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Last Updated: December 23, 2024

Claims for Patent: 8,691,185


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Summary for Patent: 8,691,185
Title:Benzothiazole derivative compounds, compositions and uses
Abstract: This invention provides benzothiazole derivative compounds, compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for detecting amyloid deposit(s) and for diagnosing a disease, disorder or condition characterized by amyloid deposit(s).
Inventor(s): Klunk; William E. (Pittsburgh, PA), Mathis, Jr.; Chester A. (Pittsburgh, PA), Wang; Yanming (Imperial, PA)
Assignee: University of Pittsburgh--Of the Commonwealth System of Higher Education (Pittsburgh, PA)
Application Number:13/548,014
Patent Claims: 1. A method for detecting amyloid deposit(s) in vivo, comprising: (i) administering to a mammal an effective amount of a compound of the following structure ##STR00010## or a pharmaceutically acceptable salt, hydrate, or solvate of the compound wherein the compound would bind any amyloid deposit(s) in the mammal; and (ii) detecting binding of the compound to amyloid deposit(s) in the mammal.

2. The method of claim 1, wherein the amyloid deposit(s) is/are located in the brain of the mammal.

3. The method of claim 1, wherein the mammal is a human who is suspected of having Alzheimer's disease, familial Alzheimer's disease, Down's syndrome, Mild Cognitive Impairment or homozygotes for apolipoprotein E4 allele.

4. The method of claim 1, wherein the detecting is effected by gamma imaging, magnetic resonance imaging or magnetic resonance spectroscopy.

5. The method of claim 4, wherein the detecting is effected by gamma imaging.

6. The method of claim 5, wherein the gamma imaging is PET or SPECT.

7. The method of claim 1, wherein the compound is administered intravenously.

8. A method for detecting amyloid deposit(s) in vitro comprising: (i) contacting a bodily tissue with an effective amount of a compound of the following structure ##STR00011## or a pharmaceutically acceptable salt, hydrate, or solvate of the compound wherein the compound would bind any amyloid deposit(s) in the tissue; and (ii) detecting binding of the compound to amyloid deposit(s) in the tissue.

9. The method of claim 8, wherein the compound is in a solution that further comprises 25-99% ethanol, with the remainder of the solution being water.

10. The method of claim 8, wherein the compound is in a solution that further comprises 0-50% ethanol, with the remainder of the solution being water, and 0.0001 to 100 .mu.M of the compound.

11. The method of claim 8 wherein the detecting is effected by bright-field, fluorescence, laser-confocal or cross-polarization microscopy.

12. The method of claim 8, wherein the method further comprises: (iii) separating from the tissue the amyloid deposit(s) bound to the compound; and (iv) quantifying the amyloid deposit(s) bound to the compound.

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