美拉肼 | 13957-36-3

• 物质功能分类: 有机原料 - 肼或胲的有机衍生物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三嗪类
• 中文名称: 美拉肼
• 中文别名: 双乙胺三嗪肼
• 英文名称: tetra-N-ethyl-6-hydrazino-[1,3,5]triazine-2,4-diamine
• 英文别名: N²,N²,N⁴,N⁴-Tetraaethyl-6-hydrazino-[1,3,5]triazin-2,4-diyldiamin；meladrazine；2,4-bis(diaethylamino)-6-hydrazino-1,3,5-triazin；2-Hydrazino-4.6-bis-(diethylamino)-1.3.5-triazin；4,6-Bis-diethylamino-2-hydrazino-1,3,5-triazin；2-N,2-N,4-N,4-N-tetraethyl-6-hydrazinyl-1,3,5-triazine-2,4-diamine
• CAS: 13957-36-3
• 化学式: C₁₁H₂₃N₇
• mdl: MFCD00867684
• 分子量: 253.351
• InChiKey: IRQOBYXMACIFKD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.727
• 拓扑面积：
  83.2
• 氢给体数：
  2
• 氢受体数：
  7

安全信息

• 海关编码：
  2933699090

反应信息

• 作为反应物：
  描述：

  美拉肼 、 5-formyl-2'-deoxycytidine 在 溶剂黄146 作用下， 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  基于新型肼标记试剂的超灵敏测定稀有修饰的胞嘧啶

  摘要：

  修饰的胞嘧啶是重要的表观遗传标记，可在活生物体的多种细胞过程中发挥关键作用。但是，由于生物学样品中的丰度极低，稀有修饰的胞嘧啶的生物学功能，尤其是5-甲酰基胞嘧啶（5fC）和5-羧基胞嘧啶（5caC）的某些功能仍不清楚。在这项工作中，首先是一系列基于肼的新型试剂，该试剂以肼基为反应基团，疏水性三嗪基团和两个带有不同烷基链的易带电荷的叔胺基团来调节标记试剂的疏水性。探索标记稀有修饰的胞嘧啶，如5fC和5caC。5fC与标记试剂之间的衍生反应非常快，仅通过涡旋而无需额外的反应时间，就可以实现超过99％的衍生化效率。5fC的检测灵敏度随着标记试剂疏水性的增加而增加，其中最好的试剂显着提高了125倍。检测限低至10 amol，实现了对5fC的全基因组最敏感的整体定量。此外，标记试剂还成功地用于检测5caC，灵敏度提高了100倍。通过这种方法，我们仅使用约600 ng的基因组DNA就可以在不同的哺乳

  DOI：

  10.1021/acs.analchem.9b03227
• 作为产物：
  描述：

  可乐津 在 乙醇 、 一水合肼 作用下， 生成 美拉肼
  参考文献：
  名称：

  DE1018424

  摘要：

  公开号：

文献信息

• Hydroxylated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014733A1

  公开（公告）日：2007-01-18

  Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外，羟基化奈必洛尔代谢物，包括但不限于4-羟基-6,6'-二氟代-、4-羟基-5-苯酚-6,6'-二氟代-和4-羟基-8-苯并-6,6'-二氟代-，在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物，以及可药用的盐。此外，本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用，或作为单一治疗。
• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• SUBSTITUTED PHENYLCYCLOHEXYLGLYCOLATES
  申请人：Gant Thomas G.

  公开号：US20090247628A1

  公开（公告）日：2009-10-01

  Disclosed herein are substituted phenylcyclohexylglycolate-based muscarinic acetylcholine receptor modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

  本文揭示了基于取代苯基环己基甘醇酸酯的 Formula I 的肌氨酸乙酰胆碱受体调节剂，其制备方法、药物组合物及使用方法。
• Glucuronidated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014734A1

  公开（公告）日：2007-01-18

  This invention provides glucuronidated nebivolol metabolites and pharmaceutical compositions of glucuronidated nebivolol metabolites for treatment of cardiovascular diseases. In addition, this invention also provides compositions comprising nebivolol and/or at least one glucuronidated metabolite of nebivolol and/or at least one other active compound in a pharmaceutically acceptable carrier. This invention also provides methods of treating and/or preventing vascular diseases, by administering at least one glucuronidated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one glucuronidated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  这项发明提供了葡萄糖醛酸化的尼布ivolol代谢物以及用于治疗心血管疾病的葡萄糖醛酸化的尼布ivolol代谢物的制药组合物。此外，该发明还提供了包含尼布ivolol和/或至少一种尼布ivolol的葡萄糖醛酸化代谢物和/或至少一种其他活性化合物的药用可接受载体的组合物。该发明还提供了通过向受影响血管疾病的靶位点投与至少一种能释放治疗有效量一氧化氮的尼布ivolol的葡萄糖醛酸化代谢物来治疗和/或预防血管疾病的方法。此外，该发明旨在通过投与至少一种尼布ivolol的葡萄糖醛酸化代谢物来治疗和/或预防偏头痛。该发明还可与代谢综合征紊乱的单一治疗或联合治疗一起使用。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。