阿扎那托 | 37855-92-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 中文名称: 阿扎那托
• 中文别名: 阿札那托
• 英文名称: 5-(1-methyl-piperidin-4-ylidene)-5H-chromeno[2,3-b]pyridine
• 英文别名: 5-(N-Methyl-4-piperyliden)-5H-<1>benzopyrano<2,3-b>pyridin；5-(N-Methyl-4-piperyliden)-5H-[1]benzopyrano[2,3-b]pyridin；azanator；5-(1-methylpiperidin-4-ylidene)chromeno[2,3-b]pyridine
• CAS: 37855-92-8
• 化学式: C₁₈H₁₈N₂O
• 分子量: 278.354
• InChiKey: ALIOEEFZPKWPAV-UHFFFAOYSA-N

物化性质

• 熔点：
  125-127 °C
• 沸点：
  432.4±45.0 °C(Predicted)
• 密度：
  1.206±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  25.4
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  阿扎那托 以46%的产率得到
  参考文献：
  名称：

  VILLANI F. J.; MANN T. A.; WEFER E. A.; HANNON J.; LARCA L. L.; LANDON M.+, J. MED. CHEM. , 1975, 18, NO 1, 1-8

  摘要：

  DOI：
• 作为产物：
  描述：

  5-(1-methyl-piperidin-4-yl)-5H-chromeno[2,3-b]pyridin-5-ol 在 PPA 作用下， 生成 阿扎那托
  参考文献：
  名称：

  Benzopyranopyridine derivatives. 1. Aminoalkyl derivatives of the azaxanthenes as bronchodilating agents

  摘要：

  The preparation of the four isomeric azaxanthones 3 and a number of their aromatic ring substituted derivatives is described. These ketones were converted into the title compounds which were examined for their biological properties. The most interesting compound in this series, the 1-methyl-4-piperidylidene derivative of 1-azaxanthene, shows the profile of an orally effective potent bronchodilating agent as well as a moderate antihistamine. Biological properties of this compound were compared to a number of antihistamines as well as known bronchodilating agents. Structure-activity relationships are also discussed.

  DOI：

  10.1021/jm00235a001

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• DHA-pharmaceutical agent conjugates
  申请人：Luitpold Pharmaceuticals, Inc.

  公开号：EP1466628A1

  公开（公告）日：2004-10-13

  The invention provides conjugates of cis-docosahexaenoic acid and pharmaceutical agents useful in treating noncentral nervous system conditions. Methods for selectively targeting pharmaceutical agents to desired tissues are provided.

  本发明提供了顺式-二十二碳六烯酸的共轭物和用于治疗非中枢神经系统疾病的药剂。本发明还提供了将药剂选择性靶向所需组织的方法。
• 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。
• 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