Title:
HYDROXAMIC ACID DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/052353
Kind Code:
A1
Abstract:
The present invention relates to the technical field of enzyme inhibitors, and relates in particular to a hydroxamic acid derivative, a preparation method therefor and an application thereof. The hydroxamic acid group in the hydroxamic acid derivative provided in the present invention is chelated with an active zinc ion in an active region of an LpxC enzyme, and contains a hydrophobic side chain that binds to a hydrophobic channel in the LpxC enzyme. The described content in the two aspects ensures that a hydroxamic acid derivative has good bactericidal activity and low toxicity for LpxC. Also provided is a preparation method for the hydroxamic acid derivative, which has a short reaction time and a high yield.
Inventors:
WANG YUCHENG (CN)
YOU XUEFU (CN)
WANG JUXIAN (CN)
DU XIAONAN (CN)
WANG MINGHUA (CN)
ZHU MEI (CN)
ZHANG GUONING (CN)
YOU XUEFU (CN)
WANG JUXIAN (CN)
DU XIAONAN (CN)
WANG MINGHUA (CN)
ZHU MEI (CN)
ZHANG GUONING (CN)
Application Number:
PCT/CN2020/115509
Publication Date:
March 25, 2021
Filing Date:
September 16, 2020
Export Citation:
Assignee:
INST MED BIOTECHNOLOGY CAMS (CN)
International Classes:
C07C259/06; A61P31/04; C07C41/30; C07C43/192; C07C45/29; C07C47/37; C07C51/09; C07C65/28; C07C67/343; C07C69/78; C07C231/12; C07C235/42; C07C269/06; C07C271/22; C07D295/155; C07D295/195
Domestic Patent References:
| WO2018115432A2 | 2018-06-28 | |||
| WO2012031298A2 | 2012-03-08 | |||
| WO2017189586A1 | 2017-11-02 | |||
| WO2013039947A1 | 2013-03-21 | |||
| WO2017223349A1 | 2017-12-28 |
Foreign References:
| CN110563611A | 2019-12-13 | |||
| CN101765585A | 2010-06-30 | |||
| CN101765585A | 2010-06-30 | |||
| CN1777577A | 2006-05-24 | |||
| CN201910885618A | 2019-09-19 |
Other References:
DU XIAONAN, ZHANG GUONING; ZHU MEI; WANG MINGHUA; WANG YUCHENG; WANG JUXIAN: "Improved Synthesis of LpxC Inhibitor ACHN-975", CHINESE JOURNAL OF PHARMACEUTICALS, HANGHAI YIYAO GONGYE YANJIUYUAN,SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, CN, vol. 50, no. 5, 1 January 2019 (2019-01-01), CN, pages 514 - 519, XP055792377, ISSN: 1001-8255
See also references of EP 4071134A4
See also references of EP 4071134A4
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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