N-{2-[4-(1-methoxy-ethyl)-1-methyl-5-nitro-1H-indol-3-yl]-ethyl}-acetamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-{2-[4-(1-methoxy-ethyl)-1-methyl-5-nitro-1H-indol-3-yl]-ethyl}-acetamide
• 英文别名: N-[2-[4-(1-methoxyethyl)-1-methyl-5-nitroindol-3-yl]ethyl]acetamide
• 化学式: C₁₆H₂₁N₃O₄
• 分子量: 319.36
• InChiKey: SQIKUYBLNVJWGL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  89.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Method for reducing intraocular pressure using indole derivatives
  申请人：——

  公开号：US20020037887A1

  公开（公告）日：2002-03-28

  The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae I-IV. A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmacuetical composition comprising an indole derivative with or without agents commonly used to treat such disorders. 1

  本发明提供了一种通过给予包含吲哚衍生物的药物组合物来降低眼压的方法。本发明中有用的药物组合物包括吲哚衍生物和公式I-IV的褪黑激素类似物。一种首选实施方式是使用5-(甲氧羰基氨基)-N-乙酰色氨酸（5-MCA-NAT），也称为GR 135531，来降低眼压，其作用持续时间较长，并且在降低眼压方面比褪黑激素具有更高的功效。本发明还提供了一种治疗与眼压升高相关的疾病的方法，以及一种治疗各种青光眼形式的方法；该方法包括给予包含吲哚衍生物的药物组合物的有效剂量，可选择性地与通常用于治疗此类疾病的药物一起使用。
• USE OF INDOLE DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT FOR REDUCING INTRACULAR PRESSURE
  申请人：Inspire Pharmaceuticals, Inc.

  公开号：EP1307191A2

  公开（公告）日：2003-05-07
• US6730707B2
  申请人：——

  公开号：US6730707B2

  公开（公告）日：2004-05-04
• [EN] METHOD FOR REDUCING INTRAOCULAR PRESSURE USING INDOLE DERIVATIVES<br/>[FR] METHODE DE REDUCTION DE LA PRESSION INTRAOCULAIRE AVEC DES DERIVES D'INDOLE
  申请人：INSPIRE PHARMACEUTICALS INC

  公开号：WO2002009702A2

  公开（公告）日：2002-02-07

  The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae (I) (II) (III) (IV). A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmaceutical composition comprising an indole derivative with or without agents commonly used to treat such disorders.