6-(2-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isooxazol-4-yl)methoxy)phenyl)cyclopropyl)-1-isopropyl-1H-indazole-3-carboxylic acid | 1268245-35-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 6-(2-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isooxazol-4-yl)methoxy)phenyl)cyclopropyl)-1-isopropyl-1H-indazole-3-carboxylic acid
• 英文别名: 6-(2-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)phenyl)cyclopropyl)-1-isopropyl-1H-indazole-3-carboxylic acid；6-[2-[2-Chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]cyclopropyl]-1-propan-2-ylindazole-3-carboxylic acid
• CAS: 1268245-35-7
• 化学式: C₃₃H₂₈Cl₃N₃O₄
• 分子量: 636.962
• InChiKey: VDOGFUNVPMEXGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.3
• 重原子数：
  43
• 可旋转键数：
  9
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  90.4
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS SE LIANT AU FXR (NR1 H4) ET MODULANT SON ACTIVITÉ
  申请人：PHENEX PHARMACEUTICALS AG

  公开号：WO2011020615A1

  公开（公告）日：2011-02-24

  The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.

  本发明涉及结合NR1 H4受体（FXR）并作为NR1 H4受体（FXR）激动剂的化合物。该发明还涉及利用这些化合物制备药物用于通过这些化合物结合所述核受体治疗疾病和/或症状，并涉及这些化合物的合成过程。
• A FARNESOID X RECEPTOR AGONSITS FORUSE AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CHRONIC HEPATITIS B VIRUS INFECTION
  申请人：INSERM (Institut National de la Santé et de la Recherche Médicale)

  公开号：EP3711762A1

  公开（公告）日：2020-09-23

  The present invention relates to methods and pharmaceutical compositions for the treatment of hepatitis B virus infection. In particular, the present invention relates to farnesoid X receptor (FXR) agonists for use in a method for the treatment of hepatitis B virus infection in a subject in need thereof.

  本发明涉及治疗乙型肝炎病毒感染的方法和药物组合物。特别是，本发明涉及法尼类固醇 X 受体（FXR）激动剂，用于治疗有需要的受试者的乙型肝炎病毒感染的方法。
• FXR agonists and methods for making and using
  申请人：Salk Institute for Biological Studies

  公开号：US10077268B2

  公开（公告）日：2018-09-18

  Novel FXR agonists are disclosed, embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.

  本文公开了新型 FXR 激动剂、其制造方法的实施方案以及包含它们的组合物。还公开了一种治疗或预防受试者代谢紊乱的方法的实施方案，包括向受试者施用（例如通过胃肠道）治疗有效量的一种或多种已公开化合物，从而激活肠道中的 FXR 受体，治疗或预防受试者的代谢紊乱。此外，还公开了一种治疗或预防受试者肠道区域炎症的方法的实施方案，该方法包括向受试者施用（例如，经由胃肠道）治疗有效量的一种或多种所公开化合物，从而激活肠道中的FXR受体，进而治疗或预防受试者肠道区域的炎症。
• Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection
  申请人：INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MEDICALE)

  公开号：US10071108B2

  公开（公告）日：2018-09-11

  The present invention relates to methods and pharmaceutical compositions for the treatment of hepatitis B virus infection. In particular, the present invention relates to farnesoid X receptor (FXR) agonists for use in a method for the treatment of hepatitis B virus infection in a subject in need thereof.

  本发明涉及治疗乙型肝炎病毒感染的方法和药物组合物。特别是，本发明涉及法尼类固醇 X 受体（FXR）激动剂，用于治疗有需要的受试者的乙型肝炎病毒感染的方法。
• NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS
  申请人：Phenex Pharmaceuticals AG

  公开号：EP2467366A1

  公开（公告）日：2012-06-27