(6-bromopyridin-2-yl)(2-(pyridin-3-yl)piperidin-1-yl)methanone | 1346555-16-5

• 分子结构分类: 有机化合物 - 生物碱及其衍生物
• 英文名称: (6-bromopyridin-2-yl)(2-(pyridin-3-yl)piperidin-1-yl)methanone
• 英文别名: (6-Bromopyridin-2-yl)(2-(pyridin-3-yl)piperidin-1-yl)methanone；(6-bromopyridin-2-yl)-(2-pyridin-3-ylpiperidin-1-yl)methanone
• CAS: 1346555-16-5
• 化学式: C₁₆H₁₆BrN₃O
• 分子量: 346.227
• InChiKey: MVHRXRIXNBGENQ-UHFFFAOYSA-N

物化性质

• 沸点：
  522.7±50.0 °C(Predicted)
• 密度：
  1.434±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  46.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  哌啶 、 (6-bromopyridin-2-yl)(2-(pyridin-3-yl)piperidin-1-yl)methanone 在 tris-(dibenzylideneacetone)dipalladium(0) 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 sodium t-butanolate 作用下， 以 甲苯 为溶剂， 反应 3.0h， 以64%的产率得到(6-(piperidin-1-yl)pyridin-2-yl)(2-(pyridin-3-yl)piperidin-1-yl)methanone
  参考文献：
  名称：

  [EN] PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME
  [FR] COMPOSÉS DE PICOLINAMIDE ET DE PYRIMIDINE-4-CARBOXAMIDE, LEUR PROCÉDÉ DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE LES COMPRENANT

  摘要：

  公开号：

  WO2011139107A3
• 作为产物：
  描述：

  6-溴-2-吡啶羧酸 、 (±)-毒藜碱 在 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 乙腈 为溶剂， 反应 3.0h， 以26%的产率得到(6-bromopyridin-2-yl)(2-(pyridin-3-yl)piperidin-1-yl)methanone
  参考文献：
  名称：

  [EN] PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME
  [FR] COMPOSÉS DE PICOLINAMIDE ET DE PYRIMIDINE-4-CARBOXAMIDE, LEUR PROCÉDÉ DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE LES COMPRENANT

  摘要：

  公开号：

  WO2011139107A3

文献信息

• PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：Ryu Je Ho

  公开号：US20130210811A1

  公开（公告）日：2013-08-15

  Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.

  本发明提供了吡啶甲酰胺和嘧啶-4-羧酰胺化合物、制备方法、含有该化合物的制药组合物以及使用该化合物作为11β-HSD1酶的选择性抑制剂，用于预防、调节和治疗与糖皮质激素调节相关的疾病的医疗用途。本发明的吡啶甲酰胺和嘧啶-4-羧酰胺化合物是人源11β-HSD1酶的选择性抑制剂，可用于预防、调节和治疗与人源11β-HSD1酶参与的糖皮质激素调节相关疾病，例如代谢综合征，如1型和2型糖尿病、糖尿病后并发症、成人隐形自身免疫性糖尿病（LADA）、胰岛素耐受综合征、肥胖症、糖耐量受损（IGT）、空腹血糖受损（IFG）、糖耐量受损、血脂异常、动脉粥样硬化、高血压等。
• Picolinamide and pyrimidine-4-carboxamide compounds, process for preparing and pharmaceutical composition comprising the same
  申请人：Ryu Je Ho

  公开号：US09096571B2

  公开（公告）日：2015-08-04

  Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.

  本发明提供了吡啶甲酰胺和嘧啶-4-羧酰胺化合物、其制备方法、含有该化合物的药物组合物，以及使用该化合物作为11β-HSD1酶的选择性抑制活性的药剂来预防、调节和治疗与糖皮质激素调节相关的疾病的医疗用途。本发明的吡啶甲酰胺和嘧啶-4-羧酰胺化合物是人源11β-HSD1酶的选择性抑制剂，在预防、调节和治疗与人源11β-HSD1酶相关的糖皮质激素调节疾病中非常有用，例如代谢综合征、1型和2型糖尿病、糖尿病后并发症、成人潜在自身免疫性糖尿病、胰岛素耐量综合征、肥胖症、糖耐量受损、空腹血糖受损、糖耐量受损、血脂异常、动脉硬化和高血压等。
• PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：Sk Chemicals Co., Ltd.

  公开号：EP2566859B1

  公开（公告）日：2016-12-21
• US9096571B2
  申请人：——

  公开号：US9096571B2

  公开（公告）日：2015-08-04
• [EN] PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME<br/>[FR] COMPOSÉS DE PICOLINAMIDE ET DE PYRIMIDINE-4-CARBOXAMIDE, LEUR PROCÉDÉ DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE LES COMPRENANT
  申请人：SK CHEMICALS CO LTD

  公开号：WO2011139107A3

  公开（公告）日：2012-05-18