1-(biphenyl-4-ylmethyl)-1H-indole-7-carboxylic acid | 1196047-32-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(biphenyl-4-ylmethyl)-1H-indole-7-carboxylic acid
• 英文别名: 1-[(4-phenylphenyl)methyl]indole-7-carboxylic acid
• CAS: 1196047-32-1
• 化学式: C₂₂H₁₇NO₂
• 分子量: 327.382
• InChiKey: CFSLWXSMCCHEMC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 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-(biphenyl-4-ylmethyl)-1H-indole-7-carboxylic acid 、 (S)-4-(1-氨基乙基)-苯甲酸甲酯盐酸盐 在 水 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 、 sodium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 73.92h， 生成 4-[(1S)-1-({[1-(biphenyl-4-ylmethyl)-1H-indol-7-yl]carbonyl}amino)ethyl]benzoic acid
  参考文献：
  名称：

  EP2277858

  摘要：

  公开号：
• 作为产物：
  描述：

  4-溴甲基联苯 在 potassium tert-butylate 、 水 、 sodium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 35.17h， 生成 1-(biphenyl-4-ylmethyl)-1H-indole-7-carboxylic acid
  参考文献：
  名称：

  EP2277858

  摘要：

  公开号：

文献信息

• [EN] BICYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS BICYCLIQUES ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER
  申请人：TEMPEST THERAPEUTICS INC

  公开号：WO2018195123A1

  公开（公告）日：2018-10-25

  The present disclosure is directed to novel compounds of Formula I and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of cancer, including glioblastoma, bone cancer, head and neck cancer, melanoma, basal cell carcinoma, squamous cell carcinoma, adenocarcinoma, oral cancer, esophageal cancer, gastric cancer, intestinal cancer, colon cancer, bladder cancer, hepatocellular carcinoma, renal cell carcinoma, pancreatic cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, and prostate cancer. The compounds of the disclosure are selective antagonists of the EP4 receptor and useful treatment of various diseases that may be ameliorated with blockade of PGE2-mediated signaling.

  本公开涉及一种新型化合物I的化学式及其药用可接受的盐、溶剂化合物、盐的溶剂化合物和前药，用于预防（例如，延迟发病或减少发展风险）和治疗（例如，控制、缓解或减缓进展）癌症，包括胶质母细胞瘤、骨癌、头颈癌、黑色素瘤、基底细胞癌、鳞状细胞癌、腺癌、口腔癌、食管癌、胃癌、肠癌、结肠癌、膀胱癌、肝细胞癌、肾细胞癌、胰腺癌、卵巢癌、宫颈癌、肺癌、乳腺癌和前列腺癌。本公开的化合物是EP4受体的选择性拮抗剂，可用于治疗多种疾病，这些疾病可能通过阻断PGE2介导的信号传导而得到缓解。
• 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。
• 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。
• Bicyclic compounds and their use in the treatment of cancer
  申请人：Tempest Therapeutics, Inc.

  公开号：US11066405B2

  公开（公告）日：2021-07-20

  The present disclosure is directed to novel compounds of Formula I and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of cancer, including glioblastoma, bone cancer, head and neck cancer, melanoma, basal cell carcinoma, squamous cell carcinoma, adenocarcinoma, oral cancer, esophageal cancer, gastric cancer, intestinal cancer, colon cancer, bladder cancer, hepatocellular carcinoma, renal cell carcinoma, pancreatic cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, and prostate cancer. The compounds of the disclosure are selective antagonists of the EP4 receptor and useful treatment of various diseases that may be ameliorated with blockade of PGE2-mediated signaling.

  本公开涉及式 I 的新型化合物及其药学上可接受的盐、溶解物、盐的溶解物和原药，这些化合物在预防（如延迟发病或降低发病风险）和治疗（如、包括胶质母细胞瘤、骨癌、头颈癌、黑色素瘤、基底细胞癌、鳞状细胞癌、腺癌、口腔癌、食管癌、胃癌、肠癌、结肠癌、膀胱癌、肝细胞癌、肾细胞癌、胰腺癌、卵巢癌、宫颈癌、肺癌、乳腺癌和前列腺癌。本公开的化合物是 EP4 受体的选择性拮抗剂，可用于治疗各种可通过阻断 PGE2 介导的信号传导而改善的疾病。