N-(4-methyl-4-piperidinyl)acetamide monohydrochloride | 155928-36-2

• 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: N-(4-methyl-4-piperidinyl)acetamide monohydrochloride
• 英文别名: N-(4-methylpiperidin-4-yl)acetamide hydrochloride；N-(4-methylpiperidin-4-yl)acetamide;hydrochloride
• CAS: 155928-36-2
• 化学式: C₈H₁₆N₂O*ClH
• 分子量: 192.689
• InChiKey: UHYBGEICIXZGQQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.69
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  41.1
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(4-methyl-4-piperidinyl)acetamide monohydrochloride 、 5,7-dichloro-2-(2-chlorophenyl)-3-(4-chlorophenyl)pyrazolo[1,5-a]pyrimidine 在 三乙胺 作用下， 以 水 、 丙酮 为溶剂， 以40 mg的产率得到N-[1-[5-chloro-2-(2-chlorophenyl)-3-(4-chlorophenyl)pyrazolo[1,5-a]pyrimidin-7-yl]-4-methyl-4-piperidyl]acetamide
  参考文献：
  名称：

  [EN] PYRAZOLOPYRIMIDINES, COMPOSITIONS COMPRISING THEM AND USES THEREOF
  [FR] PYRAZOLOPYRIMIDINES, COMPOSITIONS LES COMPRENANT ET LEURS UTILISATIONS

  摘要：

  The present document relates to pyrazolopyrimidine compounds, pharmaceutical compositions comprising the same and their use in the treatment or prevention of diseases and disorders associated with the cannabinoid CB1receptor. For example, the pyrazolopyrimidine compounds, or a tautomeric form and/or salt thereof, are of Formula I: Formula I wherein R1to R4are as defined herein.

  公开号：

  WO2023155004A1
• 作为产物：
  描述：

  N-[1-(phenylmethyl)-4-methyl-4-piperidinyl]acetamide hydrochloride 在 钯 作用下， 以 甲醇 为溶剂， 生成 N-(4-methyl-4-piperidinyl)acetamide monohydrochloride
  参考文献：
  名称：

  4-amino-N-(4-methyl-4-piperidinyl)-2-methoxybenzamides for treating

  摘要：

  公开了化学式为##STR1##的哌啶基取代苯甲酰胺，其药学上可接受的酸盐和立体异构体形式，其中R.sup.1为氢或卤素; R.sup.2为卤素; R.sup.3为氢或卤素; R.sup.4和R.sup.5各自独立地为氢，C.sub.1-4烷基或卤代C.sub.1-4烷基; 基团NR.sup.4 R.sup.5也可以是偶氮基，Alk为C.sub.2-4烷二基; 包含上述化合物的制药组合物作为活性成分; 上述化合物作为药物的用途; 制备上述化合物的方法; 包含放射性同位素的化合物; 标记5HT.sub.2 -受体位点的方法; 以及成像器官的方法。

  公开号：

  US05498618A1

文献信息

• [EN] DOPAMINE D2 RECEPTOR LIGANDS<br/>[FR] LIGANDS DES RÉCEPTEURS DOPAMINERGIQUES D2
  申请人：BROAD INST INC

  公开号：WO2016100940A1

  公开（公告）日：2016-06-23

  The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0- arrestin pathway and/or on the cAMP pathway.

  本发明涉及新型多巴胺D2受体配体。该发明进一步涉及功能偏向的多巴胺D2受体配体以及利用这些化合物治疗或预防与多巴胺活性失调相关的中枢神经系统和全身性疾病。本发明涉及调节多巴胺D2受体的新型化合物。具体而言，本发明的化合物在多巴胺D2受体上显示功能选择性，并在D2受体下游、0-阿雷斯汀途径和/或cAMP途径上表现出选择性。
• 4-amino-N-(4-methyl-4-piperidinyl)-2-methoxybenzamides
  申请人：Janssen Pharmaceutica, N.V.

  公开号：US05688814A1

  公开（公告）日：1997-11-18

  Piperidinyl substituted benzamides of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is halo; R.sup.3 is hydrogen or halo; R.sup.4 and R.sup.5 each independently are hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl; and the group NR.sup.4 R.sup.5 may also be azido, Alk is C.sub.2-4 alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT.sub.2 -receptor sites; and process for imaging an organ are disclosed.

  式(I)中，Piperidinyl取代苯甲酰胺化合物及其药学上可接受的酸加成盐和立体异构体，其中R.sup.1为氢或卤素；R.sup.2为卤素；R.sup.3为氢或卤素；R.sup.4和R.sup.5各自独立地为氢，C.sub.1-4烷基或卤代C.sub.1-4烷基；以及基团NR.sup.4R.sup.5也可以是偶氮基，Alk是C.sub.2-4烷二基；包含上述式(I)化合物作为活性成分的制药组合物；所述化合物作为药物的用途；制备上述化合物的方法；含有放射性同位素的式(I)化合物；标记5HT.sub.2-受体位点的方法；以及成像器官的方法。
• 4-amino-n-(4-methyl-4-piperidinyl)-2-methoxybenzamides
  申请人：Janssen Pharmaceutica, N.V.

  公开号：US05691358A1

  公开（公告）日：1997-11-25

  Piperidinyl substituted benzamides of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is halo; R.sup.3 is hydrogen or halo; R.sup.4 and R.sup.5 each independently are hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl; and the group NR.sup.4 R.sup.5 may also be azido, Alk is C.sub.2-4 alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT.sub.2 -receptor sites; and process for imaging an organ are disclosed.

  公开了式子##STR1##中R.sup.1是氢或卤素; R.sup.2是卤素; R.sup.3是氢或卤素; R.sup.4和R.sup.5各自独立地是氢，C.sub.1-4烷基或卤代C.sub.1-4烷基; 而且NR.sup.4R.sup.5基团也可以是偶氮基，Alk是C.sub.2-4烷二基; 包含式(I)的化合物的药物学上可接受的酸盐和其立体异构体; 以该化合物作为药物的用途; 制备该化合物的过程; 具有放射性同位素的式(I)化合物; 标记5HT.sub.2-受体位点的过程; 以及成像器官的过程。
• Dopamine D2 receptor ligands
  申请人：The Broad Institute, Inc.

  公开号：US10633336B2

  公开（公告）日：2020-04-28

  The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and/or on the cAMP pathway.

  本发明涉及新型多巴胺D2受体配体。本发明进一步涉及具有功能偏倚的多巴胺 D2 受体配体，以及使用这些化合物治疗或预防与多巴胺能活性失调相关的中枢神经系统和全身性疾病。本发明涉及调节多巴胺 D2 受体的新型化合物。特别是，本发明的化合物在多巴胺 D2 受体上表现出功能选择性，并在 D2 受体下游、0-arrestin 通路和/或 cAMP 通路上表现出选择性。
• 4-AMINO-N --(4-METHYL-4-PIPERIDINYL)-2-METHOXYBENZAMIDES
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP0650475A1

  公开（公告）日：1995-05-03