Title:
HYDROPHILIC BERBERINE DERIVATIVE WITH R10 AND R11 CONNECTED AND APPLICATION THEREOF IN PREPARATION OF DRUGS
Document Type and Number:
WIPO Patent Application WO/2019/196955
Kind Code:
A1
Abstract:
Disclosed are an 8-dihalide methyl berberine quaternary ammonium compound shown in formulas (I) and (II), a synthetic method therefor, and an application thereof in preparation of drugs. The 8-dihalide methyl berberine quaternary ammonium compound is more hydrophilic than a substrate in the absence of conventional hydrophilic groups. The 8-dihalide methyl berberine quaternary ammonium compound has a remarkable anti-microbial activity, anti-inflammatory activity and anti-ulcerative colitis activity, can explicitly and significantly regulate target molecules, associated with tumor formation, in tumor cells of the colon cancer, liver cancer, lung cancer, breast cancer, osteosarcoma, and glioma, and has anti-tumor activity. The pharmacological action of the compound of the present invention is higher than that of a control drug. Moreover, the compound has the characteristics of nontoxicity or hypotoxicity, and can be used for preparing drugs for preventing, alleviating, and/or treating microbiological contamination, inflammation, ulcerative colitis, and tumors.
Inventors:
QIN HAILIN (CN)
WU LIANQIU (CN)
LI XIANG (CN)
ZHANG HAIJING (CN)
SONG LI (CN)
SONG HUACHEN (CN)
DENG ANJUN (CN)
TANG XIAONAN (CN)
ZHANG ZHIHUI (CN)
LI XIANG (CN)
LI ZHIHONG (CN)
WU LIANQIU (CN)
LI XIANG (CN)
ZHANG HAIJING (CN)
SONG LI (CN)
SONG HUACHEN (CN)
DENG ANJUN (CN)
TANG XIAONAN (CN)
ZHANG ZHIHUI (CN)
LI XIANG (CN)
LI ZHIHONG (CN)
Application Number:
PCT/CN2019/082640
Publication Date:
October 17, 2019
Filing Date:
April 15, 2019
Export Citation:
Assignee:
INST MATERIA MEDICA CAMS (CN)
International Classes:
C07D455/03; A61K31/4375; A61P1/04; A61P29/00; A61P31/00; A61P31/04; A61P31/10; A61P35/00
Domestic Patent References:
| WO2013070910A1 | 2013-05-16 | |||
| WO2013060274A1 | 2013-05-02 | |||
| WO2008040192A1 | 2008-04-10 |
Foreign References:
| KR20150080249A | 2015-07-09 | |||
| CN107281180A | 2017-10-24 |
Other References:
JIANG, XIAO-FEI: "Synthesis and Antimicrobial Activity of 8-Alkyl Coptisine Derivatives", ASIAN JOURNAL OF CHEMISTRY, vol. 23, no. 9, 31 December 2011 (2011-12-31), pages 3849 - 3852, XP055645655
Attorney, Agent or Firm:
CCPIT PATENT AND TRADEMARK LAW OFFICE (CN)
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