哌啶-1-甲酰肼 | 107235-95-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 哌啶-1-甲酰肼
• 中文别名: 1-哌啶羧酸,酰肼(9CI)
• 英文名称: piperidine hydrazide
• 英文别名: Piperidine-1-carbohydrazide
• CAS: 107235-95-0
• 化学式: C₆H₁₃N₃O
• 分子量: 143.189
• InChiKey: JJFBQZGXZLCLRH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  58.4
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  哌啶-1-甲酰肼 、 氨甲酸,[(1S)-1-甲酰基戊基]-,1,1-二甲基乙基酯 在 4-甲基苯磺酸吡啶 作用下， 以 四氢呋喃 为溶剂， 生成 {(S)-1-[(piperidine-1-carbonyl)-hydrazonomethyl]-pentyl}-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

  摘要：

  Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.

  DOI：

  10.1016/j.bmcl.2005.10.108
• 作为产物：
  描述：

  1-哌啶酰氯 在 肼 作用下， 以 1,4-二氧六环 为溶剂， 生成 哌啶-1-甲酰肼
  参考文献：
  名称：

  Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

  摘要：

  Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.

  DOI：

  10.1016/j.bmcl.2005.10.108

文献信息

• [EN] PYRAZOLOPYRIMIDINONE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS DE PYRAZOLOPYRIMIDINONE ET LEURS UTILISATIONS
  申请人：ADURO BIOTECH INC

  公开号：WO2019055750A1

  公开（公告）日：2019-03-21

  The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

  本发明涉及吡唑吡咪啉酮化合物。本发明还涉及含有这些化合物的药物组合物，以及通过向需要的受试者施用这些化合物和药物组合物来治疗自身免疫、炎症和神经退行性疾病的方法。本发明还涉及利用这些化合物进行研究或其他非治疗目的的用途。
• Substituted Imidazole 4-Carboxamides as Cholecystokinin-1 Receptor Modulators
  申请人：Berger Richard

  公开号：US20090239862A1

  公开（公告）日：2009-09-24

  Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1, such as obesity, and diabetes.

  某些新型取代咪唑4-羧酰胺是人胆囊收缩素受体的配体，尤其是人胆囊收缩素-1受体（CCK-1R）的选择性配体。它们因此可用于治疗、控制或预防对CCK-1调节敏感的疾病和疾病，如肥胖症和糖尿病。
• Pyrazolopyrimidinone compounds and uses thereof
  申请人：Aduro BioTech, Inc.

  公开号：US10738056B2

  公开（公告）日：2020-08-11

  The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

  本发明涉及吡唑嘧啶酮化合物。本发明还涉及含有这些化合物的药物组合物，以及通过向有需要的受试者施用这些化合物和药物组合物来治疗自身免疫性、炎症性和神经退行性疾病的方法。本发明还涉及将这些化合物用于研究或其他非治疗目的。
• EP2010178A4
  申请人：——

  公开号：EP2010178A4

  公开（公告）日：2009-04-29
• SUBSTITUTED IMIDAZOLE 4-CARBOXAMIDES AS CHOLECYSTOKININ-1 RECEPTOR MODULATORS
  申请人：Merck & Co., Inc.

  公开号：EP2010178A2

  公开（公告）日：2009-01-07