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1. (WO2017152821) ISOQUINOLINE COMPOUND, AND INTERMEDIATES, PREPARATION METHOD AND APPLICATION THEREOF

Pub. No.:    WO/2017/152821    International Application No.:    PCT/CN2017/075765
Publication Date: Fri Sep 15 01:59:59 CEST 2017 International Filing Date: Tue Mar 07 00:59:59 CET 2017
IPC: C07D 401/04
C07D 471/04
C07D 405/04
C07D 491/048
C07D 409/04
C07D 495/04
C07D 413/04
A61K 31/4725
A61K 51/04
A61P 25/28
A61P 25/00
Applicants: SHANGHAI JINGWEI BIOTECHNOLOGY COMPANY, LTD
上海镜微生物科技有限公司
Inventors: CAI, Yongquan
蔡勇全
Title: ISOQUINOLINE COMPOUND, AND INTERMEDIATES, PREPARATION METHOD AND APPLICATION THEREOF
Abstract:
Disclosed are an isoquinoline compound, and intermediates, a preparation method and an application thereof. The isoquinoline compound of the present invention has a structure as represented by formula I, wherein R1 and R2 are each independently selected from one of H, F, 18F, NH2, and NO2; R3, R4, and R5 are each independently selected from one of H, NH2, NO2, CN, OH, a C1-C4 alkyl group, a C1-C4 alkoxy group, and a C1-C4 alkyl-amido group; X is selected from one of CH2, NH, O, and S; Y is CH or N; Z is CH or N. The isoquinoline compound of the present invention has a good binding capability to hyper phosphorylated tau protein, and after being radiolabeled with 18F, the isoquinoline compound can be applied to positron emission tomography (PET) as an imaging developer for tau protein to allow early diagnosis of Alzheimer's disease and tracking of drug efficacy.