1-(4-chlorobenzyl)-1H-indole-7-carboxylic acid | 1097196-92-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(4-chlorobenzyl)-1H-indole-7-carboxylic acid
• 英文别名: 1-[(4-chlorophenyl)methyl]indole-7-carboxylic acid
• CAS: 1097196-92-3
• 化学式: C₁₆H₁₂ClNO₂
• 分子量: 285.73
• InChiKey: YGQPCYAKPRCOIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(4-chlorobenzyl)-1H-indole-7-carboxylic acid 、 6-氨基己酸甲酯 盐酸盐 在 1-羟基苯并三唑 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 生成 6-({[1-(4-chlorobenzyl)-1H-indol-7-yl]carbonyl}amino)hexanoic acid
  参考文献：
  名称：

  EP2172447

  摘要：

  公开号：

文献信息

• AMIDE COMPOUND
  申请人：Nozawa Eisuke

  公开号：US20110144153A1

  公开（公告）日：2011-06-16

  [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.

  【问题】提供一种化合物，该化合物可用作药物组合物的活性成分，例如用于治疗慢性肾衰竭和/或糖尿病肾病的药物组合物。 【解决方法】本发明人对具有EP4受体拮抗活性的化合物进行了广泛的研究，并确认本发明的酰胺化合物具有EP4受体拮抗活性，从而完成了本发明。本发明的酰胺化合物具有EP4受体拮抗活性，可用作预防和/或治疗各种EP4相关疾病的药物组合物的活性成分，例如慢性肾衰竭和/或糖尿病肾病等。
• Amide compound
  申请人：Nozawa Eisuke

  公开号：US08598355B2

  公开（公告）日：2013-12-03

  [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.

  【问题】提供一种化合物，该化合物可用作药物组合物的活性成分，例如用于治疗慢性肾功能衰竭和/或糖尿病肾病的药物组合物。 【解决方法】本发明人对具有EP4受体拮抗活性的化合物进行了广泛的研究，并确认本发明的酰胺化合物具有EP4受体拮抗活性，从而完成了本发明。本发明的酰胺化合物具有EP4受体拮抗活性，可用作预防和/或治疗各种与EP4相关的疾病的药物组合物的活性成分，例如慢性肾功能衰竭和/或糖尿病肾病等。
• AMIDE COMPOUNDS
  申请人：Nozawa Eisuke

  公开号：US20110028463A1

  公开（公告）日：2011-02-03

  [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

  【问题】提供一种可用作治疗慢性肾功能不全或糖尿病肾病的药物化合物。 【解决问题的方法】本发明者对具有EP4受体拮抗作用的化合物进行了广泛的研究，结果发现具有羧酸基或其等效物的各种酰胺衍生物表现出优异的EP4受体拮抗作用，从而完成了本发明。由于本发明的化合物具有优异的EP4受体拮抗作用，因此可用作预防和/或治疗慢性肾功能不全或糖尿病肾病的药物。
• Amide compounds and their use as PGE2 antagonists.
  申请人：Astellas Pharma Inc.

  公开号：EP2460787A1

  公开（公告）日：2012-06-06

  [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

  [问题]提供一种可作为治疗慢性肾功能不全的药物或治疗糖尿病肾病的药物的化合物。 [解决问题的方法]本发明人对具有 EP4 受体拮抗作用的化合物进行了广泛的研究，结果发现具有羧基或其等价物的各种酰胺衍生物具有优异的 EP4 受体拮抗作用，从而完成了本发明。 由于本发明的化合物具有优异的 EP4 受体拮抗作用，因此可用作预防和/或治疗慢性肾功能不全或糖尿病肾病的药物。
• 4-(Indol-7-ylcarbonylaminomethyl)cyclohexanecarboxylic acid derivatives as EP4 receptor antagonists useful for the treatment of chronic renal failure or diabetic nephropathy
  申请人：Astellas Pharma Inc.

  公开号：EP2565191A1

  公开（公告）日：2013-03-06

  The present invention relates to amide compounds of formula I which are EP4 receptor antagonists and useful for treating chronic renal failure and/or diabetic nephropathy. Ring D is a group of formula II; V and W are CH; R45 is -CH2-B5; B5 represents a bicyclic hetero ring which may be substituted with one or more groups selected from the group consisting of halogen and C1-6 alkyl; R46 is H, halogen, C1-6 alkyl which may be substituted with one or more halogens, or -O-C1-6 alkyl; -NR1-YR2 - is -NH-CH2-; Ring E is cyclohexane-1,4-diyl; and -Z-R3 is -CO2H.

  本发明涉及式 I 的酰胺化合物，它们是 EP4 受体拮抗剂，可用于治疗慢性肾衰竭和/或糖尿病肾病。 环 D 是式 II 的基团； V 和 W 是 CH； R45 是-CH2-B5； B5 代表可被一个或多个选自卤素和 C1-6 烷基的基团取代的双环杂环； R46 是 H、卤素、可被一个或多个卤素取代的 C1-6 烷基或 -O-C1-6 烷基； -NR1-YR2-是-NH-CH2-； 环 E 是环己烷-1,4-二基；以及 -Z-R3为-CO2H。