托吡哌唑 | 20326-13-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 托吡哌唑
• 英文名称: 3-<2-(N'-m-Tolylpiperazino)-ethyl>-5-methylpyrazol
• 英文别名: 4-m-Tolyl-1-<β-(5-methylpyrazol-3-yl)-ethyl>-piperazin；1-[2-(5-methyl-1(2)H-pyrazol-3-yl)-ethyl]-4-m-tolyl-piperazine；1-(3-methylphenyl)-4-[2-(5-methyl-1H-pyrazol-3-yl)ethyl]piperazine
• CAS: 20326-13-0
• 化学式: C₁₇H₂₄N₄
• 分子量: 284.404
• InChiKey: IYBFBADVQPQHLQ-UHFFFAOYSA-N

物化性质

• 沸点：
  483.0±45.0 °C(Predicted)
• 密度：
  1.114±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-(3-methylphenyl)-4-[2-(5-methyl-1H-pyrazol-3-yl)ethyl]piperazine;dihydrate;trihydrochloride 以69%的产率得到
  参考文献：
  名称：

  KOPPE V.; POESTSCH E.; SCHULTE K., EUR. J. MED. CEM., 1975, 10, NO 2, 154-161,

  摘要：

  DOI：

文献信息

• Substituted pyrazole derivatives
  申请人：KING SAUD UNIVERSITY

  公开号：US10039749B1

  公开（公告）日：2018-08-07

  A substituted pyrazole derivative includes a compound of the formula: or a pharmaceutically acceptable salt thereof.

  一种取代吡唑衍生物包括以下化合物或其药学上可接受的盐：
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using same
  申请人：Pfizer Inc.

  公开号：US10952972B2

  公开（公告）日：2021-03-23

  The present disclosure generally relates to nanoparticles comprising an endo-lysosomal escape agent, a nucleic acid, and a polymer. Other aspects include methods of making and using such nanoparticles.

  本公开一般涉及由内溶酶体逃逸剂、核酸和聚合物组成的纳米颗粒。其他方面包括制造和使用这种纳米颗粒的方法。
• LYOPHILIZATION PROCESS AND PRODUCTS OBTAINED THEREBY
  申请人：Scidose, Llc

  公开号：EP1954244A1

  公开（公告）日：2008-08-13
• CONTROLLED ABSORPTION WATER-SOLUBLE PHARMACEUTICALLY ACTIVE ORGANIC COMPOUND FORMULATION FOR ONCE-DAILY ADMINISTRATION
  申请人：STI Pharma, LLC

  公开号：EP2717860A1

  公开（公告）日：2014-04-16