N-heptylpiperidin-4-amine | 1159687-29-2

• 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-heptylpiperidin-4-amine
• CAS: 1159687-29-2
• 化学式: C₁₂H₂₆N₂
• 分子量: 198.352
• InChiKey: USTRRNHNDBEFMQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  14
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  24.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-heptylpiperidin-4-amine 在 乙酰氯 作用下， 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  [35S]GTPγS binding studies of amphiphilic drugs-activated Gi proteins: A caveat

  摘要：

  This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTP gamma S to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTP gamma S and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results. (c) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.02.097
• 作为产物：
  描述：

  Tert-butyl 4-(heptylamino)piperidine-1-carboxylate 在 盐酸 作用下， 以 水 、 乙酸乙酯 为溶剂， 反应 12.0h， 以100%的产率得到N-heptylpiperidin-4-amine
  参考文献：
  名称：

  [35S]GTPγS binding studies of amphiphilic drugs-activated Gi proteins: A caveat

  摘要：

  This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTP gamma S to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTP gamma S and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results. (c) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.02.097

文献信息

• [EN] AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION<br/>[FR] DÉGRONIMÈRES DE C3-GLUTARIMIDE LIÉS À UNE AMINE POUR LA DÉGRADATION DE PROTÉINES CIBLES
  申请人：C4 THERAPEUTICS INC

  公开号：WO2017197051A1

  公开（公告）日：2017-11-16

  This invention provides amine-linked C3-glutarimide Degronimers and Degrons for therapeutic applications as described further herein, and methods of use and compositions thereof as well as methods for their preparation.

  这项发明提供了胺连接的C3-戊二酰亚胺Degronimers和Degrons，用于治疗应用，如本文进一步描述的，以及它们的使用方法、组合物以及它们的制备方法。
• [EN] C3-CARBON LINKED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION<br/>[FR] DÉGRONIMÈRES DE TYPE GLUTARIMIDE LIÉS AU CARBONE C3 POUR LA DÉGRADATION DE PROTÉINES CIBLES
  申请人：C4 THERAPEUTICS INC

  公开号：WO2017197046A1

  公开（公告）日：2017-11-16

  This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.

  这项发明提供了一种Degronimers，它具有碳连接的E3泛素连接酶靶向基团（Degrons），可以与一个靶向配体相连，该配体针对的是在体内被选为降解的蛋白质，以及它们的使用方法和组成，以及它们的制备方法。
• [EN] BROMODOMAIN TARGETING DEGRONIMERS FOR TARGET PROTEIN DEGRADATION<br/>[FR] DÉGRONIMÈRES CIBLANT UN BROMODOMAINE POUR LA DÉGRADATION DE PROTÉINES CIBLES
  申请人：C4 THERAPEUTICS INC

  公开号：WO2017197056A1

  公开（公告）日：2017-11-16

  This invention provides a Degronimer that has an E3 Ubiquitin Ligase targeting moiety (Degron) that can be linked to a Targeting Ligand for a bromodomain protein selected for in vivo degradation to achieve a therapeutic effect, and methods of use and compositions thereof as well as methods for their preparation.

  这项发明提供了一种Degronimer，它具有可与靶向配体连接的E3泛素连接酶靶向部位（Degron），该靶向配体选择用于体内降解溴结构域蛋白以实现治疗效果，并提供了使用方法、组合物以及它们的制备方法。
• [EN] HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN DEGRADATION<br/>[FR] DÉGRONIMÈRES HÉTÉROCYCLIQUES POUR LA DÉGRADATION DE PROTÉINES CIBLES
  申请人：C4 THERAPEUTICS INC

  公开号：WO2017197055A1

  公开（公告）日：2017-11-16

  This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) ("Degrons"), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.

  这项发明提供了结合到E3泛素连接酶（通常通过cereblon）的杂环化合物（“Degrons”），可以直接使用，也可以与靶向配体连接到选择的靶蛋白上，用于治疗目的，以及它们的使用方法、组合物以及制备方法。
• [35S]GTPγS binding studies of amphiphilic drugs-activated Gi proteins: A caveat
  作者：Dina Manetti、Lorenzo Di Cesare Mannelli、Silvia Dei、Luca Guandalini、Elisabetta Martini、Martina Banchelli、Carla Ghelardini

  DOI：10.1016/j.bmcl.2009.02.097

  日期：2009.4

  This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTP gamma S to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTP gamma S and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results. (c) 2009 Elsevier Ltd. All rights reserved.