Di(1H-indol-6-yl)amine | 1342948-97-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Di(1H-indol-6-yl)amine
• 英文别名: N-(1H-indol-6-yl)-1H-indol-6-amine
• CAS: 1342948-97-3
• 化学式: C₁₆H₁₃N₃
• 分子量: 247.299
• InChiKey: YCNZZOXPOJWKTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  43.6
• 氢给体数：
  3
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  6-bromo-1-(triisopropylsilyl)-1H-indole 在 四丁基氟化铵 、 palladium diacetate 、 2-二环己基磷-2,4,6-三异丙基联苯 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 生成 Di(1H-indol-6-yl)amine
  参考文献：
  名称：

  发现和表征新型的吲哚和7-氮杂吲哚衍生物作为β-淀粉样蛋白42聚集的抑制剂，用于治疗阿尔茨海默氏病。

  摘要：

  淀粉状蛋白-β肽聚集为细胞毒性寡聚体和原纤维聚集体被认为是阿尔茨海默病的主要病理事件之一。在这里，我们报告设计和合成一系列新的吲哚和7-氮杂吲哚衍生物，它们在3位上含有腈，哌啶和N-甲基-哌啶取代基，以防止淀粉样β的病理自组装。我们进一步证明，为了获得具有改善的理化特性以允许脑渗透的化合物，需要在3个位置取代氮杂吲哚和吲哚衍生物。

  DOI：

  10.1016/j.bmcl.2017.02.001

文献信息

• Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-Like Proteins
  申请人：Kroth Heiko

  公开号：US20110280808A1

  公开（公告）日：2011-11-17

  The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及一种新型化合物，可用于治疗与淀粉样蛋白相关的一组疾病和异常，如阿尔茨海默病，以及与淀粉样蛋白类似蛋白相关的疾病或病况。本发明的化合物还可用于治疗与视觉系统组织中的病理异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的药物组合物，以及利用这些化合物制备用于治疗或预防与淀粉样和/或淀粉样类似蛋白相关的疾病或病况的药物的用途。还公开了一种治疗或预防与淀粉样和/或淀粉样类似蛋白相关的疾病或病况的方法。
• [EN] COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR TRAITER DES ÉTATS ASSOCIÉS À UNE ACTIVITÉ DE STING
  申请人：IFM DUE INC

  公开号：WO2020252240A1

  公开（公告）日：2020-12-17

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

  本公开涉及抑制（例如，拮抗）干扰素基因激活因子（STING）的化学实体（例如，化合物或药用可接受的盐，和/或水合物，和/或共晶，和/或化合物的药物组合）。所述化学实体是有用的，例如，用于治疗在受试者（例如，人）中增加（例如，过量）STING激活（例如，STING信号传导）有助于病理和/或症状和/或进展的状况、疾病或失调（例如，癌症）。本公开还涉及含有相同成分的药物组合物以及使用和制备相同成分的方法。
• [EN] NOVEL COMPOUNDS FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS<br/>[FR] NOUVEAUX COMPOSÉS POUR LE TRAITEMENT DE MALADIES ASSOCIÉES AUX PROTÉINES AMYLOÏDES OU DE TYPE AMYLOÏDE
  申请人：AC IMMUNE SA

  公开号：WO2011128455A1

  公开（公告）日：2011-10-20

  The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及一类新化合物，可用于治疗与淀粉样蛋白相关的一组疾病和异常，例如阿尔茨海默病，以及与类淀粉样蛋白相关的疾病或状况。本发明的化合物还可用于治疗与视觉系统组织病理性异常/变化相关的眼病。本发明还涉及包含这些化合物的药物组合物，以及使用这些化合物制备用于治疗或预防与淀粉样和/或类淀粉样蛋白相关的疾病或状况的药物。还公开了一种治疗或预防与淀粉样和/或类淀粉样蛋白相关疾病或状况的方法。
• US9221812B2
  申请人：——

  公开号：US9221812B2

  公开（公告）日：2015-12-29
• [EN] METHODS OF TREATING CANCER<br/>[FR] MÉTHODES DE TRAITEMENT DU CANCER
  申请人：IFM DUE INC

  公开号：WO2020257621A1

  公开（公告）日：2020-12-24

  Provided herein are methods of treating a subject, such as a subject that has cancer, that include administering a therapeutically effective amount of a STING antagonist or a cGAS inhibitor or a pharmaceutically acceptable salt, solvate, or co-crystal thereof to a subject identified as having (i) one or both of (i) decreased TREX1 level and/or activity, and (ii) increased cGAS/STING signaling pathway activity, e.g., as compared to a reference level, and/or (ii) an elevated level of cGAMP in a serum or tumor sample of the subject as compared to a reference level.