2-[4-(4-Fluorophenoxy)-2-(piperidin-1-ylmethyl)phenyl]-6-[(2-oxopyrrolidin-3-yl)amino]pyrimidine-4-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-[4-(4-Fluorophenoxy)-2-(piperidin-1-ylmethyl)phenyl]-6-[(2-oxopyrrolidin-3-yl)amino]pyrimidine-4-carboxamide
• 英文别名: 2-[4-(4-fluorophenoxy)-2-(piperidin-1-ylmethyl)phenyl]-6-[(2-oxopyrrolidin-3-yl)amino]pyrimidine-4-carboxamide
• 化学式: C₂₇H₂₉FN₆O₃
• 分子量: 504.6
• InChiKey: GVTCNHOIXMOKOZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  37
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  123
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• [EN] PYRIMIDINE CARBOXAMIDES AS SODIUM CHANNEL BLOCKERS<br/>[FR] PYRIMIDINE CARBOXAMIDES À TITRE DE BLOQUEURS DES CANAUX SODIQUES
  申请人：PURDUE PHARMA LP

  公开号：WO2014135955A1

  公开（公告）日：2014-09-12

  The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

  本公开提供了公式（I）的取代嘧啶羧酰胺及其在药学上可接受的盐和溶剂化合物，其中A1、X、A2、W1、W2、W3、E、Z和R4的定义如规范中所述。本公开还涉及使用公式（I）的化合物治疗对钠通道阻断有反应的疾病。本公开的化合物特别适用于治疗疼痛。
• PYRIMIDINE CARBOXAMIDES AS SODIUM CHANNEL BLOCKERS
  申请人：LOCKMAN Jeffrey

  公开号：US20160009659A1

  公开（公告）日：2016-01-14

  The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein A 1 , X, A 2 , W 1 , W 2 , W 3 , E, Z, and R 4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

  本公开提供了式(I)的取代嘧啶羧酰胺及其药学上可接受的盐和溶剂化物，其中A1、X、A2、W1、W2、W3、E、Z和R4如规范所述。本公开还针对使用式(I)的化合物治疗对钠通道阻滞有反应的疾病。本公开的化合物特别适用于治疗疼痛。
• Pyrimidine carboxamides as sodium channel blockers
  申请人：Purdue Pharma L.P.

  公开号：US10196364B2

  公开（公告）日：2019-02-05

  The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

  本公开提供了式 (I) 的取代嘧啶羧酰胺及其药学上可接受的盐和溶剂，其中 A1、X、A2、W1、W2、W3、E、Z 和 R4 的定义如说明书所述。本公开还涉及使用式（I）化合物治疗对钠离子通道阻断有反应的疾病。本公开的化合物尤其适用于治疗疼痛。
• US9637458B2
  申请人：——

  公开号：US9637458B2

  公开（公告）日：2017-05-02