Title:
BENZOTHIAZINONE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF AS ANTI-TUBERCULOSIS DRUG
Document Type and Number:
WIPO Patent Application WO/2021/203812
Kind Code:
A1
Abstract:
Disclosed are a benzothiazinone derivative, a preparation method therefor and use thereof as an anti-tuberculosis drug. The present invention specifically relates to a new class of compounds having a benzothiazinone skeleton. Such compounds show an inhibitory effect on mycobacterium tuberculosis, and in particular, an inhibitory effect also on mycobacterium tuberculosis having clinical drug resistance. Compared with the existing clinical first-line drug isoniazide (MIC 0.5μM), the activity of such compounds has a great advantage; compared with the existing benzothiazinone antituberculosis drug pBTZ 169 at the research stage, such compounds have a lower cLogP value, and has better druggability.
Inventors:
QIAO CHUNHUA (CN)
FAN DONGGUANG (CN)
FAN DONGGUANG (CN)
Application Number:
PCT/CN2021/074579
Publication Date:
October 14, 2021
Filing Date:
January 31, 2021
Export Citation:
Assignee:
UNIV SOOCHOW (CN)
International Classes:
A61K31/5415; C07D279/08; A61P31/06; C07D417/04; C07D417/12; C07D417/14; C07D471/10; C07D491/113
Foreign References:
| CN103221399A | 2013-07-24 | |||
| CN103508980A | 2014-01-15 | |||
| CN101809009A | 2010-08-18 | |||
| CN105622596A | 2016-06-01 | |||
| CN110312725A | 2019-10-08 | |||
| CN110204546A | 2019-09-06 | |||
| CN108530448A | 2018-09-14 | |||
| CN112409294A | 2021-02-26 | |||
| CN111303075A | 2020-06-19 |
Other References:
GANG ZHANG, MICHAEL HOWE, COURTNEY C. ALDRICH: "Spirocyclic and Bicyclic 8-Nitrobenzothiazinones for Tuberculosis with Improved Physicochemical and Pharmacokinetic Properties", ACS MEDICINAL CHEMISTRY LETTERS, vol. 10, no. 3, 14 March 2019 (2019-03-14), pages 348 - 351, XP055856941, ISSN: 1948-5875, DOI: 10.1021/acsmedchemlett.8b00634
KAI LV; XUEFU YOU; BIN WANG; ZENGQUAN WEI; YUN CHAI; BO WANG; APENG WANG; GUOCHENG HUANG; MINGLIANG LIU; YU LU: "Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents", ACS MEDICINAL CHEMISTRY LETTERS, vol. 8, no. 6, 8 June 2017 (2017-06-08), pages 636 - 641, XP055418851, ISSN: 1948-5875, DOI: 10.1021/acsmedchemlett.7b00106
KAI LV; XUEFU YOU; BIN WANG; ZENGQUAN WEI; YUN CHAI; BO WANG; APENG WANG; GUOCHENG HUANG; MINGLIANG LIU; YU LU: "Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents", ACS MEDICINAL CHEMISTRY LETTERS, vol. 8, no. 6, 8 June 2017 (2017-06-08), pages 636 - 641, XP055418851, ISSN: 1948-5875, DOI: 10.1021/acsmedchemlett.7b00106
Attorney, Agent or Firm:
SUZHOU CREATOR PATENT AND TRADEMARK AGENCY, LTD (CN)
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