公开(公告)号：US20170252349A1

公开(公告)日：2017-09-07

申请号：US15598078

申请日：2017-05-17

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

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：US20240245697A1

公开(公告)日：2024-07-25

申请号：US18606925

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：US20210379076A1

公开(公告)日：2021-12-09

申请号：US17308610

申请日：2021-05-05

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

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：US20200155562A1

公开(公告)日：2020-05-21

申请号：US16660339

申请日：2019-10-22

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 ,  A61K31/553 ,  A61K31/551 ,  A61K31/506 ,  A61K31/496 ,  A61K31/4709 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/4436 ,  A61K31/4433 ,  A61K31/443 ,  A61K31/4412 ,  C07D405/14 ,  C07D213/64 ,  C07D491/107 ,  C07D491/08 ,  C07D417/12 ,  C07D413/12 ,  C07D409/12 ,  C07D405/12 ,  C07D401/12 ,  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：US20190192526A1

公开(公告)日：2019-06-27

申请号：US16291800

申请日：2019-03-04

Applicant: Epizyme, Inc.

Inventor： Kevin W. KUNTZ ,  Richard CHESWORTH ,  Kenneth W. DUNCAN ,  Masashi SEKI ,  Syuji SHIROTORI

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

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：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：US20170362217A1

公开(公告)日：2017-12-21

申请号：US15510588

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Lorna Helen MITCHELL ,  Andrew Simon BELL ,  Richard CHESWORTH ,  Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC: C07D451/04 ,  C07D487/08 ,  C07D413/14 ,  C07D519/00 ,  C07D413/12

CPC classification number: C07D451/04 ,  A61P35/00 ,  C07D413/12 ,  C07D413/14 ,  C07D487/08 ,  C07D519/00

Abstract: The present disclosure provides substituted piperidine compounds having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, B, X, and Z 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：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：US20180318309A1

公开(公告)日：2018-11-08

申请号：US15816907

申请日：2017-11-17

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

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：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.