Piperidine, 1-[(aminooxy)acetyl]- | 741246-54-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: Piperidine, 1-[(aminooxy)acetyl]-
• 英文别名: 2-aminooxy-1-piperidin-1-ylethanone
• CAS: 741246-54-8
• 化学式: C₇H₁₄N₂O₂
• 分子量: 158.2
• InChiKey: KPDZFGWNUWLGOO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Piperidine, 1-[(aminooxy)acetyl]- 在 盐酸 作用下， 以 甲醇 为溶剂， 反应 1.0h， 以20.2 g的产率得到1-[(氨基氧基)乙酰基]-哌啶单盐酸盐
  参考文献：
  名称：

  Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

  摘要：

  Pochoximes are potent inhibitors of heat shock protein 90 (HSP90) based on the radicicol pharmacophores. Herein we present a pharmacokinetics and pharmacodynamics evaluation of this compound series as well as a phosphate prodrug strategy to facilitate formulation and improve oral bioavailability. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.04.030
• 作为产物：
  描述：

  2-(2-Oxo-2-piperidin-1-ylethoxy)isoindole-1,3-dione 在 甲基肼 作用下， 以 甲醇 为溶剂， 生成 Piperidine, 1-[(aminooxy)acetyl]-
  参考文献：
  名称：

  Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

  摘要：

  Pochoximes are potent inhibitors of heat shock protein 90 (HSP90) based on the radicicol pharmacophores. Herein we present a pharmacokinetics and pharmacodynamics evaluation of this compound series as well as a phosphate prodrug strategy to facilitate formulation and improve oral bioavailability. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.04.030

文献信息

• [EN] POCHOXIME CONJUGATES USEFUL FOR THE TREATMENT OF HSP90 RELATED PATHOLOGIES<br/>[FR] DÉRIVÉS DE POCHOXIME CONVENANT POUR LE TRAITEMENT DE PATHOLOGIES EN RAPPORT AVEC HSP90
  申请人：UNIV STRASBOURG

  公开号：WO2012052843A1

  公开（公告）日：2012-04-26

  The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharamceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90).

  本发明包括天然产物radicicol、pochonins、pochoximes的新颖衍生物、类似物和中间体，以及它们的合成方法。本发明还提供了一种包含本化合物的药物组合物，以及将该化合物用作激酶抑制剂和热休克蛋白90（HSP90）酶家族的用途。
• [EN] MACROCYCLIC PRODRUG COMPOUNDS USEFUL AS THERAPEUTICS<br/>[FR] COMPOSÉS DE PROMÉDICAMENTS MACROCYCLIQUES UTILISÉS COMME AGENTS THÉRAPEUTIQUES
  申请人：NEXGENIX PHARMACEUTICALS

  公开号：WO2009105755A3

  公开（公告）日：2009-11-12
• Macrocyclic prodrug compounds useful as therapeutics
  申请人：Nexgenix Pharmaceuticals

  公开号：EP2254880B1

  公开（公告）日：2016-08-17
• Macrocyclic Prodrug Compounds Useful as Therapeutics
  申请人：Heck James

  公开号：US20110190237A1

  公开（公告）日：2011-08-04

  The present invention includes macrocyclic prodrug compounds, pharmaceutical compositions containing them. The present invention also includes use of these compounds in the treatment of various diseases including an autoimmune disease, an inflammatory disease, a neurological or neurodegenerative disease, cancer, a cardiovascular disease, allergy, asthma, a hormone-related disease, and tumors or symptoms resulting from neurofibromatosis.
• POCHOXIME CONJUGATES USEFUL FOR THE TREATMENT OF HSP90 RELATED PATHOLOGIES
  申请人：Winssinger Nicolas

  公开号：US20140031302A1

  公开（公告）日：2014-01-30

  The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90).