Benzothiazole derivatives for in vivo imaging of amyloid...

A - Human Necessities – 61 – K

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A61K 51/04 (2006.01) C07D 277/66 (2006.01)

Patent

CA 2474411

The invention provides use of a compound of formula (I): or a salt thereof, wherein:R1~ is 125~I, 124~I, 123~I, 75~Br, 76~Br, or 18~F; R2~ is C~1-6 alkyl; and R3~ is selected from hydrogen, C~1-6 alkyl, -C(O) C~1-.6 alkyl, -C(O)C~1-6 haloalkyl, and -C(O)CH(R4~)NH~2 ; wherein R4~ is selected from hydrogen, C~1- 6alkyl, C~1-6hydroxyalkyl, and C~1-6aminoalkyl; for the manufacture of a radiopharmaceutical for the in vivo diagnosis or imaging of an amyloid- associated disease, particularly Alzheimer's disease.

La présente invention concerne l'utilisation d'un composé représenté par la formule (I) ou un sel de ce dernier. Dans la formule, R1 représente 125I, 124I, 123I, 75Br, 76Br, ou 18F; R2 représente alkyle C1-6; et R3 est sélectionné parmi hydrogène, alkyle C1-6, -C(O) alkyle C1-.6, -C(O) haloalkyle C1-6, et -C(O)CH(R4)NH2; R4 étant sélectionné entre hydrogène, alkyle C1-6, hydroxyalkyle C1-6, et aminoalkyle C1-6. On utilise ce composé pour préparer un radiopharmaceutique employé dans le diagnostic ou l'imagerie in vivo de la maladie associée aux plaques amyloïdes, notamment la maladie d'Alzheimer. Formule (I)

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