4-(4-oxo-1-piperidin-1-yl)benzamide | 340756-87-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-(4-oxo-1-piperidin-1-yl)benzamide
• 英文别名: 4-(4-Oxopiperidin-1-yl)benzamide
• CAS: 340756-87-8
• 化学式: C₁₂H₁₄N₂O₂
• 分子量: 218.255
• InChiKey: FRHJTBMHMNUPCR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  63.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(4-oxo-1-piperidin-1-yl)benzamide 、 N-[5-((1R)-2-amino-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methanesulfonamide 生成 4-{4-[(2R)-2-hydroxy-2-(4-hydroxy-3-methanesulfonylamino-phenyl)-ethylamino]-piperidin-1-yl}-benzamide
  参考文献：
  名称：

  Cyclic amine phenyl beta-3 adrenergic receptor agonists

  摘要：

  本发明提供了具有以下结构的化合物I，其中R1、R2、R3、R4、R5、T、T1、T2和X如前所定义，或其药学上可接受的盐，其在治疗或抑制与胰岛素抵抗或高血糖相关的代谢性疾病（通常与肥胖或葡萄糖耐受性不良有关）、动脉粥样硬化、胃肠道疾病、神经遗传性炎症、青光眼、眼压增高和频繁排尿方面非常有用；并且在治疗或抑制2型糖尿病方面特别有用。

  公开号：

  US07022716B2
• 作为产物：
  描述：

  4-(1,4-dioxa-8-aza-spiro[4.5]dec-8-yl)-benzonitrile 在 盐酸 作用下， 以82%的产率得到4-(4-oxo-1-piperidin-1-yl)benzamide
  参考文献：
  名称：

  (4-Piperidin-1-yl)phenyl Amides:  Potent and Selective Human β₃ Agonists

  摘要：

  In search of potent and selective human beta (3) agonists as potential drugs for the treatment of human obesity and type II diabetes, a series of (4-piperidin-1-yl)phenyl amides was prepared and evaluated for their biological activity on the human beta (3)-adrenergic receptor. The leucine derivative 26e and the reverse amide 33b were found to be the two most potent and selective compounds in this study. With EC50 values of 0.008 and 0.009 muM, respectively, at the beta (3) receptor, nearly completely abolished intrinsic activity at either the beta (1) or beta (2) receptor, and significant thermogenesis effects on human beta (3)-adrenergic receptor transgenic mice, 26e and 33b are among the most potent and selective human beta (3) agonists known to date.

  DOI：

  10.1021/jm000544b

文献信息

• Benzimidazole-derivatives as factor Xa inhibitors
  申请人：Nazare Marc

  公开号：US20050009829A1

  公开（公告）日：2005-01-13

  The present invention relates to compounds of the formula I, wherein R 0 , R 1 , R 2 , Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及式I的化合物，其中R0、R1、R2、Q、V、G和M如本文所定义。式I的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓作用，适用于心血管疾病如血栓栓塞病或再狭窄的治疗和预防。它们是血凝酶酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以应用于存在因子Xa和/或因子VIIa的不良活性或者需要抑制因子Xa和/或因子VIIa以治疗或预防的情况。此外，本发明还涉及制备式I的化合物的方法，它们的使用，尤其是作为药物的活性成分，以及包含它们的制药制剂。
• CYCLIC AMINE PHENYL BETA-3 ADRENERGIC RECEPTOR AGONISTS
  申请人：Wyeth

  公开号：EP1301482A1

  公开（公告）日：2003-04-16
• BENZIMIDAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1636216A1

  公开（公告）日：2006-03-22
• JP2006528213A
  申请人：——

  公开号：JP2006528213A

  公开（公告）日：2006-12-14
• 第Ｘａ因子阻害剤としてのベンゾイミダゾール誘導体
  申请人：サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング

  公开号：JP4658940B2

  公开（公告）日：2006-12-14