| 940925-47-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• CAS: 940925-47-3
• 化学式: C₁₇H₂₁N₃O₂
• 分子量: 299.37
• InChiKey: HRNNWJHAGDNBQH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  58.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  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
• 作为产物：
  描述：

  Tert-butyl 5-formyl-4-oxo-2-phenylpiperidine-1-carboxylate 在 一水合肼 作用下， 以 甲醇 为溶剂， 生成
  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

• 5-(Arylsulfonyl)-Pyrazolopiperidines
  申请人：Ye Michael Xiaocong

  公开号：US20070155753A1

  公开（公告）日：2007-07-05

  The invention provides N-cyclic sulfonamido compounds of Formula I wherein A, B, R 1, R 1a, R 2 , R 2a, R 3 and R 3a 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.

  本发明提供了式I的N-环磺酰胺化合物，其中A、B、R1、R1a、R2、R2a、R3和R3a如规范中所述。式I的化合物在治疗或预防认知障碍，如阿尔茨海默病方面是有用的。本发明还包括含有式I的制药组合物、制备式I化合物的方法，以及治疗认知障碍，如阿尔茨海默病的方法。
• 5-(arylsulfonyl)-pyrazolopiperidines
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US07732609B2

  公开（公告）日：2010-06-08

  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.

  本发明提供了公式I中的N-环磺酰胺化合物，其中A、B、R1、R1a、R2、R2a、R3和R3a如规范中所述。公式I的化合物在治疗或预防认知障碍，如阿尔茨海默病方面有用。本发明还包括包含公式I化合物的制药组合物，制备公式I化合物的方法，以及治疗认知障碍，如阿尔茨海默病的方法。
• [EN] 5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES<br/>[FR] 5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES
  申请人：ELAN PHARM INC

  公开号：WO2007064914A3

  公开（公告）日：2007-12-27
• US7732609B2
  申请人：——

  公开号：US7732609B2

  公开（公告）日：2010-06-08
• Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors
  作者：Xiaocong M. Ye、Andrei W. Konradi、Jenifer Smith、Ying-Zi Xu、Darren Dressen、Albert W. Garofalo、Jennifer Marugg、Hing L. Sham、Anh P. Truong、Jacek Jagodzinski、Michael Pleiss、Hongbin Zhang、Erich Goldbach、John-Michael Sauer、Elizabeth Brigham、Michael Bova、Guriqbal S. Basi

  DOI：10.1016/j.bmcl.2010.02.039

  日期：2010.4

  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.