Triptolide acrylate, preparation method therefor and use thereof

US11660285B2 · kind B2 · utility

Assignees

• Guangdong Provincial Hospital of TCM · CN
• The Second Affiliated Hospital Of Guangzhou University of Chinese Medicine · CN
• The Second Clinical College Of Guangzhou University of Chinese Medicine · CN
• Guangdong Provincial Academy Of Chinese Medical Sciences · CN

Inventors

• Bo Liu · San Diego, US
• Xianzhang Huang · Longbeilingcun, CN
• Zhimin Yang · Longbeilingcun, CN
• Jun Li · Miaocheng, CN
• Quanfu Chen · Longbeilingcun, CN
• Liqiao Han · Somerville, US
• Hualun Liang · Longbeilingcun, CN
• Yiqi Yang · Lincoln, US
• Kai Wang · Longbeilingcun, CN
• Xiaowan Wang · Longbeilingcun, CN
• Ennian Li · Longbeilingcun, CN
• Yi Wang · Tianjin, CN
• Runyue Huang · Longbeilingcun, CN
• Yunshan Wu · Gangshan Subdistrict, CN
• Xiaodong Han · Longbeilingcun, CN
• Jinlang Zhong · Longbeilingcun, CN
• Bidan Zheng · Longbeilingcun, CN

Key dates

• Filing date: Dec 30, 2019
• Grant date: May 30, 2023
• Expiry date: Dec 30, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J73/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide.