二碘化氯异吲哚铵 | 69-27-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 中文名称: 二碘化氯异吲哚铵
• 中文别名: 四氯吲哚铵；松达氯铵；氯化氯异吲哚铵；氯化四氯吲哚铵
• 英文名称: Chlorisondamine chloride
• 英文别名: trimethyl-[2-(4,5,6,7-tetrachloro-2-methyl-1,3-dihydroisoindol-2-ium-2-yl)ethyl]azanium;dichloride
• CAS: 69-27-2
• 化学式: C14H20Cl6N2
• 分子量: 429.0
• InChiKey: DXXUGBPKQDTBQW-UHFFFAOYSA-L

物化性质

• 熔点：
  258-265° (dec)
• 沸点：
  579.33°C (rough estimate)
• 密度：
  1.4157 (rough estimate)
• 溶解度：
  在水中的溶解度~3.75 mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  -1.53
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 危险品标志：
  Xn,N
• 危险类别码：
  R22,R50

制备方法与用途

类别：有毒物质
毒性分级：高毒
急性毒性：口服-大鼠 LD50: 300 毫克/公斤；口服-小鼠 LD50: 380 毫克/公斤
可燃性危险特性：热分解排出有毒氮氧化物、氯化物及氨烟雾
储运特性：库房应低温通风干燥，与食品原料分开存放
灭火剂：水、二氧化碳、泡沫、干粉

文献信息

• Substituted indoles as alpha-1 agonists
  申请人：——

  公开号：US20040224973A1

  公开（公告）日：2004-11-11

  This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: 1 wherein m, A, X, Y, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

  这项发明涉及α-1受体激动剂化合物，优选为α-1A/L受体激动剂，其由以下式I表示： 1 其中m，A，X，Y，R 1 ，R 2 ，R 3 ，R 4 和R 5 如规范中所定义；或其各个异构体，消旋或非消旋异构体混合物，或其药用盐或溶剂化合物。该发明还涉及含有这种化合物的药物组合物，以及它们作为治疗剂的使用方法和其制备方法。
• Method for treating resistant hypertension
  申请人：Gerber Michael J.

  公开号：US20070196510A1

  公开（公告）日：2007-08-23

  A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

  提供了一种降低临床诊断为顽固性高血压患者血压的方法。该方法包括将达卢生坦作为辅助药物与基础抗高血压治疗方案联合给药，该基础方案包括至少一种利尿剂和至少两种抗高血压药物，这些药物选自至少两类：(a) ACE抑制剂和血管紧张素II受体阻滞剂，(b) β-肾上腺素能受体阻滞剂，以及(c) 钙通道阻滞剂。达卢生坦以有效剂量和频率口服给药，与基础治疗方案结合，能够使选自谷值坐位收缩压、谷值坐位舒张压、24小时动态收缩压、24小时动态舒张压、日间最高收缩压和日间最高舒张压的一个或多个血压参数至少降低约3 mmHg。
• Certain thiol inhibitors of endothelin-converting enzyme
  申请人：——

  公开号：US20020082218A1

  公开（公告）日：2002-06-27

  Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula 1 wherein the variables have the meanings as defined hereinbefore.

  披露的内皮素转化酶抑制剂是具有以下公式的化合物，其中变量的含义如前文所定义。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• THERAPY FOR COMPLICATIONS OF DIABETES
  申请人：Roden Robert L.

  公开号：US20090054473A1

  公开（公告）日：2009-02-26

  A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ET A ) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ET A receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ET A receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ET A receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ET A receptor antagonist.

  一种增强患有糖尿病肾病和/或代谢综合征的人类受试者的血糖控制和/或胰岛素敏感性的方法，包括向该受试者施用一种选择性内皮素A（ETA）受体拮抗剂，其剂量足以增强血糖控制和/或胰岛素敏感性。一种治疗老年糖尿病人类受试者中复合共病的方法，包括向该受试者施用一种选择性ETA受体拮抗剂，与至少一种其他药物联合或作为辅助治疗，该其他药物（i）不是选择性ETA受体拮抗剂，且（ii）在治疗糖尿病和/或至少一种除高血压外的上述共病中有效。适用于此类方法的治疗组合包括一种选择性ETA受体拮抗剂和至少一种非选择性ETA受体拮抗剂的抗糖尿病、抗肥胖或抗血脂异常药物。