公开(公告)号：US20220281854A1

公开(公告)日：2022-09-08

申请号：US17751153

申请日：2022-05-23

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah Kathleen KNUTSON ,  Kevin Wayne KUNTZ

IPC: C07D405/12 ,  A61K45/06 ,  A61K31/436 ,  A61K31/53 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7068 ,  C07D213/64 ,  A61K31/4412 ,  A61K31/5377 ,  A61K31/4439 ,  C07D413/14 ,  A61K31/444 ,  A61P35/00 ,  A61K33/243 ,  A61K31/5355 ,  A61K31/4745 ,  A61K31/675

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.

公开(公告)号：US20210198277A1

公开(公告)日：2021-07-01

申请号：US17100489

申请日：2020-11-20

Applicant: Epizyme, Inc.

Inventor： John Emmerson CAMPBELL ,  Kenneth William DUNCAN ,  Megan Alene FOLEY ,  Darren Martin HARVEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC: C07D498/04 ,  C07D401/12 ,  C07D239/48 ,  C07D231/38 ,  C07D213/74 ,  C07D215/38 ,  C07D239/49 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D473/32 ,  C07D487/04 ,  C07D491/044

Abstract: The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US20210198252A1

公开(公告)日：2021-07-01

申请号：US16864891

申请日：2020-05-01

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan Foley ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC: C07D451/04 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D401/12 ,  C07D241/26 ,  C07D249/04 ,  C07D261/10 ,  C07D263/34 ,  C07D275/03 ,  C07D209/08 ,  C07D277/56 ,  C07C271/18 ,  C07D205/04 ,  C07D211/34 ,  C07D237/24 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14

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 a SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US20190269692A1

公开(公告)日：2019-09-05

申请号：US16270752

申请日：2019-02-08

Applicant: Epizyme, Inc. ,  Eisai R&D Management Co., Ltd.

Inventor： Kevin Wayne KUNTZ ,  Kuan-Chun HUANG ,  Hyeong Wook CHOI ,  Kristen SANDERS ,  Steven MATHIEU ,  Arani CHANDA ,  Francis FANG

IPC: A61K31/5377 ,  C07D405/12

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.

公开(公告)号：US20180280422A1

公开(公告)日：2018-10-04

申请号：US15802979

申请日：2017-11-03

Applicant: Epizyme, Inc.

Inventor： Edward J. OLHAVA ,  Richard CHESWORTH ,  Kevin Wayne KUNTZ ,  Victoria M. RICHON ,  Roy M. POLLOCK ,  Scott R. DAIGLE

IPC: A61K31/7076 ,  C07H19/14 ,  C07D487/04 ,  C07H19/16 ,  A61K31/519 ,  A61K31/7064 ,  A61K31/52 ,  C07D473/34

Abstract: The present invention relates to substituted purine and 7-deazapurine 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 and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20180072702A1

公开(公告)日：2018-03-15

申请号：US15492506

申请日：2017-04-20

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne KUNTZ ,  Edward James OLHAVA ,  Richard CHESWORTH ,  Kenneth William DUNCAN

IPC: C07D401/12 ,  C07D471/04 ,  C07D413/14 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D401/12 ,  A61P35/00 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

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.

公开(公告)号：US20170355695A1

公开(公告)日：2017-12-14

申请号：US15510586

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC: C07D451/04 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D237/24 ,  C07D211/34 ,  C07D401/14 ,  C07D205/04 ,  C07C271/18 ,  C07D249/04 ,  C07D417/14 ,  C07D231/14 ,  C07D401/12

CPC classification number: C07D451/04 ,  C07C271/18 ,  C07D205/04 ,  C07D209/08 ,  C07D211/34 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D237/24 ,  C07D241/26 ,  C07D249/04 ,  C07D261/10 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14

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.

公开(公告)号：US20170247326A1

公开(公告)日：2017-08-31

申请号：US15510583

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC: C07D207/14 ,  C07D417/12 ,  C07D405/12 ,  C07D413/12 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D207/14 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

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.