公开(公告)号：US20190216838A1

公开(公告)日：2019-07-18

申请号：US16214783

申请日：2018-12-10

Applicant: Epizyme, Inc.

Inventor： Edward J. OLHAVA ,  Richard CHESWORTH ,  Kevin W. KUNTZ ,  Victoria M. RICHON ,  Roy M. POLLOCK ,  Scott Richard DAIGLE

IPC: A61K31/7076 ,  A61K31/52

CPC classification number: A61K31/7076 ,  A61K31/52

Abstract: The present invention relates to methods of treating disorders in which DOT1L-mediated protein methylation plays a part, such as cancer, by administering DOT1L inhibitor compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20180243315A1

公开(公告)日：2018-08-30

申请号：US15800983

申请日：2017-11-01

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne KUNTZ ,  Sarah Kathleen KNUTSON ,  Timothy James Nelson WIGLE ,  Robert A. COPELAND ,  Victoria M. RICHON ,  Margaret D. SCOTT ,  Christopher J. SNEERINGER ,  Roy M. POLLOCK

IPC: A61K31/5377 ,  A61K31/4545 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/551 ,  A61K31/7076 ,  C12Q1/68 ,  A61K31/496 ,  A61K31/711 ,  A61K38/17 ,  G01N33/574 ,  G01N33/50 ,  C12Q1/48 ,  C07D473/34 ,  C07D405/12 ,  A61K31/4412

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：US20210268012A1

公开(公告)日：2021-09-02

申请号：US17140331

申请日：2021-01-04

Applicant: Epizyme, Inc.

Inventor： Edward J. OLHAVA ,  Richard CHESWORTH ,  Kevin W. KUNTZ ,  Victoria M. RICHON ,  Roy M. POLLOCK ,  Scott Richard DAIGLE

IPC: A61K31/7076 ,  A61K31/52

Abstract: The present invention relates to methods of treating disorders in which DOT1L-mediated protein methylation plays a part, such as cancer, by administering DOT1L inhibitor compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20180280422A1

公开(公告)日：2018-10-04

申请号：US15802979

申请日：2017-11-03

Applicant: Epizyme, Inc.

Inventor： Edward J. OLHAVA ,  Richard CHESWORTH ,  Kevin Wayne KUNTZ ,  Victoria M. RICHON ,  Roy M. POLLOCK ,  Scott R. DAIGLE

IPC: A61K31/7076 ,  C07H19/14 ,  C07D487/04 ,  C07H19/16 ,  A61K31/519 ,  A61K31/7064 ,  A61K31/52 ,  C07D473/34

Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20210252035A1

公开(公告)日：2021-08-19

申请号：US16897690

申请日：2020-06-10

Applicant: Epizyme, Inc.

Inventor： Edward J. OLHAVA ,  Richard CHESWORTH ,  Kevin W. KUNTZ ,  Victoria M. RICHON ,  Roy M. POLLOCK ,  Scott R. DAIGLE

IPC: A61K31/7076 ,  C07D487/04 ,  C07D473/34 ,  C07H19/14 ,  C07H19/16 ,  A61K31/519 ,  A61K31/52 ,  A61K31/7064

Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20200016162A1

公开(公告)日：2020-01-16

申请号：US16453501

申请日：2019-06-26

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne KUNTZ ,  Sarah Kathleen KNUTSON ,  Timothy James Nelson WIGLE ,  Robert A. COPELAND ,  Victoria M. RICHON ,  Margaret D. SCOTT ,  Christopher J. SNEERINGER ,  Roy M. POLLOCK

IPC: A61K31/5377 ,  C07D473/34 ,  C12Q1/48 ,  G01N33/50 ,  G01N33/574 ,  A61K31/711 ,  A61K38/17 ,  C07D405/12 ,  C12Q1/68 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/551 ,  A61K31/7076

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：US20180271892A1

公开(公告)日：2018-09-27

申请号：US15924663

申请日：2018-03-19

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: A61K31/7076 ,  C12Q1/48 ,  G01N33/574 ,  C07D473/34 ,  C07D493/04 ,  C12Q1/6876 ,  G01N33/50

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：US20200009176A1

公开(公告)日：2020-01-09

申请号：US16415325

申请日：2019-05-17

Applicant: Epizyme, Inc.

Inventor： Roy M. POLLOCK ,  Scott R. DAIGLE ,  Eric HEDRICK ,  Nigel WATERS ,  Blythe THOMSON

IPC: A61K31/7076 ,  A61P35/02

Abstract: The present invention relates to DOT1L inhibitors. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof

公开(公告)号：US20190100552A1

公开(公告)日：2019-04-04

申请号：US16134520

申请日：2018-09-18

Applicant: Epizyme, Inc.

Inventor： Edward J. OLHAVA ,  Richard CHESWORTH ,  Roy M. POLLOCK ,  Lei JIN

IPC: C07H19/16 ,  C07H19/14 ,  C07D473/34 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7068 ,  A61K31/708 ,  A61K31/7064

Abstract: The present invention relates to DOT1L inhibitors and methods of identifying, designing, or optimizing them. The present invention also relates to crystals of DOT1L-inhibitor complexes, the crystal structures thereof, and the use of the crystal structures. Also disclosed are pharmaceutical compositions containing these DOT1L inhibitors and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20190076455A1

公开(公告)日：2019-03-14

申请号：US15533205

申请日：2015-12-04

Applicant: Epizyme, Inc.

Inventor： Roy M. POLLOCK ,  Scott R. DAIGLE ,  Eric HEDRICK ,  Nigel WATERS ,  Blythe THOMSON

IPC: A61K31/7076 ,  A61P35/02

Abstract: The present invention relates to a method for the treatment of leukemia and the induction of leukemic blast cell maturation or differentiation via the administration of the DOT1L inhibitor pinometostat (otherwise known as EPZ-5676; CAS Registry number 1380288-87-8) or its N-oxide or pharmaceutically acceptable salt thereof.