6-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine | 1378853-27-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
• CAS: 1378853-27-0
• 化学式: C₁₂H₁₃N₃
• 分子量: 199.255
• InChiKey: JOFFITMMZBCCLO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  40.7
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-氯苯磺酰氯 、 6-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine 在 吡啶 、 水 、 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 生成 5-(4-chloro-benzenesulfonyI)-6-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
  参考文献：
  名称：

  Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors

  摘要：

  Discovery of a series of pyrazolopiperidine sulfonamide based gamma-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.02.039
• 作为产物：
  描述：

  在 三氟乙酸 作用下， 生成 6-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
  参考文献：
  名称：

  Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors

  摘要：

  Discovery of a series of pyrazolopiperidine sulfonamide based gamma-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.02.039

文献信息

• [EN] 5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES<br/>[FR] 5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES
  申请人：ELAN PHARM INC

  公开号：WO2007064914A2

  公开（公告）日：2007-06-07

  (EN) The invention provides N-cyclic sulfonamido compounds of Formula (I) wherein A, B, R1, R1a, R2, R2a, R3 and R3a are as described in the specification. Compounds of Formula (I) are useful in treating or preventing cognitive disorders, such as Alzheimer 's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I), methods of preparing compounds of formula (I), and methods of treating cognitive disorders, such as Alzheimer's disease.(FR) La présente invention concerne des composés de sulfonamido N-cycliques de formule (I) dans laquelle A, B, R1, R1a, R2, R2a, R3 et R3a sont tels que décrits dans le mémoire descriptif. Les composés de formule (I) sont utiles pour le traitement ou la prévention de troubles de la cognition tels que la maladie d'Alzheimer. L'invention concerne également des compositions pharmaceutiques qui comprennent des composés de formule (I), des procédés de préparation de composés de formule (I) et de procédés de traitement de troubles de la cognition tels que la maladie d'Alzheimer.