N-(5-cyanopyridin-2-yl)-2-morpholinoacetamide | 1116016-07-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-(5-cyanopyridin-2-yl)-2-morpholinoacetamide
• 英文别名: N-(5-cyanopyridin-2-yl)-2-morpholin-4-ylacetamide
• CAS: 1116016-07-9
• 化学式: C₁₂H₁₄N₄O₂
• 分子量: 246.269
• InChiKey: IXSSBPCPSHYLRE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  78.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  吗啉 、 2-chloro-N-(5-cyanopyridin-2-yl)acetamide 反应 4.0h， 以56%的产率得到N-(5-cyanopyridin-2-yl)-2-morpholinoacetamide
  参考文献：
  名称：

  [EN] PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE
  [FR] DÉRIVÉS DE PYRIDYLE, LEUR PRÉPARATION ET UTILISATION.

  摘要：

  本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k）、哺乳动物雷帕霉素靶蛋白（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号的吡啶基衍生物。还公开了制备吡啶基衍生物的方法，以及它们在制造用于治疗由PI3K、mTOR和HIF-1α途径中的一个或多个信号通路失调引起的临床病症的药物组合物中的用途。吡啶基衍生物还可用于治疗由TNF-α介导的疾病或紊乱。

  公开号：

  WO2009019656A1

文献信息

• [EN] PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE<br/>[FR] DÉRIVÉS DE PYRIDYLE, LEUR PRÉPARATION ET UTILISATION.
  申请人：PIRAMAL LIFE SCIENCES LTD

  公开号：WO2009019656A1

  公开（公告）日：2009-02-12

  The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.

  本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k）、哺乳动物雷帕霉素靶蛋白（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号的吡啶基衍生物。还公开了制备吡啶基衍生物的方法，以及它们在制造用于治疗由PI3K、mTOR和HIF-1α途径中的一个或多个信号通路失调引起的临床病症的药物组合物中的用途。吡啶基衍生物还可用于治疗由TNF-α介导的疾病或紊乱。
• PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE
  申请人：Kumar Sanjay

  公开号：US20110077252A1

  公开（公告）日：2011-03-31

  The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.

  本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k）、哺乳动物雷帕霉素靶蛋白（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号的吡啶衍生物。还披露了制备吡啶衍生物的过程，并将其用于制造用于治疗由PI3K、mTOR和HIF-1α途径中一个或多个信号通路失调引起的临床情况的制药组合物。吡啶衍生物还可用于治疗由TNF-α介导的疾病或紊乱。
• Deore, Vijaykumar; Bhonde, Mandar R.; Vishwakarma, Ram A., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2009, vol. 48, # 12, p. 1761 - 1765
  作者：Deore, Vijaykumar、Bhonde, Mandar R.、Vishwakarma, Ram A.、Dagia, Nilesh M.、Kumar, Sanjay、Roychowdhury, Abhijit

  DOI：——

  日期：——
• US8314103B2
  申请人：——

  公开号：US8314103B2

  公开（公告）日：2012-11-20
• Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors
  作者：Vijaykumar Deore、Nilambari Yewalkar、Dimple Bhatia、Nikesh Desai、Ravindra D. Gupte、Shruta S. Dadarkar、Mahesh G. Jadhav、Aditi A. Tannu、Pooja Bhatt、Kumar V.S. Nemmani、Ram A. Vishwakarma、Somesh Sharma、Abhijit Roychowdhury、Nilesh M. Dagia、Mandar R. Bhonde、Sanjay Kumar

  DOI：10.1016/j.bmcl.2009.04.055

  日期：2009.6

  A series of novel cyanopyridyl based molecules (1-14) were designed, synthesized and probed for inhibition of mammalian target of rapamycin (mTOR) activity. Compound 14 was found to be a potent inhibitor of mTOR activity as assessed by enzyme-linked immunoassays and Western blot analysis. Most importantly, systemic application (intraperitoneal; ip) of compound 14 significantly suppressed macroscopic and histological abnormalities associated with chemically-induced murine colitis. (C) 2009 Elsevier Ltd. All rights reserved.