4-苯基哌啶-1-甲酰胺 | 16568-66-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 4-苯基哌啶-1-甲酰胺
• 英文名称: 4-phenyl-piperidinamide
• 英文别名: 4-Phenyl-1-piperidinecarboxamide；4-phenylpiperidine-1-carboxamide
• CAS: 16568-66-4
• 化学式: C₁₂H₁₆N₂O
• mdl: MFCD01701260
• 分子量: 204.272
• InChiKey: FZOKXDNYTHYNPE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.416
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-苯基哌啶-1-甲酰胺 、 1,1,1,3,3,3-hexafluoropropan-2-yl(fluorosulfonyl)carbamate 在 三乙烯二胺 作用下， 以 二氯甲烷 为溶剂， 以79 %的产率得到4-phenyl-N-((4-phenylpiperidin-1-yl)sulfonyl)piperidine-1-carboxamide
  参考文献：
  名称：

  N-氟磺酰基氨基甲酸六氟异丙酯：合成及其向磺胺酰脲的简便转化

  摘要：

  报道了六氟异丙基N-氟磺酰基氨基甲酸酯 (HFC)的合成及其向氨磺酰脲的简单转化。与具有腐蚀性和湿度敏感性的液体氯磺酰异氰酸酯（CSI）和氟磺酰异氰酸酯（FSI）不同，HFC为白色固体，表现出令人满意的工作台稳定性和独特的反应活性，这有利于其与胺的双重连接，直接提供一系列氨磺酰脲在环境条件下。值得注意的是，HFC 将作为实验室使用的 CSI 和 FSI 的有效替代品，特别是在温和条件下获取生物活性氨磺酰脲。

  DOI：

  10.1055/s-0043-1774860

文献信息

• [EN] AMINE COMPOUNDS<br/>[FR] DERIVES D'INDOLE SERVANT D'ANTAGONISTE DE SOMATOSTATINE
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2004046107A1

  公开（公告）日：2004-06-03

  The present invention provide a compound of the formula (I) wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.

  本发明提供了一种公式(I)的化合物，其中环A代表一个具有可选取代基的芳香环；B、Y和Ya相同或不同，分别代表一个键等；R1和R2相同或不同，每个代表一个氢原子等；R3代表一个氢原子等；R4和R5相同或不同，每个代表一个氢等；R6代表一个可选有取代基的吲哚基团；Z和Za相同或不同，每个代表一个氢原子等；或其盐或前药，具有生长抑素受体结合抑制活性，并且用于预防或治疗与生长抑素相关的疾病。
• 6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US20130085128A1

  公开（公告）日：2013-04-04

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5、R6和R7如下所示。式I的化合物是激酶抑制剂，适用于治疗与糖尿病及糖尿病并发症相关的疾病，如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变等。此外，本发明还涉及式I的化合物的用途，特别是作为药物中的活性成分以及包含它们的药物组合物。
• Compounds having growth hormone releasing activity
  申请人：——

  公开号：US20020151501A1

  公开（公告）日：2002-10-17

  Compounds that promote growth hormone releasing activity are disclosed. These compounds have the formula: A 1 -A 2 -X; A 1 -X′; or A 1 .-Y These compounds can be present in a pharmaceutical composition. The compounds can be used with a second compound that acts as an agonist at the growth hormone releasing hormone receptor or which inhibits the effects of somatostatin. These compounds can be used for a variety of uses such as treating hypothalamic pituitary dwarfism, osteoporosis, burns, or promoting wound healing.

  揭示了促进生长激素释放活性的化合物。这些化合物具有以下公式：A1-A2-X；A1-X′；或A1.-Y。这些化合物可以存在于药物组合物中。这些化合物可以与第二化合物一起使用，该化合物在生长激素释放激素受体上起作用或抑制生长抑素的作用。这些化合物可以用于治疗下丘脑垂体侏儒症、骨质疏松症、烧伤或促进伤口愈合等多种用途。
• [EN] 6-(4-HYDROXY-PHENYL)-3-ALKYL-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS D'AMIDE D'ACIDE 6-(4-HYDROXYPHÉNYL)-3-ALKYL-1H-PYRAZOLO[3,4-B] PYRIDINE-4-CARBOXYLIQUE UTILISÉS COMME INHIBITEURS DE KINASE
  申请人：SANOFI SA

  公开号：WO2013045413A1

  公开（公告）日：2013-04-04

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula (I), in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula (I) are protein kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式(I)的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5、R6和R7如下所示。式(I)的化合物是蛋白激酶C（PKC）抑制剂，并且对于治疗与糖尿病和糖尿病并发症相关的疾病，例如糖尿病肾病、糖尿病神经病和糖尿病视网膜病变等，非常有用。此外，本发明还涉及使用该式化合物，特别是作为药物中的活性成分，以及包含它们的制药组合物。
• [EN] SERINE/THREONINE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE SÉRINE/THRÉONINE KINASE
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2012118850A1

  公开（公告）日：2012-09-07

  Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

  具有公式I的化合物，其中Z，Z1，Z2，Z3，R3a，R3b和Rb如本文所定义，是ERK激酶抑制剂。还公开了用于治疗过度增殖性疾病的组合物和方法。