2-[(2-{(4S)-4-[(1E,3S)-4-(4-fluorophenyl)-3-hydroxybut-1-enyl]-2-oxo-1,3-oxazolidin-3-yl}ethyl)sulfanyl]-1,3-thiazol-4-carboxylic acid | 729611-52-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-[(2-{(4S)-4-[(1E,3S)-4-(4-fluorophenyl)-3-hydroxybut-1-enyl]-2-oxo-1,3-oxazolidin-3-yl}ethyl)sulfanyl]-1,3-thiazol-4-carboxylic acid
• 英文别名: (15α,13E)-9-oxo-15-hydroxy-16-(4-fluorophenyl)-5-(4-carboxythiazol-2-yl)-1,2,3,4,17,18,19,20-octanol-5-thia-8-aza-10-oxaprost-13-ene；2-[2-[(4S)-4-[(E,3S)-4-(4-fluorophenyl)-3-hydroxybut-1-enyl]-2-oxo-1,3-oxazolidin-3-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid
• CAS: 729611-52-3
• 化学式: C₁₉H₁₉FN₂O₅S₂
• 分子量: 438.501
• InChiKey: MJWVCEDLSGZGEQ-ICWYTKJFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  29
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  154
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• PREVENTIVE AND/OR REMEDY FOR LOWER URINARY TRACT DISEASES CONTAINING EP4 AGONIST
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1782830A1

  公开（公告）日：2007-05-09

  A preventive and/or a remedy for lower urinary tract diseases such as inflammation in the lower urinary tract, cystitis (interstitial cystitis, etc.) and urethritis; (2) an agent for improving bladder compliance and/or bladder capacity; and (3) an agent for protecting bladder mucosa and/or bladder epithelial cells and/or promoting the regeneration thereof; each containing an EP4 agonist. An EP4 agonist is useful in ameliorating symptoms of lower urinary tract diseases such as (1) frequent urination, (2) urgency of urination, (3) pain in the reproductive organs and/or lower urinary tract (for example, bladder pain, urinary tract pain, vulvar pain, vaginal pain, scrotal pain, perineal pain, pelvic pain, etc.) and/or (4) discomfort in the reproductive organs and/or lower urinary tract. Among all, a selective EP4 agonist is useful as a preventive and/or remedy for lower urinary tract diseases having no side effect.

  一种预防和/或治疗下尿路疾病，如下尿路炎症、膀胱炎（间质性膀胱炎等）和尿道炎的制剂；(2) 一种改善膀胱顺应性和/或膀胱容量的制剂；(3) 一种保护膀胱粘膜和/或膀胱上皮细胞和/或促进其再生的制剂；每种制剂都含有一种EP4激动剂。 EP4 激动剂可用于改善下尿路疾病的症状，如(1) 尿频，(2) 尿急，(3) 生殖器官和/或下尿路疼痛（例如，膀胱痛、尿道痛、外阴痛、阴道痛、阴囊痛、会阴痛、骨盆痛等）和/或(4) 生殖器官和/或下尿路不适。其中，选择性 EP4 激动剂可用于预防和/或治疗下尿路疾病，且无副作用。
• PREVENTIVE AND/OR REMEDY FOR HYPERKALEMIA CONTAINING EP4 AGONIST
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1782829A1

  公开（公告）日：2007-05-09

  The present invention relates to a preventive and/or therapeutic agent for hyperkalemia, and a potassium excretion promoter containing EP4 agonist. Since EP4 agonist promotes potassium excretion, it is useful as a preventive and/or therapeutic agent for hyperkalemia. In addition, if selective EP4 agonist uses, it is a preventive and/or therapeutic agent for hyperkalemia without side effects. Further, if EP4 agonist is used, it is useful as improving agent for various symptoms (e.g. paresthesia, error of perception, weakness, myoparalysis, nausea, vomit, abdominal pain, diarrhea, arrhythmia, atrioventricular block, ventricular fibrillation, atrial fibrillation, cardiac arrest, asphyxia and/or dyspnoea etc.).

  本发明涉及一种高钾血症的预防和/或治疗剂，以及一种含有 EP4 激动剂的钾排泄促进剂。由于 EP4 激动剂能促进钾排泄，因此可用作高钾血症的预防和/或治疗剂。此外，如果使用选择性 EP4 激动剂，它是一种无副作用的高钾血症预防和/或治疗剂。此外，如果使用 EP4 激动剂，还可作为改善各种症状（如麻痹、知觉错误、虚弱、肌麻痹、恶心、呕吐、腹痛、腹泻、心律失常、房室传导阻滞、心室颤动、心房颤动、心脏骤停、窒息和/或呼吸困难等）的药物。
• Preventive And/Or Remedy For Lower Urinary Tract Diseases Containing Ep4 Agonist
  申请人：Okada Hiroki

  公开号：US20080021021A1

  公开（公告）日：2008-01-24

  (1) A preventive and/or a remedy for lower urinary tract diseases such as inflammation in the lower urinary tract, cystitis (interstitial cystitis, etc.) and urethritis; (2) an agent for improving bladder compliance and/or bladder capacity; and (3) an agent for protecting bladder mucosa and/or bladder epithelial cells and/or promoting the regeneration thereof; each containing an EP 4 agonist. An EP 4 agonist is useful in ameliorating symptoms of lower urinary tract diseases such as (1) frequent urination, (2) urgency of urination, (3) pain in the reproductive organs and/or lower urinary tract (for example, bladder pain, urinary tract pain, vulvar pain, vaginal pain, scrotal pain, perineal pain, pelvic pain, etc.) and/or (4) discomfort in the reproductive organs and/or lower urinary tract. Among all, a selective EP 4 agonist is useful as a preventive and/or remedy for lower urinary tract diseases having no side effect.

  (1) 可用于预防和/或治疗下尿路疾病，例如下尿路炎症、膀胱炎（间质性膀胱炎等）和尿道炎；(2) 可用于改善膀胱顺应性和/或膀胱容量；以及 (3) 可用于保护膀胱黏膜和/或膀胱上皮细胞和/或促进其再生； 以上用途均包含一种EP4受体激动剂。 EP4受体激动剂在缓解以下症状方面是有用的：(1) 尿频；(2) 急性尿意；(3) 生殖器官和/或下尿路的疼痛（例如膀胱痛、尿路痛、外阴痛、阴道痛、睾丸痛、会阴痛、盆腔痛等）；以及 (4) 生殖器官和/或下尿路的不适。其中，选择性EP4激动剂作为预防和/或治疗下尿路疾病的药物，具有无副作用的优势。
• Preventive and/or Remedy for Hyperkalemia Containing Ep4 Agonist
  申请人：Kuwahara Atsukazu

  公开号：US20080234337A1

  公开（公告）日：2008-09-25

  The present invention relates to a preventive and/or therapeutic agent for hyperkalemia, and a potassium excretion promoter containing EP 4 agonist. Since EP 4 agonist promotes potassium excretion, it is useful as a preventive and/or therapeutic agent for hyperkalemia. In addition, if selective EP 4 agonist uses, it is a preventive and/or therapeutic agent for hyperkalemia without side effects. Further, if EP 4 agonist is used, it is useful as improving agent for various symptoms (e.g. paresthesia, error of perception, weakness, myoparalysis, nausea, vomit, abdominal pain, diarrhea, arrhythmia, atrioventricular block, ventricular fibrillation, atrial fibrillation, cardiac arrest, asphyxia and/or dyspnoea etc.).
• US7858610B2
  申请人：——

  公开号：US7858610B2

  公开（公告）日：2010-12-28