berberine azide

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 原小檗碱生物碱及其衍生物
• 英文名称: berberine azide
• 英文别名: 16,17-Dimethoxy-5,7-dioxa-13-azoniapentacyclo[11.8.0.02,10.04,8.015,20]henicosa-1(13),2,4(8),9,14,16,18,20-octaene;azide
• 化学式: C₂₀H₁₈NO₄*N₃
• 分子量: 378.387
• InChiKey: RLFJEJJPHALJAW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.96
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  43.8
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  盐酸小檗碱 在 sodium azide 作用下， 以 水 为溶剂， 反应 1.0h， 以74%的产率得到berberine azide
  参考文献：
  名称：

  三种小檗碱衍生物的分子和晶体结构

  摘要：

  小檗碱叠氮化物、硫氰酸小檗碱和 8-氰基-8H-小檗碱是从氯化小檗碱（一种四元原小檗碱生物碱）制备的。报告和讨论了所有化合物的分子和晶体结构。

  DOI：

  10.3390/60500433

文献信息

• Compounds and Compositions for Modulating Lipid Levels and Methods of Preparing Same
  申请人：Liu Haiyan

  公开号：US20110009628A1

  公开（公告）日：2011-01-13

  The present technology relates to compounds of Formulas I-VI and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also increase HDL-C, lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.

  目前的技术涉及到公式I-VI的化合物以及制备和使用这些化合物的方法。使用方法包括预防和治疗高脂血症、高胆固醇血症、高甘油三酯血症、肝脂肪变性和代谢综合征。本文披露的化合物还可以增加高密度脂蛋白胆固醇（HDL-C），降低总胆固醇、低密度脂蛋白胆固醇（LDL-C）和甘油三酯，并增加肝LDL受体表达，抑制PCSK9表达，并激活AMP激活蛋白激酶。
• [EN] COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING NASH, NAFLD, AND OBESITY<br/>[FR] COMPOSÉS, COMPOSITIONS ET MÉTHODES DE TRAITEMENT DE LA NASH, DE LA NAFLD ET DE L'OBÉSITÉ
  申请人：LIU JINGWEN

  公开号：WO2021067490A1

  公开（公告）日：2021-04-08

  The present technology relates to methods of treating NASH, NAFLD and/or obesity using compounds of Formulas I, II, III, IV, V, and/or VI. The methods include administering to a subject suffering from one or more of non-alcoholic steatohepatitis (NASH), non- alcoholic fatty liver disease (NAFLD) and/or obesity a therapeutically effective amount of such a compound

  目前的技术涉及使用I、II、III、IV、V和/或VI式化合物治疗NASH、NAFLD和/或肥胖的方法。这些方法包括向患有非酒精性脂肪肝炎（NASH）、非酒精性脂肪肝病（NAFLD）和/或肥胖的受试者施用这种化合物的治疗有效剂量。
• COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS
  申请人：Liu Haiyan

  公开号：US20090048246A1

  公开（公告）日：2009-02-19

  Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.

  从黄堇属植物提取物或分离纯化的化合物构成的组合物可预防和治疗高脂血症、高胆固醇血症、高甘油三酯血症、肝脂肪变性和代谢综合征。黄堇化合物及其天然和合成来源的衍生物可降低总胆固醇、LDL-胆固醇和甘油三酯，增加肝LDL受体表达并激活AMP激活蛋白激酶。具有降脂活性的黄堇化合物的特定立体异构体包括14R-(+)-可丹碱、14R,13S-(+)-可丹啉、14R-(+)-四氢棕榈碱、(+)-可鲁米丁、d-(+)-比库枯碱和(+)-艾根碱。
• [EN] METHODS AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC AND CARDIOVASCULAR DISORDERS<br/>[FR] MÉTHODES ET COMPOSITIONS UTILISÉES POUR LE TRAITEMENT DE MALADIES MÉTABOLIQUES ET CARDIOVASCULAIRES
  申请人：XINTRIA PHARMACEUTICAL CORP IN

