Title:
PSMA-TARGETING RADIOACTIVE METAL COMPLEX CONTAINING NITRO AROMATIC HETEROCYCLIC GROUP AND PREPARATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/231452
Kind Code:
A1
Abstract:
The present invention belongs to the technical field of radiopharmaceuticals and medical images. Disclosed in the present invention are a PSMA-targeting radioactive metal complex containing a nitro aromatic heterocyclic group and the preparation thereof. The PSMA-targeting radioactive metal complex containing the nitro aromatic heterocyclic group of the present invention has general formulas as shown in formula I and general formula II, wherein R1 and R2 groups are nitro aromatic heterocyclic groups; L2 is a linking group between R1 yl and L1; L1 is a linking group between a chelating agent and a PSMA-targeting structure; L4 is a linking group between R2 yl and L3; L3 is a linking group between the chelating agent and the PSMA-targeting structure; and Chelator1 and Chelator2 are chelating agents or chelating structures. In the present invention, a nitro aromatic heterocyclic group and a PSMA-targeting group are both linked to a metal chelating agent (HBED-CC, DOTA, DOTA(GA)2, NOTA, AAZTA, etc.) for the first time, which is used for performing labeling with a radioactive metal nuclide such as 68Ga, 18F-AIF, 177Lu, 90Y, 44Sc, 225Ac, 212Pb, and 213Bi, and is expected to increase the uptake of a radioactive metal label by prostate cancer and accelerate the metabolism in a non-target organ by means of the synergistic effect of the nitroaromatic heterocyclic group in vivo, thus improving the diagnosis and treatment effect of radiopharmaceuticals on tumors.
Inventors:
ZHU LIN (CN)
JIN WENBIN (CN)
LUO YANG (CN)
WANG RAN (CN)
KONG HANK F (US)
JIN WENBIN (CN)
LUO YANG (CN)
WANG RAN (CN)
KONG HANK F (US)
Application Number:
PCT/CN2023/075960
Publication Date:
December 07, 2023
Filing Date:
February 14, 2023
Export Citation:
Assignee:
UNIV BEIJING NORMAL (CN)
International Classes:
C07K5/037; A61K51/04; A61K51/08; A61P13/08; A61P35/00; C07D233/91; C07D403/12; C07K5/062; C07K7/02
Foreign References:
| CN108541302A | 2018-09-14 | |||
| US20160304555A1 | 2016-10-20 | |||
| CN112574280A | 2021-03-30 | |||
| CN114984255A | 2022-09-02 | |||
| CN114096264A | 2022-02-25 | |||
| US20130034494A1 | 2013-02-07 | |||
| US20160067361A1 | 2016-03-10 |
Other References:
KWON YOUNG-DO ET AL.: "Synthesis and Evaluation of Multifunctional Fluorescent Inhibitors with Synergistic Interaction of Prostate-Specific Membrane Antigen and Hypoxia for Prosteta Cancer", BIOCONJUGATE CHEM., vol. 30, no. 1, 28 November 2018 (2018-11-28), XP055945984, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.8b00767
KWON YOUNG-DO ET AL.: "Novel multifunctional 18F-labelled PET tracer with prostate-sepcific membrane antigen-targeting and hypoxia-sensitive moieties", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 189, 25 January 2020 (2020-01-25), XP086046624, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.112099
KWON YOUNG-DO ET AL.: "Novel multifunctional 18F-labelled PET tracer with prostate-sepcific membrane antigen-targeting and hypoxia-sensitive moieties", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 189, 25 January 2020 (2020-01-25), XP086046624, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.112099
Attorney, Agent or Firm:
BEIJING GUANGYOU PATENT OFFICE LTD. (CN)
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