5-amino-1H-pyrazol-2-ium-4-carboxamide;sulfate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-amino-1H-pyrazol-2-ium-4-carboxamide;sulfate
• 化学式: C8H14N8O6S
• 分子量: 350.32
• InChiKey: UMPKASYMNORSRO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.47
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  279
• 氢给体数：
  8
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  5-amino-1H-pyrazol-2-ium-4-carboxamide;sulfate 在 甲酰胺 、 水 、 丙酮 、 crude product 、 sodium hydroxide 、 甲烷 、 盐酸 作用下， 以 甲酰胺 为溶剂， 反应 5.0h， 生成 别嘌醇
  参考文献：
  名称：

  Method of preparing 3-morpholino-2-cyanoacrylamide

  摘要：

  一种化合物##STR1##其中R'为氢或低碳基，该化合物可用作制备4-羟基吡唑并[3,4-d]嘧啶（丙戊酸）及其有用衍生物的中间体。一种制备##STR2##的方法，包括反应R'C（OR）.sub.3，吗啉和氰乙酰胺，其中R'为氢或低碳基，R'为低碳基。

  公开号：

  US04146713A1

文献信息

• Phenyl-triazole compounds for PDE-IV inhibition
  申请人：Euro-Celtique S.A.

  公开号：US06248769B1

  公开（公告）日：2001-06-19

  Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: where R1, R2, R3, R4, X1, X2 and Z are described herein. The compounds possess improved PDE IV inhibition as compared to rolipram as well as with improved selectivity with regard to PDE III inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

  本发明揭示了一种有效的PDE IV抑制剂新化合物。这些化合物具有以下一般结构：其中R1、R2、R3、R4、X1、X2和Z的描述如下。与洛利普兰相比，这些化合物具有改善的PDE IV抑制作用，并具有改善的PDE III抑制选择性。本发明还揭示了含有该化合物的制药组合物和治疗方法。
• Aryl imidazole compounds having phosphodiesterase IV inhibitory activity
  申请人：Euro-Celtique S.A.

  公开号：US06103749A1

  公开（公告）日：2000-08-15

  Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2 and Z are described herein. The compounds possess improved PDE IV inhibition as compared to rolipram as well as with improved selectivity with regard to PDE III inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

  本发明揭示了有效的PDE IV抑制剂的新型化合物。这些化合物具有以下的一般结构：##STR1## 其中R.sub.1、R.sub.2、R.sub.3、R.sub.4、X.sub.1、X.sub.2和Z的含义如本文所述。与Rolipram相比，这些化合物具有更好的PDE IV抑制作用，并具有更好的选择性，不会抑制PDE III。本发明还揭示了含有这些化合物的药物组合物和治疗方法。
• Bridged N-Cyclic Sulfonamido Inhibitors of Gamma Secretase
  申请人：Bowers Simeon

  公开号：US20080090817A1

  公开（公告）日：2008-04-17

  The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R 1 and R 2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.

  本发明提供了N-环状磺酰胺化合物和公式I的盐：其中A如规范所述，而R1和R2组合形成[3.3.1]或[3.2.1]环系统，其中氮连接到两个桥头碳，并且[3.3.1]或[3.2.1]环系统可以与杂环芳基或杂环烷基环融合。公式I的化合物可用于治疗或预防认知障碍，如阿尔茨海默病。本发明还包括包含公式I化合物的制药组合物，治疗认知障碍的方法，如阿尔茨海默病，以及制备公式I化合物的中间体。
• Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods
  申请人：Euro-Celtique, S.A.

  公开号：US05922751A1

  公开（公告）日：1999-07-13

  Novel compounds which are effective PDE IV inhibitors are disclosed The compounds possess similar or improved PDE IV inhibition as compared to rolipram, with improved selectivity with regard to, e.g., PDE III inhibition. Preferred compounds are 3-(3-cyclopentyloxy-4-methoxy-benzylamino)-4-hydroxymethyl pyrazole and 3-(3-cyclopentyloxy-4-methoxybenzylamino)-4-methoxymethylpyrazole.

  本发明公开了一种有效的PDE IV抑制剂新化合物。这些化合物具有与罗利普兰相似或改进的PDE IV抑制作用，并具有改进的选择性，例如对PDE III抑制作用的选择性。优选的化合物为3-（3-环戊氧基-4-甲氧基苯基甲氨基）-4-羟甲基吡唑和3-（3-环戊氧基-4-甲氧基苯基甲氨基）-4-甲氧甲基吡唑。
• Bridged N-cyclic sulfonamido inhibitors of gamma secretase
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US07345056B2

  公开（公告）日：2008-03-18

  The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.

  本发明提供了公式I的N-环磺酰胺化合物和盐，其中A如规范所述，R1和R2结合形成[3.3.1]或[3.2.1]环系统，其中氮原子连接到两个桥头碳原子，并且[3.3.1]或[3.2.1]环系统可以与杂环芳基或杂环烷基环融合。公式I的化合物可用于治疗或预防认知障碍，如阿尔茨海默病。本发明还包括包含公式I化合物的制药组合物，治疗认知障碍的方法，如阿尔茨海默病，以及制备公式I化合物的中间体。

表征谱图