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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:US20140142083A1
公开(公告)日:2014-05-22
申请号:US14110873
申请日:2012-04-13
申请人: Kevin Wayne Kuntz , Richard Chesworth , Kenneth William Duncan , Heike Keilhack , Natalie Warholic , Christine Klaus , Sarah K. Knutson , Timothy James Nelson Wigle , Masashi Seki
发明人: Kevin Wayne Kuntz , Richard Chesworth , Kenneth William Duncan , Heike Keilhack , Natalie Warholic , Christine Klaus , Sarah K. Knutson , Timothy James Nelson Wigle , Masashi Seki
IPC分类号: C07D405/14 , C07D401/14 , C07D213/64 , C07D401/12 , C07D405/12
CPC分类号: C07D213/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D491/048 , C07D491/08 , C07D491/10 , C07D491/113
摘要: 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.
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公开(公告)号:US09376422B2
公开(公告)日:2016-06-28
申请号:US14110873
申请日:2012-04-13
申请人: Kevin Wayne Kuntz , Richard Chesworth , Kenneth William Duncan , Heike Keilhack , Natalie Warholic , Christine Klaus , Sarah K. Knutson , Timothy James Nelson Wigle , Masashi Seki
发明人: Kevin Wayne Kuntz , Richard Chesworth , Kenneth William Duncan , Heike Keilhack , Natalie Warholic , Christine Klaus , Sarah K. Knutson , Timothy James Nelson Wigle , Masashi Seki
IPC分类号: C07D213/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D491/10 , C07D491/113
CPC分类号: C07D213/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D491/048 , C07D491/08 , C07D491/10 , C07D491/113
摘要: 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.
摘要翻译: 本发明涉及取代的苯化合物。 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。
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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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