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公开(公告)号：US20090062255A1
公开(公告)日：2009-03-05
申请号：US12192595
申请日：2008-08-15
申请人： Henriette GOURDEAU , Pierre FALARDEAU , My-Anh WIOLAND , Nadia BOUFAIED , James B. MCALPINE , Mustapha AOUIDATE , Thierry BERTOMEU , Ashraf IBRAHIM
发明人： Henriette GOURDEAU , Pierre FALARDEAU , My-Anh WIOLAND , Nadia BOUFAIED , James B. MCALPINE , Mustapha AOUIDATE , Thierry BERTOMEU , Ashraf IBRAHIM
IPC分类号： A61K31/551 , C07D487/00 , A61P31/00 , G01N33/574
CPC分类号： A61K31/551 , C07D243/38 , C07D405/04 , C07D405/14 , G01N33/5011
摘要： The invention relates to a method for evaluating a chemotherapeutic potential of a candidate molecule. In evaluating the candidate molecule, the candidate molecule is tested for its ability to inhibit the in vitro growth of a cancer cell; to bind a cellular receptor produced by a cancer cell, wherein said receptor, such as a peripheral benzodiazepine receptor, is produced in a greater amount by said cancer cell than by a normal cell; and to inhibit the activity of at least one protein member of the MAPK pathway. The invention further relates to dibenzodiazepinone analogues and derivatives thereof.
摘要翻译： 本发明涉及一种用于评估候选分子的化疗潜力的方法。 在评估候选分子时，检测候选分子的抑制癌细胞体外生长的能力; 结合由癌细胞产生的细胞受体，其中所述受体（例如外周苯并二氮杂受体）由所述癌细胞以比正常细胞更大的量产生; 并抑制MAPK通路中至少一个蛋白质成员的活性。 本发明还涉及二苯并二氮杂酮类似物及其衍生物。
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2.发明申请公开(公告)号：US20060079509A1
公开(公告)日：2006-04-13
申请号：US11235398
申请日：2005-09-27
IPC分类号： A61K31/551 , C07D243/10
CPC分类号： C12N9/93 , A61K38/00 , C07D243/38 , C07D405/06 , C07D405/14 , C12N9/0004 , C12N9/10 , C12N9/12 , C12N9/14 , C12N9/88 , C12N9/90 , C12N15/52 , C12P17/10 , C12R1/29 , Y02A50/473
摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
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3.发明授权Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals 失效二苯并二氮杂酮类似物，其制备方法及其作为药物的用途公开(公告)号：US07655646B2
公开(公告)日：2010-02-02
申请号：US11962855
申请日：2007-12-21
IPC分类号： C07D243/10 , A61K31/55
CPC分类号： C07D243/38 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14
摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
摘要翻译： 本发明涉及由式I表示的生物活性二苯并二氮杂酮类似物，其制备方法，包含它们的药物组合物和治疗肿瘤病症的方法。
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4.发明申请Phosphate prodrugs of a farnesyl dibenzodiazepinone, processes for their production and their use as pharmaceuticals 失效法呢基二苯并二氮杂酮的磷酸酯前药，其制备方法及其作为药物的用途公开(公告)号：US20070078112A1
公开(公告)日：2007-04-05
申请号：US11527581
申请日：2006-09-27
申请人： Mustapha Aouidate , James McAlpine , Faustinus Yeboah , Ashraf Ibrahim , Arjun Banskota , Maxime Ranger , Gregory White
发明人： Mustapha Aouidate , James McAlpine , Faustinus Yeboah , Ashraf Ibrahim , Arjun Banskota , Maxime Ranger , Gregory White
IPC分类号： A61K31/551 , C07D243/10
CPC分类号： C07D243/10 , C07F9/5535
摘要： This invention relates to phosphate prodrugs of a farnesylated dibenzodiazepinone, to processes of their manufacture, to pharmaceutical compositions comprising the prodrugs, and to their use in the treatment of neoplasms.
摘要翻译： 本发明涉及法呢基化二苯并二氮杂酮的磷酸酯前药，其制备方法，包含前药的药物组合物及其在治疗赘生物中的用途。
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5.发明申请DIBENZODIAZEPINONE ANALOGUES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS PHARMACEUTICALS 失效二苯并嗪酮类似物，其生产方法及其作为药物的用途公开(公告)号：US20080161291A1
公开(公告)日：2008-07-03
申请号：US11962855
申请日：2007-12-21
IPC分类号： A61K31/551 , C07D243/10
CPC分类号： C07D243/38 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14
摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
摘要翻译： 本发明涉及由式I表示的生物活性二苯并二氮杂酮类似物，其制备方法，包含它们的药物组合物和治疗肿瘤病症的方法。
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6.发明授权Phosphate prodrugs of a farnesyl dibenzodiazepinone, processes for their production and their use as pharmaceuticals 失效法呢基二苯并二氮杂酮的磷酸酯前药，其制备方法及其作为药物的用途公开(公告)号：US07384935B2
公开(公告)日：2008-06-10
申请号：US11527581
申请日：2006-09-27
申请人： Mustapha Aouidate , James B. McAlpine , Faustinus Yeboah , Ashraf Ibrahim , Arjun H. Banskota , Maxime Ranger , Gregory L. White
发明人： Mustapha Aouidate , James B. McAlpine , Faustinus Yeboah , Ashraf Ibrahim , Arjun H. Banskota , Maxime Ranger , Gregory L. White
IPC分类号： C07D243/10 , A61K31/551 , A61P35/00
CPC分类号： C07D243/10 , C07F9/5535
摘要： This invention relates to phosphate prodrugs of a farnesylated dibenzodiazepinone, to processes of their manufacture, to pharmaceutical compositions comprising the prodrugs, and to their use in the treatment of neoplasms.
摘要翻译： 本发明涉及法呢基化二苯并二氮杂酮的磷酸酯前药，其制备方法，包含前药的药物组合物及其在治疗赘生物中的用途。
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7.发明授权Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals 失效二苯并二氮杂酮类似物，其制备方法及其作为药物的用途公开(公告)号：US07304054B2
公开(公告)日：2007-12-04
申请号：US11235398
申请日：2005-09-27
IPC分类号： C07D243/10 , A61K31/551 , A61P35/00
CPC分类号： C12N9/93 , A61K38/00 , C07D243/38 , C07D405/06 , C07D405/14 , C12N9/0004 , C12N9/10 , C12N9/12 , C12N9/14 , C12N9/88 , C12N9/90 , C12N15/52 , C12P17/10 , C12R1/29 , Y02A50/473
摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
摘要翻译： 本发明涉及由式I表示的生物活性二苯并二氮杂酮类似物，其制备方法，包含它们的药物组合物和治疗肿瘤病症的方法。
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8.发明申请Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals 审中-公开二苯并二氮杂酮类似物，其制备方法及其作为药物的用途公开(公告)号：US20060079512A1
公开(公告)日：2006-04-13
申请号：US11253658
申请日：2005-10-20
IPC分类号： A61K31/551 , C07D243/10
CPC分类号： C12N9/93 , A61K38/00 , C07D243/38 , C07D405/06 , C07D405/14 , C12N9/0004 , C12N9/10 , C12N9/12 , C12N9/14 , C12N9/88 , C12N9/90 , C12N15/52 , C12P17/10 , C12R1/29 , Y02A50/473
摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
摘要翻译： 本发明涉及由式I表示的生物活性二苯并二氮杂酮类似物，其制备方法，包含它们的药物组合物和治疗肿瘤病症的方法。
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