2-Ethoxymethyl-7-hydroxy-4(3H)-pteridinone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: 2-Ethoxymethyl-7-hydroxy-4(3H)-pteridinone
• 英文别名: 2-(ethoxymethyl)-3,8-dihydropteridine-4,7-dione
• 化学式: C₉H₁₀N₄O₃
• 分子量: 222.203
• InChiKey: GPTKOEVRJWAAMW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  92.2
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1,1,1,2-四乙氧基乙烷 、 3-amino-5-oxo-4,5-dihydro-pyrazine-2-carboxylic acid amide 在 乙酸酐 作用下， 以40%的产率得到2-Ethoxymethyl-7-hydroxy-4(3H)-pteridinone
  参考文献：
  名称：

  Synthesis and potential antiallergic activity of new pteridinones and related compounds

  摘要：

  The synthesis and pharmacological profile of a series of 2-alkoxy and 2-phenoxymethyl-3H-pteridin-4-ones and related compounds are described. These compounds displayed antiallergic activity in the passive cutaneous anaphylaxis test in rats. In contrast to both sodium cromoglycate and nedocromil sodium, many of our compounds were active when administered orally. The most potent in this series, 2-ethoxymethyl-3H-pteridin-4-one 2b (LCB 2183) was investigated in other models of allergy and inflammation. The antiallergic activity was confirmed and interesting antiinflammatory properties were observed. It was therefore selected for further development as a human therapeutic agent.

  DOI：

  10.1016/0223-5234(96)80364-3

文献信息

• 4(3H)-pteridinones, preparation processes and drugs containing them
  申请人：Lipha, Lyonnaise Industrielle Pharmaceutique

  公开号：US05167949A1

  公开（公告）日：1992-12-01

  The present invention relates to 4(3H)-pteridinones represented by the formula: ##STR1## in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-position, R.sub.1 is a hydrogen atom, a lower alkyl radical, a substituted or unsubstituted phenyl radical, a benzyl radical, a methoxymethyl group, an acetyl group, a 2-acetoxyethyl group or a 2,2,2-trifluoroethyl group and R.sub.2 is a hydrogen atom or a lower alkyl radical, especially a methyl radical. Application of these compounds as anti-allergic drugs.

  本发明涉及由以下公式表示的4（3H）-喜树碱酮：##STR1## 其中X是氧原子或硫原子，Y是氢原子，较低的烷基基团，特别是甲基基团，在6位或7位处的羟基基团，R.sub.1是氢原子，较低的烷基基团，取代或未取代的苯基基团，苄基基团，甲氧基甲基基团，乙酰基基团，2-乙酰氧乙基基团或2,2,2-三氟乙基基团，R.sub.2是氢原子或较低的烷基基团，特别是甲基基团。这些化合物作为抗过敏药物的应用。
• 4(3H)-pteridinone compounds
  申请人：Lipha, Lyonnaise Industrille Pharmaceutique

  公开号：US05270465A1

  公开（公告）日：1993-12-14

  The present invention relates to 4(3H)-pteridinones represented by the formula: ##STR1## in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-position, R.sub.1 is a hydrogen atom, a lower alkyl radical, a substituted or unsubstituted phenyl radical, a benzyl radical, a methoxymethyl group, an acetyl group, a 2-acetoxyethyl group or a 2,2,2-trifluoroethyl group and R.sub.2 is a hydrogen atom or a lower alkyl radical, especially a methyl radical. Application of these compounds as anti-allergic drugs.

  本发明涉及由以下式表示的4（3H）-喹嗪酮：##STR1## 其中，X是氧原子或硫原子，Y是氢原子，低碳基，特别是甲基基团，在6位或7位处是羟基基团，R1是氢原子，低碳基，取代或未取代的苯基基团，苄基基团，甲氧基甲基基团，乙酰基基团，2-乙酰氧乙基基团或2,2,2-三氟乙基基团，R2是氢原子或低碳基，特别是甲基基团。这些化合物的应用作为抗过敏药物。
• Pteridin-4 (3H)-ones, procédés de préparation et médicaments les contenant
  申请人：LIPHA, LYONNAISE INDUSTRIELLE PHARMACEUTIQUE

  公开号：EP0399856B1

  公开（公告）日：1995-08-09
• US5167949A
  申请人：——

  公开号：US5167949A

  公开（公告）日：1992-12-01
• US5270465A
  申请人：——

  公开号：US5270465A

  公开（公告）日：1993-12-14