8-Tert-butyl-[1,2,4]triazolo[4,3-a]pyrazine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 8-Tert-butyl-[1,2,4]triazolo[4,3-a]pyrazine
• 英文别名: 8-tert-butyl-[1,2,4]triazolo[4,3-a]pyrazine
• 化学式: C₉H₁₂N₄
• 分子量: 176.22
• InChiKey: YFOCKVYQHMIYSI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  43.1
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Inhibitors of the Renal Outer Medullary Potassium Channel
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US20140235628A1

  公开（公告）日：2014-08-21

  This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.

  本发明涉及式I的结构化合物及其药学上可接受的盐，它们是肾外髓质钾（ROMK）通道（Kir1.1）的抑制剂。式I的化合物可用作利尿剂和钠利尿剂，因此可用于治疗和预防由过多盐和水滞留引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。
• 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
  申请人：Rugen Holdings (Cayman) Limited

  公开号：US10294230B2

  公开（公告）日：2019-05-21

  Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).

  所公开的是式 (I) 的化学实体： 其中 R1 和 Z 在此定义，作为 NR2B 亚型选择性受体拮抗剂。还公开了包含式（I）化学实体的药物组合物，以及通过施用式（I）化学实体治疗与 NR2B 拮抗相关的各种疾病和紊乱的方法，例如中枢神经系统疾病和紊乱，如抑郁症。
• Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
  申请人：Rugen Holdings (Cayman) Limited

  公开号：US11000526B2

  公开（公告）日：2021-05-11

  Disclosed are methods for treating NMDA receptor-mediated disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. NMDA receptor-mediated disorders include autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders.

  所公开的是通过施用某些 NR2B 亚基选择性 NMDA（N 甲基-D 天门冬氨酸）拮抗剂来治疗 NMDA 受体介导的疾病的方法。NMDA 受体介导的疾病包括自闭症谱系障碍、强迫症和焦虑症。
• 3,3-DIFLUOROPIPERIDINE CARBAMATE HETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
  申请人：Shapiro Gideon

  公开号：US20180170935A1

  公开（公告）日：2018-06-21

  Disclosed are chemical entities of Formula (I), wherein R 1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
• TREATMENT OF AUTISM SPECTRUM DISORDERS, OBSESSIVE-COMPULSIVE DISORDER AND ANXIETY DISORDERS
  申请人：Rugen Holdings (Cayman) Limited

  公开号：US20190298725A1

  公开（公告）日：2019-10-03

  Disclosed are methods for treating NMDA receptor-mediated disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. NMDA receptor-mediated disorders include autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders.