Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles

Barrio, Jorge R; Petric, Andrej; Satyamurthy, Nagichettiar; Small, Gary W; Cole, Gregory M; Huang, Sung-Cheng

Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles

Patent · Mon Jan 01 04:00:00 EST 2001

OSTI ID:873929

Barrio, Jorge R ^[1]; Petric, Andrej ^[2]; Satyamurthy, Nagichettiar ^[3]; Small, Gary W ^[3]; Cole, Gregory M ^[4]; Huang, Sung-Cheng ^[5]

Agoura Hills, CA
Ljubljana, SI
Los Angeles, CA
Santa Monica, CA
Sherman Oaks, CA

A method for labeling .beta.-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): ##STR1## with mammalian tissue. In formula (I), 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 , ##STR2## R.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 , --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; and R.sub.8 is N, O or S. R.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. Alternatively, 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, alkylenyl-R.sub.10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl. In the compounds of formula (I), one or more of the hydrogen, halogen or carbon atoms can, optionally, be replaced with a radiolabel.

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Research Organization:: University of California

DOE Contract Number:: FC03-87ER60615

Assignee:: Regents of Univ. of California (Oakland, CA)

Patent Number(s):: US 6274119

OSTI ID:: 873929

Country of Publication:: United States

Language:: English

References (14)

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--c
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Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles

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