公开(公告)号：US20170080010A1

公开(公告)日：2017-03-23

申请号：US15248080

申请日：2016-08-26

Applicant: Epizyme, Inc.

Inventor： Christine Klaus ,  Maria Alejandra Raimondi ,  Scott R. Daigle ,  Roy MacFarlane Pollock

IPC: A61K31/7076 ,  A61K31/706 ,  A61K31/635 ,  A61K31/4745 ,  A61K31/7068 ,  A61K31/135 ,  A61K31/704 ,  A61K31/136

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

公开(公告)号：US09096634B2

公开(公告)日：2015-08-04

申请号：US14055510

申请日：2013-10-16

Applicant: Epizyme, Inc.

Inventor： Edward J. Olhava ,  Richard Chesworth ,  Kevin W. Kuntz ,  Victoria M. Richon ,  Roy M. Pollock ,  Scott R. Daigle

IPC: C07H19/16 ,  C07H19/14 ,  C07D473/34 ,  C07D487/04

CPC classification number: A61K31/7076 ,  A61K31/519 ,  A61K31/52 ,  A61K31/7064 ,  C07D473/34 ,  C07D487/04 ,  C07H19/14 ,  C07H19/16

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.

Abstract translation: 本发明涉及取代的嘌呤和7-脱氮嘌呤化合物。 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其中DOT1介导的蛋白质甲基化作用的疾病如癌症和神经障碍的方法。

公开(公告)号：US10143704B2

公开(公告)日：2018-12-04

申请号：US15036544

申请日：2014-11-13

Applicant: Epizyme, Inc.

Inventor： Roy M. Pollock ,  Scott R. Daigle ,  Eric Hedrick ,  Nigel Waters ,  Blythe Thomson

IPC: A61K31/7076 ,  C07H19/16

Abstract: The present invention relates to DOT1L inhibitors. 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, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20140323421A1

公开(公告)日：2014-10-30

申请号：US14210511

申请日：2014-03-14

Applicant: Epizyme, Inc.

Inventor： Christine Klaus ,  Maria Alejandra Raimondi ,  Scott R. Daigle ,  Roy MacFarlane Pollock

IPC: A61K31/7076 ,  A61K31/706 ,  A61K31/5377 ,  A61K31/4745 ,  A61K31/7068 ,  A61K31/135 ,  A61K31/704 ,  A61K31/136

CPC classification number: A61K31/7076 ,  A61K31/135 ,  A61K31/136 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/635 ,  A61K31/704 ,  A61K31/706 ,  A61K31/7068

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

Abstract translation: 本发明涉及包含人组蛋白甲基转移酶DOT1L的抑制剂和一种或多种治疗剂，特别是抗癌剂的组合物，以及用于给予需要其治疗癌症的受试者的组合疗法的方法。

公开(公告)号：US20140051654A1

公开(公告)日：2014-02-20

申请号：US14055510

申请日：2013-10-16

Applicant: Epizyme, Inc.

Inventor： Edward J. Olhava ,  Richard Chesworth ,  Kevin W. Kuntz ,  Victoria M. Richon ,  Roy M. Pollock ,  Scott R. Daigle

IPC: C07H19/16 ,  C07D487/04 ,  C07D473/34 ,  C07H19/14

CPC classification number: A61K31/7076 ,  A61K31/519 ,  A61K31/52 ,  A61K31/7064 ,  C07D473/34 ,  C07D487/04 ,  C07H19/14 ,  C07H19/16

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.

Abstract translation: 本发明涉及取代的嘌呤和7-脱氮嘌呤化合物。 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其中DOT1介导的蛋白质甲基化作用的疾病如癌症和神经障碍的方法。

公开(公告)号：US10525074B2

公开(公告)日：2020-01-07

申请号：US15248080

申请日：2016-08-26

Applicant: Epizyme, Inc.

Inventor： Christine Klaus ,  Maria Alejandra Raimondi ,  Scott R. Daigle ,  Roy MacFarlane Pollock

IPC: A61K31/7076 ,  A61K31/704 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/4745 ,  A61K31/135 ,  A61K31/5377 ,  A61K31/136 ,  A61K31/635

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

公开(公告)号：US20150366893A1

公开(公告)日：2015-12-24

申请号：US14752023

申请日：2015-06-26

Applicant: EPIZYME, INC.

Inventor： Edward J. Olhava ,  Richard Chesworth ,  Kevin Wayne Kuntz ,  Victoria M. Richon ,  Roy M. Pollock ,  Scott R. Daigle

IPC: A61K31/7076 ,  A61K31/519 ,  A61K31/52 ,  A61K31/7064

CPC classification number: A61K31/7076 ,  A61K31/519 ,  A61K31/52 ,  A61K31/7064 ,  C07D473/34 ,  C07D487/04 ,  C07H19/14 ,  C07H19/16

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.

Abstract translation: 本发明涉及取代的嘌呤和7-脱氮嘌呤化合物。 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其中DOT1介导的蛋白质甲基化作用的疾病如癌症和神经障碍的方法。

公开(公告)号：US20160296548A1

公开(公告)日：2016-10-13

申请号：US15036544

申请日：2014-11-13

Applicant: EPIZYME, INC.

Inventor： Roy M. Pollock ,  Scott R. Daigle ,  Eric Hedrick ,  Nigel Waters ,  Blythe Thomson

IPC: A61K31/7076

CPC classification number: A61K31/7076 ,  C07H19/16

Abstract: The present invention relates to DOT1L inhibitors. 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, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract translation: 本发明涉及DOT1L抑制剂。 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其中DOT1介导的蛋白质甲基化部分如癌症的疾病的方法。

公开(公告)号：US09446064B2

公开(公告)日：2016-09-20

申请号：US14210511

申请日：2014-03-14

Applicant: Epizyme, Inc.

Inventor： Christine Klaus ,  Maria Alejandra Raimondi ,  Scott R. Daigle ,  Roy MacFarlane Pollock

IPC: A61K31/7076 ,  A61K31/704 ,  A61K31/706 ,  A61K31/136 ,  A61K31/4745 ,  A61K31/7068 ,  A61K31/135 ,  A61K31/5377

CPC classification number: A61K31/7076 ,  A61K31/135 ,  A61K31/136 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/635 ,  A61K31/704 ,  A61K31/706 ,  A61K31/7068

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

Abstract translation: 本发明涉及包含人组蛋白甲基转移酶DOT1L的抑制剂和一种或多种治疗剂，特别是抗癌剂的组合物，以及用于给予需要其治疗癌症的受试者的组合疗法的方法。

公开(公告)号：US20150342979A1

公开(公告)日：2015-12-03

申请号：US14654125

申请日：2013-12-20

Applicant: EPIZYME, INC.

Inventor： Roy M. Pollock ,  Scott R. Daigle

IPC: A61K31/7076 ,  C12Q1/68 ,  A61K31/7064

CPC classification number: A61K31/7076 ,  A61K31/7064 ,  C12Q1/6886 ,  C12Q2600/136 ,  C12Q2600/158 ,  Y02A50/411

Abstract: The present invention relates to DOT1L inhibitors. 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, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract translation: 本发明涉及DOT1L抑制剂。 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其中DOT1介导的蛋白质甲基化部分如癌症的疾病的方法。