(3R,4R)-1-carbobutoxy-3-ethyl-4(1-methyl-1H-imidazol-5-yl) methyl-2-pyrrolidinone | 137140-73-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (3R,4R)-1-carbobutoxy-3-ethyl-4(1-methyl-1H-imidazol-5-yl) methyl-2-pyrrolidinone
• 英文别名: butyl (3R,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]-2-oxopyrrolidine-1-carboxylate
• CAS: 137140-73-9
• 化学式: C₁₆H₂₅N₃O₃
• 分子量: 307.393
• InChiKey: IMSYDQRFGBRMNE-GXTWGEPZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.69
• 拓扑面积：
  64.4
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• N-substituted derivatives of 3R,4R-ethyl-[(1-methyl-1H-imidazol-5-yl)methyl]-2-pyrrolidinone
  申请人：ALLERGAN, INC.

  公开号：EP0429232A1

  公开（公告）日：1991-05-29

  The present invention relates to new carbonyl 3R,4R-­ethyl-[(1-methyl-1H-imidazol-5-yl)methyl]-2-pyrrolidinone derivatives carrying a carboxyester-type lipophilic moiety on the pyrrolidinone nitrogen. More particularly, the present invention concerns new N-substituted carbonyl-­3R,4R-ethyl-[(1-methyl-1H-imidazol-5-yl)methyl]-2-­pyrrolidinone derivatives of the formula (I): wherein R is an optionally substituted hydrocarbon group, and pharmaceutically acceptable acid addition salts thereof. The new compounds of the formula (I) are potent ocular hypotensives that are valuable antiglaucoma agents. They are also targeted for use in the treatment of so-called dry eye.

  本发明涉及新的羰基-3R,4R-乙基-[(1-甲基-1H-咪唑-5-基)甲基]-2-吡咯烷酮衍生物，其吡咯烷酮氮上带有羧酯型亲脂分子。 更具体地说，本发明涉及式（I）的新的 N-取代羰基-3R,4R-乙基-[(1-甲基-1H-咪唑-5-基)甲基]-2-吡咯烷酮衍生物：其中 R 是任选取代的烃基，以及它们的药学上可接受的酸加成盐。 式（I）的新化合物是有效的降眼压药，是有价值的抗青光眼药物。 它们还可用于治疗所谓的干眼症。