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|Title:||Styrylpyridine derivatives and their use for binding and imaging amyloid plaques|
|Abstract:||This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.|
|Inventor(s):||Kung; Hank F. (Winnewood, PA), Kung; Mei-Ping (Winnewood, PA)|
|Assignee:||The Trustees of the University of Pennsylvania (Philadelphia, PA)|
1. A compound having the formula: ##STR00039## wherein, R.sup.a and R.sup.b are independently hydrogen or C.sub.1-4alkyl; Z is I, .sup.123I, .sup.125I, .sup.131I, Br,
.sup.76Br, .sup.77Br, F, .sup.18F, or --OTosyl; and q is an integer from 2 to 5.
2. The compound of claim 1, wherein q is 3 or 4.
3. The compound of claim 1, wherein R.sup.a is methyl and R.sup.b is hydrogen.
4. The compound of claim 1 having the formula: ##STR00040##
5. The compound of claim 4 having the formula: ##STR00041##
6. The compound of claim 5 having the formula: ##STR00042##
7. The compound of claim 1 having the formula: ##STR00043##
8. The compound of claim 1 having the formula: ##STR00044##
9. The compound of claim 1, wherein R.sup.a and R.sup.b are independently hydrogen or methyl and q is an integer equal to 5.
10. A diagnostic composition for imaging amyloid deposits, comprising a radiolabeled compound of claim 1.
11. A method of imaging amyloid deposits in a mammal, comprising: introducing into the mammal a detectable quantity of a diagnostic composition of claim 10; allowing sufficient time for the labeled compound to be associated with amyloid deposits; and detecting the labeling compound associated with one or more amyloid deposits.
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