公开(公告)号：US20250064822A1

公开(公告)日：2025-02-27

申请号：US18941480

申请日：2024-11-08

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

Inventor： Heike Keilhack ,  Brett Truitt ,  Yuta Suzuki ,  Tsukasa Murase ,  Futoshi Shikata

IPC: A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K9/28 ,  A61P35/00

Abstract: The present invention relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).

公开(公告)号：US11642347B2

公开(公告)日：2023-05-09

申请号：US16808513

申请日：2020-03-04

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

Inventor： Heike Keilhack ,  Sarah K. Knutson ,  Danielle Johnston Blackwell ,  Larisa Reyderman ,  Lone Ottesen

IPC: A61P35/02 ,  A61K31/4412 ,  A61K31/5377 ,  C07D213/65 ,  C07D405/12 ,  A61K31/4545

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  C07D213/65 ,  C07D405/12

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.

公开(公告)号：US11026949B2

公开(公告)日：2021-06-08

申请号：US16562683

申请日：2019-09-06

Applicant: Epizyme, Inc. ,  Health Research, Inc.

Inventor： Heike Keilhack ,  Roberto Pili

IPC: A61K31/5377 ,  A61K31/404 ,  A61K31/444 ,  A61K31/506 ,  A61K31/517 ,  A61K31/4412 ,  A61K31/44 ,  A61K45/06 ,  A61P35/00 ,  A61K31/496

Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

公开(公告)号：US10946024B2

公开(公告)日：2021-03-16

申请号：US16444579

申请日：2019-06-18

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack

IPC: A61K31/5377 ,  A61K45/06 ,  A61K31/45 ,  A61K31/453 ,  A61P35/00 ,  A61P37/00 ,  A61K31/5375

Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.

公开(公告)号：US10420775B2

公开(公告)日：2019-09-24

申请号：US15816907

申请日：2017-11-17

Applicant: Epizyme, Inc.

Inventor： Kevin W. Kuntz ,  Richard Chesworth ,  Kenneth W. Duncan ,  Heike Keilhack ,  Natalie Warholic ,  Christine Klaus ,  Sarah K. Knutson ,  Timothy J. N. Wigle ,  Masashi Seki ,  Syuji Shirotori ,  Satoshi Kawano

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

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.

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：US12168015B2

公开(公告)日：2024-12-17

申请号：US18606925

申请日：2024-03-15

Applicant: Epizyme, Inc.

Inventor： Kevin W. Kuntz ,  Richard Chesworth ,  Kenneth W. Duncan ,  Heike Keilhack ,  Natalie Warholic ,  Christine Klaus ,  Sarah K. Knutson ,  Timothy J. N. Wigle ,  Masashi Seki ,  Syuji Shirotori ,  Satoshi Kawano

IPC: 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.

公开(公告)号：US11642349B2

公开(公告)日：2023-05-09

申请号：US17128634

申请日：2020-12-21

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack ,  Sarah K. Knutson

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61P35/00 ,  A61K9/00

CPC classification number: A61K31/5377 ,  A61K9/0053 ,  A61K31/4412 ,  A61K31/4545 ,  A61P35/00

Abstract: The present disclosure relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).

公开(公告)号：US10369155B2

公开(公告)日：2019-08-06

申请号：US15851978

申请日：2017-12-22

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack

IPC: A61K31/45 ,  A61K45/06 ,  A61P35/00 ,  A61P37/00 ,  A61K31/453 ,  A61K31/5375 ,  A61K31/5377

Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.

公开(公告)号：US10166238B2

公开(公告)日：2019-01-01

申请号：US15319535

申请日：2015-06-17

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

Inventor： Heike Keilhack ,  Sarah K. Knutson ,  Danielle Johnston Blackwell ,  Larisa Reyderman ,  Lone Ottesen

IPC: A61K31/5375 ,  A61K31/4427 ,  A61K31/44 ,  A61K31/5377 ,  C07D213/65 ,  C07D405/12 ,  A61K31/4412 ,  A61K31/4545

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.