EYP001 | 1192171-69-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: EYP001
• 英文别名: PXL007；4-chloro-5-[4-(2,6-dichloro-benzenesulfonyl)-piperazin-1-yl]-benzofuran-2-carboxylic acid；Vonafexor；4-chloro-5-[4-(2,6-dichlorophenyl)sulfonylpiperazin-1-yl]-1-benzofuran-2-carboxylic acid
• CAS: 1192171-69-9
• 化学式: C₁₉H₁₅Cl₃N₂O₅S
• 分子量: 489.764
• InChiKey: XLGQSYUNOIJBNR-UHFFFAOYSA-N

物化性质

• 沸点：
  680.5±65.0 °C(Predicted)
• 密度：
  1.604±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  99.4
• 氢给体数：
  1
• 氢受体数：
  7

安全信息

• 包装等级：
  III
• 危险类别：
  9
• 危险性防范说明：
  P260,P264,P270,P273,P280,P301+P312+P330,P304+P312,P305+P351+P338,P314,P337+P313,P391,P501
• 危险品运输编号：
  3077
• 危险性描述：
  H302,H319,H332,H372,H400
• 储存条件：
  储存温度应保持在2-8°C，需密封保存并在干燥处存放。

制备方法与用途

vonafexor（EYP001）是一种FXR激动剂，具备抗HBV的作用。

文献信息

• Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
  申请人：Merck Sante

  公开号：EP2110374A1

  公开（公告）日：2009-10-21

  The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).

  本发明涉及式(I)的化合物，其中取代基如权利要求中定义的那样，包括其药物组合物及其用于治疗和/或预防及/或改善与FXR活性相关的疾病或障碍的一个或多个症状。本发明还涉及中间体以及化合物式(I)的制备方法。
• [EN] ACYCLIC ANTIVIRALS<br/>[FR] ANTIVIRAUX ACYCLIQUES
  申请人：ALIOS BIOPHARMA INC

  公开号：WO2017156262A1

  公开（公告）日：2017-09-14

  Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HBV and/or HDV and/or HIV infection with one or more nucleotide analogs

  本文揭示了核苷酸类似物，合成核苷酸类似物的方法以及使用一个或多个核苷酸类似物治疗HBV、HDV和/或HIV感染等疾病和/或状况的方法。
• BENZOFURANE, BENZOTHIOPHENE, BENZOTHIAZOL DERIVATIVES AS FXR MODULATORS
  申请人：Roche Didier

  公开号：US20110105475A1

  公开（公告）日：2011-05-05

  The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).

  本发明涉及公式（I）化合物，其中取代基如权利要求中所定义，包括其药物组合物以及用于治疗和/或预防和/或改善与FXR活性相关的一种或多种疾病或障碍的症状的用途。本发明还涉及中间体以及制备公式（I）化合物的方法。
• 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。
• 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。