Patents Assigned to Epizyme, Inc.
  • Substituted Piperidine Compounds
    Publication number: 20170362217
    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: Application
    Filed: September 9, 2015
    Publication date: December 21, 2017
    Applicant: 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
  • Substituted Cyclohexylamine Compounds
    Publication number: 20170362191
    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: September 9, 2015
    Publication date: December 21, 2017
    Applicant: EPIZYME, INC.
    Inventors: Megan Alene Cloonan FOLEY, Kevin Wayne KUNTZ, Lorna Helen MITCHELL, Michael John MUNCHHOF
  • SMYD Inhibitors
    Publication number: 20170355695
    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: Application
    Filed: September 9, 2015
    Publication date: December 14, 2017
    Applicant: EPIZYME, INC.
    Inventors: Megan Alene Cloonan FOLEY, Kevin Wayne KUNTZ, James Edward John MILLS, Lorna Helen MITCHELL, Michael John MUNCHHOF, Darren Martin HARVEY
  • TETRAHYDRO- AND DIHYDRO-ISOQUINOLINE PRMT5 INHIBITORS AND USES THEREOF
    Publication number: 20170334861
    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: January 30, 2017
    Publication date: November 23, 2017
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20170305922
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R1, R2a, R2b, R3 and Ring B are as defined herein, and Ring A is a group of Formula (A-i), (A-ii), or (A-iii): wherein R, R, R, R, and R 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: September 17, 2015
    Publication date: October 26, 2017
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei JIn, Robert E. Babine
  • SALTS, CO-CRYSTALS, AMORPHOUS FORMS, AND CRYSTALLINE FORMS OF A CO-ACTIVATOR-ASSOCIATED ARGININE METHYLTRANSFERASE 1 (CARM1) INHIBITOR
    Publication number: 20170298073
    Abstract: Provided herein are solid forms (e.g., salts, co-crystals, amorphous forms, and crystalline forms) of methyl (R)-2-(2-(2-chloro-5-(2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate (compound 109-3). Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve the solid forms for inhibiting the activity of co-activator-associated arginine methyltransferase 1 (CARM1) and for treating CARM1-mediated disorders (e.g., proliferative disorders and metabolic disorders).
    Type: Application
    Filed: September 17, 2015
    Publication date: October 19, 2017
    Applicant: Epizyme, Inc
    Inventors: Edward James Olhava, Oscar Miguel Moradei, Gideon Shapiro, Richard Chesworth, Lei Jin, Robert E. Babine
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20170291905
    Abstract: Described herein are compounds of Formula (S-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: September 17, 2015
    Publication date: October 12, 2017
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, John Emmerson Campbell, Lawrence Alan Reiter, Kerren Kalai Swinger
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20170283400
    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: September 17, 2015
    Publication date: October 5, 2017
    Applicant: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Kerren Kalai Swinger, Gideon Shapiro, Paula Ann Boriack-Sjodin
  • CARM1 INHIBITORS AND USES THEREOF
    Publication number: 20170283440
    Abstract: Provided herein are compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1-R3, wherein L1 and R3 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: September 17, 2015
    Publication date: October 5, 2017
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Kenneth W. Duncan, Lorna Helen Mitchell, Lei Jin, Robert E. Babine
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20170280720
    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: September 17, 2015
    Publication date: October 5, 2017
    Applicant: Epizyme, Inc.
    Inventors: Richard CHESWORTH, Lorna Helen MITCHELL, Gideon SHAPIRO, Oscar Miguel MORADEI, Kevin Wayne KUNTZ, Kenneth W. DUNCAN, Lei JIN
  • Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
    Patent number: 9776972
    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: March 14, 2014
    Date of Patent: October 3, 2017
    Assignee: Epizyme Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Lei Jin, Kenneth W. Duncan
  • PRMT5 inhibitors and uses thereof
    Patent number: 9777008
    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: June 8, 2016
    Date of Patent: October 3, 2017
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Substituted 6,5-fused bicyclic heteroaryl compounds
    Patent number: 9776996
    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: March 14, 2014
    Date of Patent: October 3, 2017
    Assignee: Epizyme, Inc.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
    Publication number: 20170267642
    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 1, 2017
    Publication date: September 21, 2017
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
  • PRMT5 inhibitors and uses thereof
    Patent number: 9765068
    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: January 13, 2016
    Date of Patent: September 19, 2017
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Arginine methyltransferase inhibitors and uses thereof
    Patent number: 9765035
    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: March 14, 2014
    Date of Patent: September 19, 2017
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • Substituted Pyrrolidine Compounds
    Publication number: 20170253601
    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: September 9, 2015
    Publication date: September 7, 2017
    Applicant: EPIZYME, INC.
    Inventors: Megan Alene Cloonan FOLEY, Kevin Wayne KUNTZ, Lorna Helen MITCHELL, Michael John MUNCHHOF, Darren Martin HARVEY
  • Substituted Pyrrolidine Carboxamide Compounds
    Publication number: 20170247326
    Abstract: The present disclosure provides pyrrolidine carboxamide compounds having Formula I and the pharmaceutically acceptable salts and solvates thereof, wherein A, B, X, Y, 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: September 9, 2015
    Publication date: August 31, 2017
    Applicant: EPIZYME, INC.
    Inventors: Megan Alene Cloonan FOLEY, Kevin Wayne KUNTZ, Lorna Helen MITCHELL, Michael John MUNCHHOF, Darren Martin HARVEY
  • PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
    Patent number: 9745291
    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: August 29, 2017
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • PRMT5 INHIBITORS AND USES THEREOF
    Publication number: 20170240537
    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: February 21, 2017
    Publication date: August 24, 2017
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof