4-nitrophenyl 6-difluoromethyloxy-benzo[4,5]furo[3,2-c]pyridine-9-carboxylate | 893555-87-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚酯
• 英文名称: 4-nitrophenyl 6-difluoromethyloxy-benzo[4,5]furo[3,2-c]pyridine-9-carboxylate
• 英文别名: 4-Nitrophenyl 6-difluoromethyloxybenzo[4,5]furo[3,2-c]pyridine-9-carboxylate；(4-nitrophenyl) 6-(difluoromethoxy)-[1]benzofuro[3,2-c]pyridine-9-carboxylate
• CAS: 893555-87-8
• 化学式: C₁₉H₁₀F₂N₂O₆
• 分子量: 400.295
• InChiKey: KSWHJNNNYBSXOI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  107
• 氢给体数：
  0
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  4-氨基-3,5-二氯吡啶 、 4-nitrophenyl 6-difluoromethyloxy-benzo[4,5]furo[3,2-c]pyridine-9-carboxylate 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 生成 N-(3,5-dichloro-4-pyridyl)-6-difluoromethoxy-benzo[4,5]furo[3,2-c]pyridine-9-carboxamide
  参考文献：
  名称：

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

  摘要：

  本发明涉及新型磷酸二酯酶4型（PDE4）抑制剂的化学式（1）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合物以及含有它们的制药组合物，这些制剂在治疗过敏性和炎症性疾病方面具有用途，包括哮喘、慢性支气管炎、特应性皮炎、荨麻疹、过敏性鼻炎、过敏性结膜炎、春季结膜炎、嗜酸性肉芽肿、牛皮癣、类风湿性关节炎、脓毒性休克、溃疡性结肠炎、克罗恩病、心肌再灌注损伤和脑再灌注损伤、慢性肾小球肾炎、内毒素休克和成人呼吸窘迫综合症。

  公开号：

  US20090306082A1
• 作为产物：
  描述：

  6-difluoromethyloxy-benzo[4,5]furo[3,2-c]pyridine-9-carboxylic acid 生成 4-nitrophenyl 6-difluoromethyloxy-benzo[4,5]furo[3,2-c]pyridine-9-carboxylate
  参考文献：
  名称：

  Processes for preparing 6-(difluoromethoxy)[1]benzofuro[3,2-c]pyridine-9-carbaldehyde, a novel intermediate for the synthesis of PDE IV inhibitors

  摘要：

  本发明涉及一种新型工艺，用于制备6-(二氟甲氧基)[1]苯并呋[3,2-c]吡啶-9-甲醛，该化合物是制备具有PDE4抑制活性的化合物的一种新型有用中间体，例如3,5-二氯-4-(6-二氟甲氧基苯并[4,5]呋[3,2-c]吡啶-9-基羧酰胺)-1-吡啶酸盐。

  公开号：

  US08524905B2

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：Gharat Laxmikant Atmaram

  公开号：US20110190303A1

  公开（公告）日：2011-08-04

  The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.

  本发明涉及一种新的磷酸二酯酶4型（PDE4）抑制剂，其化学式为（1）及其类似物、互变异构体、对映异构体、立体异构体、区域异构体、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和含有它们的制药组合物，用于治疗过敏和炎症性疾病，包括哮喘、慢性支气管炎、特应性皮炎、荨麻疹、过敏性鼻炎、过敏性结膜炎、春季结膜炎、嗜酸性肉芽肿、牛皮癣、类风湿关节炎、脓毒症休克、溃疡性结肠炎、克隆病、心肌再灌注损伤和脑再灌注损伤、慢性肾小球肾炎、内毒素性休克和成人呼吸窘迫综合征。
• NOVEL PROCESSES FOR PREPARING 6-(DIFLUOROMETHOXY)[1]BENZOFURO[3,2-C]PYRIDINE-9-CARBALDEHYDE, A NOVEL INTERMEDIATE FOR THE SYNTHESIS OF PDE IV INHIBITORS
  申请人：Gharat Laxmikant Atmaram

  公开号：US20100168151A1

  公开（公告）日：2010-07-01

  The present invention relates to novel processes for preparing 6-(difluoromethoxy)[1] benzofuro[3,2-c]pyridine-9-carbaldehyde, which is a novel and useful intermediate for preparing compounds with PDE4 inhibitory activity, such as 3,5-dichloro-4-(6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridin-9-ylcarboxamido)-1-pyridiniumolate.

  本发明涉及一种制备6-(二氟甲氧基)[1]苯并呋[3,2-c]吡啶-9-甲醛的新工艺，该化合物是制备具有PDE4抑制活性的化合物的新型有用中间体，例如3,5-二氯-4-(6-二氟甲氧基苯并[4,5]呋[3,2-c]吡啶-9-基羧酰胺)-1-吡啶酸盐。
• 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：US08129401B2

  公开（公告）日：2012-03-06

  The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.

  本发明涉及式（1）及其类似物、互变异构体、对映异构体、立体异构体、区域异构体、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及其制备的药物组合物。该组合物可用于治疗过敏和炎症性疾病，包括哮喘、慢性支气管炎、特应性皮炎、荨麻疹、过敏性鼻炎、过敏性结膜炎、春季结膜炎、嗜酸性肉芽肿、银屑病、类风湿性关节炎、感染性休克、溃疡性结肠炎、克隆氏病、心肌再灌注损伤和脑再灌注损伤、慢性肾小球肾炎、内毒素性休克和成人呼吸窘迫综合征。
• Substituted benzo[4,5]furo[3,2-c]pyridine derivatives as PDE 4 inhibitors
  申请人：Glenmark Pharmaceuticals S.A.

  公开号：US07943634B2

  公开（公告）日：2011-05-17

  The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.

  本发明涉及式（1）及其类似物、互变异构体、对映异构体、二对映异构体、区域异构体、立体异构体、多晶形、药学上可接受的盐、相应的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，用于治疗过敏性和炎症性疾病，包括哮喘、慢性支气管炎、特应性皮炎、荨麻疹、过敏性鼻炎、过敏性结膜炎、春季结膜炎、嗜酸性肉芽肿、牛皮癣、类风湿性关节炎、败血症休克、溃疡性结肠炎、克隆氏病、心肌再灌注损伤和脑再灌注损伤、慢性肾小球肾炎、内毒素性休克和成人呼吸窘迫综合征。
• WO2006/64355
  申请人：——

  公开号：——

  公开（公告）日：——