首页> 外国专利> METAL OXIDES NANOPARTICLES CONJUGATED WITH NAPHTHALENE DERIVATIVES AS CONTRAST AGENTS FOR THE DETECTION OF BETA AMYLOID PLAQUES BY MAGNETIC RESONANCE IMAGES

METAL OXIDES NANOPARTICLES CONJUGATED WITH NAPHTHALENE DERIVATIVES AS CONTRAST AGENTS FOR THE DETECTION OF BETA AMYLOID PLAQUES BY MAGNETIC RESONANCE IMAGES

机译:与萘衍生物缀合的金属氧化物纳米微粒作为造影剂通过磁共振图像检测β淀粉样蛋白斑的对比剂

摘要

This invention is directed to metal oxide nanoparticles of the general formula (I) wherein : wherein • R 1; is an organic coating to the metal oxide core, of polymeric type, catechol derivatives and trialkoxyalkylaminosilane; • R 2 : -NHCO-alkylenyl-C(0)NH-alkylenyl-R 3; • R 3 : -COO-, -CO-, -NH, -0-, -S-, -NH-alkylenyl-NH-, -NR 4-CSS-; • R 4 : -H, -CH 3, -CH 2-CH 3, -CH 2CH 2CH 3, and • M x0 y : iron oxide (Fe 3O 4 / gamma Fe 20 3), gadolinium oxide (III), manganese oxide (II) and copper (II) oxide; wherein the conjugated, functionalized and coated magnetic nanoparticle is capable of, when it is administered to a mammal, crossing the blood-brain barrier and specifically binding to the agglomerates and amyloid plaques present in brain tissue, and wherein with this nanoparticle bound to the agglomerates and beta- amyloid plaques in the brain tissue, hypo- or hyper-intense signals are observed in the region of interest through magnetic resonance imaging (MRI). The nanoparticles of formula I are capable of acting as positive (T1) and/or negative (T2) contrast agents for MRI for the early and non-
机译:本发明涉及通式(I)的金属氧化物纳米颗粒,其中:其中:•R 1 ;是金属型,聚合物型,邻苯二酚衍生物和三烷氧基烷基氨基硅烷的有机涂层; •R 2 :-NHCO-亚烷基-C(0)NH-亚烷基-R 3; •R 3 :-COO-,-CO-,-NH,-0-,-S-,-NH-亚烷基-NH-,-NR 4 -CSS -; •R 4 :-H,-CH 3 ,-CH 2 -CH 3 ,-CH 2 CH 2 CH 3 ,以及•M x 0 y :氧化铁(Fe 3 O 4 /γFe(Sub> 2 0 3 ),氧化g(III),氧化锰(II)和氧化铜(II);其中,将共轭的,官能化的和包被的磁性纳米颗粒施用于哺乳动物时能够穿过血脑屏障并特异性结合于脑组织中存在的团聚体和淀粉样蛋白斑,并且其中该纳米粒子与团聚体结合在大脑组织中的β和淀粉样蛋白斑块中,通过磁共振成像(MRI)在目标区域观察到了低强度或高强度信号。式I的纳米粒子能够在早期和非早期用于MRI的正(T1)和/或负(T2)造影剂

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