Labeling precursors with squaric acid coupling
AssigneeTelix Pharmaceuticals Limited
InventorsFrank RÖSCH, Lukas GREIFENSTEIN, Nils ENGELBOGEN, Ralf BERGMANN
Life of this patent
Estimating the term…
Abstract
The invention relates to a marking precursor comprising a chelator or fluorination group for radiolabelling with 44SC, 47SC, 55Co, 62Cu, 64Cu, 67Cu, 66Ga, 67Ga, 68Ga, 89Zr, 86Y, 90Y, 90Nb, 99mTc, 111In, 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.
Claims2
A labeling precursor for a radiopharmaceutical of the structure (A), (B), (C), (D), (E), (F), (G), (H), (I), (J), (K) or (L) with
- (A)=Ch-L1-QS-TV1,
- (B)=Ch-L1-QS-S1-TV1,
- (C)=Ch-L1-QS-S1-QS-TV1,
- (D)=Ch-L1-QS-S2-QS-S1-TV1,
- (E)=TV2-QS-L2-Ch-L1-QS-TV1,
- (F)=TV2-S3-QS-L2-Ch-L1-QS-S1-TV1,
- (G)=TV2-QS-S4-QS-L2-Ch-L1-QS-S2-QS-TV1,
- (H)=TV2-S3-QS-S4-QS-L2-Ch-L1-QS-S2-QS-S1-TV1,
- (I)=Fg-L1-QS-TV1,
- (J)=Fg-L1-QS-S1-TV1,
- (K)=Fg-L1-QS-S2-QS-TV1,
- (L)=Fg-L1-QS-S2-QS-S1-TV1;
- comprising
- a chelator Ch, selected from the group comprising EDTA (ethylenediamine-tetraacetate), EDTMP (diethylenetriaminepenta (methylenephosphonic acid)), DTPA (diethylenetriaminepentacetate) and its derivatives, DOTA (dodeca-1,4,7,10-tetraaminetetraacetate), TRITA (Trideca-1,4,7,10-tetraamine-tetraacetate), TETA (tetradeca-1,4,8,11-tetraamine-tetraacetate) and its derivatives, NOTA (Nona-1,4,7-triamine-triacetate) and its derivatives, NOPO (1,4,7-triazacyclononane-1,4-bis[methylene(hydroxymethyl)phosphinic acid]-7-[methylene(2-carboxyethyl) phosphinic acid]), PEPA (pentadeca-1,4,7,10,13-pentaamine pentaacetate), HEHA (Hexadeca-1,4,7,10,13,16-hexaamine-hexaacetate) and its derivatives, HBED (Hydroxybenzyl-ethylene-diamine) and its derivatives, DEDPA and its derivatives, DFO (deferoxamine) and its derivatives, Trishydroxypyridinone (THP) and its derivatives, TRAP (Triazacyclononane phosphinic acid), TEAP (Tetraazycyclodecane phosphinic acid) and its derivatives, AAZTA (6-Amino-6-methylperhydro-1,4-diazepine-N,N,N′,N′-tetraacetate) and its derivatives;
- SarAr (1-N-(4-aminobenzyl)-3,6,10,13,16,19-hexaazabicyclo [6.6.6]-eicosan-1,8-diamine) and salts thereof, aminothiols and their derivatives of the type
- or
- a fluorination group Fg selected from the group comprising
- 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, phosphinate, alkyl, triazole, thiourea, ethylene and maleimide;
- one or more squaric acid residues QS
- optionally one, two, three or four spacers Sj with 1≤j≤4, which are selected independently of one another from the group consisting of —(CH2)n—, —(CH2)—CH(COOH)—NH—, —(CH2CH2O)n— and —(CH2),NH— with n=1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, residues of amide, carboxamide, phosphinate, alkyl, triazole, thiourea, ethylene and maleimide;
- and
- one or two targeting vectors TV1 and TV2, which are selected independently of one another from the group comprising residues of compounds of the structure [1] to [41] with
- where Y is a protective group and X′=Cl, Br or I and the dashed bond of the targeting vectors [1]-[41] denotes a coupling site with a leaving group.
Dependencies are inferred from the claim text.