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1. WO2020094161 - METAL OXIDES NANOPARTICLES CONJUGATED WITH NAPHTHALENE DERIVATIVES AS CONTRAST AGENTS FOR THE DETECTION OF BETA AMYLOID PLAQUES BY MAGNETIC RESONANCE IMAGES

Publication Number WO/2020/094161
Publication Date 14.05.2020
International Application No. PCT/CU2019/050005
International Filing Date 13.05.2019
IPC
A61K 49/18 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance (NMR) contrast preparations; Magnetic resonance imaging (MRI) contrast preparations
18characterised by a special physical form, e.g. emulsions, microcapsules, liposomes
CPC
A61K 33/244
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33Medicinal preparations containing inorganic active ingredients
24Heavy metals; Compounds thereof
244Lanthanides; Compounds thereof
A61K 33/26
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33Medicinal preparations containing inorganic active ingredients
24Heavy metals; Compounds thereof
26Iron; Compounds thereof
A61K 49/186
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
18characterised by a special physical form, e.g. emulsions, microcapsules, liposomes
1818particles, e.g. uncoated or non-functionalised microparticles or nanoparticles
1821coated or functionalised microparticles or nanoparticles
1824coated or functionalised nanoparticles
1827having a (super)(para)magnetic core, being a solid MRI-active material, e.g. magnetite, or composed of a plurality of MRI-active, organic agents, e.g. Gd-chelates, or nuclei, e.g. Eu3+, encapsulated or entrapped in the core of the coated or functionalised nanoparticle
1851having a (super)(para)magnetic core coated or functionalised with an organic macromolecular compound, i.e. oligomeric, polymeric, dendrimeric organic molecule
1857the organic macromolecular compound being obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. PLGA
186the organic macromolecular compound being polyethyleneglycol [PEG]
Applicants
  • CENTRO DE NEUROCIENCIAS DE CUBA [CU]/[CU]
  • FACULTAD DE QUÍMICA. UNIVERSIDAD DE LA HABANA [CU]/[CU]
Inventors
  • RODRIGUEZ-TANTY, Chryslaine
  • SABLÓN CARRAZANA, Marquiza
  • GONZÁLEZ DALMAU, Evelio
  • DÍAZ GARCÍA, Alicia Marcelina
  • PANEQUE QUEVEDO, Armando Augusto
  • GUZMÁN RODRIGUEZ, Andy
  • RODRÍGUEZ IZQUIERDO, Julio Ricardo
  • RIVERA MARRERO, Suchitil
  • HERNÁNDEZ RODRÍGUEZ, Armando José
  • REYES MOLINA, Israel
  • IRIARTE MESA, Claudia
  • LEÓN CHAVIANO, Samila
  • SOTO MENÉNDEZ DEL VALLE, Roberto
  • BENCOMO MARTÍNEZ, Alberto
Agents
  • RÚA ORTIZ, Janet
Priority Data
2018-013806.11.2018CU
Publication Language Spanish (ES)
Filing Language Spanish (ES)
Designated States
Title
(EN) METAL OXIDES NANOPARTICLES CONJUGATED WITH NAPHTHALENE DERIVATIVES AS CONTRAST AGENTS FOR THE DETECTION OF BETA AMYLOID PLAQUES BY MAGNETIC RESONANCE IMAGES
(ES) NANOPARTÍCULAS DE ÓXIDOS METÁLICOS CONJUGADOS CON DERIVADOS DE NAFTALENO EN CUANTO AGENTES DE CONTRASTE PARA LA DETECCIÓN DE PLACAS BETA AMILOIDES POR IMÁGENES DE RESONANCIA MAGNÉTICA
(FR) NANOPARTICULES D'OXYDES MÉTALLIQUES CONJUGUÉS AVEC DES DÉRIVÉS DE NAPHTALÈNE EN TANT QU'AGENTS DE CONTRASTE POUR LA DÉTECTION DE PLAQUES BÊTA AMYLIOÏDES PAR IMAGES DE RÉSONANCE MAGNÉTIQUE
Abstract
(EN)
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-
(ES)
Esta invención se refiere a nanopartículas de óxidos metálicos de fórmula general I, donde R1 es una capa orgánica que recubre el núcleo del óxido de metal, de tipo polimérico, derivado del catecol o trialcoxialquilaminosilano; R2: -NHCO-alquilenil-C(0)NH-alquilenil-R3; 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, y M x0 y : óxido de hierro (Fe 3O 4 / gamma Fe 20 3), óxido de gadolinio (III), óxido de manganeso (II) u óxido de cobre (II); donde la nanopartícula magnénica recubierta, conjugada y funcionalizada, cuando se administra a mamíferos, es capaz de atravesar la barrera hematoencefálica y de unirse a los aglomerados y placas amiloides presentes en el tejido cerebral, y donde, con la nanopartícula enlazada a los aglomerados y las placas beta amiloides en el tejido cerebral, pueden observarse señales hipointensas e hiperintensas en la región de interés mediante imagen por resonancia magnética (IRM). Las nanopartículas de fórmula I pueden actuar como agentes de contraste positivos (T1) o negativos (T2) de IRM en el diagnóstico temprano y no invasivo de la EA, mediante una señal hipointensa o hiperintensa de las placas beta amiloides.
(FR)
L'invention concerne les branches de la chimie et de la physique appliquées à la médecine et se rapporte à l'obtention de nanoparticules d'oxydes métalliques de formule générale I, dont les substituants R1, R2 et R3 sont présentés dans la descritption et les revendications. Ces nanoparticules magnétiques, recouvertes, fonctionnalisées et conjuguées à des composés naphtaléniques apparentés aux agglomérats et aux plaques β-amyloïdes présentes dans les maladies neurodégénératives, traversent la barrière hémato-encéphalique (BHE) sans avoir recours à un quelconque agent perturbateur de membrane. Ces composés sont utilisés dans la détection précoce et non invasive d'agglomérats et de plaques amyloïdes au moyen de la technique d'imagerie par résonance magnétique (IRM) et peuvent agir en tant qu'agents de contraste pour IRM dans le diagnostic précoce et non invasif de la maladie d'Alzheimer.
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