公开(公告)号：US11052093B2

公开(公告)日：2021-07-06

申请号：US16660339

申请日：2019-10-22

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：US10898490B2

公开(公告)日：2021-01-26

申请号：US16660185

申请日：2019-10-22

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack ,  Sarah K. Knutson

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

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：US09949999B2

公开(公告)日：2018-04-24

申请号：US15132724

申请日：2016-04-19

Applicant: Epizyme, Inc.

Inventor： Robert A. Copeland ,  Victoria M. Richon ,  Margaret D. Scott ,  Christopher J. Sneeringer ,  Kevin W. Kuntz ,  Sarah K. Knutson ,  Roy M. Pollock

IPC: A61P35/00 ,  C12Q1/68 ,  A61K31/7076 ,  C07D473/34 ,  C12Q1/48 ,  G01N33/50 ,  G01N33/574 ,  C07D493/04 ,  A61P35/02

CPC classification number: A61K31/7076 ,  C07D473/34 ,  C07D493/04 ,  C12Q1/48 ,  C12Q1/6876 ,  G01N33/5011 ,  G01N33/57426 ,  G01N2333/91011

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：US20160303135A1

公开(公告)日：2016-10-20

申请号：US15101577

申请日：2014-12-08

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack ,  Sarah K. Knutson ,  Kevin W. Kuntz

IPC: A61K31/5377 ,  A61K31/573 ,  A61K31/404 ,  A61K31/519 ,  C07K16/28 ,  A61K31/436 ,  A61K31/675 ,  A61K31/4375 ,  A61K31/69 ,  A61K39/395 ,  A61K31/635 ,  A61K31/52

CPC classification number: A61K31/5377 ,  A61K31/404 ,  A61K31/436 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/519 ,  A61K31/52 ,  A61K31/573 ,  A61K31/635 ,  A61K31/675 ,  A61K31/69 ,  A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  C07K16/2887 ,  A61K2300/00

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：US09333217B2

公开(公告)日：2016-05-10

申请号：US14540977

申请日：2014-11-13

Applicant: Epizyme, Inc.

Inventor： Robert A. Copeland ,  Victoria M. Richon ,  Margaret D. Scott ,  Christopher J. Sneeringer ,  Kevin W. Kuntz ,  Sarah K. Knutson ,  Roy M. Pollock

IPC: A61P35/00 ,  C12Q1/68 ,  A61K31/7076 ,  C07D473/34 ,  C12Q1/48 ,  G01N33/50 ,  G01N33/574 ,  C07D493/04 ,  A61P35/02

CPC classification number: A61K31/7076 ,  C07D473/34 ,  C07D493/04 ,  C12Q1/48 ,  C12Q1/6876 ,  G01N33/5011 ,  G01N33/57426 ,  G01N2333/91011

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：US20140128393A1

公开(公告)日：2014-05-08

申请号：US14054646

申请日：2013-10-15

Applicant: Epizyme, Inc.

Inventor： Sarah K. Knutson ,  Natalie Warholic ,  Heike Keilhack

IPC: C07D405/14 ,  C07D211/86 ,  C07D405/12

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.

Abstract translation: 本发明涉及通过向有需要的受试者施用EZH2抑制剂化合物和药物组合物来治疗癌症的方法。 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：US12162865B2

公开(公告)日：2024-12-10

申请号：US17689704

申请日：2022-03-08

Applicant: Epizyme, Inc.

Inventor： Sarah K. Knutson ,  Natalie Warholic ,  Heike Keilhack

IPC: 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：US20240024331A1

公开(公告)日：2024-01-25

申请号：US18188706

申请日：2023-03-23

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 ,  A61K31/4412 ,  A61K31/4545 ,  A61P35/00 ,  A61K9/0053

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：US10463671B2

公开(公告)日：2019-11-05

申请号：US15809445

申请日：2017-11-10

Applicant: Epizyme, Inc.

Inventor： Heike Keilhack ,  Sarah K. Knutson ,  Kevin W. Kuntz

IPC: A61K31/5377 ,  C07K16/28 ,  A61K31/573 ,  A61K45/06 ,  A61K39/395 ,  A61K31/69 ,  A61K31/675 ,  A61K31/635 ,  A61K31/404 ,  A61K31/52 ,  A61K31/519 ,  A61K31/4965 ,  A61K31/496 ,  A61K31/4375 ,  A61K31/436 ,  A61K39/00

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：US20190100514A1

公开(公告)日：2019-04-04

申请号：US15979916

申请日：2018-05-15

Applicant: Epizyme, Inc.

Inventor： Sarah K. Knutson ,  Natalie Warholic ,  Heike Keilhack

IPC: C07D405/14 ,  A61K31/4545 ,  A61K31/4412 ,  C12Q1/6886 ,  C07D405/12 ,  C07D211/86 ,  A61K31/5377

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.