N-phenethyl-1,6-naphthyridine-2-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N-phenethyl-1,6-naphthyridine-2-carboxamide
• 英文别名: N-(2-phenylethyl)-1,6-naphthyridine-2-carboxamide
• 化学式: C₁₇H₁₅N₃O
• 分子量: 277.326
• InChiKey: PQSMVQIVPPFZGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  54.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-氨基-3-吡啶甲醛 在 sodium hydroxide 、 1-羟基苯并三唑 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 N-phenethyl-1,6-naphthyridine-2-carboxamide
  参考文献：
  名称：

  Discovery of 1,6-Naphthyridines as a Novel Class of Potent and Selective Human Cytomegalovirus Inhibitors

  摘要：

  DOI：

  10.1021/jm9902483

文献信息

• NAPTHYRIDINE COMPOUNDS AS ROCK INHIBITORS
  申请人：GPC Biotech AG

  公开号：EP1833832A1

  公开（公告）日：2007-09-19
• Napthyridine Compounds As Rock Inhibitors
  申请人：Muller Stefan

  公开号：US20080207677A1

  公开（公告）日：2008-08-28

  The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.
• [EN] NAPTHYRIDINE COMPOUNDS AS ROCK INHIBITORS<br/>[FR] COMPOSES DE NAPHTYRIDINE UTILISES COMME INHIBITEURS DE ROCK
  申请人：GPC BIOTECH AG

  公开号：WO2007060028A1

  公开（公告）日：2007-05-31

  [EN] The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.
  [FR] Cette invention concerne des composés comportant un échafaudage de naphthyridine et des formes stéréoisomériques, des promédicaments, des solvates, des hydrates et/ou des sels pharmaceutiquement acceptables de ces composés, ainsi que des compositions pharmaceutiques contenant au moins un de ces dérivés de naphthyridine de même qu'un vecteur, un excipient et/ou des diluants pharmaceutiquement acceptables. Ces composés de naphthyridine ont été identifiés comme étant des inhibiteurs de la protéine kinase ROCK2, aussi connue sous le nom de Rho-kinase, et sont utilisés pour traiter des cancers (croissance tumorale et métastases), la dysérection, des maladies cardio-vasculaires, l'hypertension, l'angine de poitrine, l'ischémie cérébrale, le vasospasme cérébral, l'insuffisance cardiaque, l'hypertrophie du myocarde, l'athérosclérose, la resténose, des traumatismes médullaires, la dégénérescence neuronale, des troubles thrombotiques, l'asthme, le glaucome, l'inflammation, des maladies antivirales (telles que le VIH) et l'ostéoporose.