University of California

Andrej Petric

Nagichettiar Satyamurthy

Jorge R Barrio

Gary W Small

Gregory M Cole

Sung-Cheng Huang

Compositions useful for labeling &#x3b2;-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I): wherein Ris selected from the group consisting of &#x2014;C(O)-alkyl, &#x2014;C(O)-alkylenyl-R, &#x2014;C(O)O-alkyl, &#x2014;C(O)O-alkylenyl-R, &#x2014;C&#x2550;C(CN)-alkyl, &#x2014;C&#x2550;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 &#x2014;NH, &#x2014;OH, &#x2014;SH, &#x2014;NH-alkyl, &#x2014;NHR, &#x2014;NH-alkylenyl-R, &#x2014;O-alkyl, &#x2014;O-alkylenyl-R, &#x2014;S-alkyl, and &#x2014;S-alkylenyl-R; Ris a radical selected from the group consisting of &#x2014;CN, &#x2014;COOH, &#x2014;C(O)O-alkyl, &#x2014;C(O)O-alkylenyl-R, &#x2014;C(O)-alkyl, &#x2014;C(O)-alkylenyl-R, &#x2014;C(O)-halogen, &#x2014;C(O)NH-alkyl, &#x2014;C(O)NH-alkylenyl-Rand &#x2014;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 &#x2014;OH, &#x2014;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.

Compositions for labeling &#x3b2;-amyloid plaques and neurofibrillary tangles

Methods for labeling &bgr;-amyloid plaques and neurofibrillary tangles

A method for labeling &bgr;-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I):

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Ljubljana, Slovenia

Andrej Petric