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公开(公告)号：EP2903968B1
公开(公告)日：2016-12-07
申请号：EP13770928.3
申请日：2013-10-01
发明人： LABELLE, Marc , BOESEN, Thomas , MEHROTRA, Mukund , KHAN, Qasim , ULLAH, Farman
IPC分类号： C07D213/79 , C07D401/12 , C07D405/12 , C07D413/12 , A61K31/4418 , A61P35/00
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
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公开(公告)号：EP3023415B1
公开(公告)日：2017-12-06
申请号：EP15200672.2
申请日：2013-10-01
发明人： LABELLE, Marc , BOESEN, Thomas , MEHROTRA, Mukund , KHAN, Qasim , ULLAH, Farman
IPC分类号： C07D213/79 , C07D401/12 , C07D405/12 , C07D413/12 , A61K31/4418 , A61P35/00
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).
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公开(公告)号：EP3186238A1
公开(公告)日：2017-07-05
申请号：EP15759595.0
申请日：2015-08-26
发明人： BOESEN, Thomas , LABELLE, Marc , YANG, Ying , SARASWAT, Neerja , DUDEKULA, Dastagiri , COOK, Cyril John , VAKITI, Ramkrishna Reddy , ZHANG, Rui , ULLAH, Farman
IPC分类号： C07D401/04 , C07D401/12 , C07D413/04 , C07D213/38 , C07D213/48 , C07D213/56 , A61K31/44 , A61P35/00
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： 本发明涉及式（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。 本申请的化合物可以调节组蛋白去甲基化酶（HDME）的活性，并且可以用于预防和/或治疗基因组失调涉及发病机理例如癌症的疾病。
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4.发明公开ETHYL PYRIDINE-4-CARBOXYLATE COMPOUND AS INHIBITOR OF HISTONE DEMETHYLASES 审中-公开乙基吡啶-4-羧酸 - 维生素ALS抑制剂VON HISTONDEMETHYLASEN
公开(公告)号：EP3170811A1
公开(公告)日：2017-05-24
申请号：EP16197497.7
申请日：2014-02-26
发明人： LABELLE, Marc , BOESEN, Thomas , KHAN, Qasim , VAKITI, Ramkrishna Reddy , SHARMA, Utpal , YANG, Ying , MEHROTRA, Mukund , SARASWAT, Neerja , ULLAH, Farman
IPC分类号： C07D213/79 , A61K31/44 , A61P35/00
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： Ethyl 2-{[({[2-(dimethylamino)ethyl](ethyl)carbamoyl}methyl)amino]methyl}pyridine-4-carboxylate
摘要翻译： 乙基2 - {[（{[2-（二甲基氨基）乙基]（乙基）氨基甲酰基}甲基）氨基]甲基}吡啶-4-甲酸乙酯
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公开(公告)号：EP2961736B1
公开(公告)日：2018-04-11
申请号：EP14706607.0
申请日：2014-02-26
发明人： LABELLE, Marc , BOESEN, Thomas , KHAN, Qasim , VAKITI, Ramkrishna Reddy , SHARMA, Utpal , YANG, Ying , MEHROTRA, Mukund , SARASWAT, Neerja , ULLAH, Farman
IPC分类号： C07D213/79 , C07D401/04 , C07D401/12 , A61P35/00 , A61K31/44
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： Ethyl 2-{[({[2-(dimethylamino)ethyl](ethyl)carbamoyl}methyl)amino]methyl}pyridine-4-carboxylate
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公开(公告)号：EP3150582A1
公开(公告)日：2017-04-05
申请号：EP16186022.6
申请日：2013-10-01
发明人： LABELLE, Marc , MEHROTRA, Mukund , KHAN, Qasim , ULLAH, Farman , BOESEN, Thomas
IPC分类号： C07D213/79 , C07D401/12 , C07D405/12 , C07D413/12 , A61K31/4418 , A61P35/00
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去甲基化酶（HDME）活性的化合物，其可用于预防和/或治疗其中基因组调节异常参与发病机理的疾病，例如， 癌症。 本申请还公开了包含所述化合物的药物组合物以及这些化合物作为药物的用途。 这些化合物采取（I）的形式。
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公开(公告)号：EP3126345A1
公开(公告)日：2017-02-08
申请号：EP15715631.6
申请日：2015-03-30
IPC分类号： C07D401/04 , A61K31/44 , C07D401/12 , C07D413/04 , C07D213/38 , C07D213/48 , C07D213/56 , A61P35/00
CPC分类号： C07D213/79 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K45/06 , C07D213/38 , C07D213/48 , C07D213/56 , C07D237/24 , C07D239/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： Compounds of the form in which Q is selected from -COOH -CH=NR12, -W, -CH2NHR13, -CH=0 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选自能够调节组蛋白去甲基化酶（HDME）活性的-COOH -CH = NR12，-W，-CH2NHR13，-CH = 0和-CH（OR17）2）形式的化合物，其可用于 预防和/或治疗发病机理中涉及基因组紊乱的疾病，例如， 癌症和这些化合物的制剂和使用方法。
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