1-[5-tert-Butyl-2-(2-methyl-pyrimidin-5-yl)-phenyl]-3-[4-(6-morpholin-4-ylmethyl-pyridin-3-yl)-naphthalen-1-yl]-urea | 294849-97-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 1-[5-tert-Butyl-2-(2-methyl-pyrimidin-5-yl)-phenyl]-3-[4-(6-morpholin-4-ylmethyl-pyridin-3-yl)-naphthalen-1-yl]-urea
• 英文别名: 1-[5-Tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl]-3-[4-[6-(morpholin-4-ylmethyl)pyridin-3-yl]naphthalen-1-yl]urea
• CAS: 294849-97-1
• 化学式: C₃₆H₃₈N₆O₂
• 分子量: 586.737
• InChiKey: YTISFTRMFXFAKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  44
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  92.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-amino-4-[6-(morpholin-4-ylmethyl)pyridin-3-yl]naphthalene 、 以 四氢呋喃 为溶剂， 生成 1-[5-tert-Butyl-2-(2-methyl-pyrimidin-5-yl)-phenyl]-3-[4-(6-morpholin-4-ylmethyl-pyridin-3-yl)-naphthalen-1-yl]-urea
  参考文献：
  名称：

  Discovery and characterization of the N-phenyl-N′-naphthylurea class of p38 kinase inhibitors

  摘要：

  An effort aimed at exploring structural diversity in the N-pyrazole-N'-naphthylurea class of p38 kinase inhibitors led to the synthesis and characterization of N-phenyl-N'-naphthylureas. Examples of these compounds displayed excellent inhibition of TNF-alpha production in vitro, as well as efficacy in a mouse model of lipopolysaccharide induced endotoxemia. In addition, perspective is provided on the role of a sulfonamide functionality in defining inhibitor potency.

  DOI：

  10.1016/j.bmcl.2009.03.104

文献信息

• Anticoagulant and fibrinolytic therapy uning p38 MAP kinase inhibitors
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20040033222A1

  公开（公告）日：2004-02-19

  Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.

  揭示了利用p38 MAP激酶抑制剂治疗与血液凝血和纤溶有关的疾病或症状的方法。
• Method of treating mucus hypersecretion
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：US20030220336A1

  公开（公告）日：2003-11-27

  The invention relates to the use of p38 kinase inhibitors for the preparation of a pharmaceutical composition suitable for inhalation for the treatment of mucus hypersecretion. Furthermore the invention is directed to pharmaceutical compositions suitable for inhalation comprising p38 kinase inhibitors and to methods for the preparation thereof.

  本发明涉及使用p38激酶抑制剂制备适用于治疗黏液过度分泌的吸入药物组合物。此外，本发明还涉及适用于吸入的含有p38激酶抑制剂的药物组合物以及其制备方法。
• Methods of treating cytokine mediated diseases
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20030060455A1

  公开（公告）日：2003-03-27

  Disclosed are methods of treating acute and chronic inflammation in the lung caused by inhalation of smoke, endometriosis, Behcet's disease, uveitis, ankylosing spondylitis, pancreatitis, cancer, Lyme disease, sepsis, chronic obstructive pulmonary disease, traumatic arthritis, congestive heart failure and restenosis following percutaneous transluminal coronary angioplasty, known to be cytokine mediated, using aromatic heterocyclic compounds described in WO 00/55139.

  本发明涉及使用在WO 00/55139中描述的芳香族杂环化合物治疗由吸入烟雾、子宫内膜异位症、Behcet病、葡萄膜炎、强直性脊柱炎、胰腺炎、癌症、莱姆病、败血症、慢性阻塞性肺疾病、创伤性关节炎、充血性心力衰竭和经皮冠状动脉成形术后再狭窄等已知为细胞因子介导的急性和慢性肺部炎症治疗的方法。
• Combination therapy with p38 MAP kinase inhibitors and their pharmaceutical compositions
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20040110755A1

  公开（公告）日：2004-06-10

  The present invention relates to pharmaceutical combinations therapies based on p38 kinase inhibitors and another active ingredient, pharmaceutical compositions comprising such combinations, processes for preparing them and their use in the treatment of cytokine mediated diseases.

  本发明涉及基于p38激酶抑制剂和另一种活性成分的药物组合疗法，包括这种组合物的制药组合物、制备它们的过程以及它们在治疗细胞因子介导的疾病中的应用。
• Intermediate arylamine compounds
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20030225077A1

  公开（公告）日：2003-12-04

  Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.

  本发明涉及一种新型芳香化合物，可用于治疗涉及炎症的疾病或病理状况，如慢性炎症性疾病。还公开了含有该化合物的制药组合物、中间体化合物和制备该化合物的过程。