N'-hydroxy-4-[(trifluoromethyl)sulfonyl]benzenecarboximide amide | 928202-48-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N'-hydroxy-4-[(trifluoromethyl)sulfonyl]benzenecarboximide amide
• 英文别名: N'-hydroxy-4-[(trifluoromethyl)sulphonyl]benzenecarboximide amide；N'-hydroxy-4-[(trifluoromethyl)sulphonyl]benzenecarboximidamide；N'-hydroxy-4-(trifluoromethylsulfonyl)benzenecarboximidamide
• CAS: 928202-48-6
• 化学式: C₈H₇F₃N₂O₃S
• 分子量: 268.216
• InChiKey: WSTBAENJNBLZEB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  N'-hydroxy-4-[(trifluoromethyl)sulfonyl]benzenecarboximide amide 、 (2S,3S)-3-[(tert-butoxycarbonyl)aminol-2-methy]-4-oxo-4-pyrrolidin-1-ylbutanoic acid 在 N,N'-羰基二咪唑 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  发现有效的，选择性的和口服生物利用的基于恶二唑的二肽基肽酶IV抑制剂。

  摘要：

  一系列新的基于乙二唑的酰胺已被证明是有效的DPP-4抑制剂。优化的化合物43对多种DPP-4同源物显示出极好的选择性。

  DOI：

  10.1016/j.bmcl.2006.07.061

文献信息

• HETEROAROMATIC COMPOUNDS FOR USE AS HIF INHIBITORS
  申请人：Härter Michael

  公开号：US20110301122A1

  公开（公告）日：2011-12-08

  The present application relates to novel substituted aryl compounds, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.

  本申请涉及新型取代芳基化合物，其制备方法，它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病。这种治疗可以作为单独治疗进行，也可以与其他药物或进一步的治疗措施结合使用。
• Aryl compounds with aminoalkyl substituents and their use
  申请人：Härter Michael

  公开号：US20110312930A1

  公开（公告）日：2011-12-22

  The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.

  本申请涉及具有氨基烷基取代基的新型芳基化合物，涉及其制备方法，涉及它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物的用途，特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应低氧状态而引起的疾病。这种治疗可以作为单独治疗进行，也可以与其他药物或进一步的治疗措施结合使用。
• HETEROCYCLICALLY SUBSTITUTED ARYL COMPOUNDS AS HIF INHIBITORS
  申请人：Härter Michael

  公开号：US20130196964A1

  公开（公告）日：2013-08-01

  The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.

  本申请涉及具有杂环取代基的新型芳基化合物，其制备方法，它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病。这种治疗可以作为单独治疗进行，也可以与其他药物或进一步治疗措施结合使用。
• HETEROARYL SUBSTITUTED PYRAZOLE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
  申请人：Boyer Stephen

  公开号：US20100249085A1

  公开（公告）日：2010-09-30

  This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.

  本发明涉及新型杂环取代吡唑化合物、含有这些化合物的药物组合物以及用于治疗过度增殖和/或血管生成障碍的这些化合物或组合物的用途，作为单一药物或与其他活性成分或治疗措施联合使用。
• Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors
  作者：Scott D. Edmondson、Lan Wei、Jinyou Xu、Jackie Shang、Shiyao Xu、Jianmei Pang、Ashok Chaudhary、Dennis C. Dean、Huaibing He、Barbara Leiting、Kathryn A. Lyons、Reshma A. Patel、Sangita B. Patel、Giovanna Scapin、Joseph K. Wu、Maria G. Beconi、Nancy A. Thornberry、Ann E. Weber

  DOI：10.1016/j.bmcl.2008.02.050

  日期：2008.4

  The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.