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公开(公告)号：EP2920183A1
公开(公告)日：2015-09-23
申请号：EP13798807.7
申请日：2013-11-12
申请人： GlaxoSmithKline LLC
发明人： AMANS, Dominique , BAMBOROUGH, Paul , BIT, Rino, Antonio , BROWN, John, Alexander , CAMPBELL, Matthew , LINDON, Matthew, John , SHIPLEY, Tracy, Jane , THEODOULOU, Natalie, Hope , WELLAWAY, Christopher, Roland , WESTAWAY, Susan, Marie
IPC分类号： C07D495/04 , A61K31/44
CPC分类号： C07D495/04 , A61K31/4365 , A61K31/4427 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K45/06 , A61K2300/00
摘要： or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.
摘要翻译： 或其盐，含有这些化合物的药物组合物及其在治疗中的用途，特别是治疗指示溴结构域抑制剂的疾病或病症。
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公开(公告)号：EP2496945B1
公开(公告)日：2015-04-01
申请号：EP10776336.9
申请日：2010-11-03
申请人： GlaxoSmithKline LLC
发明人： BAMBOROUGH, Paul , CHUNG, Chun-Wa
CPC分类号： G01N33/566 , C12N9/1205 , G01N33/6803 , G01N2500/02 , G01N2500/10 , Y02A50/58
摘要： A compound or a pharmaceutically acceptable salt or solvate thereof with a molecular weight in the range 100 to 750 which inhibits the binding of the first and/or second bromodomains of human BRD-2 to 4 to acetylated lysine residues of their physiological partner which is able to: a) form a hydrogen bonding interaction in which the compound accepts a hydrogen bond from the sidechain NH2 group of the asparagine residue found at: or b) accept a water-mediated hydrogen bond in which the compound accepts a hydrogen bond from a water that is itself hydrogen-bonded to the sidechain hydroxyl of the tyrosine residue found at and c) which are also able to form a Van der Waals interaction with a lipophilic binding region of a binding pocket such that one or more heavy atoms of the said compounds lie within a 5A range of any of the heavy atoms of the following bromodomain residues which define the binding pocket: for use in the treatment of chronic autoimmune and inflammatory conditions, acute inflammatory conditions or cancer.
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公开(公告)号：EP2920183B1
公开(公告)日：2017-03-08
申请号：EP13798807.7
申请日：2013-11-12
申请人： GlaxoSmithKline LLC
发明人： AMANS, Dominique , BAMBOROUGH, Paul , BIT, Rino, Antonio , BROWN, John, Alexander , CAMPBELL, Matthew , LINDON, Matthew, John , SHIPLEY, Tracy, Jane , THEODOULOU, Natalie, Hope , WELLAWAY, Christopher, Roland , WESTAWAY, Susan, Marie
IPC分类号： C07D495/04 , A61K31/44
CPC分类号： C07D495/04 , A61K31/4365 , A61K31/4427 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K45/06 , A61K2300/00
摘要： or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.
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公开(公告)号：EP2496945A1
公开(公告)日：2012-09-12
申请号：EP10776336.9
申请日：2010-11-03
申请人： GlaxoSmithKline LLC
发明人： BAMBOROUGH, Paul , CHUNG, Chun-Wa
CPC分类号： G01N33/566 , C12N9/1205 , G01N33/6803 , G01N2500/02 , G01N2500/10 , Y02A50/58
摘要： A compound or a pharmaceutically acceptable salt or solvate thereof with a molecular weight in the range 100 to 750 which inhibits the binding of the first and/or second bromodomains of human BRD-2 to 4 to acetylated lysine residues of their physiological partner which is able to: a) form a hydrogen bonding interaction in which the compound accepts a hydrogen bond from the sidechain NH2 group of the asparagine residue found at: or b) accept a water-mediated hydrogen bond in which the compound accepts a hydrogen bond from a water that is itself hydrogen-bonded to the sidechain hydroxyl of the tyrosine residue found at and c) which are also able to form a Van der Waals interaction with a lipophilic binding region of a binding pocket such that one or more heavy atoms of the said compounds lie within a 5A range of any of the heavy atoms of the following bromodomain residues which define the binding pocket: for use in the treatment of chronic autoimmune and inflammatory conditions, acute inflammatory conditions or cancer.
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