methyl 7-methoxy-1,2-dihydro-1-oxophthalazin-4-ylcarboxylate | 53960-11-5

• 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: methyl 7-methoxy-1,2-dihydro-1-oxophthalazin-4-ylcarboxylate
• 英文别名: methyl 6-methoxy-4-oxo-3H-phthalazine-1-carboxylate
• CAS: 53960-11-5
• 化学式: C₁₁H₁₀N₂O₄
• 分子量: 234.211
• InChiKey: KTTBHJYYNSLQRQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  77
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  6-methoxy-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid 、 碘甲烷 在 碳酸氢钠 作用下， 以 N-甲基乙酰胺 为溶剂， 生成 methyl 7-methoxy-1,2-dihydro-1-oxophthalazin-4-ylcarboxylate
  参考文献：
  名称：

  Phthalazin-4-ylacetic acid derivatives

  摘要：

  这项发明涉及一种酶抑制剂，通式I的新型邻苯二氮杂环戊酸衍生物：##STR1## 以及在适当情况下的药学上可接受的盐，其制药组合物，以及制造它们的类似方法。通式I的化合物是体内醣醇还原酶的抑制剂，因此可能对减少或预防外周效应的发展具有用处，例如黄斑水肿、白内障、视网膜病变或神经传导受损。一种优选化合物是2-(2-氟-4-溴苯基)-1,2-二氢-1-氧代邻苯二氮杂环戊酸。

  公开号：

  US04251528A1

文献信息

• Pharmaceutical compositions and method for the production of an
  申请人：Imperial Chemical Industries PLC

  公开号：US04393062A1

  公开（公告）日：1983-07-12

  This invention relates to enzyme inhibitory, novel phthalazin-4-ylacetic acid derivatives of the general formula I: ##STR1## and pharmaceutically acceptable salts as appropriate, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. The compounds of formula I are inhibitors of the enzyme aldose reductase in vivo and as such may be useful in the reduction or prevention of the development of the peripheral effects such as macular oedema, cataract, retinopathy or impaired neural conduction. A preferred compound is 2-(2-fluoro-4-bromobenzyl)-1,2-dihydro-1-oxophthalazin-4-ylacetic acid.

  本发明涉及一种酶抑制剂，一种新型的苯并噻唑-4-基乙酸衍生物，通式如下：##STR1##以及其药学上可接受的盐，药物组合物和类似物的制备方法。通式I的化合物在体内是醛糖还原酶的抑制剂，因此可能有助于减少或预防外周影响的发展，如黄斑水肿、白内障、视网膜病变或神经传导受损。一种优选的化合物是2-(2-氟-4-溴苯基)-1,2-二氢-1-氧化苯并噻唑-4-基乙酸。
• Enzyme inhibitory phthalazin-4-ylacetic acid derivatives, pharmaceutical compositions thereof, and process for their manufacture
  申请人：IMPERIAL CHEMICAL INDUSTRIES PLC

  公开号：EP0002895A1

  公开（公告）日：1979-07-11

  This invention relates to enzyme inhibitory, novel phthalazin-4-ylacetic acid derivatives of the general formula wherein R1 is a hydroxy or benzyloxy radical, or a C1-4- alkoxy radical optionally bearing an N-morpholino or a C1-4-alkylamino radical, X is oxygen or sulfur, the rings A and B may be substituted, pharmaceutically acceptable salts as appropriate, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. The compounds of formula I are inhibitors of the enzyme aldose reductase in vivo and as such may be useful in the reduction or prevention of the development of the peripheral effects such as macular oedema, cataract, retinopathy or impaired neural conduction. A preferred compound is 2-(2-fluoro-4-bromobenzyl)-1,2-dihydro-1-oxophthalazin-4- ylacetic acid.

  本发明涉及通式如下的酶抑制性新型酞嗪-4-基乙酸衍生物 其中 R1 是羟基或苄氧基，或 C1-4-烷氧基，可选带有 N-吗啉基或 C1-4-烷基氨基，X 是氧或硫，环 A 和 B 可被取代，适当的药学上可接受的盐，其药物组合物，以及生产它们的类比工艺。式 I 的化合物是体内醛糖还原酶的抑制剂，因此可用于减少或预防黄斑水肿、白内障、视网膜病变或神经传导受损等外周效应的发生。一种优选化合物是 2-（2-氟-4-溴苄基）-1,2-二氢-1-氧代酞嗪-4-乙酸。
• US4251528A
  申请人：——

  公开号：US4251528A

  公开（公告）日：1981-02-17
• US4393062A
  申请人：——

  公开号：US4393062A

  公开（公告）日：1983-07-12
• Phthalazin-4-ylacetic acid derivatives
  申请人：Imperial Chemical Industries Limited

  公开号：US04251528A1

  公开（公告）日：1981-02-17

  This invention relates to enzyme inhibitory, novel phthalazin-4-ylacetic acid derivatives of the general formula I: ##STR1## and pharmaceutically acceptable salts as appropriate, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. The compounds of formula I are inhibitors of the enzyme aldose reductase in vivo and as such may be useful in the reduction or prevention of the development of the peripheral effects such as macular oedema, cataract, retinopathy or impaired neural conduction. A preferred compound is 2-(2-fluoro-4-bromobenzyl)-1,2-dihydro-1-oxophthalazin-4-ylacetic acid.

  这项发明涉及一种酶抑制剂，通式I的新型邻苯二氮杂环戊酸衍生物：##STR1## 以及在适当情况下的药学上可接受的盐，其制药组合物，以及制造它们的类似方法。通式I的化合物是体内醣醇还原酶的抑制剂，因此可能对减少或预防外周效应的发展具有用处，例如黄斑水肿、白内障、视网膜病变或神经传导受损。一种优选化合物是2-(2-氟-4-溴苯基)-1,2-二氢-1-氧代邻苯二氮杂环戊酸。