varenicline salicylate | 2093452-45-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: varenicline salicylate
• 英文别名: 2-hydroxybenzoic acid;(1S,12R)-5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene
• CAS: 2093452-45-8
• 化学式: C₇H₆O₃*C₁₃H₁₃N₃
• 分子量: 349.389
• InChiKey: WXQZSRYAESPDCB-UFIFRZAQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.89
• 重原子数：
  26
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  95.3
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  varenicline 、 水杨酸 以 甲醇 为溶剂， 反应 1.0h， 以98.8%的产率得到varenicline salicylate
  参考文献：
  名称：

  KR101724301

  摘要：

  公开号：

文献信息

• TASTE-MASKED AND ORALLY ADMINISTERED PHARMACEUTICAL PREPARATION CONTAINING VARENICLINE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
  申请人：CTC Bio, Inc.

  公开号：EP3400964A1

  公开（公告）日：2018-11-14

  The present disclosure relates to a pharmaceutical preparation having varenicline or a pharmaceutically acceptable salt thereof as an active ingredient. More particularly, it relates to an orally administered pharmaceutical preparation which allows limited use of a sweetening agent or a flavoring agent by effectively masking the unique taste of varenicline, particularly bitterness, which is a bitter and burning taste, and ensures convenience in taking the pharmaceutical preparation by being orally administrable without irritation, while containing a pharmaceutically effective amount of varenicline or a pharmaceutically acceptable salt thereof, and a method for preparing the same.

  本公开涉及一种以伐尼克兰或其药学上可接受的盐作为活性成分的药物制剂。更具体地说，它涉及一种口服药物制剂，该制剂通过有效掩盖伐伦克林的独特味道，特别是苦味（一种苦味和灼烧味），允许有限地使用甜味剂或调味剂，并通过可口服而无刺激性确保服用该药物制剂的便利性，同时含有药学上有效量的伐伦克林或其药学上可接受的盐，以及制备该药物制剂的方法。
• Preparation, comprising inclusion complex of varenicline or pharmaceutically acceptable salt thereof, for oral administration
  申请人：CTC BIO, INC.

  公开号：US11266658B2

  公开（公告）日：2022-03-08

  The present disclosure relates to an orally administered pharmaceutical formulation containing an inclusion complex formed as varenicline or a pharmaceutically acceptable salt thereof is included in cyclodextrin. The pharmaceutical formulation can improve convenience of medication by effectively masking the bitter taste of the drug and the irritation during swallowing, can provide the oxidation stability of varenicline and can improve the solubility of the drug.

  本公开涉及一种口服药物制剂，其中含有环糊精中包含的伐伦克林或其药学上可接受的盐形成的包合物。该药物制剂可以有效地掩盖药物的苦味和吞咽时的刺激性，从而提高用药的便利性，可以提供伐尼克兰的氧化稳定性，并可以提高药物的溶解度。
• PREPARATION, COMPRISING INCLUSION COMPLEX OF VARENICLINE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, FOR ORAL ADMINISTRATION
  申请人：CTC BIO, INC.

  公开号：US20200061078A1

  公开（公告）日：2020-02-27

  The present disclosure relates to an orally administered pharmaceutical formulation containing an inclusion complex formed as varenicline or a pharmaceutically acceptable salt thereof is included in cyclodextrin. The pharmaceutical formulation can improve convenience of medication by effectively masking the bitter taste of the drug and the irritation during swallowing, can provide the oxidation stability of varenicline and can improve the solubility of the drug.