Thiol-reactive maleimido-based radiolabeling reagents

Details Thiol-reactive maleimido-based radiolabeling reagents Thiol-reactive maleimido-based radiolabeling reagents

C - Chemistry, Metallurgy

07

D

C07D 207/452 (2006.01) A61K 51/04 (2006.01) A61K 51/08 (2006.01) C07B 59/00 (2006.01) C07K 5/06 (2006.01) G01N 33/534 (2006.01) G01N 33/74 (2006.01) A61K 49/02 (1990.01)

Patent

CA 2070961

Novel thiol-reactive maleimido-based radiolabeling reagents are disclosed which are useful for binding and receptor studies and assays. The reagents are also useful as diagnostic imaging agents, and as radiotherapeutic drugs. (see formula I) wherein: R is (CH2)n-NH-CO-(CH2)m, (CH2)n-CO-NH-(CH2)m, (see formula II) -[(CH2)n-O-(CH2)m-(CH2)n]x, (see formula III, IV or V) R1 is neutral, charged +/-, hydrophobic or hydrophilic; R2 is H or a radionucleotide selected from 122I, 123I, 125I, 131I, 75Br, 77Br, 82Br or 211At; n is 0 to 2; m is 0 to 2; and x is 0 to 2.

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