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Title:
ACETAZOLAMIDE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF IN PREPARATION OF DRUG FOR TREATING CORONARY HEART DISEASE
Document Type and Number:
WIPO Patent Application WO/2022/083617
Kind Code:
A1
Abstract:
The present invention relates to an acetazolamide derivative, and a preparation method therefor and the use thereof in the preparation of a drug for treating coronary heart disease. The acetazolamide derivative is a type of acetazolamide derivative I obtained by bonding a carbonic anhydrase inhibitor acetazolamide Ac and a non-steroidal anti-inflammatory drug, which is represented by aspirin As and has a carboxylic acid group, by means of a linking group, and the structural general formula is shown in formula (1). In formula (1), OOC-NSAID represents a non-steroidal anti-inflammatory drug in which one carboxylic acid proton is lost, representatives of which are acetazolamide derivatives containing aspirin or indomethacin. The acetazolamide derivative I has a good activity in terms of inhibiting carbonic anhydrase 9, can effectively improve myocardial anoxia injuries in an anoxia microenvironment, and is applied to the preparation of a drug for treating coronary heart disease.

Inventors:
GOU SHAOHUA (CN)
ZHOU WEN (CN)
ZHANG BIN (CN)
Application Number:
PCT/CN2021/124900
Publication Date:
April 28, 2022
Filing Date:
October 20, 2021
Export Citation:
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Assignee:
UNIV SOUTHEAST (CN)
International Classes:
A61P9/10; C07D417/12; C07D417/14
Foreign References:
CN111961043A2020-11-20
CN101756967A2010-06-30
Other References:
SAMUELE CAZZAMALLI, ALBERTO DAL CORSO, DARIO NERI: "Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma", MOLECULAR CANCER THERAPEUTICS, AMERICAN ASSOCIATION FOR CANCER RESEARCH, US, vol. 15, no. 12, 1 December 2016 (2016-12-01), US , pages 2926 - 2935, XP055456478, ISSN: 1535-7163, DOI: 10.1158/1535-7163.MCT-16-0283
XIAO ZHONGHAI *, ET AL.: "Recent Progress in Clinical Application of the Carbonic Anhydrase Inhibitor, Acetazolamide", CHINESE JOURNAL OF NEW DRUGS, GAI-KAN BIANJIBU, BEIJING, CN, vol. 17, no. 16, 30 August 2008 (2008-08-30), CN , pages 1390 - 1394, XP055924541, ISSN: 1003-3734
Attorney, Agent or Firm:
NANJING RUIHONG PATENT & TRADEMARK AGENCY (ORDINARY PARTNERSHIP) (CN)
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