Title:
LAPPACONITINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/099937
Kind Code:
A1
Abstract:
A lappaconitine derivative, a preparation method therefor, and a use thereof. The derivative is an enantiomer, a diastereomer, a racemate, and a mixture thereof, as well as a pharmaceutically acceptable inorganic or organic salt, a crystal form, and a solvate thereof; six preparation methods are utilized to obtain the lappaconitine derivative, diterpenoid alkaloid structures are enriched, the lappaconitine derivative is superior to lappaconitine in combating arrhythmia and in analgesic activity, and the toxicity is less than lappaconitine, and thus a synthesized lappaconitine derivative may be used to prepare a drug for treating a cardio-cerebrovascular disease and pain.
Inventors:
AISA HAJI AKBER (CN)
SHEN JINGSHAN (CN)
SAGDULLAEV SHAMANSUR (UZ)
YUNUSOV MURAT (RU)
ZHAO QINGJIE (CN)
WANG BIANLIN (CN)
SADIKOV ALIMGJAN (UZ)
XIAMUXI HAINIMU (CN)
ZHAO BO (CN)
DJAHANGIROV FARHAD (UZ)
LIU XIAOYAN (CN)
JIANG XIANGRUI (CN)
WANG ZHEN (CN)
WANG YU (CN)
ZHENG WEI (CN)
XUE WENJUAN (CN)
ZHAO JIANGYU (CN)
SHEN JINGSHAN (CN)
SAGDULLAEV SHAMANSUR (UZ)
YUNUSOV MURAT (RU)
ZHAO QINGJIE (CN)
WANG BIANLIN (CN)
SADIKOV ALIMGJAN (UZ)
XIAMUXI HAINIMU (CN)
ZHAO BO (CN)
DJAHANGIROV FARHAD (UZ)
LIU XIAOYAN (CN)
JIANG XIANGRUI (CN)
WANG ZHEN (CN)
WANG YU (CN)
ZHENG WEI (CN)
XUE WENJUAN (CN)
ZHAO JIANGYU (CN)
Application Number:
PCT/CN2021/073922
Publication Date:
May 19, 2022
Filing Date:
January 27, 2021
Export Citation:
Assignee:
XINJIANG TECHNICAL INST OF PHYSICS & CHEMISTRY CHINESE ACADEMY OF SCIENCES (CN)
SHANGHAI INST MATERIA MEDICA CAS (CN)
INST OF THE CHEMISTRY OF PLANT SUBSTANCES ACADEMY OF SCIENCES OF THE REPUBLIC OF UZBEKISTAN (UZ)
UFA INST OF ORGANIC CHEMISTRY OF THE RUSSIAN ACADEMY OF SCIENCES (RU)
SHANGHAI INST MATERIA MEDICA CAS (CN)
INST OF THE CHEMISTRY OF PLANT SUBSTANCES ACADEMY OF SCIENCES OF THE REPUBLIC OF UZBEKISTAN (UZ)
UFA INST OF ORGANIC CHEMISTRY OF THE RUSSIAN ACADEMY OF SCIENCES (RU)
International Classes:
C07D221/22; A61K31/439; A61K31/506; A61P9/00; A61P9/04; A61P9/06; A61P9/10; A61P25/04; A61P29/00
Foreign References:
| CN110872253A | 2020-03-10 | |||
| CN102140079A | 2011-08-03 | |||
| CN1962639A | 2007-05-16 |
Other References:
ROMANOV V. E., SHUL’TS E. E., SHAKIROV M. M., TOLSTIKOV G. A.: "Alkaloids of Siberia and altai flora. 17.* Synthesis of N-containing derivatives of the diterpene alkaloid lappaconitine", CHEMISTRY OF NATURAL COMPOUNDS, vol. 46, no. 4, 26 August 2010 (2010-08-26), US , pages 593 - 597, XP055931109, ISSN: 0009-3130, DOI: 10.1007/s10600-010-9683-5
SONG HUIHUI: "The Extraction and Derivatization of Lappaconitine and Anti-Tumor Activity of Lappaconitine Derivatives", CHINESE MASTER'S THESES FULL-TEXT DATABASE, 1 April 2017 (2017-04-01), pages 1 - 102, XP055931116
CHEREMNYKH KIRILL P; SAVEL’EV VIKTOR А; SHKURKO OLEG P; SHULTS ELVIRA E: "Synthesis of hybrid molecules containing pyrimidine and diterpene alkaloid lappaconitine fragments", CHEMISTRY OF HETEROCYCLIC COMPOUNDS, vol. 54, no. 12, 18 January 2019 (2019-01-18), New York , pages 1131 - 1138, XP036693847, ISSN: 0009-3122, DOI: 10.1007/s10593-019-02404-w
SONG HUIHUI: "The Extraction and Derivatization of Lappaconitine and Anti-Tumor Activity of Lappaconitine Derivatives", CHINESE MASTER'S THESES FULL-TEXT DATABASE, 1 April 2017 (2017-04-01), pages 1 - 102, XP055931116
CHEREMNYKH KIRILL P; SAVEL’EV VIKTOR А; SHKURKO OLEG P; SHULTS ELVIRA E: "Synthesis of hybrid molecules containing pyrimidine and diterpene alkaloid lappaconitine fragments", CHEMISTRY OF HETEROCYCLIC COMPOUNDS, vol. 54, no. 12, 18 January 2019 (2019-01-18), New York , pages 1131 - 1138, XP036693847, ISSN: 0009-3122, DOI: 10.1007/s10593-019-02404-w
Attorney, Agent or Firm:
FASTA INTELLECTUAL PROPERTY LIMITED (CN)
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