Radiolabeled fructose derivatives for medical imaging
OwnerAdam Jason SHUHENDLER, Mojmir SUCHY +4inventors
InventorsAdam Jason SHUHENDLER, Mojmir SUCHY, Robert BEN, Thomas CHARLTON, Alexia Margarite KIRBY, Nicholas David CALVERT
Life of this patent
Estimating the term…
Abstract
There are provided fructose-based radiopharmaceuticals, pharmaceutical compositions comprising same, methods for preparing same, and methods of using same for biomedical imaging, particularly nuclear imaging using PET or PET/CT. (Compound 7)
Claims23
A compound of Formula (I), or a tautomer or anomer thereof, or a pharmaceutically acceptable salt thereof:
- wherein X is 18F, 11C, 75Br, 77Br, 124I, 131I, or 211At.
A compound of Formula (IIa) or (IIa′), or a pharmaceutically acceptable salt or ester thereof:
- wherein:
- R1, R2′, R3′, R4′ and R6′ are each independently selected from —C(═O)(lower alkyl) or —C(═O)Ph;
- and
- LG is 4-methylphenylsulfonyl (—OTs), methanesulfonyl (—OMs), trifluoromethanesulfonyl (—OTf), 4-nitrophenylsulfonyl (—ONs), phenylsulfonyl, —Br, —Cl, or —I.
A compound of formula (IIb) or (IIb′), or a pharmaceutically acceptable salt or ester thereof:
- wherein:
- R1 is lower alkyl;
- R2 is H and R3 is phenyl, or R2 and R3 are each independently lower alkyl;
- R4 and R6 are methoxymethyl (MOM), t-butyl (t-Bu), benzyl (Bn), trimethylsilyl (TMS), t-butyldimethylsilyl (TBDMS), or tetrahydropyranyl (THP);
- and
- LG is 4-methylphenylsulfonyl (—OTs), methanesulfonyl (—OMs), trifluoromethanesulfonyl (—OTf), 4-nitrophenylsulfonyl (—ONs), phenylsulfonyl, —Br, —Cl, or —I.
13-24. (canceled)
-50. (canceled)
Dependencies are inferred from the claim text.