pyrido[3,4-b]pyrazin-5-amine | 859295-23-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶吡嗪类
• 英文名称: pyrido[3,4-b]pyrazin-5-amine
• CAS: 859295-23-1
• 化学式: C₇H₆N₄
• mdl: MFCD09839070
• 分子量: 146.151
• InChiKey: YVOLUPPVPQLTHT-UHFFFAOYSA-N

物化性质

• 熔点：
  187-188 °C(Solv: water (7732-18-5))
• 沸点：
  352.2±37.0 °C(Predicted)
• 密度：
  1.385±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  64.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  pyrido[3,4-b]pyrazin-5-amine 、 三光气 、 (4S)-7-(2-methylpyridin-4-yl)-2,3,4,5-tetrahydro-1,4-methanopyrido[2,3-b][1,4]diazepine 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 17.0h， 以38%的产率得到(4S)-7-(2-methylpyridin-4-yl)-N-(pyrido[3,4-b]pyrazin-5-yl)-3,4-dihydro-1,4-methanopyrido[2,3-b][1,4]diazepine-5(2H)-carboxamide
  参考文献：
  名称：

  [EN] SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
  [FR] ANALOGUES D'URÉE PONTÉS SUBSTITUÉS EN TANT QUE MODULATEURS DE SIRTUINE

  摘要：

  本发明涉及一种新型的取代桥式脲类似物化合物，其化学式为（I）或其药学上可接受的盐，相应的药物组合物，制备这种化合物的方法以及单独使用或与其他治疗剂联合使用的这些化合物作为Sirtuin调节剂，可用于增加细胞寿命，并用于治疗和/或预防各种疾病和紊乱，包括但不限于与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块紊乱、炎症、癌症和/或潮红有关的疾病或紊乱，以及那些会受益于增加线粒体活性的疾病或紊乱。

  公开号：

  WO2016079709A1
• 作为产物：
  描述：

  2,3,4-三氨基吡啶 、 草酸醛 生成 pyrido[3,4-b]pyrazin-5-amine
  参考文献：
  名称：

  Koegl et al., Recueil des Travaux Chimiques des Pays-Bas, 1948, vol. 67, p. 29,37

  摘要：

  DOI：

文献信息

• SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
  申请人：GLAXOSMITHKLINE LLC

  公开号：US20150152108A1

  公开（公告）日：2015-06-04

  The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

  本发明涉及新型取代桥式脲化合物，相应的相关类似物，药物组合物以及其使用方法。本发明的抑制素调节化合物可用于延长细胞寿命，并治疗和/或预防各种疾病和疾病，包括但不限于与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块疾病、炎症、癌症和/或潮红有关的疾病或疾病，以及那些会受益于增加线粒体活性的疾病或疾病。本发明还涉及包含抑制素调节化合物与另一治疗剂组合的组合物。
• Substituted bridged urea analogs as sirtuin modulators
  申请人：GLAXOSMITHKLINE LLC

  公开号：US10590135B2

  公开（公告）日：2020-03-17

  The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

  本发明涉及新型取代桥基脲化合物、相应的相关类似物、药物组合物及其使用方法。本发明的Sirtuin调节化合物可用于增加细胞的寿命，治疗和/或预防多种疾病和失调，这些疾病和失调包括但不限于例如与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、凝血障碍、炎症、癌症和/或潮红有关的疾病或失调，以及将受益于线粒体活性增加的疾病或失调。本发明还涉及由sirtuin调节化合物与另一种治疗剂组合而成的组合物。
• 972. Analogues of 8-hydroxyquinoline having additional cyclic nitrogen atoms. Part I. Preparative
  作者：Adrien Albert、Alexander Hampton

  DOI：10.1039/jr9520004985

  日期：——
• US9834558B2
  申请人：——

  公开号：US9834558B2

  公开（公告）日：2017-12-05
• [EN] SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS<br/>[FR] ANALOGUES D'URÉE PONTÉS SUBSTITUÉS UTILISÉS COMME MODULATEURS DE LA SIRTUINE
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2016081692A2

  公开（公告）日：2016-05-26

  The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.