公开(公告)号：US20140315945A1

公开(公告)日：2014-10-23

申请号：US14210638

申请日：2014-03-14

Applicant: Epizyme, Inc.

Inventor： John Emmerson Campbell ,  Kevin Wayne Kuntz

IPC: C07D513/04 ,  C07D231/56 ,  C07D235/14 ,  C07D409/12 ,  C07D277/64 ,  C07D263/56 ,  C07D405/12 ,  C07D471/04 ,  C07D277/30

CPC classification number: C07D513/04 ,  C07D231/56 ,  C07D233/64 ,  C07D235/14 ,  C07D263/56 ,  C07D277/28 ,  C07D277/30 ,  C07D277/64 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention relates to azole 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.

Abstract translation: 本发明涉及唑化合物。 本发明还涉及含有这些化合物的药物组合物和通过将这些化合物和药物组合物施用于有需要的受试者来治疗癌症的方法。 本发明还涉及这些化合物用于研究或其它非治疗目的的用途。

公开(公告)号：US08598167B1

公开(公告)日：2013-12-03

申请号：US13938067

申请日：2013-07-09

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne Kuntz ,  Edward James Olhava ,  Richard Chesworth ,  Kenneth William Duncan

IPC: C07D471/04 ,  A61K31/4738 ,  A61P35/00

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：US11370781B2

公开(公告)日：2022-06-28

申请号：US16985404

申请日：2020-08-05

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack ,  Sarah Kathleen Knutson ,  Kevin Wayne Kuntz

IPC: A61K31/5355 ,  C07D213/64 ,  A61K31/4412 ,  C07D413/14 ,  A61P35/00 ,  C07D405/12 ,  A61K45/06 ,  A61K31/436 ,  A61K31/53 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7068 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/444 ,  A61K33/243 ,  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：US20210060027A1

公开(公告)日：2021-03-04

申请号：US16924962

申请日：2020-07-09

Applicant: Epizyme, Inc.

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

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

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：US10301290B2

公开(公告)日：2019-05-28

申请号：US14394463

申请日：2013-04-12

Applicant: EPIZYME, INC.

Inventor： Heike Keilhack ,  Sarah Kathleen Knutson ,  Kevin Wayne Kuntz

IPC: C07D213/64 ,  A61K31/4412 ,  C07D405/12 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/436 ,  A61K31/53 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7068 ,  A61K31/4745 ,  A61K31/675 ,  A61K33/24

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：US10266526B2

公开(公告)日：2019-04-23

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: A61K31/4192 ,  C07D249/04 ,  C07D451/04 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D401/12 ,  C07D241/26 ,  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：US10245269B2

公开(公告)日：2019-04-02

申请号：US15837390

申请日：2017-12-11

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：US10227307B2

公开(公告)日：2019-03-12

申请号：US15850367

申请日：2017-12-21

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne Kuntz ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Richard Chesworth ,  Paula Ann Boriack-Sjodin

IPC: C07D231/12 ,  A61K31/415

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.

公开(公告)号：US20190022064A1

公开(公告)日：2019-01-24

申请号：US16042542

申请日：2018-07-23

Applicant: Epizyme, Inc.

Inventor： Lorna Helen Mitchell ,  Gideon Shapiro ,  Richard Chesworth ,  Paula Ann Boriack-Sjodin ,  Oscar Miguel Moradei ,  Kevin Wayne Kuntz

IPC: A61K31/4155 ,  A61K31/415 ,  A61K31/455 ,  C07D405/12 ,  C07D401/12 ,  C07D231/12

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.

公开(公告)号：US10174019B2

公开(公告)日：2019-01-08

申请号：US15162384

申请日：2016-05-23

Applicant: Epizyme, Inc.

Inventor： John Emmerson Campbell ,  Kevin Wayne Kuntz

IPC: C07D401/02 ,  C07D401/14 ,  A61K31/437 ,  C07D401/10 ,  A61K31/4353 ,  C07D471/04 ,  C07D231/56 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D519/00

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.