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

Abstract

Compositions useful for labeling .beta.-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I): ##STR00001## 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, ##STR00002## wherein 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-alkyl, --C(O)NH-alkylenyl-R.sub.4 and --C(O)NH.sub.2; 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; and R.sub.2 is selected from the group consisting of alkyl and alkylenyl-R.sub.10 and R.sub.3 is 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.10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl, and further wherein one or more of the hydrogen, halogen or carbon atoms are optionally replaced withmore » 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.:
Regents of University of California (Oakland, CA)
Sponsoring Org.:
USDOE
OSTI Identifier:
970535
Patent Number(s):
7341709
Assignee:
Regents of University of California (Oakland, CA)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
DOE Contract Number:  
FC03-87ER60615
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES

Citation Formats

Barrio, Jorge R, Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W, Cole, Gregory M, and Huang, Sung-Cheng. Compositions for labeling .beta.-amyloid plaques and neurofibrillary tangles. United States: N. p., 2008. Web.
Barrio, Jorge R, Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W, Cole, Gregory M, & Huang, Sung-Cheng. Compositions 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. Tue . "Compositions for labeling .beta.-amyloid plaques and neurofibrillary tangles". United States. https://www.osti.gov/servlets/purl/970535.
@article{osti_970535,
title = {Compositions 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 = {Compositions useful for labeling .beta.-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I): ##STR00001## 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, ##STR00002## wherein 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-alkyl, --C(O)NH-alkylenyl-R.sub.4 and --C(O)NH.sub.2; 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; and R.sub.2 is selected from the group consisting of alkyl and alkylenyl-R.sub.10 and R.sub.3 is 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.10, 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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2008},
month = {3}
}

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