Title:
SMALL MOLECULE PROBE BINDING TO α-SYNUCLEIN AGGREGATE AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/104148
Kind Code:
A1
Abstract:
Disclosed are a compound shown in following general formula I, and a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1 is preferably a pyridyl group; R2 is preferably a halogen group, and halogenated C1-4 alkoxy groups; R3 and R4 are preferably a methyl group; and a ring A is preferably a benzene ring and a thiazole ring. The compound of the present invention can specifically strongly bind to an α-synuclein aggregate, can act as a small molecule probe of the α-synuclein aggregate, and is used for optical imaging of the α-synuclein aggregate in a biological sample or an organism (such as brain). A radioactive label thereof can act as an imaging tracer probe for imaging inspection technologies such as PET and SPECT, so as to implement non-invasive imaging visualization detection of an α-synuclein lesion in vivo (such as brain). The compound of the present invention is also used for preparing the imaging tracer probe of the radioactive label or a composition thereof. Diseases related to the α-synuclein lesion comprise Parkinson's disease, Parkinson's disease dementia, Alzheimer's disease, multiple system atrophy, dementia with Lewy bodies, etc.
Inventors:
CHU YONG (CN)
WANG JIAN (CN)
BIAN JIANG (CN)
LIU YIQI (CN)
LIN XIN (CN)
QIU CHENYANG (CN)
HE JIE (CN)
YE DEYONG (CN)
WANG JIAN (CN)
BIAN JIANG (CN)
LIU YIQI (CN)
LIN XIN (CN)
QIU CHENYANG (CN)
HE JIE (CN)
YE DEYONG (CN)
Application Number:
PCT/CN2022/137518
Publication Date:
June 15, 2023
Filing Date:
December 08, 2022
Export Citation:
Assignee:
UNIV FUDAN (CN)
International Classes:
A61K51/04; A61K49/00; C07D401/06; C07D417/14; G01N21/64; G01N30/02
Foreign References:
| CN112645891A | 2021-04-13 | |||
| CN112110829A | 2020-12-22 |
Other References:
XU, MINGMING ET AL.: "Advances in the Development of Imaging Probes and Aggregation Inhibitors for Alpha-synuclein", ACTA PHARMACOLOGICA SINICA, 4 October 2019 (2019-10-04), pages 483 - 498, XP037079648, DOI: 10.1038/s41401-019-0304-y
Attorney, Agent or Firm:
SUNSHINEIP INTELLECTUAL PROPERTY LAW FIRM (CN)
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