Patents Assigned to Epizyme, Inc.
  • Patent number: 10463671
    Abstract: The present invention 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 10, 2017
    Date of Patent: November 5, 2019
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah K. Knutson, Kevin W. Kuntz
  • Patent number: 10456407
    Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: October 29, 2019
    Assignees: Epizyme, Inc., Health Research, Inc.
    Inventors: Heike Keilhack, Roberto Pili
  • Patent number: 10428029
    Abstract: The present disclosure provides substituted isoxazole carboxamide compounds having Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, A, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: October 1, 2019
    Assignee: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, James Edward John Mills, Lorna Helen Mitchell, Michael John Munchhof, Darren Martin Harvey
  • Patent number: 10420775
    Abstract: The present invention relates to aryl- or heteroaryl-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: November 17, 2017
    Date of Patent: September 24, 2019
    Assignee: Epizyme, Inc.
    Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy J. N. Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
  • Patent number: 10400005
    Abstract: The present invention relates to substituted purine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: September 3, 2019
    Assignee: Epizyme, Inc.
    Inventor: Nigel J. Waters
  • Patent number: 10391089
    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 PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: August 27, 2019
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20190241529
    Abstract: The present disclosure provides provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, X, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Application
    Filed: January 11, 2019
    Publication date: August 8, 2019
    Applicant: EPIZYME, INC.
    Inventors: Richard Chesworth, Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Jennifer C. Petter, Carl Eric Schwartz
  • Patent number: 10369155
    Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: August 6, 2019
    Assignee: Epizyme, Inc.
    Inventor: Heike Keilhack
  • Patent number: 10307413
    Abstract: Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: June 4, 2019
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Patent number: 10301290
    Abstract: The present invention 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: April 12, 2013
    Date of Patent: May 28, 2019
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah Kathleen Knutson, Kevin Wayne Kuntz
  • Patent number: 10273223
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl 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.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: April 30, 2019
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 10266526
    Abstract: The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: April 23, 2019
    Assignee: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, James Edward John Mills, Lorna Helen Mitchell, Michael John Munchhof, Darren Martin Harvey
  • Patent number: 10245269
    Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4?-(morpholinomethyl)-[1,1?-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: April 2, 2019
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin Wayne Kuntz, Kuan-Chun Huang, Hyeong Wook Choi, Kristen Sanders, Steven Mathieu, Arani Chanda, Francis Fang
  • Publication number: 20190083482
    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 PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: September 18, 2017
    Publication date: March 21, 2019
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20190083504
    Abstract: The disclosure provides a method of treating a medulloblastoma in a subject in need thereof comprising administering to the subject a therapeutically-effective amount of an enhancer of a zeste homolog 2 (EZH2) inhibitor. In a preferred embodiment of this method, the subject is pediatric and the EZH2 inhibitor is Tazemetostat.
    Type: Application
    Filed: October 5, 2016
    Publication date: March 21, 2019
    Applicants: Epizyme, Inc., The Regents of the University of Colorado, A Body Corporate
    Inventors: Heike KEILHACK, Nigel J. WATERS, Rajeev VIBHAKAR
  • 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
  • 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
  • Patent number: 10179773
    Abstract: The present disclosure provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, X, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: January 15, 2019
    Assignee: EPIZYME, INC.
    Inventors: Richard Chesworth, Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Jennifer C. Petter, Carl Eric Schwartz
  • Patent number: 10174019
    Abstract: The present invention relates to azole bicyclic heteroaryl 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: May 23, 2016
    Date of Patent: January 8, 2019
    Assignee: Epizyme, Inc.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 10166238
    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: June 17, 2015
    Date of Patent: January 1, 2019
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Heike Keilhack, Sarah K. Knutson, Danielle Johnston Blackwell, Larisa Reyderman, Lone Ottesen