N-(3,5-dichloropyrid-4-yl)-4-methoxy-8-acetamido-dibenzo[b,d]furan-1-carboxamide | 778576-37-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: N-(3,5-dichloropyrid-4-yl)-4-methoxy-8-acetamido-dibenzo[b,d]furan-1-carboxamide
• 英文别名: 8-acetamido-N-(3,5-dichloropyridin-4-yl)-4-methoxydibenzofuran-1-carboxamide
• CAS: 778576-37-7
• 化学式: C₂₁H₁₅Cl₂N₃O₄
• 分子量: 444.274
• InChiKey: QHMQLBVJYCJJNQ-UHFFFAOYSA-N

物化性质

• 沸点：
  610.2±55.0 °C(Predicted)
• 密度：
  1.513±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  93.5
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-(3,5-dichloropyrid-4-yl)-4-methoxy-8-acetamido-dibenzo[b,d]furan-1-carboxamide 在 palladium 10% on activated carbon 氨 、 氢气 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 24.0h， 以42%的产率得到N-(pyrid-4-yl)-4-methoxy-8-acetamido-dibenzo[b,d]furan-1-carboxamide
  参考文献：
  名称：

  [EN] NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  [FR] NOUVEAUX COMPOSES HETEROCYCLIQUES POUR LE TRAITEMENT DES AFFECTIONS INFLAMMATOIRES ET ALLERGIQUES, LEUR PROCEDE DE PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT

  摘要：

  本发明涉及新颖的杂环化合物，它们的类似物，其互变异构体，其位置异构体，其立体异构体，其对映异构体，其二对映异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。本发明更具体地涉及公式（1）的新型磷酸二酯酶4型（PDE4）抑制剂，其类似物，其互变异构体，其对映异构体，其二对映异构体，其位置异构体，其立体异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。其中，X、Ar、Y、P 和 R1-R4 组在权利要求书中有定义。

  公开号：

  WO2004089940A1
• 作为产物：
  描述：

  N-(3,5-dichloropyrid-4-yl)-4-methoxy-8-amino-dibenzo[b,d]furan-1-carboxamide 、 乙酰氯 在 吡啶 作用下， 以 四氢呋喃 为溶剂， 反应 0.5h， 生成 N-(3,5-dichloropyrid-4-yl)-4-methoxy-8-acetamido-dibenzo[b,d]furan-1-carboxamide
  参考文献：
  名称：

  [EN] NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  [FR] NOUVEAUX COMPOSES HETEROCYCLIQUES POUR LE TRAITEMENT DES AFFECTIONS INFLAMMATOIRES ET ALLERGIQUES, LEUR PROCEDE DE PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT

  摘要：

  本发明涉及新颖的杂环化合物，它们的类似物，其互变异构体，其位置异构体，其立体异构体，其对映异构体，其二对映异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。本发明更具体地涉及公式（1）的新型磷酸二酯酶4型（PDE4）抑制剂，其类似物，其互变异构体，其对映异构体，其二对映异构体，其位置异构体，其立体异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。其中，X、Ar、Y、P 和 R1-R4 组在权利要求书中有定义。

  公开号：

  WO2004089940A1

文献信息

• NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：Gopalan Balasubramanian

  公开号：US20090182143A1

  公开（公告）日：2009-07-16

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

  本发明涉及新型杂环化合物、它们的类似物、互变异构体、位置异构体、立体异构体、对映异构体、顺反异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂和含有它们的制药组合物。本发明更特别地涉及式（1）的新型磷酸二酯酶4（PDE4）抑制剂、它们的类似物、互变异构体、对映异构体、顺反异构体、位置异构体、立体异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂和含有它们的制药组合物。
• Novel heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
  申请人：Gopalan Balasubramanian

  公开号：US20050027129A1

  公开（公告）日：2005-02-03

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

  本发明涉及新型杂环化合物及其类似物、互变异构体、位置异构体、立体异构体、对映异构体、二对映异构体、多晶形态、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物以及含有它们的制药组合物。本发明更特别涉及公式（1）的新型磷酸二酯酶4（PDE4）抑制剂及其类似物、互变异构体、对映异构体、二对映异构体、位置异构体、立体异构体、多晶形态、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物以及含有它们的制药组合物。
• Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
  申请人：Glenmark Pharmaceuticals S.A.

  公开号：US07384962B2

  公开（公告）日：2008-06-10

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

  本发明涉及新型杂环化合物、它们的类似物、互变异构体、区域异构体、立体异构体、对映异构体、顺反异构体、多晶异构体、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂和含有它们的药物组合物。本发明更特别地涉及公式（1）的新型磷酸二酯酶4（PDE4）抑制剂、它们的类似物、互变异构体、对映异构体、顺反异构体、区域异构体、立体异构体、多晶异构体、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂和含有它们的药物组合物。
• Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders
  申请人：Glenmark Pharmaceuticals, S.A.

  公开号：US07393846B2

  公开（公告）日：2008-07-01

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

  本发明涉及新型杂环化合物、它们的类似物、互变异构体、位置异构体、立体异构体、对映异构体、非对映异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物及含有它们的制药组合物。本发明更特别地涉及公式（1）的新型磷酸二酯酶4（PDE4）抑制剂、它们的类似物、互变异构体、对映异构体、非对映异构体、位置异构体、立体异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物及含有它们的制药组合物。
• US7223789B2
  申请人：——

  公开号：US7223789B2

  公开（公告）日：2007-05-29