Patents Assigned to Epizyme, Inc.
  • Method for treating cancer
    Patent number: 10786511
    Abstract: The present invention 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: November 17, 2015
    Date of Patent: September 29, 2020
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Heike Keilhack, Brett Truitt, Yuta Suzuki, Tsukasa Murase, Futoshi Shikata
  • Hydrochloride salt form for EZH2 inhibition
    Patent number: 10710987
    Abstract: Provided herein are novel solid forms of 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 hydrochloride, and related compositions and methods.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: July 14, 2020
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin Wayne Kuntz, Hyeong Wook Choi, Steven Mathieu, Kristen Sanders, Arani Chanda
  • Isoxazole carboxamides as irreversible SMYD inhibitors
    Patent number: 10669243
    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: Grant
    Filed: January 11, 2019
    Date of Patent: June 2, 2020
    Assignee: EPIZYME, INC.
    Inventors: Richard Chesworth, Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Jennifer C. Petter, Carl Eric Schwartz
  • PRMT5 inhibitors and uses thereof
    Patent number: 10653693
    Abstract: Described herein are methods of treating cancer using one or more PRMT5 inhibitors, for example using one or more compounds of Formulae (1-5) or (A-F), pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions thereof. Described herein are methods of treating cancer using one or more PRMT5 inhibitors, for example using one or more compounds of Formulae (1-5) or (A-F), pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions thereof.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: May 19, 2020
    Assignees: Epizyme, Inc., Glaxosmithkline Intellectual Property Development Limited
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin, Elayne Penebre, Olena I. Barbash
  • 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
  • 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
  • Substituted Cyclohexylamine Compounds
    Publication number: 20200123142
    Abstract: The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, and R7 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: October 19, 2018
    Publication date: April 23, 2020
    Applicant: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Michael John Munchhof
  • SUBSTITUTED PYRROLIDINE COMPOUNDS
    Publication number: 20200102314
    Abstract: The present disclosure provides substituted pyrrolidine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, 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: Application
    Filed: August 5, 2019
    Publication date: April 2, 2020
    Applicant: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Michael John Munchhof, Darren Martin Harvey
  • Substituted piperidine compounds
    Patent number: 10577363
    Abstract: The present disclosure provides substituted piperidine compounds having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, 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: March 3, 2020
    Assignee: EPIZYME, INC.
    Inventors: Lorna Helen Mitchell, Andrew Simon Bell, Richard Chesworth, Megan Alene Cloonan Foley, Kevin Wayne Kuntz, James Edward John Mills, Michael John Munchhof
  • Combination therapy for treating cancer
    Patent number: 10525074
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 7, 2020
    Assignee: Epizyme, Inc.
    Inventors: Christine Klaus, Maria Alejandra Raimondi, Scott R. Daigle, Roy MacFarlane Pollock
  • Method for treating cancer
    Patent number: 10493076
    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: August 24, 2016
    Date of Patent: December 3, 2019
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah K. Knutson
  • Combination therapy for treating cancer
    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
  • Combination therapy for treating cancer
    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
  • Isoxazole carboxamide compounds
    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
  • Aryl-or heteroaryl-substituted benzene compounds
    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
  • Substituted purine compounds
    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
  • PRMT5 inhibitors and uses therof
    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
  • Isoxazole Carboxamides as Irreversible SMYD Inhibitors
    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
  • Method for treating cancer
    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
  • Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof
    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