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公开(公告)号：US09221801B2
公开(公告)日：2015-12-29
申请号：US14472065
申请日：2014-08-28
申请人： EpiTherapeutics ApS
发明人： Marc Labelle , Thomas Boesen , Qasim Khan , Ramkrishna Reddy Vakiti , Utpal Sharma , Ying Yang , Mukund Mehrotra , Neerja Saraswat , Farman Ullah
IPC分类号： C07D413/04 , C07D213/56 , C07D401/04 , C07D401/12 , C07D213/38 , C07D213/48 , C07C55/06 , C07C309/30
CPC分类号： C07D213/40 , A61K31/435 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/537 , C07C55/06 , C07C55/07 , C07C57/15 , C07C59/265 , C07C309/30 , C07D213/38 , C07D213/48 , C07D213/56 , C07D213/79 , C07D307/62 , C07D401/04 , C07D401/12 , C07D413/04
摘要： Compounds of the form In which Q is selected from —CH═NR12, —W, —CH2NHR13, —CH═O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
摘要翻译： 其中Q选自可以调节组蛋白脱甲基酶（HDME）活性的-CH = NR12，-W，-CH2NHR13，-CH = O和-CH（OR17）2）形式的化合物，其可用于预防和 /或治疗涉及发病机理的基因组异常调节的疾病，例如， 癌症和这些化合物的制剂和使用方法。
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公开(公告)号：US20160237037A1
公开(公告)日：2016-08-18
申请号：US14381556
申请日：2014-02-26
申请人： EPITHERAPEUTICS APS
发明人： Marc Labelle , Thomas Boesen , Qasim Khan , Ramkrishna Reddy Vakiti , Utpal Sharma , Ying Yang , Mukund Mehrotra , Neerja Saraswat , Farman Ullah
IPC分类号： C07D213/40 , A61K31/4427 , C07D401/12 , A61K31/4545 , A61K31/4439 , A61K31/496 , C07D401/04 , A61K31/454 , A61K31/506 , C07D413/04 , A61K31/537 , A61K31/5355 , C07C55/07 , C07C59/265 , C07C57/15 , C07D307/62 , A61K31/435
CPC分类号： C07D213/40 , A61K31/435 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/537 , C07C55/06 , C07C55/07 , C07C57/15 , C07C59/265 , C07C309/30 , C07D213/38 , C07D213/48 , C07D213/56 , C07D213/79 , C07D307/62 , C07D401/04 , C07D401/12 , C07D413/04
摘要： Compounds of the form In which Q is selected from —CH═NR12, —W, —CH2NHR13, —CH═O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
摘要翻译： 其中Q选自可以调节组蛋白去甲基化酶（HDME）活性的-CH = NR12，-W，-CH2NHR13，-CH = O和-CH（OR17）2）形式的化合物，其可用于预防和 /或治疗涉及发病机理的基因组异常调节的疾病，例如， 癌症和这些化合物的制剂和使用方法。
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公开(公告)号：US20140371214A1
公开(公告)日：2014-12-18
申请号：US14472065
申请日：2014-08-28
申请人： EpiTherapeutics ApS
发明人： Marc Labelle , Thomas Boesen , Qasim Khan , Ramkrishna Reddy Vakiti , Utpal Sharma , Ying Yang , Mukund Mehrotra , Neerja Saraswat , Farman Ullah
IPC分类号： C07D413/04 , C07C309/30 , C07C55/06 , C07D213/56
CPC分类号： C07D213/40 , A61K31/435 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/537 , C07C55/06 , C07C55/07 , C07C57/15 , C07C59/265 , C07C309/30 , C07D213/38 , C07D213/48 , C07D213/56 , C07D213/79 , C07D307/62 , C07D401/04 , C07D401/12 , C07D413/04
摘要： Compounds of the form In which Q is selected from —CH═NR12, —W, —CH2NHR13, —CH═O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
摘要翻译： 其中Q选自可以调节组蛋白脱甲基酶（HDME）活性的-CH = NR12，-W，-CH2NHR13，-CH = O和-CH（OR17）2）形式的化合物，其可用于预防和 /或治疗涉及发病机理的基因组异常调节的疾病，例如， 癌症和这些化合物的制剂和使用方法。
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公开(公告)号：US20160102096A1
公开(公告)日：2016-04-14
申请号：US14836397
申请日：2015-08-26
