2-(3-nitropyridin-4-yl)ethanol | 918153-30-7

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 2-(3-nitropyridin-4-yl)ethanol
• CAS: 918153-30-7
• 化学式: C₇H₈N₂O₃
• mdl: MFCD18803212
• 分子量: 168.152
• InChiKey: GDAQJZHHPBHSQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  78.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(3-nitropyridin-4-yl)ethanol 在 偶氮二甲酸二异丙酯 、 palladium 10% on activated carbon 、 palladium on activated charcoal 、 氢气 、 N,N-二异丙基乙胺 、 三苯基膦 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 乙酸乙酯 、 乙腈 为溶剂， 反应 21.0h， 生成 N-(4-(2-((4-(3-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)ureido)naphthalen-1-yl)oxy)ethyl)pyridin-3-yl)acetamide
  参考文献：
  名称：

  Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma

  摘要：

  The discovery of a novel series of therapeutic agents that has been designed and optimized for treating chronic obstructive pulmonary disease is reported. The pharmacological strategy was based on the identification of compounds that inhibit a defined subset of kinase enzymes modulating inflammatory processes that would be effective against steroid refractory disease and exhibit a sustained duration of action after inhaled delivery.

  DOI：

  10.1021/acs.jmedchem.5b01029
• 作为产物：
  描述：

  3-硝基-4-甲基吡啶 、 聚合甲醛 在 苄基三甲基氢氧化铵 作用下， 以 二甲基亚砜 为溶剂， 反应 4.0h， 以10%的产率得到2-(3-nitropyridin-4-yl)ethanol
  参考文献：
  名称：

  WO2006/136562

  摘要：

  公开号：

文献信息

• INHIBITORS OF HEMOPOIETIC CELL KINASE (P59-HCK) AND THEIR USE IN THE TREATMENT OF INFLUENZA INFECTION
  申请人：Charron Catherine Elisabeth

  公开号：US20120244120A1

  公开（公告）日：2012-09-27

  The present invention relates inter alia to the treatment or prevention of influenza virus infection (including subtypes influenza A virus, influenza B virus, avian strain H5N1, A/H1N1, H3N2 and/or pandemic influenza) using compounds which inhibit the activity of p59-HCK and to a method of screening for a candidate drug substance intended to prevent or treat influenza virus infection in a subject, said method comprising identifying a test substance capable of inhibiting p59-HCK activity.

  本发明涉及治疗或预防流感病毒感染（包括亚型流感A病毒、流感B病毒、禽流感H5N1、A/H1N1、H3N2和/或大流行性流感）的化合物，这些化合物抑制p59-HCK的活性，并涉及一种筛选候选药物物质的方法，该方法旨在预防或治疗受试者的流感病毒感染，所述方法包括识别能够抑制p59-HCK活性的试验物质。
• Inhibitors of Hemopoietic Cell Kinase (P59-HCK) and Their Use in the Treatment of Influenza Infection
  申请人：RESPIVERT LIMITED

  公开号：US20160045512A1

  公开（公告）日：2016-02-18

  The present invention relates inter alia to the treatment or prevention of influenza virus infection (including subtypes influenza A virus, influenza B virus, avian strain H5N1, A/H1N1, H3N2 and/or pandemic influenza) using compounds which inhibit the activity of p59-HCK and to a method of screening for a candidate drug substance intended to prevent or treat influenza virus infection in a subject, said method comprising identifying a test substance capable of inhibiting p59-HCK activity.

  本发明涉及治疗或预防流感病毒感染（包括亚型流感A病毒、流感B病毒、禽流感H5N1、A/H1N1、H3N2和/或大流行性流感）的化合物，这些化合物抑制p59-HCK的活性，并涉及一种筛选候选药物物质的方法，该方法旨在预防或治疗受试者的流感病毒感染，所述方法包括识别能够抑制p59-HCK活性的试验物质。
• P38 MAP KINASE INHIBITORS
  申请人：Ito Kazuhiro

  公开号：US20110294812A1

  公开（公告）日：2011-12-01

  The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.

  本发明涉及式（I）化合物：或其药学上可接受的盐，包括所有立体异构体、互变异构体和同位素衍生物，它们是p38丝裂原活化蛋白激酶酶（以下简称p38 MAP激酶抑制剂）的抑制剂，特别是其α和γ激酶亚型，并且它们在治疗中的使用，包括在药物组合中，特别是在治疗炎症性疾病方面的使用，包括肺部的炎症性疾病，如COPD。
• p38 MAP kinase inhibitors
  申请人：Respivert Ltd.

  公开号：US08293748B2

  公开（公告）日：2012-10-23

  There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.

  其中提供了式(I)的化合物，其中R1、Ar、L、X、R3和Q的定义与说明书中定义的相同，可用于治疗炎症性疾病，特别是用于治疗。
• P38 MAP kinase inhibitors
  申请人：Respivert Ltd.

  公开号：US08299073B2

  公开（公告）日：2012-10-30

  The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.

  本发明涉及式(I)的化合物： 或其药学上可接受的盐，包括其所有立体异构体、互变异构体和同位素衍生物，它们是p38 丝裂原活化蛋白激酶酶（以下简称p38 MAP激酶抑制剂）的抑制剂，特别是它们的α和γ激酶亚型，并且它们在治疗中的使用，包括在制药组合物中，特别是在治疗炎症性疾病中，包括肺部的炎症性疾病，如COPD。