茚唑啉 | 40507-78-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 中文名称: 茚唑啉
• 中文别名: (4,5-二氢-1H-咪唑-2-基)-4-茚胺
• 英文名称: indanazoline
• 英文别名: Indanazolin；(4,5-dihydro-1H-imidazol-2-yl)-indan-4-yl-amine；2-(Indanyl-4'-amino)-Δ²-imidazolin；2-(4-Indanylamino)-2-imidazolin；N-(2,3-dihydro-1H-inden-4-yl)-4,5-dihydro-1H-imidazol-2-amine
• CAS: 40507-78-6
• 化学式: C₁₂H₁₅N₃
• 分子量: 201.271
• InChiKey: KUCWWEPJRBANHL-UHFFFAOYSA-N

物化性质

• 熔点：
  109-113°
• 沸点：
  329.2±52.0 °C(Predicted)
• 密度：
  1.30±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于氯仿（少许）、DMSO（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  36.4
• 氢给体数：
  2
• 氢受体数：
  1

安全信息

• 海关编码：
  2933290090
• 储存条件：
  -20°C，密闭保存，并保持干燥。

制备方法与用途

生物活性

Indanazoline（Farate的一水盐酸盐活性物质）具有显著的血管收缩作用。

体内研究

在动物实验中，新研发的咪唑啉衍生物Indanazoline（作为Farial的一水盐酸盐活性物质）在外用或静脉注射后表现出明显的血管收缩作用。

反应信息

• 作为产物：
  描述：

  4-氨基茚满 、 2-(4,5-dihydro-1-methyl carboxylate-imidazole) tert-butyl thioglycolate 在 溶剂黄146 作用下， 以 甲醇 为溶剂， 以1.03 g的产率得到茚唑啉
  参考文献：
  名称：

  一种合成2-氨基咪唑啉类化合物的方法

  摘要：

  本发明公开了一种合成2‑氨基咪唑啉类化合物的方法，该方法以廉价的溴乙酸酯类化合物和乙烯硫脲为原料，通过取代反应合成硫醚，然后氨解硫醚制备得到2‑氨基咪唑啉类化合物或相关的药物分子，并伴生无臭味具有附加值的巯基乙酸酯。该方法的优势在于：1)所用原料廉价易得、毒性小；2)所得中间体硫醚为固体，易于纯化分离；3)产物为固体，易与伴生的巯基乙酸酯分离，所得两种产物产率高、纯度高。这些显著的优势使本方法具有工艺简单、反应条件温和、成本低、绿色环保以及产率高等特点，使该发明具有良好的工业应用前景。

  公开号：

  CN115477613A

文献信息

• Hydroxylated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014733A1

  公开（公告）日：2007-01-18

  Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外，羟基化奈必洛尔代谢物，包括但不限于4-羟基-6,6'-二氟代-、4-羟基-5-苯酚-6,6'-二氟代-和4-羟基-8-苯并-6,6'-二氟代-，在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物，以及可药用的盐。此外，本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用，或作为单一治疗。
• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• Glucuronidated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014734A1

  公开（公告）日：2007-01-18

  This invention provides glucuronidated nebivolol metabolites and pharmaceutical compositions of glucuronidated nebivolol metabolites for treatment of cardiovascular diseases. In addition, this invention also provides compositions comprising nebivolol and/or at least one glucuronidated metabolite of nebivolol and/or at least one other active compound in a pharmaceutically acceptable carrier. This invention also provides methods of treating and/or preventing vascular diseases, by administering at least one glucuronidated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one glucuronidated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  这项发明提供了葡萄糖醛酸化的尼布ivolol代谢物以及用于治疗心血管疾病的葡萄糖醛酸化的尼布ivolol代谢物的制药组合物。此外，该发明还提供了包含尼布ivolol和/或至少一种尼布ivolol的葡萄糖醛酸化代谢物和/或至少一种其他活性化合物的药用可接受载体的组合物。该发明还提供了通过向受影响血管疾病的靶位点投与至少一种能释放治疗有效量一氧化氮的尼布ivolol的葡萄糖醛酸化代谢物来治疗和/或预防血管疾病的方法。此外，该发明旨在通过投与至少一种尼布ivolol的葡萄糖醛酸化代谢物来治疗和/或预防偏头痛。该发明还可与代谢综合征紊乱的单一治疗或联合治疗一起使用。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Use of combinations comprising non-sedating antihistamines and alpha-adrenergic drugs for the topical treatment of rhinitis/conjunctivitis and cold, cold-like and/or flu symptoms
  申请人：ASTA Medica Aktiengesellschaft

  公开号：EP0903151A1

  公开（公告）日：1999-03-24

  Pharmaceutical combination, applicable topically, containing a non-sedating antihistamine in combination with an α-adrenergic agonist and optionally conventional physiologically acceptable carriers, diluting agents and auxiliaries substances for the prophylaxis and treatment of allergic and/or vasomotoric rhinitis, conjunctivitis, cold, cold-like and/ or flu symptoms are claimed.

  声明一种适用于局部使用的药物组合，包含非镇静型抗组胺剂与α-肾上腺素受体激动剂的组合，以及可选的传统生理上可接受的载体、稀释剂和辅助物质，用于预防和治疗过敏性和/或血管运动性鼻炎、结膜炎、感冒、类似感冒和/或流感症状。