公开(公告)号：US20160243264A1

公开(公告)日：2016-08-25

申请号：US15049126

申请日：2016-02-21

申请人： Hong Kong Baptist University

发明人： Yinhui LI ,  Di XU ,  See-Lok HO ,  Chung-Yan POON ,  Hei-Nga CHAN ,  Hung Wing LI ,  Ricky M. S. WONG

IPC分类号： A61K49/10 ,  G01R33/56 ,  A61B5/055 ,  A61M5/00 ,  A61K49/00 ,  A61B5/00

CPC分类号： A61K49/106 ,  A61K47/50 ,  A61K47/547 ,  A61K49/0002 ,  A61K49/0021 ,  A61K49/0026 ,  A61K49/0052 ,  A61K49/085 ,  A61K49/10 ,  A61M5/007 ,  C07D401/06 ,  G01R33/5601

摘要： The present invention is in the field of pharmaceuticals and chemical industries. In particular, one aspect of the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro and in vivo via magnetic resonance and florescence imaging by using modified carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using the modified carbazole-based fluorophore. The modified carbazole-based fluorophore according to an embodiment of the present invention is prepared by conjugating a carbazole-based fluorophore with magnetic nanoparticles to form a conjugate which is permeable to blood brain barrier of a subject being introduced therewith.

摘要翻译： 本发明在医药和化学工业领域。 特别地，本发明的一个方面涉及通过使用修饰的咔唑类荧光团通过磁共振和荧光成像在体外和体内标记，成像和检测β-淀粉样蛋白（Aβ）肽，寡聚体和原纤维的方法。 本发明的另一方面涉及减少和预防阿尔茨海默病（AD）的β-淀粉样肽聚集以及通过使用经修饰的咔唑类荧光团治疗和/或预防阿尔茨海默氏病的方法。 根据本发明的实施方案的经修饰的咔唑类荧光团通过将咔唑类荧光团与磁性纳米颗粒结合以形成可导入受试者的血脑屏障的缀合物来制备。