Title:
RADIOACTIVELY LABELED LIGAND FOR FIBROBLAST ACTIVATION PROTEIN-ALPHA IMAGING AGENT AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2022/160338
Kind Code:
A1
Abstract:
The present invention relates to a radioactively labeled ligand for a fibroblast activation protein-alpha imaging agent and a preparation method therefor, and belongs to the field of radiopharmaceutical chemistry. The radioactively labeled ligand for the fibroblast activation protein-alpha imaging agent has structural formula (I). The compound has a good 68Ga labeling property, a high stability and a good affinity for FAP tumors. Therefore, the radioactively labeled ligand for 68Ga-labeled FAPi can be used as a tumor positron imaging agent.
Inventors:
KUNG HANK F (US)
ZHA ZHIHAO (CN)
PLOESSL KARL (US)
CHOI SEOK RYE (US)
ALEXOFF DAVID (US)
ZHA ZHIHAO (CN)
PLOESSL KARL (US)
CHOI SEOK RYE (US)
ALEXOFF DAVID (US)
Application Number:
PCT/CN2021/074671
Publication Date:
August 04, 2022
Filing Date:
February 01, 2021
Export Citation:
Assignee:
FIVE ELEVEN PHARMA INC (US)
BIOMOLECULAR PROBES BIOTECHNOLOGY BEIJING CO LTD (CN)
BIOMOLECULAR PROBES BIOTECHNOLOGY BEIJING CO LTD (CN)
International Classes:
C07D401/14; A61K31/4709; A61K51/04; A61K103/00
Domestic Patent References:
| WO2021005125A1 | 2021-01-14 |
Foreign References:
| CN111699181A | 2020-09-22 | |||
| CN111991570A | 2020-11-27 | |||
| CN112194651A | 2021-01-08 |
Other References:
MATTHIAS EDER, MARTIN SCHÄFER, ULRIKE BAUDER-WÜST, WILLIAM-EDMUND HULL, CARMEN WÄNGLER, WALTER MIER, UWE HABERKORN, MICHAEL EISENH: "68 Ga-Complex Lipophilicity and the Targeting Property of a Urea-Based PSMA Inhibitor for PET Imaging", BIOCONJUGATE CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 23, no. 4, 18 April 2012 (2012-04-18), pages 688 - 697, XP055043532, ISSN: 10431802, DOI: 10.1021/bc200279b
LIOLIOS, CHRISTOS ET AL.,: "Synthesis, characterization and evaluation of 68Ga labelled monomeric and dimeric quinazoline derivatives of the HBED-CC chelator targeting the epidermal growth factor receptor,", BIOORGANIC CHEMISTRY,, vol. 100, 26 April 2020 (2020-04-26), XP086186241, DOI: 10.1016/j.bioorg.2020.103855
LIOLIOS CHRISTOS, BUCHMULLER BENJAMIN, BAUDER-WÜST ULRIKE, SCHÄFER MARTIN, LEOTTA KARIN, HABERKORN UWE, EDER MATTHIAS, KOPKA KLAUS: "Monomeric and Dimeric 68 Ga-Labeled Bombesin Analogues for Positron Emission Tomography (PET) Imaging of Tumors Expressing Gastrin-Releasing Peptide Receptors (GRPrs)", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 61, no. 5, 8 March 2018 (2018-03-08), US , pages 2062 - 2074, XP055954783, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.7b01856
GIESEL, FREDERIK L. ET AL.,: "68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers,", THE JOURNAL OF NUCLEAR MEDICINE,, vol. 60, no. 3, 31 March 2019 (2019-03-31), XP055732757, DOI: 10.2967/jnumed.118.215913
LIOLIOS, CHRISTOS ET AL.,: "Synthesis, characterization and evaluation of 68Ga labelled monomeric and dimeric quinazoline derivatives of the HBED-CC chelator targeting the epidermal growth factor receptor,", BIOORGANIC CHEMISTRY,, vol. 100, 26 April 2020 (2020-04-26), XP086186241, DOI: 10.1016/j.bioorg.2020.103855
LIOLIOS CHRISTOS, BUCHMULLER BENJAMIN, BAUDER-WÜST ULRIKE, SCHÄFER MARTIN, LEOTTA KARIN, HABERKORN UWE, EDER MATTHIAS, KOPKA KLAUS: "Monomeric and Dimeric 68 Ga-Labeled Bombesin Analogues for Positron Emission Tomography (PET) Imaging of Tumors Expressing Gastrin-Releasing Peptide Receptors (GRPrs)", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 61, no. 5, 8 March 2018 (2018-03-08), US , pages 2062 - 2074, XP055954783, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.7b01856
GIESEL, FREDERIK L. ET AL.,: "68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers,", THE JOURNAL OF NUCLEAR MEDICINE,, vol. 60, no. 3, 31 March 2019 (2019-03-31), XP055732757, DOI: 10.2967/jnumed.118.215913
Attorney, Agent or Firm:
BEIJING GUANGYOU PATENT OFFICE LTD (CN)
Download PDF: