Imaging agents

Patent metadata

Field	Value
Publication number	US-10259781-B2
Application number	US-201815891819-A
Country	US
Kind code	B2
Filing date	Feb 8, 2018
Priority date	Sep 25, 2012
Publication date	Apr 16, 2019
Grant date	Apr 16, 2019

Abstract

Provided herein is technology relating to imaging agents and particularly, but not exclusively, to methods of manufacturing fluorine-18-labeled phenethylguanidines and uses thereof.

First claim

We claim:

1. A compound comprising a structure according to:

wherein
Y is O;
n is 1, 2, or 3;
one of R 1 -R 5 is 18 F; and
each of R 1 -R 5 , when not 18 F, is independently selected from the group consisting of halo, hydroxy, and hydrogen.

2. The compound according to claim 1 wherein n is 2.

3. The compound according to claim 1 wherein
at least one of R 2 -R 4 is hydroxy; and
each of R 1 -R 5 , when not 18 F or hydroxy, is hydrogen.

4. The compound according to claim 1 wherein
n is 2,
at least one of R 2 -R 4 is hydroxy; and
each of R 1 -R 5 , when not 18 F or hydroxy, is hydrogen.

5. A radiotracing composition comprising a compound according to claim 1 .

6. The radiotracing composition according to claim 5 further comprising a physiologically acceptable carrier.

7. The radiotracing composition of claim 5 formulated for intravenous administration.

8. The radiotracing composition of claim 5 formulated for systemic administration.

9. An iodonium salt precursor of the compound according to claim 1 , wherein said iodonium salt precursor has a structure according to:

wherein
Y is O;
n is 1, 2, or 3;
one of R 1 -R 5 comprises iodonium;
each of R 1 -R 5 , when not comprising iodonium, is independently selected from the group consisting of halo, protected hydroxy, and hydrogen; and
each of R 6 -R 9 comprises a nitrogen-protecting group.

10. The iodonium salt precursor according to claim 9 wherein n is 2.

11. The iodonium salt precursor according to claim 9 wherein at least one of R 2 -R 4 is protected hydroxy; and
each of R 1 -R 5 , when not comprising iodonium or protected hydroxy, is hydrogen.

12. The iodonium salt precursor according to claim 9 wherein
n is 2,
at least one of R 2 -R 4 is protected hydroxy; and
each of R 1 -R 5 , when not comprising iodonium or protected hydroxy, is hydrogen.

Assignees

• Univ Michigan Regents

Inventors

• Raffel David M
• Jung Yong-Woon
• Jang Keun-Sam

Classifications

• C07B59/001

  Acyclic or carbocyclic compounds · CPC title

• C07C279/06

  being further substituted by halogen atoms, or by nitro or nitroso groups · CPC title

• C07B59/002

  Heterocyclic compounds · CPC title

• A61K31/155 Primary

  Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2) · CPC title

• C07C277/08

  of substituted guanidines · CPC title