(R)-tert-butyl 3-((1-methyl-1H-pyrrolo[2,3-c]pyridin-7-yl)amino)piperidine-1-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: (R)-tert-butyl 3-((1-methyl-1H-pyrrolo[2,3-c]pyridin-7-yl)amino)piperidine-1-carboxylate
• 英文别名: tert-butyl (R)-3-((1-methyl-1H-pyrrolo[2,3-c]pyridin-7-yl)amino)piperidine-1-carboxylate；tert-butyl (3R)-3-[(1-methylpyrrolo[2,3-c]pyridin-7-yl)amino]piperidine-1-carboxylate
• 化学式: C₁₈H₂₆N₄O₂
• 分子量: 330.43
• InChiKey: AUMLERMFALYCGA-CQSZACIVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  59.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-tert-butyl 3-((1-methyl-1H-pyrrolo[2,3-c]pyridin-7-yl)amino)piperidine-1-carboxylate 在 sodium hydride 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 2.33h， 生成
  参考文献：
  名称：

  Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9

  摘要：

  A series of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides were identified as small molecule PCSK9 mRNA translation inhibitors. Analogues from this new chemical series, such as 4d and 4g, exhibited improved PCSK9 potency, ADME properties, and in vitro safety profiles when compared to earlier lead structures.

  DOI：

  10.1016/j.bmcl.2018.10.029
• 作为产物：
  描述：

  7-氯-6-氮杂吲哚 在 tris-(dibenzylideneacetone)dipalladium(0) 、 2-(二环己基膦)3,6-二甲氧基-2′,4′,6′-三异丙基-1,1′-联苯 、 sodium hydride 、 sodium t-butanolate 作用下， 以 四氢呋喃 、 甲苯 、 mineral oil 为溶剂， 反应 6.33h， 生成 (R)-tert-butyl 3-((1-methyl-1H-pyrrolo[2,3-c]pyridin-7-yl)amino)piperidine-1-carboxylate
  参考文献：
  名称：

  SUBSTITUTED AMIDE COMPOUNDS

  摘要：

  本发明涉及替代酰胺化合物，含有这种化合物的药物组合物以及利用这种化合物降低血浆脂质水平，如LDL-胆固醇和甘油三酯，并据此治疗由高水平的LDL-胆固醇和甘油三酯加重的疾病，如动脉粥样硬化和心血管疾病，在哺乳动物，包括人类中的应用。

  公开号：

  US20140315928A1

文献信息

• Substituted amide compounds
  申请人：Pfizer Inc.

  公开号：US09227956B2

  公开（公告）日：2016-01-05

  The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

  本发明涉及取代酰胺化合物、含有该类化合物的药物组合物及使用该类化合物降低血浆脂质水平，例如低密度脂蛋白胆固醇和甘油三酯，并因此治疗由高水平低密度脂蛋白胆固醇和甘油三酯引起的疾病，例如动脉硬化和心血管疾病，在哺乳动物，包括人类中的应用。
• N-PIPERIDIN-3-YLBENZAMIDE DERIVATIVES FOR TREATING CARDIOVASCULAR DISEASES
  申请人：Pfizer Inc.

  公开号：EP2986599A1

  公开（公告）日：2016-02-24
• US9227956B2
  申请人：——

  公开号：US9227956B2

  公开（公告）日：2016-01-05
• [EN] N-PIPERIDIN-3-YLBENZAMIDE DERIVATIVES FOR TREATING CARDIOVASCULAR DISEASES<br/>[FR] DÉRIVÉS DE N-PIPÉRIDIN-3-YLBENZAMIDE DANS LE TRAITEMENT DES MALADIES CARDIOVASCULAIRES
  申请人：PFIZER

  公开号：WO2014170786A1

  公开（公告）日：2014-10-23

  The present invention is directed at substituted amide compounds of formula (I), pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL- cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.
• SUBSTITUTED AMIDE COMPOUNDS
  申请人：Pfizer Inc.

  公开号：US20140315928A1

  公开（公告）日：2014-10-23

  The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

  本发明涉及替代酰胺化合物，含有这种化合物的药物组合物以及利用这种化合物降低血浆脂质水平，如LDL-胆固醇和甘油三酯，并据此治疗由高水平的LDL-胆固醇和甘油三酯加重的疾病，如动脉粥样硬化和心血管疾病，在哺乳动物，包括人类中的应用。