1-(quinolin-2-ylmethyl)-1H-indole-7-carboxylic acid methyl ester | 1097197-29-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 1-(quinolin-2-ylmethyl)-1H-indole-7-carboxylic acid methyl ester
• 英文别名: methyl 1-(quinolin-2-ylmethyl)-1H-indole-7-carboxylate；methyl 1-(quinolin-2-ylmethyl)indole-7-carboxylate
• CAS: 1097197-29-9
• 化学式: C₂₀H₁₆N₂O₂
• 分子量: 316.359
• InChiKey: YAZZGPUSTYQMEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  44.1
• 氢给体数：
  0
• 氢受体数：
  3

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 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。
• COMPOUND FOR INHIBITING PGE2/EP4 SIGNALING TRANSDUCTION INHIBITING, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
  申请人：Keythera (Suzhou) Pharmaceuticals Co. Ltd.

  公开号：EP3889134A1

  公开（公告）日：2021-10-06

  A compound of formula (I), a preparation method therefor, a pharmaceutical composition containing a derivative thereof, and the therapeutic uses thereof, especially inhibiting PGE2/EP4 signalling transduction and the uses thereof for treating cancer, acute or chronic pain, migraine, osteoarthritis, rheumatoid arthritis, gout, bursitis, ankylosing spondylitis, primary dysmenorrhea, tumour or arteriosclerosis.

  一种式（I）化合物、其制备方法、含有其衍生物的药物组合物及其治疗用途，特别是抑制 PGE2/EP4 信号转导及其治疗癌症、急性或慢性疼痛、偏头痛、骨关节炎、类风湿性关节炎、痛风、滑囊炎、强直性脊柱炎、原发性痛经、肿瘤或动脉硬化的用途。
• [EN] AMIDE COMPOUND<br/>[FR] COMPOSÉ AMIDE
  申请人：ASTELLAS PHARMA INC

  公开号：WO2009139373A1

  公开（公告）日：2009-11-19

  【課題】医薬組成物、例えば慢性腎不全、及び／又は糖尿病性腎症の治療用医薬組成物の有効成分として有用な化合物を提供する。 【解決手段】本発明者らは、EP4受容体拮抗作用を有する化合物について鋭意検討し、本発明のアミド化合物がEP4受容体拮抗作用を有することを確認し、本発明を完成した。本発明のアミド化合物は、EP4受容体拮抗作用を有し、EP4が関与する種々の疾患、例えば、慢性腎不全、及び／又は糖尿病性腎症等の予防及び／又は治療用医薬組成物の有効成分として使用しうる。