|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) |
1. A compound of formula I ##STR00010## or a pharmaceutically acceptable salt, hydrate, solvate or prodrug of the compound, wherein: R.sup.1 is hydrogen, --OH, --NO.sub.2, --CN,
--COOR, --OCH.sub.2OR, C.sub.1-C.sub.6 alkyl, C.sub.2-C.sub.6 alkenyl, C.sub.2-C.sub.6 alkynyl, C.sub.1-C.sub.6 alkoxy or halo; R is C.sub.1-C.sub.6 alkyl; R.sup.2 is a radiofluoro; R.sup.3 is hydrogen, C.sub.1-C.sub.6 alkyl, C.sub.2-C.sub.6 alkenyl
or C.sub.2-C.sub.6 alkynyl; and R.sup.4 is hydrogen, C.sub.1-C.sub.6 alkyl, C.sub.2-C.sub.6 alkenyl or C.sub.2-C.sub.6 alkynyl.
2. The compound of claim 1, wherein: R.sup.1 is --OH or C.sub.1-C.sub.6 alkoxy; R.sup.2 is .sup.18F; R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1-C.sub.6 alkyl.
3. The compound of claim 1 having the following structure: ##STR00011##
4. A pharmaceutical composition comprising (i) an effective amount of a compound of claim 1; and (ii) a pharmaceutically acceptable carrier.