公开(公告)号：US09243001B2

公开(公告)日：2016-01-26

申请号：US14210638

申请日：2014-03-14

Applicant: Epizyme, Inc.

Inventor： John Emmerson Campbell ,  Kevin Wayne Kuntz

IPC: C07D491/02 ,  A61K31/44 ,  C07D513/04 ,  C07D471/04 ,  C07D231/56 ,  C07D235/14 ,  C07D277/30 ,  C07D277/64 ,  C07D263/56 ,  C07D405/12 ,  C07D409/12

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：US20150266854A1

公开(公告)日：2015-09-24

申请号：US14733690

申请日：2015-06-08

Applicant: Epizyme, Inc.

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

IPC: C07D401/12 ,  C07D471/04

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.

Abstract translation: 本发明涉及取代的6,5-稠合双环杂芳基化合物。 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。

公开(公告)号：US20150174136A1

公开(公告)日：2015-06-25

申请号：US14639878

申请日：2015-03-05

Applicant: EPIZYME, INC.

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

IPC: A61K31/5377 ,  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.

Abstract translation: 本发明涉及取代的苯化合物。 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：US20140296283A1

公开(公告)日：2014-10-02

申请号：US14211248

申请日：2014-03-14

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。

公开(公告)号：US20140288129A1

公开(公告)日：2014-09-25

申请号：US14212965

申请日：2014-03-14

Applicant: Epizyme, Inc.

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

IPC: C07D405/12 ,  C07D401/12 ,  C07D231/12

CPC classification number: A61K31/4155 ,  A61K31/415 ,  A61K31/455 ,  C07D231/12 ,  C07D401/12 ,  C07D405/12

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.

Abstract translation: 本文描述了式（I-a）和（I-b）的化合物，其药学上可接受的盐及其药物组合物。 本发明化合物可用于抑制PRMT1活性。 还描述了使用该化合物治疗PRMT1介导的病症的方法。

公开(公告)号：US20140288124A1

公开(公告)日：2014-09-25

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: C07D231/56 ,  C07D403/12 ,  C07D401/12

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.

公开(公告)号：US20140288041A1

公开(公告)日：2014-09-25

申请号：US14275667

申请日：2014-05-12

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 ,  C07D405/14 ,  C07D405/12 ,  C07D401/12

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：US08765732B2

公开(公告)日：2014-07-01

申请号：US13722807

申请日：2012-12-20

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: A61K31/00 ,  A61K31/55 ,  A61K31/535 ,  A61K31/445 ,  A61K31/44 ,  C07D281/02 ,  C07D243/08 ,  C07D419/00 ,  C07D401/00

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：US20140073597A1

公开(公告)日：2014-03-13

申请号：US14018171

申请日：2013-09-04

Applicant: Epizyme, Inc.

Inventor： Richard Chesworth ,  Kevin Wayne Kuntz ,  Edward James Olhava ,  Michael A. Patane

IPC: C07H19/14

CPC classification number: C07H19/14 ,  C07D487/04

Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.

Abstract translation: 公开了化合物，含有这些化合物的药物组合物，化合物和组合物用作组蛋白甲基转移酶的调节剂，以及治疗受组蛋白甲基转移酶活性调节影响的疾病的方法。

公开(公告)号：US20250109123A1

公开(公告)日：2025-04-03

申请号：US18734942

申请日：2024-06-05

Applicant: Epizyme, Inc.

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

IPC: C07D405/12 ,  A61K31/436 ,  A61K31/4412 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/53 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/573 ,  A61K31/675 ,  A61K31/704 ,  A61K31/7068 ,  A61K33/243 ,  A61K45/06 ,  A61P35/00 ,  C07D213/64 ,  C07D413/14

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.