Compounds for Non-Invasive Measurement of Aggregates of Amyloid Peptides
OwnerHenriksen Gjermund, Behrooz Hooshyar Yousefi +1inventors
InventorsHenriksen Gjermund, Behrooz Hooshyar Yousefi, Hans-Juergen Wester
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Abstract
The invention relates to the provision of compounds, methods for producing them, and their use for imaging and quantification of aggregates of β-amyloid peptides in vivo. In a preferred aspect of the invention, a tracer is administered to humans and displays enrichment in body parts that are containing aggregates of amyloid peptides. Tracers of the invention can be used for non-invasive depiction and quantification of aggregates of β-amyloid peptides in humans affected with diseases that are characterized in the generation of such aggregates.
Claims26
1-18. (canceled)
A tracer for aggregates of amyloid peptides comprising the structure
- wherein R1 is selected from the group consisting of H, F, Cl, Br, I, CN, CF3, alkyl, heteroaryl, heterocycloalkyl and NHR3, with R3 being an alkyl,
- R2 is —O—R4, wherein R4 is selected from the group consisting of CnH2n+1, CnH2n, CnH2n-halo, —CH2—CH═CH-halo, and —[CH2—CH2—O]m,—[CH2—CH2]o-halo, in which halo can be any halogen, and with n being in the range of from 1 to 5, with m being in the range of from 1 to 3 and with o being 1, and
- wherein Z is selected from the group consisting of S, O, N, NH and CH, and
- wherein p is 0 or 1, wherein the tracer comprises at least one F.
A method for the preparation of a tracer having the general formula
- wherein R1 is selected from the group consisting of H, F, Cl, Br, I, CN, CF3, alkyl, heteroaryl, heterocycloalkyl and NHR3, with R3 being an alkyl, wherein R2 is selected from the group consisting of —O—CnH2n—F, —O—CH2—CH═CH—F and —O—[CH2—CH2—O]m—[CH2—CH2]o—F, and wherein Z is selected from the group consisting of S, O, N, NH and CH, and wherein p is 0 or 1, the method comprising fluorinating a derivative of the general formula II
- wherein R1 is selected from the group consisting of H, F, Cl, Br, I, CN, CF3, alkyl, heteroaryl, heterocycloalkyl and NHR3, with R3 being an alkyl, wherein R2 is selected from the group consisting of —O—CnH2n-leaving group, —O—CH2—CH═CH-leaving group and —O—[CH2—CH2—O]m—[CH2—CH2]o— leaving group, and wherein Z is selected from the group consisting of S, O, N, NH and CH, and wherein p is 0 or 1,
- with [18F]fluoride.
Dependencies are inferred from the claim text.