申请人： Epitherapeutics ApS
发明人： Thomas Boesen , Marc Labelle , Ying Yang , Neerja Saraswat , Dastagiri Dudekula , Cyril John Cook , Ramkrishna Reddy Vakiti , Rui Zhang , Farman Ullah
IPC分类号： C07D487/04 , A61K31/4439 , A61K31/444 , C07D401/14 , A61K31/506 , A61K31/4985 , A61K31/5355 , C07D409/14 , C07D413/12 , C07D213/79 , A61K31/4412 , A61K31/501 , C07D401/12 , C07D413/14
CPC分类号： C07D487/04 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5355 , C07D213/38 , C07D213/48 , C07D213/56 , C07D213/79 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The present application relates to compounds being of Formula (I), (II), (III), (IV), (V), (VI), (IIIa), (IIIb), (IIIc), (IIId), (IIIe), (IIIf), and (IIIg). Compounds of Formula (I) have the structure: wherein Q, R1, R18, R19, M, A and Y are as defined herein. The compounds of the application can modulate the activity of histone demethylases (HDMEs), and can be useful for the prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, e.g., cancer.
摘要翻译： 本申请涉及式（I），（II），（III），（IV），（V），（VI），（IIIa），（IIIb），（IIIc），（IIId） IIIe），（IIIf）和（IIIg）。 式（I）的化合物具有以下结构：其中Q，R 1，R 18，R 19，M，A和Y如本文所定义。 该应用的化合物可以调节组蛋白脱甲基酶（HDME）的活性，并且可用于预防和/或治疗其中发生基因组紊乱参与发病机理的疾病，例如癌症。
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公开(公告)号：US20140371195A1
公开(公告)日：2014-12-18
申请号：US14472059
申请日：2014-08-28
申请人： EpiTherapeutics ApS
发明人： Marc Labelle , Thomas Boesen , Mukund Mehrotra , Qasim Khan , Farman Ullah
IPC分类号： C07D213/79 , A61K31/4439 , A61K31/444 , C07D405/12 , A61K31/443 , A61K31/496 , C07D401/12 , A61K31/44
CPC分类号： C07D213/79 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/12
摘要： The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form
摘要翻译： 本申请公开了能够调节组蛋白脱甲基酶（HDME）的活性的化合物，其可用于预防和/或治疗其中涉及发病机理的基因组异常调节的疾病，例如， 癌症。 本申请还公开了包含所述化合物的药物组合物和作为药物的这种化合物的用途。 化合物采取形式
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公开(公告)号：US20150203453A1
公开(公告)日：2015-07-23
申请号：US14381558
申请日：2013-10-01
申请人： EpiTherapeutics Aps
发明人： Marc Labelle , Thomas Boesen , Mukund Mehrotra , Qasim Khan , Farman Ullah
IPC分类号： C07D213/79 , A61K31/4439 , A61K31/44 , C07D401/06 , A61K31/443 , A61K31/496 , A61K31/4545 , C07D401/12 , C07D405/12
CPC分类号： C07D213/79 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/12
摘要： The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form (I)
摘要翻译： 本申请公开了能够调节组蛋白脱甲基酶（HDME）的活性的化合物，其可用于预防和/或治疗其中涉及发病机理的基因组异常调节的疾病，例如， 癌症。 本申请还公开了包含所述化合物的药物组合物和作为药物的这种化合物的用途。 化合物以（I）
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公开(公告)号：US09611219B2
公开(公告)日：2017-04-04
申请号：US14381558
申请日：2013-10-01
申请人： EpiTherapeutics ApS
发明人： Marc Labelle , Thomas Boesen , Mukund Mehrotra , Qasim Khan , Farman Ullah
IPC分类号： A61K31/00 , A61K31/44 , C07D213/44 , C07D401/00 , C07D421/00 , C07D413/00 , C07D405/00 , C07D213/79 , C07D401/12 , C07D405/12 , C07D413/12 , A61K31/443 , A61K31/4439 , A61K31/4545 , A61K31/496 , C07D401/06 , A61K31/444
摘要： The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form (I)
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