Title:
QUINOXALINE DERIVATIVE AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/239046
Kind Code:
A1
Abstract:
Disclosed are a quinoxaline derivative and a preparation method therefor and the use thereof. Specifically provided are a compound as shown in formula I, or a pharmaceutically acceptable salt thereof, or a hydrate thereof, or a solvate thereof, or a conformational isomer thereof, or a crystal form thereof, or a isotopic substitution form thereof, and a preparation method therefor and the use thereof. Experiment results show that the above-mentioned quinoxaline derivative, after being labeled with a radionuclide, can be used as a Tau protein tracer for identifying neurofibrillary tangles (NFT) formed by the abnormal aggregation of hyperphosphorylated Tau protein in the brain, and can be used in diagnosis of diseases related to neurofibrillary tangles, and also in monitoring of the progress of the disease over the course of treatment, providing higher and more accurate diagnosis and tracking for patients or potential patients with diseases related to neurofibrillary tangles, thus having a good application prospect in clinical diagnosis.
Inventors:
KUANG WEIHONG (CN)
LI JIN (CN)
XIE YONGMEI (CN)
TIAN RONG (CN)
WU XIAOAI (CN)
ZHANG NI (CN)
LI JIN (CN)
XIE YONGMEI (CN)
TIAN RONG (CN)
WU XIAOAI (CN)
ZHANG NI (CN)
Application Number:
PCT/CN2020/093066
Publication Date:
December 03, 2020
Filing Date:
May 29, 2020
Export Citation:
Assignee:
WEST CHINA HOSPITAL SICHUAN UNIV (CN)
International Classes:
C07D241/42; A61K49/00; A61K51/00; A61K101/02
Foreign References:
| CN102985411A | 2013-03-20 | |||
| CN107118586A | 2017-09-01 | |||
| US20040242615A1 | 2004-12-02 | |||
| CN102438660A | 2012-05-02 | |||
| CN102725285A | 2012-10-10 | |||
| CN1392143A | 2003-01-22 |
Other References:
BIYUE ZHU, ZHANG TING, JIANG QIAN, LI YING, FU YU, DAI JIAPEI, LI GE, QI QINGRONG, CHENG YAN: "Synthesis and evaluation of pyrazine and quinoxaline fluorophores for in vivo detection of cerebral tau tangles in Alzheimer’s models", CHEMICAL COMMUNICATIONS, vol. 54, no. 82, 3 September 2018 (2018-09-03), pages 11558 - 11561, XP055757712, ISSN: 1359-7345, DOI: 10.1039/C8CC06897F
DATABASE Registry 6 August 2018 (2018-08-06), ANONYMOUS, XP055757891, retrieved from STN Database accession no. 2235372-98-0
HARUN M. PATEL, BHARDWAJ VARUN, SHARMA POONAM, NOOLVI MALLESHAPPA N., LOHAN SANDEEP, BANSAL SUMIT, SHARMA AMIT: "Quinoxaline-PABA bipartite hybrid derivatization approach: Design and search for antimicrobial agents", JOURNAL OF MOLECULAR STRUCTURE, vol. 1184, 15 May 2019 (2019-05-15), pages 562 - 568, XP055757708, ISSN: 0022-2860, DOI: 10.1016/j.molstruc.2019.02.074
DATABASE Registry 6 August 2018 (2018-08-06), ANONYMOUS, XP055757891, retrieved from STN Database accession no. 2235372-98-0
HARUN M. PATEL, BHARDWAJ VARUN, SHARMA POONAM, NOOLVI MALLESHAPPA N., LOHAN SANDEEP, BANSAL SUMIT, SHARMA AMIT: "Quinoxaline-PABA bipartite hybrid derivatization approach: Design and search for antimicrobial agents", JOURNAL OF MOLECULAR STRUCTURE, vol. 1184, 15 May 2019 (2019-05-15), pages 562 - 568, XP055757708, ISSN: 0022-2860, DOI: 10.1016/j.molstruc.2019.02.074
Attorney, Agent or Firm:
GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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