14-oxa-14-(3,5-dichlorophenyl)-5-(4-carboxythiazol-2-yl)-9-oxo-1,2,3,4,15,16,17,18,19,20-decanor-5-thia-8-azaprostane | 597572-16-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 14-oxa-14-(3,5-dichlorophenyl)-5-(4-carboxythiazol-2-yl)-9-oxo-1,2,3,4,15,16,17,18,19,20-decanor-5-thia-8-azaprostane
• 英文别名: 2-[(2-{(2R)-2-[(3,5-dichlorophenoxy)methyl]-5-oxo-1-pyrrolidinyl}ethyl)sulfanyl]-1,3-thiazol-4-carboxylic acid；2-[(2-{(2R)-2-[(3,5-dichlorophenoxy)methyl]-5-oxopyrrolidin-1-yl}ethyl)thio]-1,3-thiazole-4-carboxylic acid；2-[2-[(2R)-2-[(3,5-dichlorophenoxy)methyl]-5-oxopyrrolidin-1-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid
• CAS: 597572-16-2
• 化学式: C₁₇H₁₆Cl₂N₂O₄S₂
• 分子量: 447.363
• InChiKey: BZOXXAITHKNLTR-GFCCVEGCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  133
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  14-oxa-14-(3,5-dichlorophenyl)-5-(4-carboxythiazol-2-yl)-9-oxo-1,2,3,4,15,16,17,18,19,20-decanor-5-thia-8-azaprostane 在 N,N-二甲基甲酰胺 草酰氯 、 氨 作用下， 以 甲苯 、 四氢呋喃 、 水 为溶剂， 反应 1.17h， 生成 2-(2-((2R)-2-(3,5-dichlorophenoxymethyl)-5-oxopyrrolidin-1-yl)ethylthio)-1,3-thiazole-4-carboxamide
  参考文献：
  名称：

  8-AZAPROSTAGLANDIN DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT

  摘要：

  公开号：

  EP1481976B1

文献信息

• Medicinal Composition for Inhalation
  申请人：Yamamoto Shigeki

  公开号：US20080114043A1

  公开（公告）日：2008-05-15

  A medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist topically exhibits a prolonged bronchodilating and antiinflammatory effects. Namely, the medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist is useful as a safe preventive and/or a remedy for respiratory diseases (for example, asthma, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, adult respiratory distress syndrome, cystic fibrosis, pulmonary hypertension or the like) without causing any systemic effect such as lowering blood pressure. Thus, a safe and useful remedy for respiratory diseases is provided.

  一种含有EP2激动剂的持续释放型前药的吸入药物组合物，局部表现出持续的支气管扩张和抗炎作用。换言之，含有EP2激动剂的持续释放型前药的吸入药物组合物可作为安全的预防和/或治疗呼吸系统疾病（例如哮喘、肺损伤、肺纤维化、肺气肿、支气管炎、慢性阻塞性肺病、成人呼吸窘迫综合征、囊性纤维化、肺动脉高压等），而不会引起任何降低血压等全身作用。因此，提供了一种安全有效的呼吸系统疾病治疗药物。
• REMEDY FOR SPINAL CANAL STENOSIS
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1609480A1

  公开（公告）日：2005-12-28

  A remedy for spinal canal stenosis which comprises a combination of a compound having EP2 agonism with a compound having EP3 agonism. A drug comprising a combination of a compound having EP2 agonism with a compound having EP3 agonism shows an efficacy in a rat gait disorder model induced by compression of cauda equina. Namely, it is efficacious against spinal canal stenosis to use a combination of a compound having EP2 agonism with a compound having EP3 agonism or a compound having both EP2 agonism and EP3 agonism.

  一种治疗椎管狭窄症的药物，由一种具有 EP2 激动作用的化合物和一种具有 EP3 激动作用的化合物组合而成。一种由具有 EP2 激动作用的化合物和具有 EP3 激动作用的化合物组合而成的药物在马尾受压诱发的大鼠步态障碍模型中显示出疗效。也就是说，将具有 EP2 激动作用的化合物与具有 EP3 激动作用的化合物或同时具有 EP2 激动作用和 EP3 激动作用的化合物组合使用，对椎管狭窄症有疗效。
• MEDICINAL COMPOSITION FOR INHALATION
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1806148A1

  公开（公告）日：2007-07-11

  A medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist topically exhibits a prolonged bronchodilating and antiinflammatory effects. Namely, the medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist is useful as a safe preventive and/or a remedy for respiratory diseases (for example, asthma, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, adult respiratory distress syndrome, cystic fibrosis, pulmonary hypertension or the like) without causing any systemic effect such as lowering blood pressure. Thus, a safe and useful remedy for respiratory diseases is provided.

  一种吸入用药物组合物含有一种 EP2 激动剂的持续释放型原药，局部使用后具有延长支气管扩张和抗炎作用。也就是说，含有 EP2 激动剂持续释放型原药的吸入用药物组合物可作为呼吸系统疾病（例如哮喘、肺损伤、肺纤维化、肺气肿、支气管炎、慢性阻塞性肺病、成人呼吸窘迫综合征、囊性纤维化、肺动脉高压或类似疾病）的安全预防和/或治疗药物，而不会引起任何全身效应，例如降低血压。因此，我们提供了一种安全有用的治疗呼吸系统疾病的药物。
• EP1806148
  申请人：——

  公开号：——

  公开（公告）日：——
• Remedy for spinal canal stenosis
  申请人：Takenobu Yoshifumi

  公开号：US20070167403A1

  公开（公告）日：2007-07-19

  A remedy for spinal canal stenosis which comprises a combination of a compound having EP2 agonism with a compound having EP3 agonism. A drug comprising a combination of a compound having EP2 agonism with a compound having EP3 agonism shows an efficacy in a rat gait disorder model induced by compression of cauda equina. Namely, it is efficacious against spinal canal stenosis to use a combination of a compound having EP2 agonism with a compound having EP3 agonism or a compound having both EP2 agonism and EP3 agonism.