2-(5-fluoro-6-(pyrrolidin-1-yl)pyridin-3-yl)acetic acid | 953780-54-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-(5-fluoro-6-(pyrrolidin-1-yl)pyridin-3-yl)acetic acid
• 英文别名: (5-Fluoro-6-pyrrolidin-1-ylpyridin-3-yl)acetic acid；2-(5-fluoro-6-pyrrolidin-1-ylpyridin-3-yl)acetic acid
• CAS: 953780-54-6
• 化学式: C₁₁H₁₃FN₂O₂
• 分子量: 224.235
• InChiKey: SFTGZUJFXRPOQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  53.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-(5-fluoro-6-(pyrrolidin-1-yl)pyridin-3-yl)acetic acid 、 (R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethylamine bishydrochloride 在 N-羟基-7-氮杂苯并三氮唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以39.2%的产率得到2-(5-fluoro-6-pyrrolidin-1-ylpyridin-3-yl)-N-((1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl)acetamide bistrifluoroacetate
  参考文献：
  名称：

  WO2007/120729

  摘要：

  公开号：

文献信息

• [EN] PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS<br/>[FR] COMPOSÉS DE PYRAZOLE ET LEUR UTILISATION EN TANT QUE BLOQUEURS DES CANAUX CALCIQUES DE TYPE T
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2015186056A1

  公开（公告）日：2015-12-10

  The invention relates to compounds of formula (I) Formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.

  这项发明涉及式(I)的化合物。式(I)中X、Y、R1、R2、(R4)n和(R5)m的定义如描述中所述，并且涉及这些化合物的药用盐。这些化合物可用作钙T通道阻滞剂。
• Pyridyl Amide T-Type Calcium Channel Antagonists
  申请人：Barrow James C.

  公开号：US20090275550A1

  公开（公告）日：2009-11-05

  The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

  本发明涉及对T型钙通道具有拮抗作用的吡啶酰胺化合物，其在治疗或预防与T型钙通道有关的疾病和疾病中具有用途。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物和组合物预防或治疗与T型钙通道有关的疾病的用途。
• Pyridyl amide T-type calcium channel antagonists
  申请人：Merck Sharp & Dohme Corp.

  公开号：US07875636B2

  公开（公告）日：2011-01-25

  The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

  本发明涉及吡啶酰胺类化合物，其是T型钙通道的拮抗剂，适用于治疗或预防涉及T型钙通道的疾病和疾病。本发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及T型钙通道的疾病中使用这些化合物和组合物。
• Pyrazole compounds and their use as T-type calcium channel blockers
  申请人：IDORSIA PHARMACEUTICALS LTD

  公开号：US10065929B2

  公开（公告）日：2018-09-04

  The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.

  本发明涉及式 (I) 的化合物 其中X、Y、R1、R2、(R4)n和(R5)m如描述中所定义，并涉及此类化合物的药学上可接受的盐。这些化合物可用作钙 T 通道阻滞剂。
• PYRIDYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS
  申请人：Merck & Co., Inc.

  公开号：EP2010493A2

  公开（公告）日：2009-01-07