Patent ID: 6274119
Filing Date: 2001-08-14
Classification: A61K

Abstract:
A method for labeling structures selected from the group consisting of .beta.-amyloid plaques and neurofibrillary tangles in vivo, comprising:contacting brain tissue with a compound of formula (I): ##STR17##wherein:R.sub.1 is selected from the group consisting of --C(O)-alkyl, --C(O)-alkylenyl-R.sub.4, --C(O)O-alkyl, --C(O)O-alkylenyl-R.sub.4, --C.dbd.C(CN).sub.2 -alkyl, --C.dbd.C(CN).sub.2 -alkylenyl-R.sub.4, ##STR18##whereinR.sub.4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;R.sub.5 is a radical selected from the group consisting of --NH.sub.2, --OH, --SH, --NH-alkyl, --NHR.sub.4, --NH-alkylenyl-R.sub.4, --O-alkyl, --O-alkylenyl-R.sub.4, --S-alkyl, and --S-alkylenyl-R.sub.4 ;R.sub.6 is a radical selected from the group consisting of --CN, --COOH, --C(O)O-alkyl, --C(O)O-alkylenyl-R.sub.4, --C(O)-alkyl, ---C(O)-alkylenyl-R.sub.4, --C(O)-halogen, --C(O)NH.sub.2, --C(O)NH-alkyl, --C(O)NH-alkylenyl-R.sub.4 ;R.sub.7 is a radical selected from the group consisting of O, NH, and S; andR.sub.8 is N, O or S; andR.sub.2 and R.sub.3 are each independently selected from the group consisting of alkyl and alkylenyl-R.sub.10, wherein R.sub.10 is selected from the group consisting of --OH, --OTs, halogen, spiperone, spiperone ketal, and spiperone-3-yl,or R.sub.2 and R.sub.3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkyl-R.sub.5, carbonyl, spiperone, spiperone ketal and spiperone-3-yl,and further wherein one or more of the hydrogen, halogen or carbon atoms are replaced with a radiolabel; anddetermining whether the structures have been labeled.