Aggrenox

• 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: Aggrenox
• 英文别名: 2-acetyloxybenzoic acid;2-[[2-[bis(2-hydroxyethyl)amino]-4,8-di(piperidin-1-yl)pyrimido[5,4-d]pyrimidin-6-yl]-(2-hydroxyethyl)amino]ethanol
• 化学式: C33H48N8O8
• 分子量: 684.8
• InChiKey: NOHUXXDTQJPXSB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.29
• 重原子数：
  49
• 可旋转键数：
  15
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  209
• 氢给体数：
  5
• 氢受体数：
  16

文献信息

• Methods and compositions for treating conditions associated with an abnormal inflammatory responses
  申请人：First Wave Bio, Inc.

  公开号：US10292951B2

  公开（公告）日：2019-05-21

  This disclosure features chemical entities (e.g., a compound exhibiting activity as a mitochondrial uncoupling agent or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as niclosamide or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as a niclosamide analog, or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof) that are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

  本公开的化学实体（例如，具有线粒体解偶联剂活性的化合物或其药学上可接受的盐和/或水合物和/或共晶体；例如，化合物，如烟酰胺或其药学上可接受的盐和/或水合物和/或共晶体；例如、化合物，如尼可刹米类似物，或其药学上可接受的盐和/或水合物和/或共晶体），这些化合物可用于治疗受试者（如人类）中以异常炎症反应（如炎症性肠病）为特征的病理学的一种或多种症状。本公开内容还包括组合物以及使用和制造组合物的其他方法。
• Methods and compositions for treating conditions associated with an abnormal inflammatory response
  申请人：First Wave Bio, Inc.

  公开号：US10772854B2

  公开（公告）日：2020-09-15

  This disclosure features chemical entities (e.g., a compound exhibiting activity as a mitochondrial uncoupling agent or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as niclosamide or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as a niclosamide analog, or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof) that are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

  本公开的化学实体（例如，具有线粒体解偶联剂活性的化合物或其药学上可接受的盐和/或水合物和/或共晶体；例如，化合物，如烟酰胺或其药学上可接受的盐和/或水合物和/或共晶体；例如、化合物，如尼可刹米类似物，或其药学上可接受的盐和/或水合物和/或共晶体），这些化合物可用于治疗受试者（如人类）中以异常炎症反应（如炎症性肠病）为特征的病理学的一种或多种症状。本公开内容还包括组合物以及使用和制造组合物的其他方法。
• Methods of treatment
  申请人：First Wave Bio, Inc.

  公开号：US10980756B1

  公开（公告）日：2021-04-20

  This disclosure features compounds and compositions that are useful in methods of treating coronavirus infections (e.g., useful in methods of treating COVID-19) in a subject in need thereof. The methods include administering to the subject niclosamide compounds (or pharmaceutically acceptable salts and/or co-crystals thereof, e.g., niclosamide). In some embodiments, the niclosamide compounds have one or more properties that include, but are not limited to: a particular purity (e.g., a chemical purity of greater than about 99.0%) or a particular particle size (e.g., a particular particle size distribution and/or a particular particle size range and/or a specific surface area range). In an aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for respiratory administration (e.g., via inhalation and/or intranasally). In another aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for administration to the GI tract (e.g., orally or rectally such as via enema)).

  本公开的化合物和组合物适用于治疗有需要的受试者的冠状病毒感染的方法（例如，适用于治疗COVID-19的方法）。这些方法包括向受试者施用烟酰胺化合物（或其药学上可接受的盐和/或共晶体，例如烟酰胺）。在一些实施方案中，烟酰胺化合物具有一种或多种特性，包括但不限于：特定的纯度（例如化学纯度大于约99.0%）或特定的粒度（例如特定的粒度分布和/或特定的粒度范围和/或比表面积范围）。在一个方面，本文所述的烟酰胺化合物（如烟酰胺）可以构成组合物、剂型（如单位剂型）等的一部分，适合呼吸道给药（如通过吸入和/或鼻内给药）。在另一方面，本文所述的烟酰胺化合物（如烟酰胺）可构成组合物、剂型（如单位剂型）等的一部分，适合于消化道给药（如口服或直肠给药，如通过灌肠））。
• Solid matrix therapeutic compositions
  申请人：ImaRx Therapeutics, Inc.

  公开号：US20010018072A1

  公开（公告）日：2001-08-30

  The present invention is directed to a solid porous matrix comprising a surfactant in combination with a bioactive agent. The solid porous matrix may be prepared by combining a surfactant and a therapeutic, together with a solvent, to form an emulsion containing random aggregates of the surfactant and the therapeutic, and processing the emulsion by controlled drying, or controlled agitation and controlled drying to form the solid porous matrix.

  本发明涉及一种包含表面活性剂和生物活性剂的固体多孔基质。固体多孔基质的制备方法是：将表面活性剂和治疗剂与溶剂结合，形成含有表面活性剂和治疗剂无规聚集体的乳液，然后通过控制干燥或控制搅拌和控制干燥处理乳液，形成固体多孔基质。
• SOLID POROUS MATRICES AND METHODS OF MAKING AND USING THE SAME
  申请人：——

  公开号：US20020039594A1

  公开（公告）日：2002-04-04

  The present invention is directed to a solid porous matrix comprising a solvent and a surfactant in combination with a bioactive agent. The solvent and the surfactant may, if desired, form vesicles, an agglomeration of which comprises the matrix. The composition optionally comprises a gas or a gaseous precursor. The emulsion may be dried, and subsequently reconstituted in an aqueous or organic solution. The present invention is also directed to a method of preparing a solid porous matrix comprising combining a solvent, a surfactant, and a therapeutic to form an emulsion; and processing the emulsion by controlled drying, or controlled agitation and controlled drying to form a solid porous matrix. The resulting solid porous matrix may also comprise a gas or gaseous precursor and be added to a resuspending medium. A method for the controlled delivery of a targeted therapeutic to a region of a patient is another embodiment of the present invention. The method comprises administering to the patient a composition having a solid porous matrix comprising a solvent, a surfactant, a therapeutic, and a gas or gaseous precursor, monitoring the composition using energy to determine the presence of the composition in the region; and releasing the therapeutic from the composition in the region using energy.

  本发明涉及一种固体多孔基质，由溶剂和表面活性剂以及生物活性剂组成。如果需要，溶剂和表面活性剂可以形成囊泡，囊泡的聚集体构成基质。组合物可选择包含气体或气态前体。乳液可以干燥，然后在水溶液或有机溶液中重组。 本发明还涉及一种制备固体多孔基质的方法，包括将溶剂、表面活性剂和治疗剂混合形成乳液；并通过控制干燥或控制搅拌和控制干燥处理乳液以形成固体多孔基质。所形成的固体多孔基质还可包含气体或气态前体，并加入到重悬介质中。 本发明的另一个实施方案是一种将靶向治疗药物有控制地输送到患者区域的方法。该方法包括向患者施用具有固体多孔基质的组合物，该固体多孔基质包含溶剂、表面活性剂、治疗剂和气体或气态前体；使用能量监测组合物，以确定该区域存在组合物；以及使用能量从该区域的组合物中释放治疗剂。