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公开(公告)号：US08912186B2
公开(公告)日：2014-12-16
申请号：US13124773
申请日：2009-10-16
IPC分类号： A01N43/58 , A61K31/50 , C07C59/88 , C07C59/90 , C07D213/55 , C07D307/80 , C07D333/56 , C07D209/18
CPC分类号： C07D209/18 , C07C59/88 , C07C59/90 , C07D213/55 , C07D307/80 , C07D333/56
摘要： The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
摘要翻译： 本发明提供了特异性调节AGC蛋白激酶和Aurora家族蛋白激酶的活性或调节蛋白质 - 蛋白质相互作用的特异性小分子化合物，其生产方法，包含其的药物组合物及其用于制备药物用于治疗和 预防与AGC蛋白激酶或Aurora家族蛋白激酶异常活动有关的疾病。
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公开(公告)号：US20120046307A1
公开(公告)日：2012-02-23
申请号：US13124773
申请日：2009-10-16
IPC分类号： A61K31/517 , A61K31/515 , A61K31/47 , A61K31/4184 , A61K31/404 , A61K31/381 , A61K31/343 , A61K31/192 , C07D239/72 , C07D239/02 , C07D215/14 , C07D235/12 , C07D209/18 , C07D333/56 , C07D307/87 , C07C57/42 , A61P9/12 , A61P35/00 , A61P3/10 , A61P29/00 , A61P37/00 , A61P25/28 , A61P31/00 , C12N9/12
CPC分类号： C07D209/18 , C07C59/88 , C07C59/90 , C07D213/55 , C07D307/80 , C07D333/56
摘要： The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
摘要翻译： 本发明提供了特异性调节AGC蛋白激酶和Aurora家族蛋白激酶的活性或调节蛋白质 - 蛋白质相互作用的特异性小分子化合物，其生产方法，包含其的药物组合物及其用于制备药物用于治疗和 预防与AGC蛋白激酶或Aurora家族蛋白激酶异常活动有关的疾病。
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公开(公告)号：US20140017701A1
公开(公告)日：2014-01-16
申请号：US14001539
申请日：2012-02-24
IPC分类号： C12N9/12 , G01N33/573
CPC分类号： C12N9/12 , C07K2299/00 , C12Q1/485 , C12Y207/11001 , G01N33/573 , G01N2333/912 , G01N2500/00 , G01N2500/02 , G01N2500/04
摘要： The invention provides chimeric 3-phosphoinositide-dependent protein kinase 1 (PDK1), the PIF-binding pocket of which has mutations to mimic a second protein kinase, its production and use. The invention further provides a method for screening for compounds interacting with the PIF-pocket of an AGC kinase.
摘要翻译： 本发明提供嵌合的3-磷酸肌醇依赖性蛋白激酶1（PDK1），其PIF结合口袋具有模拟第二蛋白激酶的突变体，其生产和用途。 本发明还提供了用于筛选与AGC激酶的PIF-袋相互作用的化合物的方法。
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4.发明申请HIGH RESOLUTION COMPLEX STRUCTURE AND ALLOSTERIC EFFECTS OF LOW MOLECULAR WEIGHT ACTIVATORS ON THE PROTEIN KINASE PDK1 审中-公开低分子重量激活剂对蛋白激酶PDK1的高分辨率复合结构和免疫效应公开(公告)号：US20120003668A1
公开(公告)日：2012-01-05
申请号：US13124495
申请日：2009-10-19
申请人： Valerie Hindie , Ricardo M. Biondi
发明人： Valerie Hindie , Ricardo M. Biondi
CPC分类号： G01N33/573 , C07C57/60 , C12N9/1205 , G01N2333/912
摘要： The present invention provides a mutant form of a protein kinase its production and its use for identifying compounds that bind to the PIF-binding pocket allosteric site of the protein kinase.
摘要翻译： 本发明提供蛋白激酶的突变形式，其生产及其用于鉴定结合蛋白激酶的PIF结合口袋变构位点的化合物。
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5.发明申请METHOD OF MODULATION OF PROTEIN PHOSPHORYLATION-DEPENDENT CONFORMATIONAL TRANSITIONS WITH LOW MOLECULAR WEIGHT COMPOUNDS 审中-公开蛋白质磷酸化依赖性配体转移与低分子重量化合物的调节方法公开(公告)号：US20110152166A1
公开(公告)日：2011-06-23
申请号：US12441890
申请日：2007-08-20
申请人： Ricardo M. Biondi , Mathias Engel , Frodin Morten
发明人： Ricardo M. Biondi , Mathias Engel , Frodin Morten
IPC分类号： A61K38/02 , G01N33/573 , G01N33/574 , C12N9/12 , C07C323/56 , C40B30/02 , C12Q1/48 , C12Q1/68 , A61P35/00 , A61P3/10 , A61P3/00
CPC分类号： C12Q1/485 , C07C323/52 , C07C2602/08 , C07C2602/10 , G01N33/5011 , G01N33/5088 , G01N33/542 , G01N2333/9121 , G01N2500/00
摘要： The present patent application discloses a method of identifying or validating a compound that modulates the phosphorylation-dependent activity of a target protein or protein complex, where the target protein or protein complex activity is regulated by phosphorylation, as well as the use of identified compounds for the production of a pharmaceutical preparation especially for the treatment of cancer, insulin resistance and diabetes.
摘要翻译： 本专利申请公开了一种鉴定或验证调节靶蛋白或蛋白质复合物的磷酸化依赖性活性的化合物的方法，其中靶蛋白或蛋白质复合物活性通过磷酸化调节，以及使用鉴定的化合物 制备特别是用于治疗癌症，胰岛素抵抗和糖尿病的药物制剂。
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