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US 6,696,039 B2Granted
Amyloid plaque aggregation inhibitors and diagnostic imaging agents
AssigneeThe Trustees of the University of Pennsylvania
InventorsHank F. 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.
Claims24
A compound of Formula III:
- or a pharmaceutically acceptable salt thereof, wherein
- R3 is Br, I, F, 125I, 131I, 123I, 18F, 76Br, 77Br of Sn(alkyl)3;
- and
- R1 and R2 are independently hydrogen, C1-4 alkyl C2-4 aminoalkyl, C1-4 haloalkyl, haloarylalkyl, 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.
2 more elements
A compound of Formula III′:
- or a pharmaceutically acceptable salt thereof, wherein
- A, B and D are CH or N,
- provided that no more than two of A, B and D is N;
- R3 is Br, I, F, 125I, 131I, 123I, 18F, 76Br, 77Br, haloalkyl, Sn(alkyl)3 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, such as —(CH2)n—, or —(CH2)n—C(O)—
- where
- n is 0-5;
- and
- Ch is a tetradentate ligand capable of complexing with a metal;
- with the proviso that only one of R1, R2 and R3 can be —L—Ch.
9 more elements
Dependencies are inferred from the claim text.