公开(公告)号：US11491163B2

公开(公告)日：2022-11-08

申请号：US17032432

申请日：2020-09-25

Applicant: Epizyme, Inc. ,  Eisai R&D Management Co., Ltd.

Inventor： Kevin Wayne Kuntz ,  Kuan-Chun Huang ,  Hyeong Wook Choi ,  Kristen Sanders ,  Steven Mathieu ,  Arani Chanda ,  Francis Fang

IPC: A61K31/5377 ,  C07D405/12

Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

公开(公告)号：US10821113B2

公开(公告)日：2020-11-03

申请号：US16270752

申请日：2019-02-08

Applicant: Epizyme, Inc. ,  Eisai R&D Management Co., Ltd.

Inventor： Kevin Wayne Kuntz ,  Kuan-Chun Huang ,  Hyeong Wook Choi ,  Kristen Sanders ,  Steven Mathieu ,  Arani Chanda ,  Francis Fang

IPC: A61K31/5377 ,  C07D405/12

Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

公开(公告)号：US10273223B2

公开(公告)日：2019-04-30

申请号：US15492506

申请日：2017-04-20

Applicant: Epizyme, Inc.

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

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

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：US10179773B2

公开(公告)日：2019-01-15

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 ,  Jennifer C. Petter ,  Carl Eric Schwartz

IPC: A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D261/18 ,  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.

公开(公告)号：US10106510B2

公开(公告)日：2018-10-23

申请号：US15510605

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  Lorna Helen Mitchell ,  Michael John Munchhof

IPC: A61K31/42 ,  C07D261/18 ,  C07D261/08

Abstract: The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, and R7 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：US09943504B2

公开(公告)日：2018-04-17

申请号：US15178696

申请日：2016-06-10

Applicant: Epizyme, Inc.

Inventor： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kevin Wayne Kuntz

IPC: A61K31/416 ,  A61K31/4439

CPC classification number: C07D231/56 ,  A61K31/416 ,  A61K31/4439 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12

Abstract: 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：US20170290837A1

公开(公告)日：2017-10-12

申请号：US15359538

申请日：2016-11-22

Applicant: Epizyme, Inc.

Inventor： Kevin Wayne Kuntz ,  John Emmerson Campbell ,  Masashi Seki

IPC: A61K31/5377 ,  C07D213/64 ,  A61K31/5375 ,  C07D405/14 ,  A61K31/4412 ,  A61K31/4545

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/5375 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14

Abstract: The present invention relates to 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：US20170119735A1

公开(公告)日：2017-05-04

申请号：US15178696

申请日：2016-06-10

Applicant: Epizyme, Inc.

Inventor： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kevin Wayne Kuntz

IPC: A61K31/416 ,  A61K31/4439

CPC classification number: C07D231/56 ,  A61K31/416 ,  A61K31/4439 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12

Abstract: 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：US09365570B2

公开(公告)日：2016-06-14

申请号：US14699100

申请日：2015-04-29

Applicant: Epizyme, Inc.

Inventor： John Emmerson Campbell ,  Kevin Wayne Kuntz

IPC: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  C07D471/04 ,  C07D231/56

CPC classification number: C07D471/04 ,  C07D231/56 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D519/00

Abstract: The present invention relates to azole 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. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Abstract translation: 本发明涉及唑类双环杂芳基化合物。 本发明还涉及含有这些化合物的药物组合物和通过将这些化合物和药物组合物施用于有需要的受试者来治疗癌症的方法。 本发明还涉及这些化合物用于研究或其它非治疗目的的用途。

公开(公告)号：US20160068559A1

公开(公告)日：2016-03-10

申请号：US14680339

申请日：2015-04-07

Applicant: Epizyme, Inc.

Inventor： Richard Chesworth ,  Kevin Wayne Kuntz ,  Edward James Olhava ,  Michael A. Patane

IPC: C07H19/16

CPC classification number: C07H19/16 ,  C07D473/34 ,  C07H19/167

Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.