(2-phenylquinazolin-4-yl) N-ethyl-N-methylcarbamate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: (2-phenylquinazolin-4-yl) N-ethyl-N-methylcarbamate
• 化学式: C₁₈H₁₇N₃O₂
• 分子量: 307.3
• InChiKey: NZQSUVLGPAWCSA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  55.3
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] QUINAZOLINE SCAFFOLD BASED COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS À BASE DE CHARPENTE QUINAZOLINE, COMPOSITIONS PHARMACEUTIQUES ET MÉTHODES D'UTILISATION CORRESPONDANTES
  申请人：TECHNION RES & DEV FOUNDATION

  公开号：WO2015162615A1

  公开（公告）日：2015-10-29

  The present invention relates to novel heterocyclic compounds based on a quinazoline scaffold of formula (I), which bind effectively to the mitochondrial translocator protein (TSPO), and counteract cell death processes. These compounds can also stimulate neuronal differentiation. The present invention further relates to pharmaceutical compositions including such compounds, and methods of using these compounds for the prevention and treatment of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in preventing, treating, and curing brain damage due to neurodegenerative diseases, including underlying and associated pathological and mental disorders. The compounds can also be used to prevent and treat brain damage due to infection, toxic challenges, and excessive drug use, e.g., recreational, over the counter, or prescription drugs. These compounds can also prevent heart failure, for example associated with brain injuries and brain diseases.

  本发明涉及一种基于喹唑啉支架的新型杂环化合物，其化学式为(I)，能够有效结合线粒体转运蛋白（TSPO），并对抗细胞死亡过程。这些化合物还可以刺激神经元分化。本发明还涉及包括这些化合物的制药组合物，以及使用这些化合物预防和治疗脑损伤，特别是由创伤性脑损伤（TBI）引起的继发性脑损伤的方法。本发明的化合物还可用于预防、治疗和治愈由神经退行性疾病引起的脑损伤，包括潜在的和相关的病理和精神障碍。这些化合物还可用于预防和治疗由感染、毒性挑战和过度药物使用（例如娱乐、非处方或处方药物）引起的脑损伤。这些化合物还可以预防心力衰竭，例如与脑损伤和脑疾病有关的心力衰竭。
• Quinazoline scaffold based compounds, pharmaceutical compositions and methods of use thereof
  申请人：TECHNION RESEARCH & DEVELOPMENT FOUNDATION LTD.

  公开号：US10035780B2

  公开（公告）日：2018-07-31

  The present invention relates to novel heterocyclic compounds based on a quinazoline scaffold, which bind effectively to the mitochondrial translocator protein (TSPO), and counteract cell death processes. These compounds can also stimulate neuronal differentiation. The present invention further relates to pharmaceutical compositions including such compounds, and methods of using these compounds for the prevention and treatment of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in preventing, treating, and curing brain damage due to neurodegenerative diseases, including underlying and associated pathological and mental disorders. The compounds can also be used to prevent and treat brain damage due to infection, toxic challenges, and excessive drug use, e.g., recreational, over the counter, or prescription drugs. These compounds can also prevent heart failure, for example associated with brain injuries and brain diseases.

  本发明涉及基于喹唑啉支架的新型杂环化合物，它们能有效地与线粒体转运蛋白（TSPO）结合，抵消细胞死亡过程。这些化合物还能刺激神经元分化。本发明进一步涉及包括此类化合物的药物组合物，以及使用这些化合物预防和治疗脑损伤导致的脑损伤，特别是创伤性脑损伤（TBI）导致的继发性脑损伤的方法。本发明的化合物还可用于预防、治疗和治愈神经退行性疾病导致的脑损伤，包括潜在的和相关的病理和精神障碍。这些化合物还可用于预防和治疗因感染、毒性挑战和过度使用药物（如娱乐性药物、非处方药或处方药）造成的脑损伤。这些化合物还可以预防心力衰竭，例如与脑损伤和脑疾病相关的心力衰竭。
• QUINAZOLINE SCAFFOLD BASED COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
  申请人：Technion Research & Development Foundation Limited

  公开号：EP3134389B1

  公开（公告）日：2021-04-14