • Publication number: 20230357208
    Abstract: The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: February 16, 2023
    Publication date: November 9, 2023
    Applicant: Epizyme, Inc.
    Inventors: Darren Martin Harvey, John Emmerson Campbell, Kenneth William Duncan
  • Patent number: 11786533
    Abstract: The disclosure provides a method for treating cancer in a subject in need thereof comprising administering to the subject: (a) a therapeutically effective amount of an EZH2 inhibitor and (b) a therapeutically effective amount of an immune checkpoint inhibitor. In certain embodiments of the methods of the disclosure, the EZH2 inhibitor is tazemetostat.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: October 17, 2023
    Assignee: Epizyme, Inc.
    Inventors: Scott Ribich, Michael Thomenius
  • Patent number: 11753433
    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
    Type: Grant
    Filed: April 5, 2021
    Date of Patent: September 12, 2023
    Assignee: EPIZYME, INC.
    Inventor: Edward James Olhava
  • 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
  • Patent number: 11685732
    Abstract: The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: June 27, 2023
    Assignee: Epizyme, Inc.
    Inventors: Darren Martin Harvey, John Emmerson Campbell, Kenneth William Duncan
  • Patent number: 11672800
    Abstract: The present disclosure relates to a method of preventing or treating a cancer via administering an EHMT2 inhibitor or a combination comprising an EHMT2 inhibitor compound and one or more additional therapeutic agent disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds or combinations for research or other non-therapeutic purposes.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: June 13, 2023
    Assignee: Epizyme, Inc.
    Inventors: John Emmerson Campbell, Kenneth William Duncan, Maria Alejandra Raimondi, Christine Klaus, Elayne Penebre
  • Patent number: 11642348
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: July 9, 2020
    Date of Patent: May 9, 2023
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki, Syuji Shirotori, Wataru Itano, Wanjun Zheng
  • Patent number: 11642349
    Abstract: The present disclosure relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).
    Type: Grant
    Filed: December 21, 2020
    Date of Patent: May 9, 2023
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah K. Knutson
  • Patent number: 11642347
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.
    Type: Grant
    Filed: March 4, 2020
    Date of Patent: May 9, 2023
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Heike Keilhack, Sarah K. Knutson, Danielle Johnston Blackwell, Larisa Reyderman, Lone Ottesen
  • Patent number: 11642346
    Abstract: The present disclosure relates to methods of a malignant rhabdoid tumor (MRT), a rhabdoid tumor of the kidney (RTK), an atypical teratoid/rhabdoid tumor (AT/RT), an epithelioid malignant peripheral nerve sheath tumor, a myoepithelial carcinoma, and/or a renal medullary carcinoma by using an EZH2 inhibitor in combination with one or more additional treatment modalities.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: May 9, 2023
    Assignee: Epizyme, Inc.
    Inventors: Christine Klaus, Maria Alejandra Raimondi
  • Publication number: 20230133671
    Abstract: The present disclosure provides SETD2 protein inhibitors, and methods, compositions, and kits for treating diseases, disorders, or conditions in a subject with a SETD2 protein inhibitor and, optionally, a second therapeutic agent, wherein the second therapeutic agent comprises one or more glucocorticoid receptor agonists, one or more immunomodulatory drugs, one or more proteasome inhibitors, one or more Bcl-2 inhibitors, one or more pleiotropic pathway modulators, one or more XPO1 inhibitors, one or more histone deacetylase inhibitors, or one or more EZH2 inhibitors, or a combination thereof.
    Type: Application
    Filed: February 19, 2021
    Publication date: May 4, 2023
    Applicant: EPIZYME, INC.
    Inventors: Maria Alejandra RAIMONDI, Jennifer Anne TOTMAN, Vinny MOTWANI, Katherine Louise COSMOPOULOS, John LAMPE
  • Patent number: 11633420
    Abstract: The present invention relates to methods of treating disorders in which DOT1L-mediated protein methylation plays a part, such as cancer, by administering DOT1L inhibitor compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: January 4, 2021
    Date of Patent: April 25, 2023
    Assignee: Epizyme, Inc.
    Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott Richard Daigle
  • Patent number: 11602529
    Abstract: The disclosure provides methods of treating, identifying and/or selecting for treatment a subject having a cancer in which an immune checkpoint protein is upregulated. In certain embodiments, the methods for treating cancer in a subject in need thereof comprise administering to the subject: (a) a therapeutically effective amount of an EZH2 inhibitor and (b) a therapeutically effective amount of an immune checkpoint inhibitor. In certain embodiments of the methods of the disclosure, the EZH2 inhibitor is tazemetostat.
    Type: Grant
    Filed: June 1, 2018
    Date of Patent: March 14, 2023
    Assignee: Epizyme, Inc.
    Inventors: Scott Daigle, Kat Cosmopoulos
  • Publication number: 20230046656
    Abstract: The present disclosure provides novel cancer therapies. The treatment of cancers harboring EP300 mutations with CREBBP inhibition therapy is described.
    Type: Application
    Filed: February 9, 2022
    Publication date: February 16, 2023
    Applicant: Epizyme, Inc.
    Inventors: Alexandra Grassian, Scott Ribich, Jesse Smith, Darren Martin Harvey
  • Patent number: 11572383
    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
    Type: Grant
    Filed: September 18, 2020
    Date of Patent: February 7, 2023
    Assignee: Epizyme, Inc.
    Inventor: Edward J. Olhava