N-(1-phenethylpiperidin-4-yl)propionamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(1-phenethylpiperidin-4-yl)propionamide
• 英文别名: N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
• 化学式: C₁₆H₂₄N₂O
• 分子量: 260.379
• InChiKey: QYNQIJZXBWWVMO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(1-phenethylpiperidin-4-yl)propionamide 、 草酸 以to obtain N-(1 -phenethylpip eridin-4-yl)propionamide oxalate的产率得到N-(1-phenethylpiperidin-4-yl)propionamide oxalate
  参考文献：
  名称：

  Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation

  摘要：

  该发明提供了与μ-, δ-和κ-阿片受体以及α2-肾上腺素受体高亲和力结合的化合物。除了提供这些具有新型药理学结合特性的化合物外，该发明还描述了制备代表性化合物的详细新方法，并提供了一种合成与阿片受体和/或α2-肾上腺素受体结合的相关化合物的方案。

  公开号：

  US20160052882A1
• 作为产物：
  描述：

  N-(2-苯乙基)-4-哌啶酮 在 羟胺 、 sodium 、 三乙胺 作用下， 以 乙醇 、 异戊醇 、 氯仿 、 水 为溶剂， 反应 2.0h， 生成 N-(1-phenethylpiperidin-4-yl)propionamide
  参考文献：
  名称：

  [EN] SMALL MOLECULE ADRENORECEPTOR ANTAGONISTS AND USES THEREOF
  [FR] ANTAGONISTES D'ADRÉNORÉCEPTEUR À PETITES MOLÉCULES ET LEURS UTILISATIONS

  摘要：

  This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a piperdinyl-formamide (or similar) structure which function as adrenoreceptor antagonists, and their use as therapeutics for the treatment and/or prevention of pain and related conditions. In addition, the present invention provides compositions comprising a mixture of opioid receptor agonist compounds and such adrenoreceptor antagonists for the treatment and/or prevention of pain and related conditions.

  公开号：

  WO2023133135A2

文献信息

• [EN] HYDROPHILIC FENTANYL DERIVATIVES<br/>[FR] DÉRIVÉS DE FENTANYLE HYDROPHILES
  申请人：ALLEGHENY-SINGER RES INST

  公开号：WO2017041095A1

  公开（公告）日：2017-03-09

  Various fentanyl derivatives are described. The derivatives exhibit high binding affinity to opioid receptors, but also have decreased blood brain permeability as compared to standard fentanyl. This, the resulting derivatives can be less addictive than standard fentanyl. Methods of making such derivatives are also disclosed in this document.

  描述了各种芬太尼衍生物。这些衍生物具有高结合亲和力与阿片受体，但与标准芬太尼相比，它们的血脑屏障透过性降低。因此，由此产生的衍生物可能比标准芬太尼更不容易上瘾。本文档还披露了制作这些衍生物的方法。
• [EN] PIPERIDINYLALKYLAMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN<br/>[FR] DÉRIVÉS DE PIPÉRIDINYLALKYLAMIDE AYANT UNE ACTIVITÉ MULTIMODALE CONTRE LA DOULEUR
  申请人：ESTEVE LABOR DR

  公开号：WO2017178515A1

  公开（公告）日：2017-10-19

  The present invention relates to piperidinylalkylamide derivatives having dual pharmacological activity towards both the sigma (σ) receptor and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

  本发明涉及具有对σ受体和μ-阿片受体双重药理活性的哌啶基烷酰胺衍生物，以及制备这类化合物的方法、包含它们的药物组合物，以及它们在治疗中的应用，特别是用于疼痛治疗。
• Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation
  申请人：The Arizona Board of Regents of Behalf of the University of Arizona

  公开号：US20160052882A1

  公开（公告）日：2016-02-25

  The invention provides compounds that bind with high affinities to the μ-, δ-and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.

  该发明提供了与μ-, δ-和κ-阿片受体以及α2-肾上腺素受体高亲和力结合的化合物。除了提供这些具有新型药理学结合特性的化合物外，该发明还描述了制备代表性化合物的详细新方法，并提供了一种合成与阿片受体和/或α2-肾上腺素受体结合的相关化合物的方案。
• Anaesthetic composition
  申请人：Anaquest, Inc.

  公开号：EP0256798A1

  公开（公告）日：1988-02-24

  An injectable anaesthetic pharmaceutical composition which does not exhibit muscle rigidity to any substantial degree includes an effective to induce anaesthesia of at least one substituted N-(4-piperidinyl)-N-amide and an amount effective to inhibit muscle rigidity of at least one alpha-2 adrenergic agonist as principle ingredients. Typically, the composition comprises a solution of fentanyl and clonidine. The clonidine reduces the amount of fentanyl that is required to induce anaesthesia.

  一种可注射的麻醉药物组合物，它不会在很大程度上表现出肌肉僵硬，其主要成分包括至少一种有效诱导麻醉的取代N-(4-哌啶基)-N-酰胺和至少一种有效抑制肌肉僵硬的α-2肾上腺素能激动剂。 通常，该组合物包括芬太尼和氯尼替胺的溶液。 氯尼替胺可减少诱导麻醉所需的芬太尼用量。
• 1-arylalkyl-4-acylaminopiperidine compounds
  申请人：ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

  公开号：US10617681B2

  公开（公告）日：2020-04-14

  The present invention provides a compound of the formula: wherein ring Z is a 5-, 6- or 7-membered ring; R1 is C1-10 alkyl, C1-10 haloalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heteroaralkyl; R2 is C1-10 alkylene; and Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(═O)—X1, wherein X1 is —OR3 or —NR4R5, where each of R3, R4 and R5 is H or C1-10 alkyl. The present invention also provides a method for using compound of Formula I to treat a wide variety of clinical conditions.

  本发明提供了一种式化合物： 式中 环 Z 是 5、6 或 7 元环； R1 是 C1-10 烷基、C1-10 卤代烷基、任选取代的芳基、任选取代的芳烷基、任选取代的杂芳基或任选取代的杂烷基； R2 是 C1-10 亚烷基；以及 Y 是任选取代的芳基、任选取代的杂芳基或式-C(═O)-X1 的分子，其中 X1 是-OR3 或-NR4R5，其中 R3、R4 和 R5 各为 H 或 C1-10 烷基。 本发明还提供了一种使用式 I 化合物治疗多种临床疾病的方法。