Marking precursor with squaric acid coupling
AssigneeTelix Pharmaceuticals Limited
InventorsFrank Rösch, Lukas Greifenstein, Nils Engelbogen, Ralf Bergmann
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Abstract
The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with 44Sc, 47Sc, 55Co, 62Cu, 64Cu, 67Cu, 66Ga, 67Ga, 68Ga, 89Zr, 86Y, 90Y, 90Nb, 99mTc, 111ln, 135Sm, 140Pr, 159Gd, 149Tb, 160Tb, 161Tb, 165Er, 166Dy, 166Ho, 175Yb, 177Lu, 186Re, 188Re, 213Bi and 225Ac or with 18F, 131I or 211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.
Claims6
A labeling precursor for a radiopharmaceutical of the structure (A), (B), (E) or (F) with
- (A)=Ch-L1-QS-TV1,
- (B)=Ch-L1-QS-S-TV1,
- (E)=TV2-QS-L2-Ch-L1-QS-TV1,
- (F)=TV2-S3-QS-L2-Ch-Li-QS-S-TV1,
- comprising
- a chelator Ch, selected from the group consisting of DOTA (dodeca-1,4,7,10-tetraamine-tetraacetate), DOTAGA (2-(1,4,7,10-tetraazacyclododecane-4,7,10)-pentanedioic acid),
- one or two linkers L1 and L2, which are selected independently of one another from the group consisting of —(CH2)m, —(CH2CH2O)m— and —(CH2) mNH— with m=1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, residues of amide, carboxamide, alkyl, triazole, thiourea and ethylene;
- one or more squaric acid residues QS
- optionally one or two spacers S1 and S3 respectively, which are selected independently of one another from the group consisting of —(CH2)n—,
- —(CH2)—CH(COOH)—NH—, —(CH2CH2O)n and —(CH2)nNH— with n=1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, residues of amide, carboxamide, alkyl, triazole, thiourea and ethylene;
- and
- one or two targeting vectors, TV1 and TV2 respectively, which are selected independently of one another from the group comprising residues of compounds of the structures [5] and [6] with
- where the dashed bond of the targeting vectors [5] and [6] denotes a coupling site with a leaving group.
Dependencies are inferred from the claim text.