3,4-Dihydro-1,6-naphthyridine

• 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: 3,4-Dihydro-1,6-naphthyridine
• 英文别名: 3,4-dihydro-1,6-naphthyridine
• 化学式: C₈H₈N₂
• 分子量: 132.16
• InChiKey: BPQDZSCQAVBSIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  25.2
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF<br/>[FR] INHIBITEURS DE LA KALLIKRÉINE PLASMATIQUE ET UTILISATIONS ASSOCIÉES
  申请人：DYAX CORP

  公开号：WO2019028362A1

  公开（公告）日：2019-02-07

  Provided herein are compounds that inhibit pKal, a serine protease whose activity is responsible for proteolytically cleaving kininogen and generating the potent vasodilator and pro-inflammatory peptide bradykinin, which can lead to painful and debilitating inflammatory attacks (e.g., edema). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating pKal-related diseases and disorders (e.g., edema) with the compounds in a subject, by administering the compounds and/or compositions described herein.

  本文提供了抑制pKal的化合物，pKal是一种丝氨酸蛋白酶，其活性负责蛋白酶解切激肽原并生成强效的血管舒张剂和促炎肽布雷金因，这可能导致疼痛和令人痛苦的炎症发作（例如水肿）。还提供了包含这些化合物的药物组合物和试剂盒，以及使用这些化合物在受试者中治疗pKal相关疾病和紊乱（例如水肿）的方法，通过给予本文所述的化合物和/或组合物。
• Inhibitors of Plasma Kallikrein and uses thereof
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US11168083B2

  公开（公告）日：2021-11-09

  Provided herein are compounds that inhibit pKal, a serine protease whose activity is responsible for proteolytically cleaving kininogen and generating the potent vasodilator and pro-inflammatory peptide bradykinin, which can lead to painful and debilitating inflammatory attacks (e.g., edema). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating pKal-related diseases and disorders (e.g., edema) with the compounds in a subject, by administering the compounds and/or compositions described herein.

  本文提供了抑制 pKal 的化合物，pKal 是一种丝氨酸蛋白酶，其活性负责蛋白水解激肽原并生成强效血管扩张剂和促炎肽缓激肽，后者可导致疼痛和衰弱性炎症发作（如水肿）。此外，还提供了包含所述化合物的药物组合物和试剂盒，以及通过施用所述化合物和/或组合物在受试者体内用所述化合物治疗pKal相关疾病和失调（如水肿）的方法。
• INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
  申请人：Dyax Corp.

  公开号：EP3661922A1

  公开（公告）日：2020-06-10