Aryloxyanilide imaging agents
AssigneeGe Healthcare Limited
InventorsHarry John Wadsworth, Dennis O'Shea
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Abstract
The present invention provides a novel radiolabelled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
Claims8
A method for the preparation of an in vivo imaging agent of Formula I:
- wherein:
- A1 is —CR1R2—(CH2)n— wherein R1 and R2 are independently selected from hydrogen, fluoro, or C1-3 alkyl, and n is 0, 1 or 2;
- A2 is —CH2—, —O— or —O—CH2—;
- or,
- -A1-A2- is —CH═CH—
- said method comprises reacting a suitable source of 18F with a precursor compound of Formula II:
- wherein A1 is —CR1R2—(CH2)n— wherein R1 and R2 are independently selected from hydrogen, fluoro, or C1-3 alkyl, and n is 0, 1 or 2;
- A2 is —CH2—, —O—CH2—;
- or, -A1-A2 is —CH═CH—, and LG is a leaving group.
A kit comprising a precursor compound of Formula II in a sealed container wherein A1 is —CR1R2—(CH2)n— wherein R1 and R2 are independently selected from hydrogen, fluoro, or C1-3 alkyl, and n is 0, 1 or 2;
- A2 is —CH2—, —O—CH2—;
- or, -A1-A2 is —CH═CH—, and LG is a leaving group.
Dependencies are inferred from the claim text.