公开(公告)号：US11512053B2

公开(公告)日：2022-11-29

申请号：US17004881

申请日：2020-08-27

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kerren Kalai Swinger

IPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  C07D401/04 ,  C07D403/08 ,  C07D405/04 ,  C07D405/08 ,  C07D405/12 ,  C07D493/10 ,  C07D403/04

摘要： 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：US20210155631A1

公开(公告)日：2021-05-27

申请号：US16822478

申请日：2020-03-18

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Oscar Miguel Moradei ,  Gideon Shapiro ,  Lei Jin ,  Robert E. Babine

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

摘要： 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.

公开(公告)号：US20210078951A1

公开(公告)日：2021-03-18

申请号：US17004881

申请日：2020-08-27

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kerren Kalai Swinger

IPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  C07D401/04 ,  C07D403/08 ,  C07D405/04 ,  C07D405/08 ,  C07D405/12 ,  C07D493/10 ,  C07D403/04

摘要： 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：US10391089B2

公开(公告)日：2019-08-27

申请号：US15844097

申请日：2017-12-15

申请人： Epizyme, Inc.

发明人： Kenneth W. Duncan ,  Richard Chesworth ,  Paula Ann Boriack-Sjodin ,  Michael John Munchhof ,  Lei Jin

IPC分类号： C07D401/14 ,  A61K31/4725 ,  C07D217/12 ,  C07D401/12 ,  C07D405/12 ,  C07D217/04 ,  C07D405/14 ,  C07D413/12 ,  A61K31/506 ,  C12N9/10 ,  A61P7/06 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/538

摘要： Described herein are compounds of Formula (I), 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：US20190218194A1

公开(公告)日：2019-07-18

申请号：US16217881

申请日：2018-12-12

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro

IPC分类号： C07D285/10 ,  C07D261/08 ,  C07D233/64 ,  C07D285/06 ,  C07D263/32 ,  C07D231/14 ,  C07D405/12 ,  C07D233/54 ,  C07D231/12 ,  A61P35/00 ,  C07D249/06

CPC分类号： C07D285/10 ,  A61P35/00 ,  C07D231/12 ,  C07D231/14 ,  C07D233/54 ,  C07D233/64 ,  C07D249/06 ,  C07D261/08 ,  C07D263/32 ,  C07D285/06 ,  C07D405/12

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention 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：US10273223B2

公开(公告)日：2019-04-30

申请号：US15492506

申请日：2017-04-20

申请人： Epizyme, Inc.

发明人： Kevin Wayne Kuntz ,  Edward James Olhava ,  Richard Chesworth ,  Kenneth William Duncan

IPC分类号： C07D401/12 ,  C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61P35/00

摘要： The present invention relates to substituted 6,5-fused bicyclic heteroaryl 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.

公开(公告)号：US10179773B2

公开(公告)日：2019-01-15

申请号：US15510589

申请日：2015-09-09

申请人： EPIZYME, INC.

发明人： Richard Chesworth ,  Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  Lorna Helen Mitchell ,  Jennifer C. Petter ,  Carl Eric Schwartz

IPC分类号： A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D261/18 ,  C07D413/12

摘要： The present disclosure provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, X, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US20180289671A1

公开(公告)日：2018-10-11

申请号：US15881323

申请日：2018-01-26

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro

IPC分类号： A61K31/415 ,  C07D405/04 ,  C12N9/10 ,  A61K31/4155 ,  C07D413/08 ,  C07D231/12 ,  C07D413/02 ,  A61K31/454 ,  A61K31/5377 ,  C07D401/02 ,  C07D231/10 ,  C07D401/04

摘要： 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：US20180282343A1

公开(公告)日：2018-10-04

申请号：US15835758

申请日：2017-12-08

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Oscar Miguel Moradei ,  Gideon Shapiro ,  Lei Jin ,  Robert E. Babine

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

CPC分类号： 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

摘要： 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.

公开(公告)号：US20180237397A1

公开(公告)日：2018-08-23

申请号：US15677238

申请日：2017-08-15

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Paula Ann Boriack-Sjodin ,  Oscar Miguel Moradei ,  Lei Jin ,  Kenneth W. Duncan

IPC分类号： C07D233/64 ,  C07D405/04 ,  C07D405/10 ,  C07D401/06 ,  C07D405/06 ,  C07D231/12 ,  C07D405/12 ,  C07D413/04 ,  C07D403/12

CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D401/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D413/04

摘要： 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. Formula (I).