Title:
NOVEL BENZOTROPONE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/228577
Kind Code:
A1
Abstract:
The present invention provides a novel benzotropone derivative, and a preparation method therefor and an application thereof. The novel benzotropone derivative has a structure as represented by general formula (I) or formula (II), wherein R1 and R2 are both selected from a linear alkyl group consisting of 1-5 carbon atoms, a cycloalkyl group or cycloalcoylmethyl group consisting of 3-6 carbon atoms, a C2-C6 saturated or unsaturated alkyl group, or a fluorine-containing alkyl group consisting of 1-5 carbon atoms, and X is selected from carbon or nitrogen. The present invention proves, by means of pharmacological experiments, that the novel benzotropone derivative has the effects of inhibiting phosphodiesterase PDES activity, TNF-α release, neutrophilia or eosinophilia, and also can protect nerve cells, myocardial cells and vascular endothelial cells, has good safety, and thus has an important development significance.
Inventors:
HAO JIEJIE (CN)
WANG DE (CN)
YU GUANGLI (CN)
LI HAIHUA (CN)
WANG DE (CN)
YU GUANGLI (CN)
LI HAIHUA (CN)
Application Number:
PCT/CN2022/090821
Publication Date:
November 03, 2022
Filing Date:
April 30, 2022
Export Citation:
Assignee:
OCEAN UNIV CHINA (CN)
International Classes:
C07D213/82; A61K31/4412; A61P25/16; A61P37/08; C07D239/36
Domestic Patent References:
| WO2020115231A1 | 2020-06-11 |
Foreign References:
| CN109705034A | 2019-05-03 |
Other References:
ZHOU HAIBO, LI LIYUAN, WU CHONGMING, KURTÁN TIBOR, MÁNDI ATTILA, LIU YANKAI, GU QIANQUN, ZHU TIANJIAO, GUO PENG, LI DEHAI: "Penipyridones A–F, Pyridone Alkaloids from Penicillium funiculosum", JOURNAL OF NATURAL PRODUCTS, vol. 79, no. 7, 22 July 2016 (2016-07-22), US , pages 1783 - 1790, XP055975240, ISSN: 0163-3864, DOI: 10.1021/acs.jnatprod.6b00218
TURNER MARK J., LUO YISHAN, THOMAS DAVID Y., HANRAHAN JOHN W.: "The dual phosphodiesterase 3/4 inhibitor RPL554 stimulates rare class III and IV CFTR mutants", AMERICAN JOURNAL OF PHYSIOLOGY - LUNG CELLULAR AND MOLECULAR PHYSIOLOGY, vol. 318, no. 5, 1 May 2020 (2020-05-01), US , pages 908 - 920, XP055980248, ISSN: 1040-0605, DOI: 10.1152/ajplung.00285.2019
GAO SUFAN, XU QINLONG, LI JIAMING, CHU ZHAOXING, HE GUANGWEI, LIN GAOFENG, ZHU ZHENWEI, CUI YONG, MO JIAJIA, GUO JING, ZHAO YAN: "Design, Synthesis, and Biological Evaluation of Novel PDE-4 Inhibitors", CHINESE JOURNAL OF ORGANIC CHEMISTRY, vol. 38, no. 2, 11 October 2017 (2017-10-11), CN , pages 478 - 485, XP055980270, ISSN: 0253-2786, DOI: 10.6023/cjoc201705042
TURNER MARK J., LUO YISHAN, THOMAS DAVID Y., HANRAHAN JOHN W.: "The dual phosphodiesterase 3/4 inhibitor RPL554 stimulates rare class III and IV CFTR mutants", AMERICAN JOURNAL OF PHYSIOLOGY - LUNG CELLULAR AND MOLECULAR PHYSIOLOGY, vol. 318, no. 5, 1 May 2020 (2020-05-01), US , pages 908 - 920, XP055980248, ISSN: 1040-0605, DOI: 10.1152/ajplung.00285.2019
GAO SUFAN, XU QINLONG, LI JIAMING, CHU ZHAOXING, HE GUANGWEI, LIN GAOFENG, ZHU ZHENWEI, CUI YONG, MO JIAJIA, GUO JING, ZHAO YAN: "Design, Synthesis, and Biological Evaluation of Novel PDE-4 Inhibitors", CHINESE JOURNAL OF ORGANIC CHEMISTRY, vol. 38, no. 2, 11 October 2017 (2017-10-11), CN , pages 478 - 485, XP055980270, ISSN: 0253-2786, DOI: 10.6023/cjoc201705042
Attorney, Agent or Firm:
QINGDAO HECHUANG INTELLECTUAL PROPERTY AGENCY FIRM (GENERAL PARTNERSHIP ) (CN)
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