Title:
18F-LABELED FLUOROPICOLINYLGLYCINE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/253824
Kind Code:
A1
Abstract:
The present invention belongs to the technical field of radiopharmaceutical chemistry, and provided are 18F-labeled fluoropicolinylglycine as well as a preparation method therefor and an application thereof. The 18F-labeled fluoropicolinylglycine provided in the present invention is 6-[18F]-fluoro-3-picolinylglycine, 5-[18F]-fluoro-2-picolinoylglycine, or 4-[18F]-fluoro-2-picolinoylglycine. The 18F-labeled fluoropicolinylglycine provided in the present invention has excellent stability and good biological properties, and has no adverse effects on an organism after decay. It may be known by means of an in vivo distribution test that the 18 F-labeled fluoropicolinylglycine is mainly absorbed by the kidneys and is then quickly discharged from the body. 10 min after injecting the 18F-labeled fluoropicolinylglycine into the body of a mouse, almost all of same is discharged into the bladder. The 18F-labeled fluoropicolinylglycine provided in the present invention is particularly advantageous for the evaluation of renal function in renal diseases.
More Like This:
Inventors:
WANG HONGLIANG (CN)
WU ZHIFANG (CN)
LI SIJIN (CN)
DONG WEIXUAN (CN)
ZHAO QINAN (CN)
WU ZHIFANG (CN)
LI SIJIN (CN)
DONG WEIXUAN (CN)
ZHAO QINAN (CN)
Application Number:
PCT/CN2020/097092
Publication Date:
December 24, 2020
Filing Date:
June 19, 2020
Export Citation:
Assignee:
FIRST HOSPITAL OF SHANXI MEDICAL UNIV (CN)
International Classes:
C07D213/82; A61K51/04; C07B59/00; C07D213/81; A61K101/02
Foreign References:
| CN110204484A | 2019-09-06 | |||
| CN104703963A | 2015-06-10 | |||
| CN104645362A | 2015-05-27 |
Other References:
LATIFA RBAH-VIDAL; AURELIEN VIDAL; SOPHIE BESSE; FLORENT CACHIN; MATHILDE BONNET; LAURENT AUDIN; SERGE ASKIENAZY; FREDERIC DOLLE; : "Early detection and longitudinal monitoring of experimental primary and disseminated melanoma using [18F]ICF01006, a highly promising melanoma PET tracer", EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, vol. 39, no. 9, 16 June 2012 (2012-06-16), pages 1449 - 1461, XP035094692, ISSN: 1619-7070, DOI: 10.1007/s00259-012-2168-y
JOSE L IZQUIERDO-GARCIA, NIN NICOLÁS, CARDINAL-FERNANDEZ PABLO, ROJAS YENNY, DE PAULA MARTA, GRANADOS ROSARIO, MARTÍNEZ-CARO LETIC: "Identification of novel metabolomic biomarkers in an experimental model of septic acute kidney injury", AMERICAN JOURNAL PHYSIOL RENAL PHYSIOL, vol. 316, 31 October 2018 (2018-10-31), pages F54 - F62, XP055767251, ISSN: 0002-9513, DOI: 10.1152/ajprenal.00315.2018
AWASTHI V; PATHURI G; AGASHE H B; GALI H: "Synthesis and in vivo evaluation of p-18F-fluorohippurate as a new radiopharmaceutical for assessment of renal function by PET", JOURNAL OF NUCLEAR MEDICINE, vol. 52, no. 1, 1 January 2011 (2011-01-01), pages 147 - 153, XP055263009, ISSN: 0161-5505, DOI: 10.2967/jnumed.110.075895
JOSE L IZQUIERDO-GARCIA, NIN NICOLÁS, CARDINAL-FERNANDEZ PABLO, ROJAS YENNY, DE PAULA MARTA, GRANADOS ROSARIO, MARTÍNEZ-CARO LETIC: "Identification of novel metabolomic biomarkers in an experimental model of septic acute kidney injury", AMERICAN JOURNAL PHYSIOL RENAL PHYSIOL, vol. 316, 31 October 2018 (2018-10-31), pages F54 - F62, XP055767251, ISSN: 0002-9513, DOI: 10.1152/ajprenal.00315.2018
AWASTHI V; PATHURI G; AGASHE H B; GALI H: "Synthesis and in vivo evaluation of p-18F-fluorohippurate as a new radiopharmaceutical for assessment of renal function by PET", JOURNAL OF NUCLEAR MEDICINE, vol. 52, no. 1, 1 January 2011 (2011-01-01), pages 147 - 153, XP055263009, ISSN: 0161-5505, DOI: 10.2967/jnumed.110.075895
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
Download PDF: