1-cyclopropyl-3-(4-(4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalen-1-yloxy)pyrimidin-2-yl)urea | 1229607-34-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-cyclopropyl-3-(4-(4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalen-1-yloxy)pyrimidin-2-yl)urea
• 英文别名: 1-[5-Tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-[2-(cyclopropylcarbamoylamino)pyrimidin-4-yl]oxynaphthalen-1-yl]urea
• CAS: 1229607-34-4
• 化学式: C₃₃H₃₄N₈O₃
• 分子量: 590.685
• InChiKey: DXLIDCWBUAERSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.1
• 重原子数：
  44
• 可旋转键数：
  8
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  135
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  prop-1-en-2-yl 4-(4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalen-1-yloxy)pyrimidin-2-ylcarbamate 、 环丙胺 在 N-甲基吗啉 作用下， 以 四氢呋喃 为溶剂， 反应 96.0h， 以41%的产率得到1-cyclopropyl-3-(4-(4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalen-1-yloxy)pyrimidin-2-yl)urea
  参考文献：
  名称：

  [EN] P38 MAP KINASE INHIBITORS
  [FR] INHIBITEURS DE KINASE MAP P38

  摘要：

  公开号：

  WO2010067130A8

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。
• UREIDO-PYRAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF RHINOVIRUS INFECTIONS
  申请人：Cass Lindsey

  公开号：US20130102607A1

  公开（公告）日：2013-04-25

  Medicinal use The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of respiratory syncitial virus (RSV) infection in particular viral exacerbation of a respiratory disorder such as bronchitis, asthma, COPD and/or cystic fibrosis, methods of treating or preventing RSV infection employing said compounds or pharmaceutical composition comprising the same.

  药用途径：本公开涉及公式（I）的化合物，用于治疗或预防呼吸道合胞病毒(RSV)感染，特别是针对呼吸系统疾病如支气管炎、哮喘、慢性阻塞性肺疾病（COPD）和/或囊性纤维化的病毒加重的治疗，以及使用该化合物或含有该化合物的药物组合物进行治疗或预防RSV感染的方法。
• 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。
• Methods
  申请人：Charron Catherine Elisabeth

  公开号：US20130123260A1

  公开（公告）日：2013-05-16

  The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of rhinovirus infection, methods of treating or preventing rhinovirus infection employing said compounds or pharmaceutical composition comprising the same. The disclosure also relates to compounds of formula (I) for use in the treatment or prophylaxis of exacerbation of respiratory disorders (such as asthma, COPD, bronchitis and/or cystic fibrosis) by rhinovirus infection.