Boronic acid adducts of rhenium and radioactive isotopes of...

C - Chemistry – Metallurgy – 07 – F

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260/383, 260/428

C07F 13/00 (2006.01)

Patent

CA 1284649

ABSTRACT BORONIC ACID ADDUCTS OF RHENIUM DIOXIME COMPLEXES Boronic acid adducts of radioactive isotopes of rhenium dioxime complexes having the formula ReX(Y)3Z, wherein X is an anion; Y is a vicinal dioxime having the formula Image or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are -(CR8R9)N-wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; and Z is a boron derivative of the formula B-R3 wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxy- alkenyl, haloalkyl, haloalkenyl, aryl,arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle, are useful for labeling biologically active compounds as agents for radiotherapy.

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