Title:
TUMOR STROMA IMAGING AGENT AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2022/032844
Kind Code:
A1
Abstract:
A tumor stroma imaging agent. The tumor stroma imaging agent has the following chemical structural formula (I): wherein R is hydrogen or fluorine. Compared with the prior art, the tumor stroma imaging agent shows remarkable affinity for FAP, has a high amount of uptake for an FAP high expression malignant tumor in the tumor stroma, and has high sensitivity and specificity in diagnosis of malignant tumors, and it is not prone to false positives, thus the present invention can be effectively and safely applied to diagnosis and treatment of multiple types of malignant tumors; moreover, the half life is long, and a window period is prolonged, thereby facilitating clinical use.
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Inventors:
HUANG GANG (CN)
LI BIN (CN)
LI BIN (CN)
Application Number:
PCT/CN2020/120721
Publication Date:
February 17, 2022
Filing Date:
October 13, 2020
Export Citation:
Assignee:
SHANGHAI UNIV OF MEDICINE&HEALTH SCIENCES (CN)
International Classes:
A61K51/04; A61K31/4709; A61P35/00; C07D215/50; C07D401/12; C07D401/14; C07F5/06
Domestic Patent References:
| WO2019154886A1 | 2019-08-15 |
Foreign References:
| CN102123739A | 2011-07-13 |
Other References:
WILLIAM J MCBRIDE, ROBERT M SHARKEY, DAVID M GOLDENBERG: "Radiofluorination using aluminum-fluoride (Al18F)", EJNMMI RESEARCH, vol. 3, no. 1, 1 January 2013 (2013-01-01), pages 36, XP055242822, ISSN: 2191-219X, DOI: 10.1186/2191-219X-3-36
GIESEL FL, ADEBERG S, SYED M, LINDNER T, STAUDINGER F, RATHKE H, ROEHRICH M, MIER W, MAVRIOPOULOU E, DEBUS J, ALTMANN A, HABERKORN: "Biodistribution, radiation dosimetry and tumor detection of 18F-AlF-labeled FAPI-PET/CT in lung cancer patients", NUKLEARMEDIZIN, vol. 59, no. 2, 30 April 2020 (2020-04-30), DE , pages 114, XP009534243, ISSN: 0029-5566
GIESEL FREDERIK L., ADEBERG SEBASTIAN, SYED MUSTAFA, LINDNER THOMAS, JIMÉNEZ-FRANCO LUIS DAVID, MAVRIOPOULOU ELENI, STAUDINGER FAB: "FAPI-74 PET/CT Using Either 18 F-AlF or Cold-Kit 68 Ga Labeling: Biodistribution, Radiation Dosimetry, and Tumor Delineation in Lung Cancer Patients", THE JOURNAL OF NUCLEAR MEDICINE, vol. 62, no. 2, 1 February 2021 (2021-02-01), US , pages 201 - 207, XP055899873, ISSN: 0161-5505, DOI: 10.2967/jnumed.120.245084
RUIVO EDUARDO; ADHIKARI KARUNA; ELVAS FILIPE; FISSERS JENS; VANGESTEL CHRISTEL; STAELENS STEVEN; STROOBANTS SIGRID; VAN DER VEKEN : "Improved stability of a novel fluorine-18 labeled TCO analogue for pretargeted PET imaging", NUCL. MED. BIOL., vol. 76, 1 September 2019 (2019-09-01), US , pages 36 - 42, XP085928193, ISSN: 0969-8051, DOI: 10.1016/j.nucmedbio.2019.11.001
GIESEL FL, ADEBERG S, SYED M, LINDNER T, STAUDINGER F, RATHKE H, ROEHRICH M, MIER W, MAVRIOPOULOU E, DEBUS J, ALTMANN A, HABERKORN: "Biodistribution, radiation dosimetry and tumor detection of 18F-AlF-labeled FAPI-PET/CT in lung cancer patients", NUKLEARMEDIZIN, vol. 59, no. 2, 30 April 2020 (2020-04-30), DE , pages 114, XP009534243, ISSN: 0029-5566
GIESEL FREDERIK L., ADEBERG SEBASTIAN, SYED MUSTAFA, LINDNER THOMAS, JIMÉNEZ-FRANCO LUIS DAVID, MAVRIOPOULOU ELENI, STAUDINGER FAB: "FAPI-74 PET/CT Using Either 18 F-AlF or Cold-Kit 68 Ga Labeling: Biodistribution, Radiation Dosimetry, and Tumor Delineation in Lung Cancer Patients", THE JOURNAL OF NUCLEAR MEDICINE, vol. 62, no. 2, 1 February 2021 (2021-02-01), US , pages 201 - 207, XP055899873, ISSN: 0161-5505, DOI: 10.2967/jnumed.120.245084
RUIVO EDUARDO; ADHIKARI KARUNA; ELVAS FILIPE; FISSERS JENS; VANGESTEL CHRISTEL; STAELENS STEVEN; STROOBANTS SIGRID; VAN DER VEKEN : "Improved stability of a novel fluorine-18 labeled TCO analogue for pretargeted PET imaging", NUCL. MED. BIOL., vol. 76, 1 September 2019 (2019-09-01), US , pages 36 - 42, XP085928193, ISSN: 0969-8051, DOI: 10.1016/j.nucmedbio.2019.11.001
Attorney, Agent or Firm:
D&S IP LAW FIRM (CN)
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