4'-dimethylamino-7,8-dihydroxyflavone | 1205548-04-4

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: 4'-dimethylamino-7,8-dihydroxyflavone
• 英文别名: 2-(4-(Dimethylamino)phenyl)-7,8-dihydroxy-4H-chromen-4-one；2-[4-(dimethylamino)phenyl]-7,8-dihydroxychromen-4-one
• CAS: 1205548-04-4
• 化学式: C₁₇H₁₅NO₄
• 分子量: 297.31
• InChiKey: YPAYCZOHGRSGJS-UHFFFAOYSA-N

物化性质

• 沸点：
  535.1±50.0 °C(Predicted)
• 密度：
  1.388±0.06 g/cm3(Predicted)
• 溶解度：
  二甲基亚砜（微溶）

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  70
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-(4-(dimethylamino)phenyl)-7,8-dimethoxy-4H-chromen-4-one 在 三溴化硼 作用下， 以 二氯甲烷 为溶剂， 以66%的产率得到4'-dimethylamino-7,8-dihydroxyflavone
  参考文献：
  名称：

  走向原肌球蛋白相关激酶B（TrkB）受体配体的PET脑成像：放射性合成和2-（4- [ 18 F]氟苯基）-7,8-dihydroxy-4 H -chromen-4-one和2-的评估。（4-（[[ N-甲基-11 C]-二甲基氨基）苯基）-7,8-二羟基-4 H-铬-4--4-

  摘要：

  原肌球蛋白相关激酶B（TrkB）与同源配体脑源性神经营养因子（BDNF）的相互作用介导了神经系统发育的基本途径。TrkB信号改变与许多神经退行性疾病和状况有关。在这里，我们报告基于最近确定的7,8-二羟基黄酮化学型的第一个TrkB放射性配体的合成，生物学评估和放射性合成。通过高效的S N Ar放射性氟化，涉及对位-，以高放射化学收率合成了2-（4- [ 18 F]氟苯基）-7,8-二羟基-4 H -chromen-4-one（[ 18 F] 10b）。迈克尔受体取代的芳基，接着是BBr 3-促进的双去甲基化。选择性的N- [ 11 C]甲基化得到2-（4-（[ N-甲基-11 C]-二甲基氨基）苯基）-7,8-二羟基-4 H-铬烯-4-酮（[ 11 C] 10c）从具有[ 11 C] MeOTf的完全脱保护的含邻苯二酚的去甲甲基前体13中分离得到。[ 18 F] 10b的体外放射自显影具有

  DOI：

  10.1016/j.bmc.2013.10.012

文献信息

• Treating various disorders with 7,8-dihydroxyflavone and derivatives thereof
  申请人：Ye Keqiang

  公开号：US09895344B2

  公开（公告）日：2018-02-20

  Novel compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of 7,8-dihydroxyflavone or derivative thereof. Specifically, methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof. A further method of promoting neuroprotection in a subject also is provided, which includes selecting a subject in need of neuroprotection, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof.

  提供了与激活TrkB受体相关的新化合物和方法。这些方法包括在体内或体外给予治疗有效量的7,8-二羟基黄酮或其衍生物。具体提供了用于治疗包括神经疾病、神经精神疾病和代谢性疾病（如肥胖症）的方法和化合物。例如，提供了第一种方法，用于治疗或减少受试者患抑郁症、焦虑症或肥胖症的风险，包括选择患有或有发展抑郁症、焦虑症或肥胖症风险的受试者，并向受试者给予治疗有效量的7,8-二羟基黄酮或其衍生物。还提供了另一种促进受试者神经保护的方法，包括选择需要神经保护的受试者，并向受试者给予治疗有效量的7,8-二羟基黄酮或其衍生物。
• TREATING VARIOUS DISORDERS WITH 7,8-DIHYDROXYFLAVONE AND DERIVATIVES THEREOF
  申请人：Ye Keqiang

  公开号：US20110144196A1

  公开（公告）日：2011-06-16

  Novel compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of 7,8-dihydroxyflavone or derivative thereof. Specifically, methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof. A further method of promoting neuroprotection in a subject also is provided, which includes selecting a subject in need of neuroprotection, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof.

  本发明提供了与TrkB受体激活相关的新化合物和方法。该方法包括在体内或体外给予7,8-二羟基黄酮或其衍生物的治疗有效量。具体提供了用于治疗神经疾病、神经精神疾病和代谢性疾病（例如肥胖症）的方法和化合物。例如，提供了一种用于治疗或减少患者患抑郁症、焦虑症或肥胖症风险的第一种方法，其中包括选择患有或有发展抑郁症、焦虑症或肥胖症风险的患者，并向该患者给予7,8-二羟基黄酮或其衍生物的治疗有效量。还提供了一种促进患者神经保护的进一步方法，包括选择需要神经保护的患者，并向该患者给予7,8-二羟基黄酮或其衍生物的治疗有效量。
• TRKB AGONISTS AND METHODS OF USE
  申请人：Ye Keqiang

  公开号：US20130040947A1

  公开（公告）日：2013-02-14

  Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-di-hydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.

  本文提供与TrkB受体激活相关的化合物和方法。这些方法包括将带有改性黄酮或杂环环的7,8-二羟基黄酮衍生物注射给需要的受试者。本文还提供了治疗神经系统疾病、神经精神疾病和代谢性疾病（例如肥胖症）的方法和化合物。
• Method of treating pain using agents that promote neuronal differentiation
  申请人：Rusanescu Gabriel

  公开号：US10398760B2

  公开（公告）日：2019-09-03

  The present invention is based on the seminal concept of treating pain by promoting neuronal differentiation. The invention provides a method of treating pain utilizing agents that induce neuronal differentiation by activating specific receptors. The invention also provides a method of screening of agents for the purpose of use in treating pain, based on their neuronal differentiation activity.

  本发明基于通过促进神经元分化来治疗疼痛的开创性概念。本发明提供了一种利用通过激活特定受体诱导神经元分化的制剂治疗疼痛的方法。本发明还提供了一种根据制剂的神经元分化活性筛选用于治疗疼痛的制剂的方法。
• Triglyceride otic formulations and uses thereof
  申请人：Otonomy, Inc.

  公开号：US10821185B2

  公开（公告）日：2020-11-03

  Disclosed herein are triglyceride based formulations, compositions, and methods for the treatment of otic diseases and conditions. Such triglyceride based formulations and compositions are derived from medium chain triglycerides and allow for the delivery of a variety of therapeutic agents to the outer, middle, and/or inner ear.

  本文公开了用于治疗耳部疾病和病症的甘油三酯制剂、组合物和方法。 此类甘油三酯制剂和组合物源自中链甘油三酯，可向外耳、中耳和/或内耳输送多种治疗剂。