TL8-506 | 1268163-15-0

• 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: TL8-506
• 英文别名: (1E,4E)-ethyl 2-amino-8-(3-cyanophenyl)-3H-benzo[b]azepine-4-carboxylate；3H-1-Benzazepine-4-carboxylic acid, 2-aMino-8-(3-cyanophenyl)-, ethyl ester；ethyl 2-amino-8-(3-cyanophenyl)-3H-1-benzazepine-4-carboxylate
• CAS: 1268163-15-0
• 化学式: C₂₀H₁₇N₃O₂
• 分子量: 331.374
• InChiKey: YHRYTTWRVKXODS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  88.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• 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。
• Method of treating cancer with a biomaterial and a toll-like receptor agonist
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10413612B2

  公开（公告）日：2019-09-17

  Provided are drug delivery compositions and devices useful for the treatment and/or prevention of cancer and metastatic tumors. For example, a drug delivery device is provided that comprises a biodegradable scaffold carrying one or more anti-cancer therapeutic agents that activate the innate immune system (e.g., STING agonists) and/or the adaptive immune system (e.g., anti-PD-1 antibodies). The compositions and devices may include a cytokine (e.g., IL-15 superagonist). The drug delivery device can be implanted in the void volume of a resected tumor to prevent tumor regrowth and tumor metastasis. Also provided are methods of making the drug delivery compositions and devices as well as kits containing materials to provide the compositions and devices.

  本文提供了用于治疗和/或预防癌症和转移性肿瘤的给药组合物和装置。例如，提供了一种药物输送装置，它包括一种可生物降解的支架，其中携带一种或多种激活先天性免疫系统（如 STING 激动剂）和/或适应性免疫系统（如抗 PD-1 抗体）的抗癌治疗剂。组合物和装置可包括细胞因子（如 IL-15 超拮抗剂）。该给药装置可植入切除肿瘤的空隙中，以防止肿瘤再生和肿瘤转移。此外，还提供了制造给药组合物和装置的方法，以及含有提供组合物和装置的材料的试剂盒。
• Drug delivery compositions and uses thereof
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10435469B2

  公开（公告）日：2019-10-08

  Provided are drug delivery compositions and devices useful for the treatment and/or prevention of cancer and metastatic tumors. For example, a drug delivery device is provided that comprises a biodegradable scaffold carrying one or more anti-cancer therapeutic agents that activate the innate immune system (e.g., STING agonists) and/or the adaptive immune system (e.g., anti-PD-1 antibodies). The compositions and devices may include a cytokine (e.g., IL-15 superagonist). The drug delivery device can be implanted in the void volume of a resected tumor to prevent tumor regrowth and tumor metastasis. Also provided are methods of making the drug delivery compositions and devices as well as kits containing materials to provide the compositions and devices.

  本文提供了用于治疗和/或预防癌症和转移性肿瘤的给药组合物和装置。例如，提供了一种药物输送装置，它包括一种可生物降解的支架，其中携带一种或多种激活先天性免疫系统（如 STING 激动剂）和/或适应性免疫系统（如抗 PD-1 抗体）的抗癌治疗剂。组合物和装置可包括细胞因子（如 IL-15 超拮抗剂）。该给药装置可植入切除肿瘤的空隙中，以防止肿瘤再生和肿瘤转移。此外，还提供了制造给药组合物和装置的方法，以及含有提供组合物和装置的材料的试剂盒。
• DRUG DELIVERY COMPOSITIONS AND USES THEREOF
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20190083626A1

  公开（公告）日：2019-03-21

  Provided are drug delivery compositions and devices useful for the treatment and/or prevention of cancer and metastatic tumors. For example, a drug delivery device is provided that comprises a biodegradable scaffold carrying one or more anti-cancer therapeutic agents that activate the innate immune system (e.g., STING agonists) and/or the adaptive immune system (e.g., anti-PD-1 antibodies). The compositions and devices may include a cytokine (e.g., IL-15 superagonist). The drug delivery device can be implanted in the void volume of a resected tumor to prevent tumor regrowth and tumor metastasis. Also provided are methods of making the drug delivery compositions and devices as well as kits containing materials to provide the compositions and devices.