1-(1-Ethyl-piperidin-4-yl)-1H-indole | 170364-85-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(1-Ethyl-piperidin-4-yl)-1H-indole
• 英文别名: 1-(1-Ethyl-piperidin-4-yl)-indole；1-(1-ethylpiperidin-4-yl)indole
• CAS: 170364-85-9
• 化学式: C₁₅H₂₀N₂
• 分子量: 228.337
• InChiKey: PFDCSCAAZRVKEE-UHFFFAOYSA-N

物化性质

• 沸点：
  364.6±35.0 °C(Predicted)
• 密度：
  1.09±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  8.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-(1-Ethyl-piperidin-4-yl)-1H-indole 在 三乙胺 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 8.0h， 生成 3-[1-(1-Ethyl-piperidin-4-yl)-indol-3-yl]-4-(1-methyl-indol-3-yl)-pyrrole-2,5-dione
  参考文献：
  名称：

  Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ

  摘要：

  The synthesis and structure-activity relationship (SAR) trends of a new class of N-(azacycloalkyl)bisindolylmaleimides 1, acyclic derivatives of staurosporine, is described. The representative compound for this series (1e) exhibits an IC50 of 40-50 nM against the human PKCbeta(1) and PKCbeta(2) isozymes and selectively inhibits the PKCbeta isozymes in comparison to other PKC isozymes (alpha, gamma, delta, epsilon, lambda, and eta). The series is also kinase selective for PKC in comparison to other ATP-dependent kinases. A comparison of the PKC isozyme and kinase activity of the series is made to the kinase inhibitor staurosporine. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00286-5
• 作为产物：
  描述：

  1-哌啶-4-基-1H-吲哚 、 对甲苯磺酸乙酯 在 potassium carbonate 作用下， 以 乙醇 为溶剂， 生成 1-(1-Ethyl-piperidin-4-yl)-1H-indole
  参考文献：
  名称：

  Protein kinase C inhibitors

  摘要：

  本发明公开了一般公式的化合物：##STR1## 这些化合物是高度异构酶选择性的蛋白激酶C beta-1和beta-2异构酶抑制剂。因此，本发明提供了一种选择性抑制蛋白激酶C异构酶beta-1和beta-2的方法。作为beta-1和beta-2的异构酶选择性抑制剂，这些化合物在治疗与糖尿病及其并发症相关的疾病状态以及与beta-1和beta-2异构酶升高相关的其他疾病状态方面具有治疗作用。

  公开号：

  US05545636A1

文献信息

• [EN] PROTEIN KINASE C INHIBITORS<br/>[FR] INHIBITEURS DE LA PROTEINE-KINASE C
  申请人：ELI LILLY AND COMPANY

  公开号：WO1995017182A1

  公开（公告）日：1995-06-29

  (EN) The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozymes.(FR) La présente invention décrit des composés qui sont des inhibiteurs des isozymes béta-1 et béta-2 de la protéine-kinase C, qui sont hypersélectifs des isozymes. En conséquence, la présente invention décrit un procédé d'inhibition sélective des isozymes béta-1 et béta-2 de la protéine-kinase C. En temps qu'inhibiteurs sélectifs des isozymes béta-1 et béta-2, ces composés sont thérapeutiquement utiles pour traiter des pathologies associées au diabète sucré et à ses complications, ainsi que d'autres états pathologiques associés à une élévation des isozymes béta-1 et béta-2.

  本发明揭示了高度特异的蛋白激酶C beta-1和beta-2同工酶抑制剂化合物。因此，本发明提供了一种选择性抑制蛋白激酶C同工酶beta-1和beta-2的方法。作为beta-1和beta-2的同工酶选择性抑制剂，这些化合物在治疗与糖尿病及其并发症相关的疾病状态以及与beta-1和beta-2同工酶升高相关的其他疾病状态方面具有治疗用途。
• 1,2,3-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THIER USE FOR THE TREATMENT OF PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
  申请人：Cid-Nunez Jose Maria

  公开号：US20120184525A1

  公开（公告）日：2012-07-19

  The present invention relates to novel triazolo[4,3- a ]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

  本发明涉及一种新型的三唑并[4,3-a]吡啶衍生物，其化学式为（I），其中所有基团均如权利要求中所定义。本发明中的化合物是代谢型谷氨酸受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体的mGluR2亚型的疾病。本发明还涉及包含这些化合物的制药组合物，制备这些化合物和组合物的过程，以及使用这些化合物预防或治疗涉及mGluR2的神经和精神障碍和疾病的方法。
• 1,2,4-Triazolo [4,3-A] Pyridine Derivatives and Their Use For The Treatment of Prevention of Neurological and Psychiatric Disorders
  申请人：JANSSEN PHARMACEUTICALS, INC.

  公开号：US20150141403A1

  公开（公告）日：2015-05-21

  The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

  本发明涉及一种新型的三唑并[4,3-a]吡啶衍生物，其化学式为（I），其中所有基团如权利要求所定义。本发明的化合物是代谢型谷氨酸受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。本发明还涉及包含这种化合物的制药组合物、制备这种化合物和组合物的过程，以及使用这种化合物预防或治疗涉及mGluR2的神经和精神障碍和疾病的方法。
• Protein Kinase C Inhibitors
  申请人：ELI LILLY AND COMPANY

  公开号：EP1449529A1

  公开（公告）日：2004-08-25

  The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.

  本发明公开了具有高度同工酶选择性的蛋白激酶 C β-1和β-2同工酶抑制剂化合物。因此，本发明提供了一种选择性抑制蛋白激酶 C 同工酶 beta-1 和 beta-2 的方法。作为β-1和β-2的同工酶选择性抑制剂，这些化合物在治疗与糖尿病及其并发症有关的病症以及与β-1和β-2同工酶升高有关的其他疾病状态方面具有治疗作用。
• PROTEIN KINASE C INHIBITORS
  申请人：ELI LILLY AND COMPANY

  公开号：EP0817627A1

  公开（公告）日：1998-01-14