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    PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS WITH IMPROVED TISSUE SPECIFICITY
    5.
    发明申请
    PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS WITH IMPROVED TISSUE SPECIFICITY 有权

    公开(公告)号：US20220118121A1

    公开(公告)日：2022-04-21

    申请号：US17431396

    申请日：2020-02-14

    申请人： Ruprecht-Karls-Universität Heidelberg ,  Deutsches Krebsforschungszentrum

    发明人： Matthias Eder ,  Ann-Christin Baranski ,  Michael Eisenhut ,  Uwe Haberkorn

    IPC分类号： A61K51/08 ,  A61K51/04 ,  A61P35/00

    摘要： The present invention relates to a compound of formula (1), and to a complex comprising said compound and a radionuclide, and to the respective pharmaceutical composition, the compound having the following structure or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is H or —CH3, preferably H, wherein R2, R3 and R4 are independently of each other, selected from the group consisting of —CO2H, —SO2H, —SO3H, —OSO3H, —PO2H, —PO3H and —OPO3H2, Q1 is selected from the group consisting of alkylaryl, arylalkyl, aryl, alkylheteroaryl, heteroarylalkyl and heteroaryl, Q2 is selected from the group consisting of aryl, alkylaryl, arylalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, heteroarylalkyl and alkylheteroaryl, A is a chelator residue derived from a chelator selected from the group consisting of 1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (=DOTA), N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid, 1,4,7-triazacyclononane-1,4,7-triacetic acid (=NOTA), 2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid, (NODAGA), 2-(4,7, 10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (DOTAGA), 1,4,7-riazacyclononane phosphinic acid (TRAP), 1,4,7-triazacyclononane phosphinic acid (TRAP), 1,4,7-triazacyclononane-1-[methyl(2-carboxyethyl)phosphinic acid]-4,7-bis[methyl(2-hydroxymethyl)phosphinic acid](NOPO), 3,6,9, 15-tetraazabicyclo[9.3.1.]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (=PCTA), N′-{5-[Acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-aminopentyl)(hydroxy)amino]-4-oxobutanoyl}amino)pentyl]-N-hydroxysuccinamide (DFO), Diethylenetriaminepentaacetic acid (DTPA), Trans-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-DTPA), 1-oxa-4,7, 10-triazacyclododecane-4,7, 10-triacetic acid (oxo-Do3A) p-isothiocyanatobenzyl-DTPA (SCN-Bz-DTPA), 1-(p-isothiocyanatobenzyl)-3-methyl-DTPA (1 B3M), 2-(p-isothiocyanatobenzyl)-4-methyl-DTPA (1 M3B) and 1-(2)-methyl-4-isocyanatobenzyl-DTPA (MX-DTPA), X1, X2, Y1, Y2, Z1 and Z2, are independently of each other, charged amino acids, q is an integer of from 0-3, n, m and p, are independently of each other an integer of from 0 to 9, n1, n2, m1, m2, p1, p2, are independently of ach other, an integer of from 0 to 3, and wherein n1+n2>0, m1+m2>0 and p1+p2>0, and wherein n+m+p>0. Further, the present invention relates to the compound, the complex, and the pharmaceutical composition for use in treating, ameliorating or preventing PSMA-expressing cancers, in particular prostate cancer, and/or metastases thereof.