N-[2,6-dimethyl-4-(2-trifluoromethyl-7,8-dihydro-5H-[1,6]naphthyridin-6-yl)-phenyl]-3,3-dimethyl-butyramide | 1108192-85-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N-[2,6-dimethyl-4-(2-trifluoromethyl-7,8-dihydro-5H-[1,6]naphthyridin-6-yl)-phenyl]-3,3-dimethyl-butyramide
• 英文别名: N-[2,6-dimethyl-4-[2-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]phenyl]-3,3-dimethylbutanamide
• CAS: 1108192-85-3
• 化学式: C₂₃H₂₈F₃N₃O
• 分子量: 419.49
• InChiKey: YFDJIFKMYBIYBA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  45.2
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  N-(4-bromo-2,6-dimethylphenyl)-3,3-dimethylbutanamide 、 2-(三氟甲基)-5,6,7,8-四氢-1,6-萘啶盐酸盐 在 bis(dibenzylideneacetone)-palladium⁽⁰⁾ 、 2-二环己膦基-2'-(N,N-二甲胺)-联苯 potassium tert-butylate 作用下， 以 甲苯 为溶剂， 生成 N-[2,6-dimethyl-4-(2-trifluoromethyl-7,8-dihydro-5H-[1,6]naphthyridin-6-yl)-phenyl]-3,3-dimethyl-butyramide
  参考文献：
  名称：

  [EN] NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS
  [FR] DÉRIVÉS DE NAPHTYRIDINE EN TANT QUE MODULATEURS DE CANAUX POTASSIQUES

  摘要：

  这项发明提供了化合物的结构式(I)，其中W和Z分别为CH或N，其他取代基在此定义。这些化合物是钾通道调节剂。该发明还提供了一种包含药用载体或赋形剂以及以下至少一种成分的组合物：结构式(I)的化合物的药用有效量；结构式(I)的化合物的药用可接受盐；结构式(I)的化合物的药用可接受酯。该发明还提供了一种预防或治疗受钾通道活性影响的疾病或疾病的方法，包括向需要的患者施用结构式(I)的化合物或其盐或酯或溶剂的治疗有效量。

  公开号：

  WO2009018466A1

文献信息

• Naphthyridine derivatives as potassium channel modulators
  申请人：Vernier Jean-Michel

  公开号：US08563566B2

  公开（公告）日：2013-10-22

  This invention provided compounds of formula I where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula I; a pharmaceutically acceptable salt of a compound of formula I; a pharmaceutically acceptable ester of a compound of formula I. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt or ester or solvate thereof.

  本发明提供了公式I的化合物，其中W和Z分别为CH或N，其他取代基在此定义。这些化合物是钾通道调节剂。本发明还提供了一种组合物，包括药学上可接受的载体或赋形剂和以下至少一种：公式I的化合物的药学有效量，公式I的化合物的药学上可接受的盐，公式I的化合物的药学上可接受的酯。本发明还提供了一种预防或治疗受钾通道活性影响的疾病或紊乱的方法，包括向需要治疗的患者施用公式I的化合物或其盐或酯或溶剂的治疗有效量。
• NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS
  申请人：VERNIER JEAN-MICHEL

  公开号：US20090170885A1

  公开（公告）日：2009-07-02

  This invention provided compounds of formula I where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula I; a pharmaceutically acceptable salt of a compound of formula I; a pharmaceutically acceptable ester of a compound of formula I. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt or ester or solvate thereof.

  该发明提供了化合物I的公式，其中W和Z独立地为CH或N，其他取代基在此定义。这些化合物是钾通道调节剂。该发明还提供了一种组合物，包括药学上可接受的载体或赋形剂，以及以下至少一种：化合物I的药学有效量；化合物I的药学上可接受的盐；化合物I的药学上可接受的酯。该发明还提供了一种预防或治疗受钾通道活性影响的疾病或疾病的方法，包括向需要治疗的患者施用化合物I或其盐或酯或溶剂的治疗有效量。
• Process for preparing naphthyridine derivatives.
  申请人：Valeant Pharmaceuticals International, Inc.

  公开号：EP2311836A1

  公开（公告）日：2011-04-20

  The present invention is directed to a method of preparing a compound of formula I the method comprising the palladium-catalyzed cross-coupling of compound II with compound III:

  本发明涉及一种制备式 I 化合物的方法 该方法包括化合物 II 与化合物 III 的钯催化交叉偶联：
• US8563566B2
  申请人：——

  公开号：US8563566B2

  公开（公告）日：2013-10-22
• [EN] NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS<br/>[FR] DÉRIVÉS DE NAPHTYRIDINE EN TANT QUE MODULATEURS DE CANAUX POTASSIQUES
  申请人：VALEANT PHARMACEUTICALS INT

  公开号：WO2009018466A1

  公开（公告）日：2009-02-05

  This invention provided compounds of formula (I), where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula (I); a pharmaceutically acceptable salt of a compound of formula (I); a pharmaceutically acceptable ester of a compound of formula (I). The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I) or a salt or ester or solvate thereof.

  这项发明提供了化合物的结构式(I)，其中W和Z分别为CH或N，其他取代基在此定义。这些化合物是钾通道调节剂。该发明还提供了一种包含药用载体或赋形剂以及以下至少一种成分的组合物：结构式(I)的化合物的药用有效量；结构式(I)的化合物的药用可接受盐；结构式(I)的化合物的药用可接受酯。该发明还提供了一种预防或治疗受钾通道活性影响的疾病或疾病的方法，包括向需要的患者施用结构式(I)的化合物或其盐或酯或溶剂的治疗有效量。