公开(公告)号：US20190060322A1

公开(公告)日：2019-02-28

申请号：US16120702

申请日：2018-09-04

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne KUNTZ ,  John Emmerson CAMPBELL ,  Masashi SEKI ,  Syuji SHIROTORI ,  Wataru ITANO ,  Wanjun ZHENG

IPC: A61K31/5377 ,  C07D405/12 ,  C07D401/12 ,  A61K31/4545 ,  C07D405/14 ,  A61K31/5375 ,  C07D213/64 ,  A61K31/4412

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.

公开(公告)号：US20180282312A1

公开(公告)日：2018-10-04

申请号：US16000539

申请日：2018-06-05

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

Inventor： Kevin Wayne KUNTZ ,  Hyeong Wook CHOI ,  Steven MATHIEU ,  Kristen SANDERS ,  Arani CHANDA

IPC: C07D405/12 ,  A61K31/5377 ,  C07D413/12

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.

公开(公告)号：US20170362217A1

公开(公告)日：2017-12-21

申请号：US15510588

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Lorna Helen MITCHELL ,  Andrew Simon BELL ,  Richard CHESWORTH ,  Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC: C07D451/04 ,  C07D487/08 ,  C07D413/14 ,  C07D519/00 ,  C07D413/12

CPC classification number: C07D451/04 ,  A61P35/00 ,  C07D413/12 ,  C07D413/14 ,  C07D487/08 ,  C07D519/00

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.

公开(公告)号：US20170143729A1

公开(公告)日：2017-05-25

申请号：US15199522

申请日：2016-06-30

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 ,  Frances FANG

IPC: A61K31/5377

CPC classification number: 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：US20240165121A1

公开(公告)日：2024-05-23

申请号：US18188700

申请日：2023-03-23

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne KUNTZ ,  John Emmerson Campbell ,  Masashi Seki ,  Syuji Shirotori ,  Wataru Itano ,  Wanjun Zheng

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/5375 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/5375 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14

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.

公开(公告)号：US20230101819A1

公开(公告)日：2023-03-30

申请号：US17532422

申请日：2021-11-22

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

公开(公告)号：US20190315725A1

公开(公告)日：2019-10-17

申请号：US16372657

申请日：2019-04-02

Applicant: Epizyme, Inc.

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

IPC: C07D405/12 ,  A61K31/704 ,  C07D213/64 ,  A61K31/436 ,  A61K31/4745 ,  A61K31/4412 ,  A61K31/573 ,  A61K31/7068 ,  A61K45/06 ,  A61K31/53 ,  A61K31/675 ,  A61K31/5377

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：US20180243315A1

公开(公告)日：2018-08-30

申请号：US15800983

申请日：2017-11-01

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne KUNTZ ,  Sarah Kathleen KNUTSON ,  Timothy James Nelson WIGLE ,  Robert A. COPELAND ,  Victoria M. RICHON ,  Margaret D. SCOTT ,  Christopher J. SNEERINGER ,  Roy M. POLLOCK

IPC: A61K31/5377 ,  A61K31/4545 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/551 ,  A61K31/7076 ,  C12Q1/68 ,  A61K31/496 ,  A61K31/711 ,  A61K38/17 ,  G01N33/574 ,  G01N33/50 ,  C12Q1/48 ,  C07D473/34 ,  C07D405/12 ,  A61K31/4412

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/551 ,  A61K31/7076 ,  A61K31/711 ,  A61K38/17 ,  C07D405/12 ,  C07D473/34 ,  C12Q1/48 ,  C12Q1/68 ,  G01N33/5011 ,  G01N33/57426 ,  G01N2333/91011 ,  G01N2333/91017 ,  G01N2800/52 ,  Y10T436/143333

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.

公开(公告)号：US20180230110A1

公开(公告)日：2018-08-16

申请号：US15510589

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Richard CHESWORTH ,  Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  Lorna Helen MITCHELL ,  Russell C. PETTER ,  Carl Eric SCHWARTZ

IPC: C07D261/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D413/12

CPC classification number: C07D261/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D413/12

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.

公开(公告)号：US20170362191A1

公开(公告)日：2017-12-21

申请号：US15510605

申请日：2015-09-09

Applicant: EPIZYME, INC.

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

IPC: C07D261/08

CPC classification number: C07D261/08 ,  C07D261/18

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.