skip to main content
DOE Patents title logo U.S. Department of Energy
Office of Scientific and Technical Information

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

Abstract

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),more » one or more of the hydrogen, halogen or carbon atoms can, optionally, be replaced with a radiolabel.« less

Inventors:
 [1];  [2];  [3];  [3];  [4];  [5]
  1. (Agoura Hills, CA)
  2. (Ljubljana, SI)
  3. (Los Angeles, CA)
  4. (Santa Monica, CA)
  5. (Sherman Oaks, CA)
Issue Date:
Research Org.:
University of California
OSTI Identifier:
873929
Patent Number(s):
6274119
Assignee:
Regents of Univ. of California (Oakland, CA) OAK
DOE Contract Number:  
FC03-87ER60615
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
methods; labeling; beta; -amyloid; plaques; neurofibrillary; tangles; method; vivo; vitro; comprises; contacting; compound; formula; str1; mammalian; tissue; selected; consisting; -c; -alkyl; -alkylenyl-r; o-alkyl; o-alkylenyl-r; dbd; cn; str2; radical; alkyl; substituted; aryl; -nh; -oh; -sh; -nh-alkyl; -nhr; -nh-alkylenyl-r; -o-alkyl; -o-alkylenyl-r; -s-alkyl; -s-alkylenyl-r; -cn; -cooh; -halogen; nh; nh-alkyl; nh-alkylenyl-r; independently; alkylenyl-r; 10; -ots; halogen; spiperone; ketal; spiperone-3-yl; alternatively; form; heterocyclic; optionally; alkoxy; oh; ots; carbonyl; compounds; hydrogen; carbon; atoms; replaced; radiolabel; radical selected; independently selected; comprises contacting; carbon atoms; carbon atom; mammalian tissue; optionally substituted; neurofibrillary tangles; substituted alkyl; -amyloid plaques; /424/

Citation Formats

Barrio, Jorge R., Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W., Cole, Gregory M., and Huang, Sung-Cheng. Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles. United States: N. p., 2001. Web.
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. United States.
Barrio, Jorge R., Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W., Cole, Gregory M., and Huang, Sung-Cheng. Mon . "Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles". United States. https://www.osti.gov/servlets/purl/873929.
@article{osti_873929,
title = {Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles},
author = {Barrio, Jorge R. and Petric, Andrej and Satyamurthy, Nagichettiar and Small, Gary W. and Cole, Gregory M. and Huang, Sung-Cheng},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2001},
month = {1}
}

Patent:

Save / Share: