2-(2-phenyl-chroman-6-yloxy)-4-trifluoromethyl-thiazole-5-carboxylic acid methyl ester | 1426900-23-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: 2-(2-phenyl-chroman-6-yloxy)-4-trifluoromethyl-thiazole-5-carboxylic acid methyl ester
• 英文别名: methyl 2-[(2-phenyl-3,4-dihydro-2H-chromen-6-yl)oxy]-4-(trifluoromethyl)-1,3-thiazole-5-carboxylate
• CAS: 1426900-23-3
• 化学式: C₂₁H₁₆F₃NO₄S
• 分子量: 435.424
• InChiKey: XGTYMOKLBJHVPZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  85.9
• 氢给体数：
  0
• 氢受体数：
  9

文献信息

• SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS
  申请人：CZECHTIZKY Werngard

  公开号：US20130065859A1

  公开（公告）日：2013-03-14

  The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的取代2-(色甘醇-6-氧基)-噻唑衍生物，其中Ar、R2、R3和R4如权利要求中所定义。式I的化合物是钠-钙交换蛋白（NCX）的抑制剂，特别是亚型1的钠-钙交换蛋白（NCX1），适用于处理细胞内钙离子稳态受扰的各种疾病，如心律失常、心力衰竭和中风。本发明还涉及制备式I的化合物的方法，它们作为药物的用途，以及包含它们的药物组合物。
• [EN] SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] 2-(CHROMAN-6-YLOXY)-THIAZOLES SUBSTITUÉS ET LEUR UTILISATION EN TANT QUE PRODUITS PHARMACEUTIQUES
  申请人：SANOFI SA

  公开号：WO2013037724A1

  公开（公告）日：2013-03-21

  The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1 ), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及公式I中Ar、R2、R3和R4所定义的取代的2-(色甘醇-6-氧基)-噻唑。公式I的化合物是钠钙交换蛋白(NCX)的抑制剂，特别是亚型1的钠钙交换蛋白(NCX1)，适用于治疗细胞内钙稳态紊乱的各种疾病，如心律失常、心力衰竭和中风。此外，该发明还涉及制备公式I化合物的方法，它们作为药物的用途，以及包含它们的药物组合物。
• [EN] SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] THIAZOLES À SUBSTITUTION 2-(CHROMAN-6-YLOXY) ET LEUR UTILISATION COMME PRODUITS PHARMACEUTIQUES
  申请人：SANOFI SA

  公开号：WO2013037388A1

  公开（公告）日：2013-03-21

  The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula (I), in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式(I)的取代2-(色苷-6-氧基)-噻唑，其中Ar、R2、R3和R4如权利要求中所定义。式(I)的化合物是钠钙交换蛋白(NCX)的抑制剂，特别是钠钙交换蛋白的亚型1(NCX1)的抑制剂，并适用于治疗细胞内钙离子稳态紊乱的各种疾病，如心律失常、心力衰竭和中风。此外，该发明还涉及制备式(I)化合物的方法，它们作为药物的用途，以及包含它们的药物组合物。
• SUBSITUTED 2-(CHROMAN-6-YLOXYL)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS
  申请人：Sanofi

  公开号：US20140243292A1

  公开（公告）日：2014-08-28

  The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的取代2-(色烯-6-氧基)-噻唑，其中Ar，R2，R3和R4如权利要求所定义。公式I化合物是钠钙交换器（NCX）的抑制剂，特别是钠钙交换器亚型1（NCX1）的抑制剂，并适用于治疗细胞内钙离子稳态受到干扰的多种疾病，如心律失常，心力衰竭和中风。本发明还涉及制备公式I化合物的方法，它们作为药物的用途，以及包含它们的制药组合物。
• Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals
  申请人：SANOFI

  公开号：EP2567958A1

  公开（公告）日：2013-03-13

  Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  取代的 2-(色满-6-氧基)噻唑及其药物用途 本发明涉及式 I 的取代的 2-(色满-6-氧基)-噻唑、 其中 Ar、R2、R3 和 R4 如权利要求中所定义。式 I 的化合物是钠钙交换子（NCX），特别是亚型 1 的钠钙交换子（NCX1）的抑制剂，适用于治疗细胞内钙平衡紊乱的各种疾病，如心律失常、心力衰竭和中风。本发明还涉及式 I 化合物的制备工艺、其作为药物的用途以及包含它们的药物组合物。