公开(公告)号：US20190240230A1

公开(公告)日：2019-08-08

申请号：US16237867

申请日：2019-01-02

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON

IPC: A61K31/5377 ,  A61K31/4545 ,  A61K31/4412 ,  A61K31/444

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/4545

Abstract: The present invention relates to methods of treating cancer by administering an EZH2 inhibitor or a pharmaceutical composition thereof to the subject in need thereof.

公开(公告)号：US20190070188A1

公开(公告)日：2019-03-07

申请号：US15773757

申请日：2016-11-07

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON ,  Nigel WATERS

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

Abstract: The disclosure provides a method of treating a an INI1-deficient tumor in a subject in need thereof comprising administering to the subject a therapeutically-effective amount of an enhancer of a zeste homolog 2 (EZH2) inhibitor. In a preferred embodiment of this method, the subject is pediatric and the EZH2 inhibitor is Tazemetostat.

公开(公告)号：US20180071300A1

公开(公告)日：2018-03-15

申请号：US15496653

申请日：2017-04-25

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON

IPC: A61K31/5377 ,  A61K31/4545 ,  A61K31/4412 ,  A61K31/444

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/4545

Abstract: The present invention relates to methods of treating cancer by administering an EZH2 inhibitor or a pharmaceutical composition thereof to the subject in need thereof.

公开(公告)号：US20170305889A1

公开(公告)日：2017-10-26

申请号：US15598261

申请日：2017-05-17

Applicant: Epizyme, Inc.

Inventor： Sarah K. KNUTSON ,  Natalie WARHOLIC ,  Heike KEILHACK

IPC: C07D405/14 ,  C07D405/12 ,  C07D211/86 ,  A61K31/5377 ,  A61K31/4545 ,  C12Q1/68 ,  A61K31/4412

CPC classification number: C07D405/14 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/5377 ,  C07D211/86 ,  C07D405/12 ,  C12Q1/6886

Abstract: The present invention relates to methods of treating cancer by administering the EZH2 inhibitor 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：US20170252349A1

公开(公告)日：2017-09-07

申请号：US15598078

申请日：2017-05-17

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

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.

公开(公告)号：US20170216300A1

公开(公告)日：2017-08-03

申请号：US15319535

申请日：2015-06-17

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON ,  L. Danielle JOHNSTON ,  Larisa REYDERMAN ,  Lone OTTESEN

IPC: A61K31/5377 ,  A61K31/4412

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：US20220218714A1

公开(公告)日：2022-07-14

申请号：US17557649

申请日：2021-12-21

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/4545

Abstract: The present invention relates to methods of treating cancer by administering an EZH2 inhibitor or a pharmaceutical composition thereof to the subject in need thereof

公开(公告)号：US20220160721A1

公开(公告)日：2022-05-26

申请号：US17515979

申请日：2021-11-01

Applicant: Epizyme, Inc.

Inventor： Jesse SMITH ,  Heike KEILHACK ,  Scott RIBICH

IPC: A61K31/5377 ,  A61P35/00 ,  A61K31/4412 ,  A61K9/00 ,  A61K31/551 ,  A61K31/553 ,  A61K31/496 ,  G01N33/574 ,  A61K31/4545 ,  A61K31/5386 ,  A61K31/4439 ,  A61K31/4433 ,  A61K45/06

Abstract: The disclosure relates to a method for treating cancer comprising administering a therapeutically effective amount of an EZH2 inhibitor to a subject in need thereof, wherein the cancer is characterized by at least one cancer cell originating from a stem cell, a progenitor cell, or an immature cell and wherein the at least one cancer cell comprises one or more genetic lesion(s) that confer(s) dependence of the cancer cell on an EZH2 function. In certain embodiments, the EZH2 inhibitor of the disclosure is tazemetostat or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20210008075A1

公开(公告)日：2021-01-14

申请号：US16867717

申请日：2020-05-06

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON ,  Nigel WATERS

IPC: A61K31/5377 ,  A61K31/501 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/4412 ,  A61K31/444 ,  A61P35/00 ,  A61K9/00

Abstract: The disclosure provides a method of treating a an INI1-deficient tumor in a subject in need thereof comprising administering to the subject a therapeutically-effective amount of an enhancer of a zeste homolog 2 (EZH2) inhibitor. In a preferred embodiment of this method, the subject is pediatric and the EZH2 inhibitor is Tazemetostat.

公开(公告)号：US20200323866A1

公开(公告)日：2020-10-15

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: 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.