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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。
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公开(公告)号：US20150216890A1
公开(公告)日：2015-08-06
申请号：US14426331
申请日：2013-09-06
Applicant: Epizyme, Inc.
Inventor： Edward J. Olhava , Richard Chesworth , Kevin W. Kuntz , Victoria M. Richon , Roy M. Pollock , Scott Richard Daigle
IPC: A61K31/7076
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.
Abstract translation: 本发明涉及通过向有需要的受试者施用DOT1L抑制剂化合物和药物组合物来治疗其中DOT1L介导的蛋白质甲基化部分如癌症的病症的方法。
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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。
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公开(公告)号：US09949999B2
公开(公告)日：2018-04-24
申请号：US15132724
申请日：2016-04-19
Applicant: Epizyme, Inc.
Inventor： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC: A61P35/00 , C12Q1/68 , A61K31/7076 , C07D473/34 , C12Q1/48 , G01N33/50 , G01N33/574 , C07D493/04 , A61P35/02
CPC classification number: A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
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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。
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Patent Agency Ranking
公开(公告)号：US09333217B2
公开(公告)日：2016-05-10
申请号：US14540977
申请日：2014-11-13
Applicant: Epizyme, Inc.
Inventor： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC: A61P35/00 , C12Q1/68 , A61K31/7076 , C07D473/34 , C12Q1/48 , G01N33/50 , G01N33/574 , C07D493/04 , A61P35/02
CPC classification number: A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
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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。
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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.
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公开(公告)号：US20170065628A1
公开(公告)日：2017-03-09
申请号：US15132724
申请日：2016-04-19
Applicant: Epizyme, Inc.
Inventor： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC: A61K31/7076
CPC classification number: A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
Abstract translation: 本发明涉及抑制人组蛋白甲基转移酶EZH2的野生型和某些突变体形式，其是催化组蛋白H3（H3-K27）上赖氨酸27的单通三甲基化的PRC2复合物的催化亚单位。 在一个实施方案中，抑制对于EZH2的突变体形式是选择性的，使得与某些癌症相关的H3-K27的三甲基化被抑制。 该方法可用于治疗包括滤泡性淋巴瘤和弥漫性大B细胞淋巴瘤（DLBCL）的癌症。 还提供了用于鉴定EZH2的突变形式的小分子选择性抑制剂的方法以及用于测定受试者中对EZH2抑制剂的反应性的方法。
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公开(公告)号：US20170065600A1
公开(公告)日：2017-03-09
申请号：US15132610
申请日：2016-04-19
Applicant: EPIZYME, INC.
Inventor： Kevin Wayne Kuntz , Sarah Kathleen Knutson , Timothy James Nelson Wigle , Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Roy M. Pollock
IPC: A61K31/5377 , A61K31/444 , A61K31/4545 , A61K31/551 , G01N33/50 , A61K31/4439 , A61K31/4427 , A61K31/496 , A61K31/497 , A61K31/7076 , A61K31/4412
CPC classification number: A61K31/5377 , A61K31/4412 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/551 , A61K31/7076 , A61K31/711 , A61K38/17 , C07D405/12 , C07D473/34 , C12Q1/48 , C12Q1/68 , G01N33/5011 , G01N33/57426 , G01N2333/91011 , G01N2333/91017 , G01N2800/52 , Y10T436/143333
Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
Abstract translation: 本发明涉及抑制人组蛋白甲基转移酶EZH2的野生型和某些突变体形式，其是催化组蛋白H3（H3-K27）上赖氨酸27的单通三甲基化的PRC2复合物的催化亚单位。 在一个实施方案中，抑制对于EZH2的突变体形式是选择性的，使得与某些癌症相关的H3-K27的三甲基化被抑制。 该方法可用于治疗包括滤泡性淋巴瘤和弥漫性大B细胞淋巴瘤（DLBCL）的癌症。 还提供了用于鉴定EZH2的突变形式的小分子选择性抑制剂的方法以及用于测定受试者中对EZH2抑制剂的反应性的方法。
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