(1E,4E)-2-amino-N,N-dipropyl-8-(pyridin-3-yl)-3H-benzo[b]azepine-4-carboxamide | 1268163-04-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: (1E,4E)-2-amino-N,N-dipropyl-8-(pyridin-3-yl)-3H-benzo[b]azepine-4-carboxamide
• 英文别名: US11046671, Vtx-133；2-amino-N,N-dipropyl-8-pyridin-3-yl-3H-1-benzazepine-4-carboxamide
• CAS: 1268163-04-7
• 化学式: C₂₂H₂₆N₄O
• 分子量: 362.475
• InChiKey: PBBAJCCCVCCZPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  71.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] DIHYDROPYRIMIDINYL BENZAZEPINE CARBOXAMIDE COMPOUNDS<br/>[FR] COMPOSÉS DE DIHYDROPYRIMIDINYL-BENZAZÉPINE CARBOXAMIDE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2017216054A1

  公开（公告）日：2017-12-21

  This invention relates to new benzazepine carboxamide compounds of the formula (i) wherein X and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR8 agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.

  本发明涉及新的苯并氮杂环羧酰胺化合物，其化学式为（i），其中X和R1至R6如描述和权利要求中所定义，并且其药学上可接受的盐。这些化合物是TLR8激动剂，因此可能作为治疗癌症、自身免疫疾病、炎症、败血症、过敏、哮喘、移植排斥、移植物抗宿主病、免疫缺陷和传染病等疾病的药物而有用。
• SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS
  申请人：Howbert James Jeffry

  公开号：US20110118235A1

  公开（公告）日：2011-05-19

  Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

  提供了用于调节Toll样受体TLR7和/或TLR8信号传导的组合物和方法。这些组合物和方法可用于治疗或预防疾病，包括癌症、自身免疫疾病、传染病、炎症性疾病、移植排斥和移植物抗宿主病。
• Substituted Benzoazepines as Toll-Like Receptor Modulators
  申请人：ARRAY BIOPHARMA, INC.

  公开号：US20140142086A1

  公开（公告）日：2014-05-22

  Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

  提供了对通过Toll样受体TLR7和/或TLR8信号传导进行调节的组合物和方法。这些组合物和方法在治疗或预防疾病方面有用，包括癌症、自身免疫疾病、传染病、炎症性疾病、移植排斥和移植物对宿主病。
• Dihydropyrimidinyl benzazepine carboxamide compounds
  申请人：Hoffmann-La Roche Inc.

  公开号：US10590112B2

  公开（公告）日：2020-03-17

  This invention relates to new benzazepine carboxamide compounds of the formula wherein X and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR8 agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.

  本发明涉及新的苯并氮杂卓羧酰胺化合物，其式为 其中 X 和 R1 至 R6 如说明书和权利要求书中所定义，以及其药学上可接受的盐。这些化合物是 TLR8 激动剂，因此可用作治疗癌症、自身免疫性疾病、炎症、败血症、过敏、哮喘、移植物排斥、移植物抗宿主疾病、免疫缺陷和传染性疾病等疾病的药物。
• DIHYDROPYRIMIDINYL BENZAZEPINE CARBOXAMIDE COMPOUNDS
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3468963B1

  公开（公告）日：2021-10-27