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US 11,629,201 B2Granted
PSMA-binding agents and uses thereof
AssigneesITM Isotope Technologies Munich SE, Paul Scherrer Institut
InventorsMartina Benesova, Cristina Müller, Christoph Umbricht, Roger Schibli, Konstantin Zhernosekov
Life of this patent
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Abstract
The present invention provides novel compounds that are useful as radiopharmaceuticals, imaging agents and for treatment of cancer.
Claims61
A radiolabeled complex comprising a radionuclide and a compound according to general Formula (1)(i) or (1)(ii):
- wherein Abm is an albumin binding entity,
- Pbm is a PSMA binding entity,
- D is a chelator complexed with a radionuclide, X is each independently selected from O, N, S or P,
- R1 and R2 are each independently selected from H, F, Cl, Br, I, branched, unbranched or cyclic C1-C12 hydrocarbyl, C2-C12 alkenyl, C2-C12 alkylnyl, OR6, OCOR6, CHO, COR6, CH2OR6, NR6R7, CONR6R7, COOR6, CH2NR6R7, SR6, ═O, ═S or ═NH, or R1 and R2 are joined to form a cyclic structure comprising a branched, unbranched or cyclic C1-C10 hydrocarbyl group, wherein said hydrocarbyl group is optionally interrupted by up to 2 heteroatoms and optionally substituted by up to 3 groups independently selected from F, Cl, Br, I, OR6, OCOR6, COOR6, CHO, COR6, CH2OR6, NR6R7, CH2NR6R7, and SR7, ═O, ═S and ═NH,
- Y is selected from a single bond or a linear, branched or cyclic, optionally substituted C1-C12 alkyl, optionally interrupted by up to two heteroatoms, OR6, OCOR6, CHO, COR6, CH2OR6, NR6R7, COOR6, CH2NR6R7, SR6, ═O, ═S or ═NH, wherein one or more of the non-adjacent CH2-groups may independently be replaced by —O—, —CO—, —CO—O—, —O—CO—, —NR6—, —NR6—CO—, —CO—NR6—, —NR6—COO—, —O—CO—NR6—, —NR6—CO—NR6—, —CH═CH—, —C≡C—, —O—CO—O—, SR6—, SO3R6—,
- R6 and R7 are each independently selected from H or branched, unbranched or cyclic C1-12 hydrocarbyl,
- R3, R4 and R5 are each independently selected from —COH, —CO2H, —SO2H, —SO3H, —SO4H, —PO2H, —PO3H, —PO4H2, —C(O)—(C1-C10)alkyl, —C(O)—O(C1-C10)alkyl, —C(O)—NHR8, or —C(O)—NR8R9, wherein R8 and R9 are each independently selected from H, bond, (C1-C10)alkylene, F, Cl, Br, I, C(O), C(S), —C(S)—NH-benzyl-, —C(O)—NH-benzyl, —C(O)—(C1-C10)alkylene, —(CH2)p—NH, —(CH2)p—(C1-C10)alkylene, —(CH2)p—NH—C(O)—(CH2)q, —(CHrCH2)t—NH—C(O)—(CH2)p, —(CH2)p—CO—COH, —(CH2)p—CO—CO2H, —(CH2)p-C(O)NH—C[(CH2)q—COH]3, —C[(CH2)p—COH]3, —(CH2)p-C(O)NH—C[(CH2)q—CO2H]3, —C[(CH2)p—CO2H]3 or —(CH2)p—(C5-C14)heteroaryl,
- the spacer comprises at least one C—N bond,
- the linker is characterized by General Formula (6)
- and
- a, b, p, q, r, and t are each independently an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10;
- or pharmaceutically acceptable salts, esters, or solvates thereof.
9 more elements
Dependencies are inferred from the claim text.