申请人:Tamagnan Gilles D.
公开号:US20100143251A1
公开(公告)日:2010-06-10
The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus. The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions, derivatives, prodrugs, racemic mixtures or tautomeric forms thereof.
本发明提供了化合物及其淀粉样探针,可通过体内成像淀粉样和/或脑部区域的淀粉样沉积物,从而实现诊断AD和量化淀粉样沉积物(斑块)的程度或进展的生前方法。优选地,本发明的淀粉样探针可以穿过血脑屏障,区分AD脑和正常脑。可以向患者施用本发明的淀粉样探针,以适量成像淀粉样沉积物。本发明的淀粉样探针还可用于检测和量化包括但不限于唐氏综合症、家族性AD和载脂蛋白E4等位基因纯合子在内的疾病中的淀粉样沉积物。在一方面,这些化合物可以用于治疗或预防包括但不限于AD和2型糖尿病的疾病。本发明的化合物和淀粉样探针包括其类似物、盐、制药组合物、衍生物、前药、外消旋混合物或其互变异构体。