Patent ID: 6660530
Filing Date: 2003-12-09
Classification: A61K

Abstract:
A method for labeling structures selected from the group consisting of &bgr;-amyloid plaques and neurofibrillary tangles in vitro, comprising contacting brain tissue with a compound of formula (I): wherein:R1 is selected from the group consisting of â€”C(O)-alkyl, â€”C(O)-alkylenyl-R4, â€”C(O)O-alkyl, â€”C(O)O-alkylenyl-R4, â€”C&boxH;C(CN)2-alkyl, â€”C&boxH;C(CN)2-alkylenyl-R4, â€ƒwherein R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5 is a radical selected from the group consisting of â€”NH2, â€”OH, â€”SH, â€”NH-alkyl, â€”NHR4, â€”NH-alkylenyl-R4, â€”O-alkyl, â€”O-alkylenyl-R4, â€”S-alkyl, and â€”S-alkylenyl-R4; R6 is a radical selected from the group consisting of â€”CN, â€”COOH, â€”C(O)O-alkyl, â€”C(O)O-alkylenyl-R4, â€”C(O)-alkyl, â€”C(O)-alkylenyl-R4, â€”C(O)-halogen, â€”C(O)NH2, â€”C(O)NH-alkyl, â€”C(O)NH-alkylenyl-R4; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S; and R2 and R3 are each independently selected from the group consisting of alkyl and alkylenyl-R10, wherein R10 is selected from the group consisting of â€”OH, â€”OTs, halogen, spiperone, spiperone ketal, and spiperone-3-yl, or R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkyl-R5, 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.