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Title:
SELECTIVE BUTYRYLCHOLINESTERASE INHIBITOR OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/042410
Kind Code:
A1
Abstract:
Disclosed are a selective butyrylcholinesterase inhibitor having general formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, and use thereof. By testing the efficacy of treatment of Alzheimer's disease, especially moderate to severe Alzheimer's disease, by means of the butyrylcholinesterase inhibitory activity and the selective screening as well as the toxicity to nerve cells, it is found that the selective butyrylcholinesterase inhibitor or a pharmaceutically acceptable salt thereof has good in-vitro target activity as well as high selectivity and drug safety, and can be used as a precursor substance for further development of the treatment of Alzheimer's disease by selectively inhibiting butyrylcholinesterase.

Inventors:
SUN HAOPENG (CN)
YANG HONGYU (CN)
CHEN TINGKAI (CN)
CHEN YAO (CN)
FENG FENG (CN)
DU CHENXI (CN)
Application Number:
PCT/CN2019/105879
Publication Date:
March 11, 2021
Filing Date:
September 16, 2019
Export Citation:
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Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
C07D333/38; A61K31/167; A61K31/341; A61K31/381; A61K31/40; A61K31/4164; A61K31/426; A61P25/28; C07D233/54; C07D277/20; C07D307/34
Domestic Patent References:
WO2000058270A22000-10-05
WO2009103778A12009-08-27
Other References:
DATABASE REGISTRY STN; 18 May 2011 (2011-05-18), ANONYMOUS: "1296484-21-3 et al.", XP055789003, Database accession no. 1296484-21-3
JIANSONG FANG, RANYAO YANG, LI GAO, DAN ZHOU, SHENGQIAN YANG, AI-LIN LIU, GUAN-HUA DU: "Predictions of BuChE Inhibitors Using Support Vector Machine and Naive Bayesian Classification Techniques in Drug Discovery", JOURNAL OF CHEMICAL INFORMATION AND MODELING, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, US, vol. 53, no. 11, 25 November 2013 (2013-11-25), US, pages 3009 - 3020, XP055747277, ISSN: 1549-9596, DOI: 10.1021/ci400331p
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM (ORDINARY PARTNERSHIP) (CN)
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