Pobilukast edamine | 137232-03-2

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: Pobilukast edamine
• 英文别名: (2S,3R)-3-(2-carboxyethylsulfanyl)-2-hydroxy-3-[2-(8-phenyloctyl)phenyl]propanoic acid;ethane-1,2-diamine;hydrate
• CAS: 137232-03-2
• 化学式: C28H44N2O6S
• 分子量: 536.7
• InChiKey: DIUCVZXIHDZZBV-LBDKHHEASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.59
• 重原子数：
  37
• 可旋转键数：
  17
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  173
• 氢给体数：
  6
• 氢受体数：
  9

文献信息

• [EN] PRODRUG COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] COMPOSITIONS DE PROMÉDICAMENT ET PROCÉDÉS DE TRAITEMENT
  申请人：AQUESTIVE THERAPEUTICS INC

  公开号：WO2021087359A1

  公开（公告）日：2021-05-06

  Pharmaceutical compositions include a prodrug of epinephrine are described.

  药物组合物包括表述的肾上腺素前药。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• [EN] DUAL FUNCTIONING IONIC LIQUIDS AND SALTS THEREOF<br/>[FR] LIQUIDES IONIQUES À DOUBLE FONCTION ET SELS DE CEUX-CI
  申请人：UNIV ALABAMA

  公开号：WO2010078300A1

  公开（公告）日：2010-07-08

  Disclosed herein are ionic liquid compositions comprising active pharmaceutical, biological, and nutritional compounds, and methods of use. Further disclosed are compositions of matter including liquid ion pairs alone or in solution and their use; compositions of ionic liquids that are 'solvated,' for example, 'hydrated' and their uses.

  本文揭示了包括活性药物、生物学和营养化合物的离子液体组合物，以及其使用方法。进一步揭示了包括液态离子对的物质组合物，单独或溶解后使用；以及离子液体的“溶剂化”组合物，例如“水合”的组合物及其用途。
• Calcium channel blockers
  申请人：Massachusetts College of Pharmacy

  公开号：US20020115655A1

  公开（公告）日：2002-08-22

  The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel activity, such as, cardiovascular diseases, for example hypertension, congestive heart failure, arrhythmia and angina.

  这项发明涉及识别一类阻断钙通道的化合物家族。这些化合物可以制成药物载体并用于治疗相关于钙通道活性的疾病，例如心血管疾病，如高血压、心力衰竭、心律失常和心绞痛。
• PROKINETIC AGENTS FOR TREATING GASTRIC HYPOMOTILITY AND RELATED DISORDERS
  申请人：——

  公开号：US20030176421A1

  公开（公告）日：2003-09-18

  Stasis is treated or prevented in all or any part or parts of the stomach of a patient, especially a human patient, in need of such treatment, where said stasis results from hypomotility in the stomach, particularly gastric hypomotility with delayed emptying of the liquid and/or solid contents of the stomach. Gastric or gastrointestinal disorders are also treated which are characterized by one or more symptoms selected from pain, nausea, vomiting, heartburn, postprandial discomfort, indigestion and gastroesophageal reflux. Such treatment or prevention is achieved by administering to the patient a therapeutically effective amount of an inhibitor of phosphodiesterase-4 (PDE4), including isozyme subtypes thereof, sufficient to treat or prevent such hypomotility or gastric or gastrointestinal disorder in said patient. The PDE4 inhibitor comprises a compound of Formula (IA) or (IB): 1 where in a preferred embodiment, R is cyclopentyl or cyclohexyl; R 1 is (C 1 -C 2 ) alkyl; one of R 2 a and R 2 b is hydrogen and the other is a substituent of partial Formula (1.0.0) above, where the dashed line represents a single bond, m is 0, R 113 and R 114 are in a cis relationship to each other, R 113 is cyano, R 115 is hydrogen, and R 114 is carboxy, —CH 2 OH, or —CH 2 C(═O)NH 2 . Pharmaceutical compositions are also described which are useful for carrying out the above-mentioned methods of treatment and prevention, and which are also useful in the treatment of a gastric or gastrointestinal disorder in a patient which comprises with respect to said patient, (i) a sign or concomitant of diabetic neuropathy, anorexia nervosa, achlorhydria, gastrointestinal surgery, post-surgical recovery in the period of emergence from general anesthesia; or the administration of morphine and morphine-like opioids; (ii) a secondary aspect of a primary disease or disorder in said patient which is organic, wherein said disease or disorder involves particularly a gastroenteric or gastroesophageal organ or tissue, or an organ or tissue of the central nervous system of said patient; or (iii) an adverse side effect of a different therapeutic agent administered to said patient in the course of treating another unrelated disease or disorder in said patient.

  本发明涉及一种治疗或预防患者（尤其是人类患者）胃部任何部位或全部的停滞，其中该停滞是由于胃肠道低动力性，尤其是胃肠道低动力性导致胃液和/或固体食物的排空延迟。同时，本发明还涉及治疗或预防胃或胃肠道疾病，这些疾病的特征是疼痛、恶心、呕吐、胃灼热、餐后不适、消化不良和胃食管反流中的一个或多个症状。通过向患者施用磷酸二酯酶-4（PDE4）的抑制剂，包括其同工酶亚型，治疗或预防该患者的低动力性或胃或胃肠道疾病所需的治疗剂量就可以实现。所述PDE4抑制剂包括化合物公式（IA）或（IB）的化合物：其中在一种优选实施例中，R为环戊基或环己基；R1为（C1-C2）烷基；R2a和R2b中的一个是氢，另一个是上述部分式（1.0.0）的取代基，其中虚线表示单键，m为0，R113和R114在相互的顺式关系下，R113为氰基，R115为氢，R114为羧基，-CH2OH或-CH2C（═ O）NH2。本发明还描述了药物组合物，用于执行上述治疗和预防方法，并且还用于治疗患者的胃或胃肠道疾病，该患者具有以下特征：（i）糖尿病神经病变、厌食症、无酸胃、胃肠道手术、全身麻醉恢复期间的术后恢复；或吗啡和吗啡样的阿片类药物的使用的标志或伴随症状；（ii）该患者的原发性疾病或疾病的次要方面是器质性疾病或疾病，其中该疾病或疾病特别涉及该患者的胃肠道或胃食管器官或组织，或该患者的中枢神经系统的器官或组织；或（iii）在治疗该患者的另一种无关疾病或疾病的过程中向该患者施用的不同治疗剂的不良副作用。