Radiofluorination methods

Details Radiofluorination methods Radiofluorination methods

2008-05-06

2008-05-06

Gupta, Anish (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C424S001690, C424S001890

Reexamination Certificate

active

10508682

ABSTRACT:
The present invention relates to methods and reagents for [18F]-fluorination, particularly of peptides. The resultant18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET). Thus, a compound of formula18F-(Linker)-SH, such as a compound of formula (IV), (V), or (VI):in-line-formulae description="In-line Formulae" end="lead"?18F—(CH2CH2O)n—(CH2)m—SH   (IV)in-line-formulae description="In-line Formulae" end="tail"?in-line-formulae description="In-line Formulae" end="lead"?18F—(CH2)p—SH   (V)in-line-formulae description="In-line Formulae" end="tail"?may be reacted with an activated peptide as a means for18F-labelling.

REFERENCES:
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Hwang, D.R., et.al., “Positron-Labeled Angiotensin-converting Enzyme (ACE) Inhibitor: Fluorine-18-Fluorocaptopril. Probing the Ace Activity in vivo by Positron Emission Tomography” Journal of Nuclear Medicine, Society of Nuclear Medicine, New York, US, vol. 32, No. 9 Sep. 1, 1991 pp. 1730-1737.
Okarvi, “Recent progress in fluorine-18 labelled peptide radiopharmaceuticals”, Eur. J. Nuclear Medicine 2001, 28(7) pp. 929-938.
Int'l Search Report for PCT/GB03/01332 dated Jul. 23, 2003.
Great Britain Search Report for GB 0206750.2 dated Oct. 21, 2002.

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