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Title:
RADIOACTIVE FLUORINE-LABELED LAROTRECTINIB COMPOUND AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2020/119205
Kind Code:
A1
Abstract:
A radioactive fluorine-labeled Larotrectinib compound and a preparation method therefor, particularly, an in-vivo imaging agent of a Trk receptor subtype in a refractory solid tumor. Provided are a radioactive fluorine compound 18F-Larotrectinib based on a novel Larotrectinib inhibitor aiming at a tyrosine receptor kinase (TRK) as well as an 18F-Larotrectinib analogue thereof, more particularly, a Larotrectinib, an analogous radioactive fluorine-18-labeled compound 18 F-Larotrectinib thereof, and a preparation method for the 18F-Larotrectinib analogue thereof. Compared with the prior art, the method has the advantages of quick reaction speed, relatively mild conditions, simple operation, short reaction time, simple post-treatment, and high radiochemical purity, can emit positrons and prepare a carrier-free radiolabeled compound. By means of a positron emission tomography-computed tomography (PET-CT), the Larotrectinib compound and the analogue thereof in vivo as well as distribution conditions in a tumor are visually displayed, and a new developing agent is provided for early diagnosis of the tumor.

Inventors:
HUANG GANG (CN)
LI BIN (CN)
Application Number:
PCT/CN2019/106690
Publication Date:
June 18, 2020
Filing Date:
September 19, 2019
Export Citation:
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Assignee:
SHANGHAI UNIV OF MEDICINE&HEALTH SCIENCES (CN)
International Classes:
C07D487/04; A61K51/04; A61P35/00; C07F7/10; C07F7/18; A61K101/02
Domestic Patent References:
WO2010048314A12010-04-29
Foreign References:
CN109705124A2019-05-03
CN107987082A2018-05-04
CN101805247A2010-08-18
Other References:
LI, GONGMING ET AL.: "Recent Advances of Direct Incorporation of Fluorine-Containing Groups and 18F-Labeling Methods", CHINESE JOURNAL OF ORGANIC CHEMISTRY, vol. 36, no. 8, 15 April 2016 (2016-04-15), pages 1715 - 1740
Attorney, Agent or Firm:
SHANGHAI KESHENG INTELLECTUAL PROPERTY AGENCY LTD. (CN)
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