Methods of using benzothiazole derivative compounds and compositions

摘要

This invention provides benzothiazole derivative compounds, compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for detecting amyloid deposit(s) and for diagnosing a disease, disorder or condition characterized by amyloid deposit(s).

主权项

1. A method for distinguishing an Alzheimer's diseased brain from a normal brain comprising:
(i) obtaining tissues from the cerebellum and another area of the same brain, of a normal mammal and of a mammal suspected of having Alzheimer's disease; (ii) contacting the tissues with a compound of formula I; (iii) quantifying the amyloid bound to the compound; (iv) calculating the ratio of (a) the amount of amyloid in the area of the brain other than the cerebellum to (b) the amount of amyloid in the cerebellum; and (v) comparing the ratio for a normal mammal with the ratio for a mammal suspected of having Alzheimer's disease, wherein the compound of formula I is represented by formula I or a pharmaceutically acceptable salt of the compound, wherein: R1 is hydrogen, —OH, —NO2, —CN, —COOR, —OCH2OR, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, or halo; R is C1-C6 alkyl; R2 is a non-radioactive halo or a radioactive halo; R3 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; and R4 is C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl, wherein when R2 is a non-radioactive halo, the alkyl, alkenyl or alkynyl of R4 comprises a radioactive carbon or 3H, or is substituted with a radioactive halo.