4-[(2-Amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol;hydron;chloride | 1146648-86-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-[(2-Amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol;hydron;chloride
• CAS: 1146648-86-3
• 化学式: C13H19Br2ClN2O
• 分子量: 414.56
• InChiKey: QNVKOSLOVOTXKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.61
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  58.3
• 氢给体数：
  4
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  trans-4-[(2-Amino-3,5-dibromobenzyl)amino]cyclohexanol 、 4-[(2-Amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol;hydron;chloride 、 乳糖 、 、 、 原硅酸 、 Stearic acid magnesium salt 以 水 为溶剂， 生成 左羟丙哌嗪
  参考文献：
  名称：

  COMPOSITE FORMULATION COMPRISING MULTI-UNIT SPHEROIDAL TABLET (MUST) ENCAPSULATED IN HARD CAPSULE AND METHOD FOR PREPARING SAME

  摘要：

  提供了一种复合配方，其中包括封装在硬胶囊中的多单元球形片剂（MUSTs）和一种制备方法。创新的硬胶囊复合配方可以有效地在胶囊的有限空间中充填MUSTs，这使得可以在相对较小的胶囊中充填高剂量的不同药物活性成分，从而增加生产力并使其易于给患者使用。此外，由于胶囊中含有的药物活性成分是相互分离的，因此胶囊具有良好的溶解速度；因此，成分的溶解速度彼此之间的影响较小。还可以通过复合配方的稳定性最大化药物活性成分的治疗效果。

  公开号：

  US20150098992A1

文献信息

• Auris Formulations for Treating Otic Diseases and Conditions
  申请人：Otonomy, Inc.

  公开号：US20160243028A1

  公开（公告）日：2016-08-25

  Disclosed herein are compositions and methods for the treatment of otic disorders with immunomodulating agents and auris pressure modulators. In these methods, the auris compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of the immunomodulating and/or auris pressure modulating compositions and formulations onto the auris media and/or auris interna target areas, or via perfusion into the auris media and/or auris interna structures.

  本文公开了使用免疫调节剂和耳压调节剂治疗耳部疾病的组合物和方法。在这些方法中，通过将免疫调节和/或耳压调节组合物和配方直接应用于耳媒介和/或耳内靶区，或通过向耳媒介和/或耳内结构灌注，局部给予患有耳部疾病的个体耳部组合物和配方。
• ANTI-INFLUENZA DRUGS
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP1437134A1

  公开（公告）日：2004-07-14

  An anti-influenzal agent comprises, as an effective component, ambroxol, bromhexin or a pharmaceutically acceptable salt thereof. This agent is characterized in that it has an anti-influenzal effect through the promotion of the secretion of biological factors, which possess influenza virus-proliferation-inhibitory effect and are included in the fluid secreted in the respiratory tract. It is also characterized in that it can inhibit the influenza virus-proliferation in the respiratory tract through promoting the secretion of substances capable of inhibiting proteases in the respiratory tract, which induce the influenza virus infection, that it can inhibit the influenza virus-proliferation in the respiratory tract through promoting the secretion of mucosal immune substances or IgA and IgG and that it can inhibit any release of inflammatory cytokines in the respiratory tract. The present invention also relates to an agent for treating or preventing influenza virus-infectious diseases.

  一种抗流感剂包括作为有效成分的氨溴索、溴己新或其药学上可接受的盐。这种制剂的特点是，它通过促进呼吸道分泌液中含有的具有抑制流感病毒增殖作用的生物因子的分泌来发挥抗流感作用。本发明的另一个特点是，它可以通过促进呼吸道中能够抑制蛋白酶的物质的分泌来抑制流感病毒在呼吸道中的扩散，这些蛋白酶会诱发流感病毒感染；它可以通过促进粘膜免疫物质或 IgA 和 IgG 的分泌来抑制流感病毒在呼吸道中的扩散；它还可以抑制呼吸道中任何炎症细胞因子的释放。本发明还涉及一种用于治疗或预防流感病毒感染性疾病的制剂。
• AMBROXOL FOR DNA DAMAGE REPAIR DISEASE THERAPIES
  申请人：Universitat Autònoma de Barcelona

  公开号：EP3566700A1

  公开（公告）日：2019-11-13

  The present invention provides Ambroxol or a pharmaceutically salt thereof for use in the treatment and/or prevention of a disease caused by a defect in DNA damage repair mechanisms. The treatment of the invention can substantially prevent, among others, chromosome instability and cell cycle defects in cells with defective DNA damage repair mechanism. In vivo, the treatment of the invention improves the health and lifespan of subjects suffering from these diseases.

  本发明提供了氨溴索或其药用盐，用于治疗和/或预防由DNA损伤修复机制缺陷引起的疾病。本发明的治疗方法可以从根本上防止 DNA 损伤修复机制缺陷细胞的染色体不稳定性和细胞周期缺陷。在体内，本发明的治疗方法可以改善患有这些疾病的受试者的健康和寿命。
• Formulations for the treatment of ocular surface diseases and related methods
  申请人：Wang Mingwu

  公开号：US10265280B2

  公开（公告）日：2019-04-23

  Formulations for treating ocular surface diseases, such as dry eye disease, and related methods are disclosed. The formulations include ambroxol or a chemical derivative thereof (for example, ambroxol hydrochloride) dispersed in a carrier and may optionally include a biocompatible polymer to provide extended release properties.

  本发明公开了用于治疗干眼症等眼表疾病的制剂及相关方法。这些制剂包括分散在载体中的氨溴索或其化学衍生物（例如盐酸氨溴索），还可选择包括生物相容性聚合物，以提供缓释特性。
• Isotope enhanced ambroxol for long lasting autophagy induction
  申请人：STC.UNM

  公开号：US10583099B2

  公开（公告）日：2020-03-10

  The present invention is directed to 2H isotope enhanced ambroxol (“isotope enhanced ambroxol”) and its use in the treatment of autophagy infections, especially mycobacterial and other infections, disease states and/or conditions of the lung, such as tuberculosis, especially including drug resistant and multiple drug resistant tuberculosis. Pharmaceutical compositions comprising isotope enhanced ambroxol, alone or in combination with an additional bioactive agent, especially rifamycin antibiotics, including an additional autophagy modulator (an agent which is active to promote or inhibit autophagy) are also disclosed. These compositions are useful against an autophagy mediated disease state and/or condition), especially an autophagy mediated disease state and/or condition which occurs in the lungs.

  本发明涉及2H同位素增强型氨溴索（"同位素增强型氨溴索"）及其在治疗自噬感染，特别是分枝杆菌和其他感染、疾病状态和/或肺部状况，如结核病，尤其包括耐药性和多重耐药性结核病中的应用。此外，还公开了包含同位素增强型氨溴索的药物组合物，该药物组合物可单独使用，也可与其他生物活性制剂（尤其是利福霉素抗生素）组合使用，包括其他自噬调节剂（具有促进或抑制自噬活性的制剂）。这些组合物可用于防治自噬介导的疾病状态和/或病症，尤其是发生在肺部的自噬介导的疾病状态和/或病症。

表征谱图