3-amino-N-(4-fluorophenyl)-4-phenyl-6-(2-thienyl)thieno[2,3-b]pyridine-2-carboxamide

• 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: 3-amino-N-(4-fluorophenyl)-4-phenyl-6-(2-thienyl)thieno[2,3-b]pyridine-2-carboxamide
• 英文别名: 3-amino-N-(4-fluorophenyl)-4-phenyl-6-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide
• 化学式: C₂₄H₁₆FN₃OS₂
• 分子量: 445.5
• InChiKey: KOJCITYQTOGCGM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.3
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  125
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• THIENO[2,3-B]PYRIDINE DERIVATIVES AS EPAC INHIBITORS AND THEIR PHARMACEUTICAL USES
  申请人：INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE - INSERM

  公开号：EP3801511A1

  公开（公告）日：2021-04-14
• EPAC1 INHIBITORS FOR THE TREATMENT OF IDIOPATHIC PULMONARY FIBROSIS
  申请人：INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE - INSERM

  公开号：EP4072547A1

  公开（公告）日：2022-10-19
• [EN] THIENO[2,3-B]PYRIDINE DERIVATIVES AS EPAC INHIBITORS AND THEIR PHARMACEUTICAL USES<br/>[FR] DÉRIVÉS DE THIÉNO[2,3-B] PYRIDINE EN TANT QU'INHIBITEURS D'EPAC ET LEURS UTILISATIONS PHARMACEUTIQUES
  申请人：INST NAT SANTE RECH MED

  公开号：WO2019234197A1

  公开（公告）日：2019-12-12

  The present invention relates to thieno[2,3-b]pyridine derivatives for use in the treatment and/or the prevention of a disease selected from the group consisting of inflammation, cancer, vascular diseases, kidney diseases, cognitive disorders, pain, infections, obesity, and cardiac diseases. Indeed, the inventors found that thieno[2,3- b]pyridine derivatives of the invention are inhibitors of the Epac protein and can thus be useful for the prevention and/or treatment of diseases wherein the Epac protein is involved. Particularly, the inventors showed that thieno[2,3-b]pyridine derivatives of the invention are potent and non-competitive inhibitors of Epac and demonstrated that they also inhibit the activation of Epac downstream effectors such as Rap1 in cells.
• [EN] EPAC1 INHIBITORS FOR THE TREATMENT OF IDIOPATHIC PULMONARY FIBROSIS<br/>[FR] INHIBITEURS D'EPAC1 POUR LE TRAITEMENT DE LA FIBROSE PULMONAIRE IDIOPATHIQUE
  申请人：INST NAT SANTE RECH MED

  公开号：WO2021116389A1

  公开（公告）日：2021-06-17

  The present invention relates to the treatment of idiopathic pulmonary fibrosis. Today, there is no cure for IFF. The inventors showed that EPAC1 inhibitors, in particular CE3F4 and AM-001, represent a promising therapeutic strategy for treating patients with pulmonary fibrosis. The present invention thus relates to an EPAC1 inhibitor for use in the treatment and/or prevention of idiopathic pulmonary fibrosis.
• [EN] THIENOPYRIDINE DERIVATIVES FOR USE IN THE TREATMENT OF CORONAVIRUS INFECTION<br/>[FR] DÉRIVÉS DE THIÉNOPYRIDINE DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT D'UNE INFECTION À CORONAVIRUS
  申请人：INST NAT SANTE RECH MED

  公开号：WO2021250231A1

  公开（公告）日：2021-12-16

  Coronaviridae is a family of enveloped, positive-sense, single-stranded RNA viruses. The emergence of a new betacoronavirus SARS-CoV-2 has led to a major health-related crisis associated with a significant mortality in intensive care units, due to the pulmonary complications of COVID-19. The inventors showed that an inhibitor of EPAC1 (i.e. AM-001) is suitable for inhibiting replication of coronavirus and thus would be suitable for the treatment of infections mediated by said type of virus.