4-(4-bromophenylamino)-piperidine | 862652-46-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-(4-bromophenylamino)-piperidine
• 英文别名: N-(4-bromophenyl)piperidin-4-amine
• CAS: 862652-46-8
• 化学式: C₁₁H₁₅BrN₂
• mdl: MFCD12822106
• 分子量: 255.157
• InChiKey: BQRJDKYBLYPKSY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  24.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(4-bromophenylamino)-piperidine 在 Pd catalyst 、 三乙酰氧基硼氢化钠 、 sodium carbonate 、 溶剂黄146 作用下， 以 二氯甲烷 为溶剂， 反应 24.0h， 生成 (3'-Chloro-biphenyl-4-yl)-(1-cyclopentyl-piperidin-4-yl)-amine
  参考文献：
  名称：

  Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

  摘要：

  Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure-activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound I exhibited oral efficacy in chronic (28 d) rodent models at 3-30 mpk showing significant reduction in food intake and weight gain relative to controls.

  DOI：

  10.1021/jm0503852
• 作为产物：
  描述：

  1-Boc-4-(4-溴苯氨基)-哌啶 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 4-(4-bromophenylamino)-piperidine
  参考文献：
  名称：

  Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

  摘要：

  Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure-activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound I exhibited oral efficacy in chronic (28 d) rodent models at 3-30 mpk showing significant reduction in food intake and weight gain relative to controls.

  DOI：

  10.1021/jm0503852

文献信息

• [EN] 1, 4-SUBSTITUTED PIPERIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE PIPÉRIDINE 1,4-SUBSTITUÉS
  申请人：CEPHALON INC

  公开号：WO2016205633A1

  公开（公告）日：2016-12-22

  Described herein are 1,4-substituted piperidine compounds according to Formula (I) that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

  本文描述了按照式（I）的1,4-取代哌啶化合物，这些化合物已经表现出作为脂肪酸合成酶抑制剂的活性。本文还描述了含有所述1,4-取代哌啶化合物的药物组合物，以及通过给予所述化合物或药物配方中的一个或多个来治疗由脂肪酸合成酶介导的疾病的方法。本文还描述了合成所述化合物的方法，包括所述的1,4-取代哌啶化合物和在这些合成中有用的合成中间体。
• 1,4-substituted piperidine derivatives
  申请人：89BIO LTD

  公开号：US10221135B2

  公开（公告）日：2019-03-05

  Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

  本文描述了根据式 I 的 1,4-取代的哌啶化合物，这些化合物已被证明具有脂肪酸合酶抑制剂的活性。本文还描述了含有所述 1,4-取代哌啶化合物的药物组合物，以及通过施用一种或多种本文所述化合物或药物制剂治疗由脂肪酸合成酶介导的疾病的方法。本文还描述了合成所述化合物的方法，包括所述 1,4-取代的哌啶化合物和用于这些合成的合成中间体。
• 1, 4-SUBSTITUTED PIPERIDINE DERIVATIVES
  申请人：89Bio Ltd.

  公开号：EP3310441B1

  公开（公告）日：2020-07-29
• 1,4-SUBSTITUTED PIPERIDINE DERIVATIVES
  申请人：Cephalon, Inc.

  公开号：US20160368874A1

  公开（公告）日：2016-12-22

  Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.
• 1,4-Substituted Piperidine Derivatives
  申请人：89BIO LTD

  公开号：US20210230116A1

  公开（公告）日：2021-07-29

  Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.