公开(公告)号：US20240182426A1

公开(公告)日：2024-06-06

申请号：US18482475

申请日：2023-10-06

Applicant: Epizyme, Inc.

Inventor： Richard CHESWORTH ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kerren Kalai Swinger

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

CPC classification number: C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  C07D401/04 ,  C07D403/04 ,  C07D403/08 ,  C07D405/04 ,  C07D405/08 ,  C07D405/12 ,  C07D493/10

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：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：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：US20240245698A1

公开(公告)日：2024-07-25

申请号：US18606946

申请日：2024-03-15

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 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

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：US20200317643A1

公开(公告)日：2020-10-08

申请号：US16817791

申请日：2020-03-13

Applicant: Epizyme, Inc.

Inventor： Kevin W. KUNTZ ,  Edward J. OLHAVA ,  Richard CHESWORTH ,  Kenneth W. DUNCAN

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

Abstract: 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：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.

公开(公告)号：US20240277723A1

公开(公告)日：2024-08-22

申请号：US18606903

申请日：2024-03-15

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 ,  Suji SHIROTORI ,  Satoshi KAWANO

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

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：US20190300502A1

公开(公告)日：2019-10-03

申请号：US16299722

申请日：2019-03-12

Applicant: Epizyme, Inc.

Inventor： Kevin W. KUNTZ ,  Edward J. OLHAVA ,  Richard CHESWORTH ,  Kenneth W. DUNCAN

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

Abstract: 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：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：US20180230110A1

公开(公告)日：2018-08-16

申请号：US15510589

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Richard CHESWORTH ,  Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  Lorna Helen MITCHELL ,  Russell C. PETTER ,  Carl Eric SCHWARTZ

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

CPC classification number: C07D261/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D413/12

Abstract: 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.