5-ethoxycarbonyl-2-phenyl-3,4-dihydropyrimidine-4-on-3-yl-acetic acid | 235763-45-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 5-ethoxycarbonyl-2-phenyl-3,4-dihydropyrimidine-4-on-3-yl-acetic acid
• 英文别名: 2-(5-Ethoxycarbonyl-6-oxo-2-phenylpyrimidin-1-yl)acetic acid
• CAS: 235763-45-8
• 化学式: C₁₅H₁₄N₂O₅
• 分子量: 302.287
• InChiKey: LVXYJQQPJKRLGP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  96.3
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• NOVEL ACETAMIDE DERIVATIVE AND USE THEREOF
  申请人：Nippon Kayaku Kabushiki Kaisha

  公开号：EP1055683A1

  公开（公告）日：2000-11-29

  The present Invention relates to a novel acetamide derivative represented by the following Formula 1, which has an inhibition activity for chymotrypsin type proteases and is usefull as an inhibitor for the above enzyme, especially as an inhibitor for chymase, and the use thereof as a medicine, for example, an antiasthma drug or a drug for curing vascular injuries complicated with angiogenesis and atheroma.    wherein R0 represents a substituted or unsubstituted phenyl group, R1 represents an aryl group, a heteroaryl or an aliphatic lower alkyl group with or without substituents, R2 represents a substituted or unsubstituted alkyl, an aryl alkyl, a heteroaryl alkyl, and a heteroaryloxy alkyl or the like, J represents a carbonyl group, or a methylene group or the like, L represents a methoxy, hydroxyl or acetyloxy group or the like, X and Y independently represents a nitrogen atom or a carbon atom, Z represents a methylene group or a polyethylene group optionally having a substituent.

  本发明涉及一种由下式 1 表示的新型乙酰胺衍生物，该衍生物对糜蛋白酶型蛋白酶具有抑制活性，可用作上述酶的抑制剂，特别是糜蛋白酶的抑制剂，并可将其用作药物，例如抗哮喘药物或治疗并发血管生成和动脉粥样硬化的血管损伤的药物。 其中 R0 代表取代或未取代的苯基，R1 代表芳基、杂芳基或带或不带取代基的脂族低级烷基，R2 代表取代或未取代的烷基、芳基烷基、杂芳基烷基和杂芳基氧基烷基或类似物、J 代表羰基或亚甲基或类似基团，L 代表甲氧基、羟基或乙酰氧基或类似基团，X 和 Y 独立地代表氮原子或碳原子，Z 代表亚甲基或可选具有取代基的聚乙烯基团。
• US6300337B1
  申请人：——

  公开号：US6300337B1

  公开（公告）日：2001-10-09