IP Library Granted Patent US 12679818
Granted Patent B2
US 12679818 · App. 18/037,038 · Granted Jul 14, 2026

Radioactive halogen labeling precursor compound

Inventors: Hiroshi Tanaka (Tokyo, JP); Kazuhiro Takahashi (Fukushima, JP); Miho Suzuki (Fukushima, JP)
Assignees: Institute of Science Tokyo; Fukushima Medical University; Taiyo Nippon Sanso Corporation
C07D319/06C07B59/002C07C309/83C07D405/06C07D407/12
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Quick Facts
Patent No.
US 12679818
App. No.
18/037,038
Granted
Jul 14, 2026
Kind
B2
Abstract

Provided is, as a radioactive halogen labeling precursor compound that is highly reactive and stable, a compound represented by the following general formula (II): wherein R 1 and R 2 each independently represent an alkyl group having 5 to 20 carbon atoms, X 1 and X 2 each independently represent a halogen atom, and R 3 represents a monovalent group derived from a sugar, or the like.

Claims (13)

1 . A compound represented by the following general formula (I):

wherein R 1 and R 2 each independently represent an alkyl group having 5 to 20 carbon atoms, X 1 and X 2 each independently represent a halogen atom, and X 3 represents a halogen atom.

2 . The compound according to claim 1 , wherein R 1 and R 2 in the general formula (I) are each an alkyl group having 7 to 11 carbon atoms.

3 . The compound according to claim 1 , wherein X 1 and X 2 in the general formula (I) are each a fluorine atom or a chlorine atom.

4 . A compound represented by the following general formula (II):

wherein R 1 and R 2 each independently represent an alkyl group having 5 to 20 carbon atoms, X 1 and X 2 each independently represent a halogen atom, and R 3 represents (i) a monovalent group derived from a sugar, which is a monovalent group obtained by removing one hydrogen atom in the sugar; (ii) a monovalent group derived from a peptide, which is a monovalent group obtained by removing one hydrogen atom in the peptide; or (iii) a group represented by the following general formula (A) or (B):

wherein L represents a divalent group that functions as a spacer, R 4 represents an aryl group optionally substituted with a substituent, a heteroaryl group optionally substituted with a substituent, or an aminocarbonyl group optionally protected by a protective group, and * represents a bonding site.

5 . The compound according to claim 4 , wherein R 1 and R 2 in the general formula (II) are each an alkyl group having 7 to 11 carbon atoms.

6 . The compound according to claim 4 , wherein X 1 and X 2 in the general formula (II) are each a fluorine atom or a chlorine atom.

7 . The compound according to claim 4 , wherein L in the general formula (A) or (B) is an alkylene group, and one or more —CH 2 — of the alkylene group are optionally replaced with —O— or a phenylene group.

8 . The compound according to claim 4 , wherein R 4 in the general formula (A) or (B) is a 4-[2,3-bis(tert-butoxycarbonyl)guanidinomethyl]phenyl group, a naphthalen-2-yl group, a 2-nitro-1H-imidazol-1-yl group, or an aminocarbonyl group protected by a tert-butoxycarbonyl group.

9 . A reagent for producing a labeling precursor compound, comprising the compound according to claim 1 .

10 . A labeling precursor reagent for a radioactive halogen-labeled compound, comprising the compound according to claim 4 .