美沙洛尔 | 56290-94-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 美沙洛尔
• 中文别名: 柳椒心定
• 英文名称: medroxalol
• 英文别名: 5-[2-[4-(1,3-benzodioxol-5-yl)butan-2-ylamino]-1-hydroxyethyl]-2-hydroxybenzamide
• CAS: 56290-94-9
• 化学式: C₂₀H₂₄N₂O₅
• 分子量: 372.421
• InChiKey: MPQWSYJGFLADEW-UHFFFAOYSA-N

物化性质

• 溶解度：
  soluble in No data available

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  114
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  methyl 5-<2-<<3-(1,3-benzodioxol-5-yl)-1-methylpropyl>amino>-1-hydroxyethyl>-2-hydroxybenzoate 在 氨 、 sodium methylate 作用下， 以 甲醇 为溶剂， 反应 72.0h， 以82%的产率得到美沙洛尔
  参考文献：
  名称：

  Salicylamide derivatives related to medroxalol with .alpha.- and .beta.-adrenergic antagonist and antihypertensive activity

  摘要：

  Analogues of medroxalol (1) were prepared in which the carboxamide function, the phenolic hydroxy group, and the aralkylamine side chain were modified. N-alkyl-substituted amide analogues of 1 showed diminishing beta-blocking activity with increasing steric bulk of the alkyl group. This allowed the conclusion that deactivation of the phenolic hydroxy group of 1 by the carbonyl group of the amide function is responsible for the beta-adrenergic antagonistic properties of 1. This conclusion was strengthened by the finding that the phenolic O-methyl analogue 5-[2-[[3-(1,3-benzodioxol-5-yl)-1-methylpropyl]amino]-1hydroxyethyl]-2-methoxybenzamide (13) was found to have enhanced beta-adrenergic blocking activity. The finding that 13 also had decreased alpha-blocking activity compared to 1 indicated that the phenolic hydroxy group of 1 enhances alpha-adrenergic antagonism. The finding that 1 and 13 showed such a large difference in relative alpha- to beta-blocking potency while exhibiting approximately equal antihypertensive activity in spontaneously hypertensive rats was surprising. In indicated that pharmacologic properties other than alpha- and beta-adrenergic blockade may contribute to the antihypertensive activity of medroxalol. One of the analogues in which the aralkylamine side chain of 1 was replaced by a fragment of a known alpha-adrenergic receptor blocker, 2-hydroxy-5-[1-hydroxy-2-[4-(2-methylphenyl)-1-piperazinyl]ethyl]benzamide (22), showed an interesting pharmacologic profile of potential therapeutic usefulness.

  DOI：

  10.1021/jm00135a017

文献信息

• Synthesis of triethylenetetramines
  申请人：Jonas Marco

  公开号：US20060041170A1

  公开（公告）日：2006-02-23

  Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.

  合成三乙烯四胺及其盐的方法和中间体，以及新型三乙烯四胺盐及其晶体结构，以及高纯度的三乙烯四胺盐。
• Method for treating fibrotic diseases or other indications IC
  申请人：Alteon, Inc.

  公开号：US20020068729A1

  公开（公告）日：2002-06-06

  Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I: 1

  提供了一种处理、改善或预防动物包括人类发明的指示的方法，包括给予公式I的化合物的有效量：1
• Method for treating fibrotic diseases or other indications with imidazolium agents
  申请人：Alteon, Inc.

  公开号：US20030176426A1

  公开（公告）日：2003-09-18

  Provided is a method of treating or ameliorating an indication of the invention in an animal, including a human, by administering an effective amount of a compound of the formula I: 1 wherein R 1 , R 2 , M, X and Z are as described supra. Also provided are certain imidazolium compounds and pharmaceutical compositions containing the imidazolium compounds.

  提供了一种治疗或改善动物（包括人类）发明的征兆的方法，通过给予公式I的有效量的化合物： 1 其中R 1 ，R 2 ，M，X和Z如上所述。还提供了一些咪唑啉化合物和包含咪唑啉化合物的药物组合物。
• [EN] CARBONATE PRODRUGS AND METHODS OF USING THE SAME<br/>[FR] PROMÉDICAMENTS CARBONATÉS ET LEURS MÉTHODES D'UTILISATION
  申请人：NEUROGESX INC

  公开号：WO2009143297A1

  公开（公告）日：2009-11-26

  The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

  本发明提供了碳酸盐前药，其包括连接到母药基团的羟基或羧基上的碳酸磷酸酐前药基团。这些前药可能比母药具有改进的物理化学性质。还提供了使用碳酸盐前药治疗对母药具有响应的疾病或症状的方法，以及配套工具和单剂量。
• [EN] PRODRUG COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] COMPOSITIONS DE PROMÉDICAMENT ET PROCÉDÉS DE TRAITEMENT
  申请人：AQUESTIVE THERAPEUTICS INC

  公开号：WO2021087359A1

  公开（公告）日：2021-05-06

  Pharmaceutical compositions include a prodrug of epinephrine are described.

  药物组合物包括表述的肾上腺素前药。