Amyloid plaque aggregation inhibitors and diagnostic imaging agents
AssigneeThe Trustees of the University of Pennsylvania
InventorsHank Kung, Mei-Ping Kung, Zhi-Ping Zhuang
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Abstract
This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled 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.
Claims20
A pharmaceutical composition, comprising a compound of Formula III and a pharmaceutically acceptable excipient or diluent, wherein a compound of Formula III is selected from:
- or a pharmaceutically acceptable salt thereof, wherein
- R3 is hydrogen or -L-Ch;
- R1 and R2 are independently hydrogen, C1-4 alkyl, C2-4 aminoalkyl, C1-4 haloalkyl, haloarylalkyl, -L-Ch, or R1 and R2 are taken together with the nitrogen to which they are attached to form a 5- to 7-member heterocyclic ring optionally having O, S or NR5 in said ring, where
- R5 is hydrogen or C1-4 alkyl;
- L is a covalent bond or linking group selected from the group consisting of:
- —(CH2)n—, or —(CH2)n—C(O)— where
- n is an integer from 0 to 5;
- and
- Ch is a tetradentate ligand capable of complexing with a metal;
- with the proviso that one and only one of R1, R2 and R3 is -L-Ch.
The pharmaceutical composition of claim 12, wherein R1 and R2 are both methyl.
Dependencies are inferred from the claim text.