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：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.