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1. 发明申请

WO2014047447A2 FTO MODULATING COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译： FTO调节化合物及其使用方法
公开(公告)号：WO2014047447A2
公开(公告)日：2014-03-27
申请号：PCT/US2013/060934
申请日：2013-09-20
申请人： MIDWESTERN UNIVERSITY , OLSEN, Mark , ROWLES, Joie , IACOBAN, Paulina , TRIBBEY, Leah Mary , COX, Thomas
发明人： OLSEN, Mark , ROWLES, Joie , IACOBAN, Paulina , TRIBBEY, Leah Mary , COX, Thomas
IPC分类号： A61K31/34
CPC分类号： C07D417/04 , A61P35/00 , C07D307/32 , C07D307/66 , C07D405/04 , C07D405/12 , C07D409/04 , C12Q1/26
摘要： The present invention relates to compounds which modulate the level or activity of polypeptides having Fe(II) and 2-oxoglutarate (2QG)-dependent oxygenase activity in a cell, tissue, or subject, exemplified by the Fat Mass and Obesity Associated protein (FTO). Aspects relate to N-(3,4-dihydroxy-5-aryl-2-furanyl)-sulfonamides, methods for their synthesis, and methods of using these compounds to modulate the activity of FTO in a cell-free sample, a cell-based assay, and in a subject. Aspects are also directed to compositions comprising compounds which modulate the activity of FTO, including pharmaceutically-acceptable compositions, and to methods of preventing, ameliorating, or treating FTO-mediated conditions or diseases in a subject, including stroke, epilepsy, depression, and degenerative central nervous system disorders such as Alzheimer's and Parkinson's disease. Other aspects elate to use of the compounds to ameliorate or treat conditions associated with metabolic disorders, such as diabetes and obesity.
摘要翻译：本发明涉及调节在细胞，组织或受试者中具有Fe（II）和2-氧戊二酸（2QG） - 依赖性加氧酶活性的多肽的水平或活性的化合物，例如脂肪和肥胖相关蛋白（FTO ）。方面涉及N-（3,4-二羟基-5-芳基-2-呋喃基） - 磺酰胺，其合成方法以及使用这些化合物调节无细胞样品中FTO活性的方法，并且在受试者中。方面还涉及包含调节FTO的活性的化合物的组合物，包括药学上可接受的组合物，以及预防，改善或治疗受试者中的FTO介导的病症或疾病的方法，包括中风，癫痫，抑郁和退行性疾病中枢神经系统疾病如阿尔茨海默病和帕金森病。使用化合物改善或治疗与代谢紊乱如糖尿病和肥胖相关的病症的其它方面也是令人鼓舞的。

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