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US 2017/0044080 A1Published application
Radioconjugation method
AssigneeGe Healthcare Limited
InventorBard Indrevoll
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Abstract
The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to a method of labelling a biological targeting molecule with a radioisotope. The method of the invention is particularly suitable for use with an automated synthesizer apparatus. Also provided are precursors in sterile form, as well as cassettes comprising such precursors useful in the method.
Claims20
A method for radiolabelling a biological targeting molecule which comprises:
- (i) providing a compound of Formula (IB)
- Q-[linker]-X1 (IB)
- (ii) deprotection of the protected compound of Formula (IB) of step (i) to give an aminooxy compound of Formula (IIB) respectively
- Q-[linker]-O—NH2 (IIB)
- (iii) condensation of the aminooxy compound of Formula (IIB) with a carbonyl compound of Formula (IIIB),
- [BTM]-(C═O)Y1 (IIIB)
- to give a radiolabelled conjugate of Formula (IVB):
- [BTM]-(CY1)═N—O-[linker]Q (IVB)
- wherein:
- [BTM] is a biological targeting molecule;
- X1 is a protected aminooxy group of formula:
- wherein R1 and R2 are independently chosen from C1-3 alkyl, C1-3 fluoroalkyl or C4-6 aryl;
- Q is a group which comprises a radioisotope suitable for PET or SPECT imaging in vivo;
- Y1 is H, C1-6 alkyl or C4-10 aryl, [linker] is a linker group.
11 more elements
A protected compound of Formula (IB)
- Q-[linker]-X1 (IB)
- wherein Xis a protected aminooxy group of formula:
- wherein R1 and R2 are independently chosen from C1-3 alkyl, C1-3 fluoroalkyl or C4-6 aryl;
- and Q is a group which comprises a radioisotope suitable for PET or SPECT imaging in vivo.
1 more element
Dependencies are inferred from the claim text.