8-chloro-4-methyl-1-(3-methyl-pyridin-4-yl)-[1,2,4]triazolo[4,3-a]quinoxaline | 1392412-34-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 8-chloro-4-methyl-1-(3-methyl-pyridin-4-yl)-[1,2,4]triazolo[4,3-a]quinoxaline
• 英文别名: 8-chloro-4-methyl-1-(3-methylpyridin-4-yl)-[1,2,4]triazolo[4,3-a]quinoxaline
• CAS: 1392412-34-8
• 化学式: C₁₆H₁₂ClN₅
• 分子量: 309.758
• InChiKey: FBZARNOHVPPHSV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  56
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] (1,2,4)TRIAZOLO[4,3-A]QUINOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES<br/>[FR] DÉRIVÉS DE (1,2,4)TRIAZOLO[4,3-A]QUINOXALINE UTILISÉS COMME INHIBITEURS DES PHOSPHODIESTÉRASES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012104293A1

  公开（公告）日：2012-08-09

  The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives of Formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases.

  该发明涉及式(I)的(1,2,4)三唑并[4,3-a]喹喔啉衍生物，它们是磷酸二酯酶2和/或10的抑制剂，可用于治疗中枢神经系统疾病。
• Imaging Agents for Detecting Neurological Dysfunction
  申请人：Szardenings Anna Katrin

  公开号：US20120302755A1

  公开（公告）日：2012-11-29

  Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

  本文公开了一种诊断哺乳动物阿尔茨海默病或其易感性的化合物和方法，其中该方法包括向哺乳动物施加诊断有效量的放射性标记化合物，所述化合物选自放射性标记的咔唑衍生物和其衍生物以及三唑衍生物组成的群体，允许该化合物分布到脑组织中，并成像脑组织，其中与正常控制结合水平相比，化合物对脑组织的结合增加表明哺乳动物正在患有或有发展阿尔茨海默病的风险。
• (1,2,4)TRIAZOLO[4,3-A]QUINOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES
  申请人：Lankau Hans-Joachim

  公开号：US20120302564A1

  公开（公告）日：2012-11-29

  The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases.

  这项发明涉及（1,2,4）三唑并[4,3-a]喹啉衍生物，它们是磷酸二酯酶2和/或10的抑制剂，可用于治疗中枢神经系统疾病。
• Imaging agents for detecting neurological dysfunction
  申请人：Eli Lilly and Company

  公开号：US20150030540A1

  公开（公告）日：2015-01-29

  Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

  本文中披露了在哺乳动物中诊断阿尔茨海默病或其易感性的化合物和方法，该方法包括向哺乳动物施用诊断有效量的放射性标记化合物，所述化合物选自放射性标记的咔唑衍生物和其衍生物以及三唑衍生物的群组，使化合物分布到脑组织中，并成像脑组织，其中化合物与脑组织的结合增加，与正常对照水平的结合相比，表明哺乳动物正在患有或有发展阿尔茨海默病的风险。
• COMPOUNDS FOR TAU PROTEIN DEGRADATION
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20210154184A1

  公开（公告）日：2021-05-27

  Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.