公开(公告)号：US20180243316A1

公开(公告)日：2018-08-30

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

CPC classification number: A61K31/5377 ,  C07D405/12 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411

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：US20170198006A1

公开(公告)日：2017-07-13

申请号：US15321280

申请日：2015-06-25

Applicant: Epizyme, Inc.

Inventor： Kenneth W. Duncan ,  Richard Chesworth ,  Gideon Shapiro ,  Edward James Olhava ,  Michael A. Patane ,  Michael John Munchhof ,  Kevin Wayne Kuntz ,  Lei Jin

IPC: C07H19/16 ,  C07D405/06 ,  C07D401/12 ,  C07D403/04 ,  C07C311/41 ,  C07D233/64 ,  C07D207/14

CPC classification number: C07H19/16 ,  A61P3/00 ,  A61P3/10 ,  A61P7/00 ,  A61P35/00 ,  C07C311/41 ,  C07D205/04 ,  C07D207/14 ,  C07D207/273 ,  C07D211/28 ,  C07D231/12 ,  C07D233/64 ,  C07D233/88 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D487/04 ,  C07D513/04 ,  C07H19/167

Abstract: Described herein are compounds of Formula (I)-(XIII), 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.

公开(公告)号：US09637472B2

公开(公告)日：2017-05-02

申请号：US14536162

申请日：2014-11-07

Applicant: Epizyme, Inc.

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

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

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：US09394258B2

公开(公告)日：2016-07-19

申请号：US14213144

申请日：2014-03-14

Applicant: Epizyme, Inc.

Inventor： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kevin Wayne Kuntz

IPC: A61K31/44 ,  A61K31/415 ,  C07D401/00 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12

CPC classification number: C07D231/56 ,  A61K31/416 ,  A61K31/4439 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12

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.

Abstract translation: 本文描述了式（I）的化合物，其药学上可接受的盐及其药物组合物。 本发明的化合物可用于抑制精氨酸甲基转移酶活性。 还描述了使用该化合物治疗精氨酸甲基转移酶介导的病症的方法。

公开(公告)号：US09334527B2

公开(公告)日：2016-05-10

申请号：US14290642

申请日：2014-05-29

Applicant: EPIZYME, INC.

Inventor： Kevin Wayne Kuntz ,  Sarah Kathleen Knutson ,  Timothy James Nelson Wigle

IPC: A61P35/00 ,  C12Q1/68 ,  C07D473/34 ,  C12Q1/48 ,  G01N33/50 ,  G01N33/574 ,  A61K31/711 ,  A61K38/17 ,  C07D405/12 ,  A61P35/02

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：US20160024017A1

公开(公告)日：2016-01-28

申请号：US14775246

申请日：2014-03-14

Applicant: EPIZYME, INC.

Inventor： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kevin Wayne Kuntz

IPC: C07D231/56 ,  C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/04

CPC classification number: C07D231/56 ,  A61K31/416 ,  A61K31/4439 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12

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.

公开(公告)号：US20150353494A1

公开(公告)日：2015-12-10

申请号：US14742481

申请日：2015-06-17

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne Kuntz ,  Richard Chesworth ,  Kenneth William Duncan ,  Heike Keilhack ,  Natalie Warholic ,  Christine Klaus ,  Sarah Kathleen Knutson ,  Timothy James Nelson Wigle ,  Masashi Seki ,  Syuji Shirotori ,  Satoshi Kawano

IPC: C07D213/64 ,  C07D401/12 ,  C07D498/08 ,  C07D405/14

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

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.

Abstract translation: 本发明涉及芳基或杂芳基取代的苯化合物。 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：US20150352119A1

公开(公告)日：2015-12-10

申请号：US14742466

申请日：2015-06-17

Applicant: EPIZYME, INC.

Inventor： Kevin Wayne Kuntz ,  John Emmerson Campbell ,  Masashi Seki

IPC: A61K31/5375 ,  A61K31/4545 ,  A61K31/4412

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：US20150284370A1

公开(公告)日：2015-10-08

申请号：US14435704

申请日：2013-10-15

Applicant: EPIZYME, INC.

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

IPC: C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D213/64

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：US20150246916A1

公开(公告)日：2015-09-03

申请号：US14699100

申请日：2015-04-29

Applicant: EPIZYME, INC.

Inventor： John Emmerson Campbell ,  Kevin Wayne Kuntz

IPC: C07D471/04 ,  C07D231/56

CPC classification number: C07D471/04 ,  C07D231/56 ,  C07D401/14 ,  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.

Abstract translation: 本发明涉及唑类双环杂芳基化合物。 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。