Patents Assigned to Epizyme, Inc.
  • Substituted isoxazoles for treating cancer
    Patent number: 10106510
    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: Grant
    Filed: September 9, 2015
    Date of Patent: October 23, 2018
    Assignee: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Michael John Munchhof
  • Substituted benzene compounds
    Patent number: 10098888
    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: November 22, 2016
    Date of Patent: October 16, 2018
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
  • Substituted benzene compounds
    Patent number: 10092572
    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: October 15, 2013
    Date of Patent: October 9, 2018
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki, Syuji Shirotori, Wataru Itano, Wanjun Zheng
  • HYDROCHLORIDE SALT FORM FOR EZH2 INHIBITION
    Publication number: 20180282312
    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: Application
    Filed: June 5, 2018
    Publication date: October 4, 2018
    Applicants: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin Wayne KUNTZ, Hyeong Wook CHOI, Steven MATHIEU, Kristen SANDERS, Arani CHANDA
  • 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
  • Isoxazole Carboxamides as Irreversible SMYD Inhibitors
    Publication number: 20180230110
    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: Application
    Filed: September 9, 2015
    Publication date: August 16, 2018
    Applicant: EPIZYME, INC.
    Inventors: Richard CHESWORTH, Megan Alene Cloonan FOLEY, Kevin Wayne KUNTZ, Lorna Helen MITCHELL, Russell C. PETTER, Carl Eric SCHWARTZ
  • PRMT1 inhibitors and uses thereof
    Patent number: 10039748
    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: Grant
    Filed: August 8, 2016
    Date of Patent: August 7, 2018
    Assignee: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Kevin Wayne Kuntz
  • Hydrochloride salt form for EZH2 inhibition
    Patent number: 10040782
    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: October 15, 2014
    Date of Patent: August 7, 2018
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin W. Kuntz, Hyeong-wook Choi, Steven Mathieu, Kristen Sanders, Arani Chanda
  • PRMT5 INHIBITORS CONTAINING A DIHYDRO- OR TETRAHYDROISOQUINOLINE AND USES THEREOF
    Publication number: 20180162847
    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: Application
    Filed: July 18, 2017
    Publication date: June 14, 2018
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Inhibitors of human EZH2, and methods of use thereof
    Patent number: 9949999
    Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
    Type: Grant
    Filed: April 19, 2016
    Date of Patent: April 24, 2018
    Assignee: Epizyme, Inc.
    Inventors: Robert A. Copeland, Victoria M. Richon, Margaret D. Scott, Christopher J. Sneeringer, Kevin W. Kuntz, Sarah K. Knutson, Roy M. Pollock
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20180105497
    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: August 11, 2017
    Publication date: April 19, 2018
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 9943504
    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: Grant
    Filed: June 10, 2016
    Date of Patent: April 17, 2018
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • PRMT5 Inhibitors and Uses Thereof
    Publication number: 20180098987
    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: May 4, 2017
    Publication date: April 12, 2018
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • SUBSTITUTED 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS
    Publication number: 20180072702
    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: Application
    Filed: April 20, 2017
    Publication date: March 15, 2018
    Applicant: Epizyme, Inc.
    Inventors: Kevin Wayne KUNTZ, Edward James OLHAVA, Richard CHESWORTH, Kenneth William DUNCAN
  • PRMT5 inhibitors and uses thereof
    Patent number: 9908887
    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: December 20, 2013
    Date of Patent: March 6, 2018
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Method for treating cancer
    Patent number: 9889138
    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: July 15, 2016
    Date of Patent: February 13, 2018
    Assignee: Epizyme, Inc.
    Inventor: Heike Keilhack
  • Salt form of a human histone methyltransferase EZH2 inhibitor
    Patent number: 9872862
    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: June 30, 2016
    Date of Patent: January 23, 2018
    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, Frances Fang
  • PRMT1 inhibitors and uses thereof
    Patent number: 9868703
    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: September 26, 2016
    Date of Patent: January 16, 2018
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
  • CARM1 inhibitors and uses thereof
    Patent number: 9856267
    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: July 13, 2017
    Date of Patent: January 2, 2018
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Aryl-or heteroaryl-substituted benzene compounds
    Patent number: 9855275
    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: May 17, 2017
    Date of Patent: January 2, 2018
    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