Title:
SALT OF BENZOTHIOPYRONE COMPOUND, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/047525
Kind Code:
A1
Abstract:
The present invention relates to the technical field of medicine, and provides a salt of a benzothiopyrone compound, and a preparation method therefor and an application thereof, in particular, a salt of 2-(4-(cyclohexylmethyl)piperazin-1-yl)-6-(trifluoromethyl)-8-nitro-benzothiopyran-4-one as represented by formula (I), a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of a drug for treating and/or preventing an infectious disease caused by Mycobacterium tuberculosis. The present invention aims to prepare a salt of 2-(4-(cyclohexylmethyl)piperazin-1-yl)-6-(trifluoromethyl)-8-nitro-benzothiopyran-4-one having significantly improved pharmacokinetic properties and physicochemical properties and having strong anti-Mycobacterium tuberculosis activity in vivo and in vitro; as a potential novel drug, the salt can be used for treatment or preventive treatment of an infectious disease caused by bacteria, particularly tuberculosis (TB) caused by Mycobacterium tuberculosis, and can also be used for overcoming a problem related to drug resistance of Mycobacterium tuberculosis.
Inventors:
LI GANG (CN)
HUANG HAIHONG (CN)
LI PENG (CN)
LI YAN (CN)
ZHANG TINGTING (CN)
WANG BAOLIAN (CN)
LI YAN (CN)
HUANG HAIHONG (CN)
LI PENG (CN)
LI YAN (CN)
ZHANG TINGTING (CN)
WANG BAOLIAN (CN)
LI YAN (CN)
Application Number:
PCT/CN2020/114126
Publication Date:
March 18, 2021
Filing Date:
September 09, 2020
Export Citation:
Assignee:
INST MATERIA MEDICA CAMS (CN)
International Classes:
C07D335/04; A61K31/4535; A61P31/06
Foreign References:
| CN108929329A | 2018-12-04 | |||
| JPS49101379A | 1974-09-25 | |||
| CN108947952A | 2018-12-07 | |||
| CN104211708A | 2014-12-17 |
Other References:
LI PENG; WANG BIN; ZHANG XINWEI; BATT SARAH M.; BESRA GURDYAL S.; ZHANG TINGTING; MA CHEN; ZHANG DONGFENG; LIN ZIYUN; LI GANG; HUA: "Identification of novel benzothiopyranone compounds againstMycobacterium tuberculosisthrough scaffold morphing from benzothiazinones", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 160, 17 September 2018 (2018-09-17), AMSTERDAM, NL, pages 157 - 170, XP085521522, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2018.09.042
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