Amitriptyline ketamine

• 分子结构分类: 有机化合物 - 苯类化合物 - 二苯并环庚烯
• 英文名称: Amitriptyline ketamine
• 英文别名: 2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one;N,N-dimethyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylidene)propan-1-amine
• 化学式: C33H39ClN2O
• 分子量: 515.1
• InChiKey: PREXBGKRNGULGL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.07
• 重原子数：
  37
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  盐酸氯氨酮 、 盐酸阿米替林 、 二乙二醇乙醚 、 生成 Amitriptyline ketamine
  参考文献：
  名称：

  Topical pain relief composition and carrier

  摘要：

  提供了一种乳霜载体，用于局部传递包括镇痛剂在内的药物。该载体包括以下混合物：角鲨烷NF、乳化剂如Tween 80、甘油、棕榈醇NF、单硬脂酸甘油酯、有机明胶磷脂保藏、BHT、尿素USP、EDTA、水、硬脂酸、聚二甲基硅氧烷USP和乙氧基二甘醇试剂。该发明还包括将该载体与左旋卡西酮盐酸盐和阿米替林盐酸盐中的任一种或两种组合，其用作局部应用的镇痛剂。

  公开号：

  US20020028789A1

文献信息

• THERAPEUTIC AGENT FOR PAIN
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1900363A1

  公开（公告）日：2008-03-19

  The present invention relates to an agent for prevention, treatment or inhibition of symptom progression of a pain and/or for control of an analgesic comprising (2R)-2-propyloctanoic acid, a salt thereof or a prodrug thereof, in which an amount per dose is from 1 mg to 5000 mg (preferably from 10 mg to 5000 mg). By administering (2R)-2-propyloctanoic acid, a salt thereof or a prodrug thereof in an amount per dose within the range as described above, a pain, in particular, a neurogenic pain associated with a disease such as cancer pain, postherpetic pain, diabetic pain, HIV-associated neurogenic pain, calculus-induced pain, neuralgia, orofacial pain or hyperalgesia can be remarkably relieved. Moreover, undesirable effects on the living body relating to the use of an analgesic can be relieved.

  本发明涉及一种用于预防、治疗或抑制疼痛症状进展和/或控制镇痛的制剂，该制剂由(2R)-2-丙辛酸、其盐或其原药组成，其中每剂量的用量为1毫克至5000毫克（最好为10毫克至5000毫克）。通过施用(2R)-2-丙辛酸、其盐或其原药，每次剂量在上述范围内，可显著缓解疼痛，特别是与癌症疼痛、带状疱疹后疼痛、糖尿病疼痛、艾滋病相关神经源性疼痛、结石引起的疼痛、神经痛、口面部疼痛或痛觉减退等疾病相关的神经源性疼痛。此外，还能缓解因使用镇痛剂而对人体造成的不良影响。
• Therapeutic agent for treating pain
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP2465499A2

  公开（公告）日：2012-06-20

  The present invention relates to an agent for prevention, treatment or inhibition of symptom progression of a pain and/or for control of an analgesic comprising (2R)-2-propyloctanoic acid, a salt thereof or a prodrug thereof, in which an amount per dose is from 1 mg to 5000 mg (preferably from 10 mg to 5000 mg). By administering (2R)-2-propyloctanoic acid, a salt thereof or a prodrug thereof in an amount per dose within the range as described above, a pain, in particular, a neurogenic pain associated with a disease such as cancer pain, postherpetic pain, diabetic pain, HIV-associated neurogenic pain, calculus-induced pain, neuralgia, orofacial pain or hyperalgesia can be remarkably relieved. Moreover, undesirable effects on the living body relating to the use of an analgesic can be relieved.

  本发明涉及一种用于预防、治疗或抑制疼痛症状进展和/或控制镇痛的制剂，该制剂由(2R)-2-丙辛酸、其盐或其原药组成，其中每剂量的用量为1毫克至5000毫克（最好为10毫克至5000毫克）。通过施用(2R)-2-丙辛酸、其盐或其原药，每次剂量在上述范围内，可显著缓解疼痛，特别是与癌症疼痛、带状疱疹后疼痛、糖尿病疼痛、艾滋病相关神经源性疼痛、结石引起的疼痛、神经痛、口面部疼痛或痛觉减退等疾病相关的神经源性疼痛。此外，还能缓解因使用镇痛剂而对人体造成的不良影响。
• 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））。