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    LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PSMA-EXPRESSING CANCERS
    5.
    发明申请
    LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PSMA-EXPRESSING CANCERS 有权

    公开(公告)号：US20250057993A1

    公开(公告)日：2025-02-20

    申请号：US18921856

    申请日：2024-10-21

    Applicant: Universität Heidelberg ,  Deutsches Krebsforschungszentrum

    Inventor： Uwe HABERKORN ,  José Carlos DOS SANTOS ,  Walter MIER ,  Clemens KRATOCHWIL ,  Ulrike BAUDER-WUEST ,  Klaus KOPKA ,  Martin SCHÄFER

    IPC: A61K51/04

    Abstract: The present invention relates to a compound of formula (1) or a pharmaceutically acceptable salt or solvate thereof, wherein Y3 is O or S, wherein s, t, u and w are, independently of each other, 0 or 1, wherein i is an integer of from 1 to 3, wherein j is an integer of from 3 to 5, and wherein Z1, Z2 and Z3 are independently of each other, selected from the group consisting of CO2H, —SO2H, —SO3H, —OSO3H, and —OPO3H2, R1 is —CH3 or H, preferably H, X is selected from the group consisting of alkylaryl, aryl, alkylheteroaryl and heteroaryl, Y1 and Y2 are independently, of each other, selected from the group consisting of aryl, alkylaryl, cycloalkyl, heterocycloalkyl, heteroaryl and alkylheteroaryl, and wherein A is a chelator residue having a structure selected from the group consisting of (Ia), (Ib) and (Ic) wherein R2, R3, R4 and R5 are, independently of each other, selected from the group consisting of H, —CH2—COOH and —CH2—C(═O)—NH2 or wherein R2 and R4 form a —(CH2)n— bridge with n being an integer of from 1 to 3, wherein n is preferably 2, and wherein r, v and q, are independently of each other, 0 or 1, with the proviso that in case u and w are 0, q and v are 0, and (A) wherein u and w are 1, or (B) wherein u is 0 and w is 1, and wherein A is selected from (Ia) or (Ib), or (C) wherein A is not Further, the present invention relates to a complex comprising (a) a radionuclide, and (b) the compound, as described above or below, or a salt, solvate, metabolite or prodrug thereof. Further, the present invention relates to a pharmaceutical composition comprising a compound, as described above or below, or a complex, as described above or below. Further, the present invention relates to a compound, as described above or below, or a complex, as described above or below, or a pharmaceutical composition, as described above or below, for use in treating, ameliorating or preventing PSMA-expressing cancer and/or metastases thereof, in particular prostate cancer and/or metastases thereof. Further, the present invention relates to a compound, as described above or below, or a complex, as described above or below, or a pharmaceutical composition, as described above or below, for use in diagnostics. In addition, the present invention relates to a compound, as described above or below, or a complex, as described above or below, or a pharmaceutical composition, as described above or below, for use in the diagnosis of cancer, in particular of PSMA-expressing cancer and/or metastases thereof, in particular prostate cancer and/or metastases thereof.

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