Compositions for labeling β-amyloid plaques and neurofibrillary tangles

Abstract

Compositions useful for labeling β-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I): wherein Ris selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R, —C(O)O-alkyl, —C(O)O-alkylenyl-R, —C═C(CN)-alkyl, —C═C(CN)-alkylenyl-R, wherein Ris a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; Ris a radical selected from the group consisting of —NH, —OH, —SH, —NH-alkyl, —NHR, —NH-alkylenyl-R, —O-alkyl, —O-alkylenyl-R, —S-alkyl, and —S-alkylenyl-R; Ris a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R, —C(O)-alkyl, —C(O)-alkylenyl-R, —C(O)-halogen, —C(O)NH-alkyl, —C(O)NH-alkylenyl-Rand —C(O)NH; Ris a radical selected from the group consisting of O, NH, and S; and Ris N, O or S; and Ris selected from the group consisting of alkyl and alkylenyl-Rand Ris alkylenyl-R, wherein Ris selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal, and spiperone-3-yl, or Rand Rtogether form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkyl-R, carbonyl, spiperone, spiperone ketal and spiperone-3-yl, and further wherein one or more of the hydrogen, halogen or carbon atoms are optionally replaced with a radiolabel.