  公开号：WO2010104595A1

  公开（公告）日：2010-09-16

  Methods and compositions containing a berberine related compound are provided for the prevention and treatment of metabolic and cardiovascular disorders including metabolic syndrome, hyperlipidemia, obesity, diabetes, insulin resistance, hyperglycemia, hypertension and elevated cholesterol in mammalian subjects. The methods and compositions of the invention are effective for prevention and treatment of metabolic syndrome, hyperlipidemia, obesity, diabetes, insulin resistance, hyperglycemia, hypertension and elevated cholesterol. Additional compositions and methods are provided which employ a berberine related or derivative compound including demethylated derivatives in combination with a second anti- therapeutic agent to yield more effective treatment tools against metabolic disorders, and/or dual activity therapeutic methods and formulations useful to prevent or reduce hyperlipidemia and/or hyperglycemia and one or more causal or related symptoms or conditions associated with hyperlipidemia and/or hyperglycemia in mammalian subjects.

  本发明提供了一种含有黄连素相关化合物的方法和组合物，用于预防和治疗代谢和心血管疾病，包括代谢综合征、高脂血症、肥胖症、糖尿病、胰岛素抵抗、高血糖、高血压和高胆固醇等哺乳动物主体的疾病。本发明的方法和组合物对于预防和治疗代谢综合征、高脂血症、肥胖症、糖尿病、胰岛素抵抗、高血糖、高血压和高胆固醇具有有效性。提供了使用黄连素相关或衍生化合物（包括去甲基化衍生物）与第二种抗治疗剂组合的附加组合物和方法，以产生更有效的治疗工具，用于治疗代谢性疾病和/或双重活性治疗方法和配方，有助于预防或减少哺乳动物主体中与高脂血症和/或高血糖有关的一个或多个原因或相关症状或状况。
• Methods and compositions for the treatment of hyperlipidemia
  申请人：Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences

  公开号：EP2361625A1

  公开（公告）日：2011-08-31

  Methods and compositions containing a berberine compound or berberine related or derivative compound are provided for the prevention and treatment of hyperlipidemia, elevated cholesterol, and/or cardiovascular disease in mammalian subjects. The methods and compositions of the invention are effective for prevention and treatment of atherosclerosis, coronary artery disease, angina pectoris, carotid artery disease, stroke, cerebral arteriosclerosis, high blood pressure, myocardial infarction, cerebral infarction, restenosis following balloon angioplasty, intermittent claudication, dyslipidemia post-prandial lipidemia or xanthoma. Additional compositions and methods are provided which employ a berberine compound or berberine related or derivative compound in combination with a second anti-hyperlipidemia agent, or a different therapeutic agent to yield more effective treatment tools against hyperlipidemia and/or cardiovascular disease, and/or dual activity therapeutic methods and formulations useful to prevent or reduce hyperlipidemia and one or more causal or related symptoms or conditions associated with hyperlipidemia in mammalian subjects.

  本发明提供了含有小檗碱化合物或小檗碱相关或衍生物化合物的方法和组合物，用于预防和治疗哺乳动物的高脂血症、胆固醇升高和/或心血管疾病。本发明的方法和组合物可有效预防和治疗动脉粥样硬化、冠状动脉疾病、心绞痛、颈动脉疾病、中风、脑动脉硬化、高血压、心肌梗塞、脑梗塞、球囊血管成形术后再狭窄、间歇性跛行、餐后血脂异常或黄疽。还提供了其他组合物和方法，这些组合物和方法采用小檗碱化合物或小檗碱相关或衍生物化合物与第二种抗高脂血症药剂或不同的治疗药剂结合使用，以产生更有效的抗高脂血症和/或心血管疾病的治疗工具，和/或双重活性治疗方法和制剂，用于预防或减轻哺乳动物体内的高脂血症以及与高脂血症相关的一种或多种因果或相关症状或病症。