公开(公告)号：US20160214985A1

公开(公告)日：2016-07-28

申请号：US14654303

申请日：2013-12-20

Applicant: EPIZYME, INC.

Inventor： Kenneth W. DUNCAN ,  Richard CHESWORTH ,  Michael John MUNCHHOF ,  Lei JIN

IPC: C07D487/04 ,  C07D401/10 ,  C07D405/12 ,  C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D409/12 ,  C07D217/04 ,  C07D413/12

CPC classification number: C07D487/04 ,  C07D217/02 ,  C07D217/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：US20170280720A1

公开(公告)日：2017-10-05

申请号：US15511514

申请日：2015-09-17

Applicant: EPIZYME, INC.

Inventor： Richard CHESWORTH ,  Lorna Helen MITCHELL ,  Gideon SHAPIRO ,  Oscar Miguel MORADEI ,  Kevin Wayne KUNTZ ,  Kenneth W. DUNCAN ,  Lei JIN

IPC: A01N47/10 ,  C07D277/20 ,  C07D233/54 ,  C07D209/10 ,  C07D241/02

CPC classification number: A01N47/10 ,  A61K38/45 ,  C07D209/10 ,  C07D233/54 ,  C07D241/02 ,  C07D277/20 ,  C07D471/04 ,  C07D487/04

Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

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：US20170320883A1

公开(公告)日：2017-11-09

申请号：US15648701

申请日：2017-07-13

Applicant: EPIZYME, INC.

Inventor： Richard CHESWORTH ,  Oscar Miguel MORADEI ,  Gideon SHAPIRO ,  Lei JIN ,  Robert E. BABINE

IPC: C07D487/10 ,  C07D239/42 ,  C07D495/04 ,  C07D493/10 ,  C07D493/04 ,  C07D487/08 ,  C07D487/04 ,  C07D471/10 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D413/12 ,  C07D413/04 ,  C07D409/14 ,  C07D405/14 ,  C07D405/12 ,  C07D405/04 ,  C07D403/12 ,  C07D403/04 ,  C07D401/04 ,  C07D498/04 ,  C07D498/10

CPC classification number: C07D487/10 ,  C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D493/04 ,  C07D493/10 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10

Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.