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US 2012/0237444 A1Published application
Iodine radiolabelling method
AssigneeGe Healthcare Limited
InventorMichelle Avory
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Abstract
The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.
Claims20
A method of radioiodination of a biological targeting moiety, said method comprising:
- (i) provision of a compound of Formula (I):
- (ii) reaction of said compound of Formula (I) with a compound of Formula (IIa) or Formula (IIb):
- I*—Y1-L2-N3 (IIa)
- I*—Y1-L3-C≡N+—O− (IIb)
- in the presence of a click cycloaddition catalyst, to give a conjugate of Formula (IIIa) or (IIIb) respectively:
- wherein:
- I* is a radioisotope of iodine suitable for in vivo imaging, chosen from 123I, 124I or 131I;
- L1, L2 and L3 are each independently a linker group which may be present or absent;
- Y1 is —Ar1— or —X1—;
- where —Ar1— is C3-10 arylene, and
- —X1— is —CH═CH—(CH2)n—(Ar1)j— or —CH═CH—(Ar1)j—(CH2)n—
- where j is 0 or 1, and n is an integer of value 0 to 4,
- wherein when Y1 is —X1—, I* is attached to —CH═CH terminus of X1;
- BTM is the biological targeting moiety.
11 more elements
Dependencies are inferred from the claim text.