s-Triazolo<4,3-a>chinoxalin-1(2H)on | 19848-93-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: s-Triazolo<4,3-a>chinoxalin-1(2H)on
• 英文别名: 3-Oxo-1,2,4-triazol-2H-benzopyrazin；2H-[1,2,4]triazolo[4,3-a]quinoxalin-1-one；[1,2,4]triazolo[4,3-a]quinoxalin-1(2H)-one；2H-[1,2,4]triazolo[4,3-a]quinoxalin-1-one
• CAS: 19848-93-2
• 化学式: C₉H₆N₄O
• mdl: MFCD14729475
• 分子量: 186.173
• InChiKey: NBXOKUUXBOFVIJ-UHFFFAOYSA-N

物化性质

• 密度：
  1.63±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  57.1
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Selective antagonists of A2A adenosine receptors
  申请人：Beauglehole Anthony

  公开号：US20090118309A1

  公开（公告）日：2009-05-07

  The present invention provides compounds of formulae Ia and Ib: wherein R 1-5 , Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A 2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.

  本发明提供了式子Ia和Ib的化合物：其中R1-5，Q，X，Y，Z，p，q和r的定义如本文所述。这些化合物是A2A腺苷受体（ARs）的有效和选择性拮抗剂。该发明还包括含有这些化合物的制药组合物和使用它们的方法。
• SELECTIVE ANTAGONISTS OF A2A ADENOSINE RECEPTORS
  申请人：BEAUGLEHOLE Anthony

  公开号：US20120035192A1

  公开（公告）日：2012-02-09

  The present invention provides compounds of formulae Ia and Ib: wherein R 1-5 , Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A 2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.

  本发明提供了式Ia和Ib的化合物：其中R1-5，Q，X，Y，Z，p，q和r的定义如本文所述。这些化合物是A2A腺苷受体（ARs）的有效和选择性拮抗剂。本发明还包括含有这些化合物的药物组合物以及使用它们的方法。
• Treatment of demyelinating disorders
  申请人：——

  公开号：US20040204347A1

  公开（公告）日：2004-10-14

  This invention is directed to pharmaceutical compositions and methods for treating demyelinating disorders based upon inhibitors of the interaction of glutamate with the AMPA and of the interaction of glutamate with the kainate receptor complex.

  本发明涉及治疗脱髓鞘疾病的药物组合物和方法，其基础是抑制谷氨酸与 AMPA 的相互作用以及谷氨酸与 kainate 受体复合物的相互作用的抑制剂。
• Enhancing treatment of cancer and HIF-1 mediated disorders with adenosine A3 receptor antagonists
  申请人：Borea Andrea Pier

  公开号：US20060204502A1

  公开（公告）日：2006-09-14

  The present invention relates to the use of adenosine receptor antagonists, preferably A 3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with overexpression of HIF-1α and/or increased HIF-1α activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1α (HIF-1α) using the A 3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.

  本发明涉及使用腺苷受体拮抗剂，最好是 A 3 受体拮抗剂，单独或与其他制剂联合用于治疗、预防和/或控制与 HIF-1α 过度表达和/或 HIF-1α 活性增加有关的疾病或紊乱（如癌症、呼吸系统疾病）。本发明的方法和组合物特别适用于预防、治疗或改善与缺氧诱导因子 1α （HIF-1α）相关的癌症、疾病或失调有关的症状。 3 受体拮抗剂。本发明提供了抑制肿瘤，特别是实体瘤，更特别是缺氧性肿瘤生长的方法。
• [1,2,4]TRIAZOLO[4,3-a]QUINOXALINONE DERIVATIVES, THEIR PREPARATION AND USE
  申请人：NOVO NORDISK A/S

  公开号：EP0781282B1

  公开（公告）日：1999-08-11