Mesaconin | 6792-09-2

• 物质功能分类: 生物化工 - 提取物
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: Mesaconin
• 英文别名: 6,16,18-trimethoxy-13-(methoxymethyl)-11-methyl-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecane-4,5,7,8,14-pentol
• CAS: 6792-09-2
• 化学式: C₂₄H₃₉NO₉
• 分子量: 485.575
• InChiKey: GQRPJUIKGLHLLN-UHFFFAOYSA-N

物化性质

• 沸点：
  617.1±55.0 °C(Predicted)
• 密度：
  1.44±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于酸性水溶液（轻微）、氯仿（轻微）、甲醇（轻微）

计算性质

• 辛醇/水分配系数(LogP)：
  -2.9
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  141
• 氢给体数：
  5
• 氢受体数：
  10

制备方法与用途

背景

药附子为毛茛科植物乌头（Aconitum carmichaeli Debxy）的子根的加工品。它具有回阳救逆、补火助阳、逐风寒湿邪、温经止痛的功能，常用于治疗以下病症：亡阳虚脱、肢冷脉微、阳痿、宫寒、心腹冷痛、虚寒吐泻、阴寒水肿及阳虚外感、寒湿痹痛。

用途

新乌头原碱在制备预防和/或治疗心肌纤维化及其引起的慢性心衰的药物中具有新的应用价值。

药理作用

1. 抑制或逆转心肌组织纤维化；
2. 改善心脏异常重构；
3. 改善心功能障碍；
4. 提高心肌纤维化所致慢性心衰小鼠的生存率；
5. 对抗心肌组织炎症；
6. 抑制心肌细胞凋亡；
7. 增强死小鼠心肌酶活性，其作用机制与抑制阿霉素引起的心肌组织炎症和纤维化、对抗心肌细胞凋亡有关。

生物活性

Mesaconine是从Aconitum carmichaelii Debx. 中提取的活性成分之一，对心血管系统具有显著的作用。

文献信息

• Crystalline Forms Of Mesaconine And Preparation Methods Therefor
  申请人：Gooddoctor Pharmaceutical Group Co., Ltd.

  公开号：US20200339514A1

  公开（公告）日：2020-10-29

  The present invention relates to crystalline forms of mesaconine. Specifically, the present invention relates to crystalline form A, crystalline form B and crystalline form C of mesaconine and preparation methods thereof. In the method, the mesaconine is crystallized in solvent, and then the crude crystal is dried to obtain target crystalline form. The crystalline forms of mesaconine according to the present invention have good solubility, good stability, low hygroscopicity, long-term storage capability and good reproducibility, and have a good prospect to be developed as pharmaceuticals.

  本发明涉及美沙酮的晶体形态。具体而言，本发明涉及美沙酮的晶体形态A、晶体形态B和晶体形态C以及其制备方法。在该方法中，美沙酮在溶剂中结晶，然后粗晶体经干燥后得到目标晶体形态。本发明所述的美沙酮晶体形态具有良好的溶解性、稳定性、低吸湿性、长期储存能力和良好的可重复性，并有望开发为药物。
• CRYSTALLINE FORMS OF MESACONINE AND PREPARATION METHOD THEREFOR
  申请人：GOODDOCTOR PHARMACEUTICAL GROUP CO., LTD.

  公开号：EP3744712A1

  公开（公告）日：2020-12-02

  The present invention relates to crystalline forms of mesaconine. Specifically, the present invention relates to crystalline form A, crystalline form B and crystalline form C of mesaconine and preparation methods thereof. In the method, the mesaconine is crystallized in solvent, and then the crude crystal is dried to obtain target crystalline form. The crystalline forms of mesaconine according to the present invention have good solubility, good stability, low hygroscopicity, long-term storage capability and good reproducibility, and have a good prospect to be developed as pharmaceuticals.

  本发明涉及美沙康宁的结晶形式。具体而言，本发明涉及中乌头碱的结晶形式 A、结晶形式 B 和结晶形式 C 及其制备方法。在该方法中，中乌头原碱在溶剂中结晶，然后将粗晶体干燥以获得目标晶型。本发明的美沙康宁结晶具有良好的溶解性、稳定性、低吸湿性、长期储存性和良好的重现性，具有良好的医药开发前景。
• METHOD FOR PREPARING MESACONINE AND RELATED INTERMEDIARIES
  申请人：Gooddoctor Pharmaceutical Group

  公开号：EP3744711A1

  公开（公告）日：2020-12-02

  The present invention relates to a method for preparing mesaconine and related intermediaries. Specifically, in the method for preparing mesaconine of the present invention, aconitine extracted from the Aconitum soongaricum Stapf. of aconitum plant is used as a raw material and subjected to alkalization, acetylation, N-de-ethylation, N-methylation, and hydrolysis to obtain mesaconine. The method for preparing mesaconine in the present invention is simple in operation, high in yield, environmentally friendly and pollution-free, and suitable for industrial production.

  本发明涉及一种制备中乌头碱及相关中间体的方法。具体来说，在本发明的中乌头碱制备方法中，以乌头属植物 Aconitum soongaricum Stapf.中提取的乌头碱为原料，经过碱化、乙酰化、N-去乙基化、N-甲基化、水解等步骤得到中乌头碱。本发明制备中乌头碱的方法操作简单，产量高，环保无污染，适合工业化生产。
• Crystalline forms of mesaconine and preparation methods therefor
  申请人：Gooddoctor Pharmaceutical Group Co., Ltd.

  公开号：US10941116B2

  公开（公告）日：2021-03-09

  The present invention relates to crystalline forms of mesaconine. Specifically, the present invention relates to crystalline form A, crystalline form B and crystalline form C of mesaconine and preparation methods thereof. In the method, the mesaconine is crystallized in solvent, and then the crude crystal is dried to obtain target crystalline form. The crystalline forms of mesaconine according to the present invention have good solubility, good stability, low hygroscopicity, long-term storage capability and good reproducibility, and have a good prospect to be developed as pharmaceuticals.

  本发明涉及美沙康宁的结晶形式。具体而言，本发明涉及中乌头碱的结晶形式 A、结晶形式 B 和结晶形式 C 及其制备方法。在该方法中，中乌头原碱在溶剂中结晶，然后将粗晶体干燥以获得目标晶型。本发明的美沙康宁结晶具有良好的溶解性、稳定性、低吸湿性、长期储存性和良好的重现性，具有良好的医药开发前景。
• Method For Preparing Mesaconine And Related Intermediaries Thereof
  申请人：Gooddoctor Pharmaceutical Group Co., Ltd.

  公开号：US20210040042A1

  公开（公告）日：2021-02-11

  The present invention relates to a method for preparing mesaconine and related intermediaries. Specifically, in the method for preparing mesaconine of the present invention, aconitine extracted from the Aconitum soongaricum Stapf. of aconitum plant is used as a raw material and subjected to alkalization, acetylation, N-de-ethylation, N-methylation, and hydrolysis to obtain mesaconine. The method for preparing mesaconine in the present invention is simple in operation, high in yield, environmentally friendly and pollution-free, and suitable for industrial production.