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公开(公告)号：US20130040906A1
公开(公告)日：2013-02-14
申请号：US13418242
申请日：2012-03-12
CPC分类号： 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
摘要： 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：US08895245B2
公开(公告)日：2014-11-25
申请号：US13230703
申请日：2011-09-12
申请人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
发明人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC分类号： C12Q1/68 , C07D493/04 , A61K31/7076 , C07D473/34 , C12Q1/48 , G01N33/50 , G01N33/574 , A61P35/00 , C07H21/00 , C07H21/04
CPC分类号： A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
摘要： 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.
摘要翻译： 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：US20120071418A1
公开(公告)日：2012-03-22
申请号：US13230703
申请日：2011-09-12
申请人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
发明人： Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Kevin W. Kuntz , Sarah K. Knutson , Roy M. Pollock
IPC分类号： A61K38/00 , C12Q1/68 , G01N33/574 , G01N33/566 , A61P35/00 , C07H19/19 , A61K31/7076 , G01N33/567 , C12N5/02
CPC分类号： A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
摘要： 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.
摘要翻译： 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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4.发明授权7-deazapurine modulators of histone methyltransferase, and methods of use thereof 有权组氨酸甲基转移酶的7-脱氮嘌呤调节剂及其使用方法公开(公告)号：US09145438B2
公开(公告)日：2015-09-29
申请号：US13991328
申请日：2011-12-05
IPC分类号： A01N43/04 , A61K31/70 , C07H19/14 , C07D487/04
CPC分类号： C07H19/14 , C07D487/04
摘要： Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.
摘要翻译： 公开了化合物，含有化合物的药物组合物，化合物和组合物用作组蛋白甲基转移酶的调节剂，以及用于治疗受组蛋白甲基转移酶活性调节影响的疾病的方法。
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公开(公告)号：US20130338173A1
公开(公告)日：2013-12-19
申请号：US13991145
申请日：2011-12-05
IPC分类号： C07D487/04 , C07D473/34
CPC分类号： C07D487/04 , C07D473/34
摘要： The present invention relates to carbocycle-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.
摘要翻译： 本发明涉及碳环取代的嘌呤和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：US08410088B2
公开(公告)日：2013-04-02
申请号：US13447007
申请日：2012-04-13
IPC分类号： C07D211/76 , C07D413/10 , C07D413/12 , A61K31/4412
CPC分类号： 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
摘要： 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.
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公开(公告)号：US09029343B2
公开(公告)日：2015-05-12
申请号：US13991321
申请日：2011-12-05
IPC分类号： C07H19/16 , C07H19/167 , C07D473/34
CPC分类号： C07H19/16 , C07D473/34 , C07H19/167
摘要： 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.
摘要翻译： 公开了化合物，含有这些化合物的药物组合物，以及化合物和组合物作为组蛋白甲基转移酶调节剂的用途，以及用于治疗受组蛋白甲基转移酶活性调节影响的疾病。
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公开(公告)号：US09394310B2
公开(公告)日：2016-07-19
申请号：US13991145
申请日：2011-12-05
IPC分类号： C07D487/04 , C07D473/34
CPC分类号： C07D487/04 , C07D473/34
摘要： The present invention relates to carbocycle-substituted purine and 7-deazapurine compounds of Formula (I). 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.
摘要翻译： 本发明涉及式（I）的碳环取代的嘌呤和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：US20120142625A1
公开(公告)日：2012-06-07
申请号：US13310157
申请日：2011-12-02
申请人： Edward J. Olhava , Richard Chesworth , Kevin W. Kuntz , Victoria M. Richon , Roy M. Pollock , Scott R. Daigle
发明人： Edward J. Olhava , Richard Chesworth , Kevin W. Kuntz , Victoria M. Richon , Roy M. Pollock , Scott R. Daigle
IPC分类号： A61K31/7076 , C07H19/167 , C07D473/34 , A61P35/02 , A61K31/7064 , A61K31/52 , A61K31/519 , A61P35/00 , C07D487/04 , C07H19/14
CPC分类号： A61K31/7076 , A61K31/519 , A61K31/52 , A61K31/7064 , C07D473/34 , C07D487/04 , C07H19/14 , C07H19/16
摘要： 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.
摘要翻译： 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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10.发明申请公开(公告)号：US20080269298A1
公开(公告)日：2008-10-30
申请号：US12113224
申请日：2008-05-01
申请人： Clarence W. Andrews , Mui Cheung , Ronda G. Davis-Ward , David Harold Drewry , Kyle Allen Emmitte , Robert Dale Hubbard , Kevin W. Kuntz , James Andrew Linn , Robert Anthony Mook , Gary Keith Smith , James Marvin Veal
发明人： Clarence W. Andrews , Mui Cheung , Ronda G. Davis-Ward , David Harold Drewry , Kyle Allen Emmitte , Robert Dale Hubbard , Kevin W. Kuntz , James Andrew Linn , Robert Anthony Mook , Gary Keith Smith , James Marvin Veal
IPC分类号： A61K31/4184 , A61P35/00 , A61K31/4439 , C07D409/14 , C07D409/04
CPC分类号： C07D491/04 , C07D409/04 , C07D409/14
摘要： The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
摘要翻译： 本发明提供式（I）化合物：含有该化合物的药物组合物，其制备方法及其作为药剂的用途。
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