1-cyclopropyl-6-fluoro-7-(3-methylamino-1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid

• 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: 1-cyclopropyl-6-fluoro-7-(3-methylamino-1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
• 英文别名: 1-Cyclopropyl-6-fluoro-7-[3-(methylamino)pyrrolidin-1-yl]-4-oxo-1,8-naphthyridine-3-carboxylic acid
• 化学式: C₁₇H₁₉FN₄O₃
• 分子量: 346.361
• InChiKey: VZAOXSYWEWYGDW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  85.8
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  1-cyclopropyl-6-fluoro-7-(3-methylamino-1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid 、 potassium tert-butylate 、 乙基(2Z)-3-(环丙基氨基)丙烯酸酯 在 三乙胺 作用下， 以 1,4-二氧六环 、 dioxane, 2,6-dichloro-5-fluoronicotinoyl chloride 为溶剂， 生成 环丙基萘啶羧酸乙酯
  参考文献：
  名称：

  Antibacterial

  摘要：

  本发明涉及一种式为##STR1##的1,8-萘啉衍生物，其中R.sub.1、R.sub.2和R.sub.3相同或不同，每个是氢或具有1至5个碳原子的低级烷基；以及其酯和盐的制备过程。这些化合物表现出优异的抗菌活性，是有用的抗菌剂。

  公开号：

  US04649144A1

文献信息

• Novel 1,8-Naphthyridine derivatives, and process for preparation thereof
  申请人：Dainippon Pharmaceutical Co., Ltd.

  公开号：EP0132845A2

  公开（公告）日：1985-02-13

  The present invention relates to a 1,8-naphthyridine derivative of the formula wherein R1, R2 and R3 are the same or different and each hydrogen or lower alkyl having 1 to 5 carbon atoms; and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.

  本发明涉及一种 1,8-萘啶衍生物，其式中 R1、R2 和 R3 是相同或不同的，每个都是氢或具有 1 至 5 个碳原子的低级烷基；以及其酯和盐及其制备方法。 这些化合物显示出优异的抗菌活性，是有用的抗菌剂。
• SUSTAINED-RELEASE ORAL OINTMENT
  申请人：TOYAMA CHEMICAL CO., LTD.

  公开号：EP0788801A1

  公开（公告）日：1997-08-13

  The preent invention relates to a sustained-release oral ointment which comprises a hydrophobic ointment base, an adhesive substance, an aluminum compound and a drug. The ointment is useful as a sustained-release oral ointment which has applicability to an oral mucosa, particularly to a peridontal pocket, sustained-release properties to supply a drug to affected part over a long period of time while maintaining the concentration thereof at a sufficiently high level, and enhanced ratio of utilization of drug (the ratio of the total amount of drug released to affected part to the total amount of drug in the ointment applied).

  本发明涉及一种缓释口服软膏，它由疏水性软膏基质、粘合物质、铝化合物和药物组成。该软膏可作为一种缓释口腔软膏，适用于口腔粘膜，特别是牙周袋；具有缓释特性，可在将药物浓度保持在足够高的水平的同时，长期向患部提供药物；并可提高药物利用率（释放到患部的药物总量与软膏中药物总量之比）。
• Method for stabilizing acriylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized acrylcarboxylic acid
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP0856310A2

  公开（公告）日：1998-08-05

  A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an aqueous solution containing a stabilized arylcarboxylic acid. According to the stabilization method of the present invention, arylcarboxylic acid and pharmacologically acceptable salts thereof, particularly pranoprofen, can be stabilized at every temperature range, particularly at lower temperatures, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.

  一种稳定芳基羧酸的方法，它包括向芳基羧酸或其药理上可接受的盐、其稳定剂和含有稳定的芳基羧酸的水溶液中加入杂环碱。根据本发明的稳定化方法，芳基羧酸及其药理学上可接受的盐，特别是普拉洛芬，可以在各种温度范围内稳定化，尤其是在较低温度下，从而使生产用作滴眼剂、滴鼻剂、滴耳剂等的水溶液成为可能。
• Method for solubilizing pyridonecarboxylic acid, solubilizer thereof and aqueous solution containing solubilized pyridonecarboxylic acid
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP0856316A1

  公开（公告）日：1998-08-05

  A method for solubilizing a pyridonecarboxylic acid or a pharmacologically acceptable salt thereof, which comprises adding an arylcarboxylic acid of the formula (I):         L1 -R1 COOH     (I) wherein L1 is an optionally substituted heterocyclic group or aryl group having not more than 14 carbon atoms, and R1 is an optionally substituted alkyl group having not more than 4 carbon atoms or a single bond, to the pyridonecarboxylic acid or the pharmacologically acceptable salt thereof, a solubilizer thereof and an aqueous solution containing a solubilized pyridonecarboxylic acid. According to the solubilization method of the present invention, the solubility of pyridonecarboxylic acid compounds and salts thereof at near physiological pH can be increased, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.

  一种增溶吡啶甲酸或其药理可接受盐的方法，包括加入式 (I) 的芳基羧酸： L1 -R1 COOH (I) 其中 L1 是具有不超过 14 个碳原子的任选取代的杂环基团或芳基，R1 是具有不超过 4 个碳原子或单键的任选取代的烷基。根据本发明的增溶方法，可以提高吡啶羧酸化合物及其盐在接近生理pH值时的溶解度，从而可以生产出用作滴眼剂、滴鼻剂、滴耳剂等的水溶液。
• METHOD FOR SOLUBILIZING PYRIDONECARBOXYLIC ACID, SOLUBILIZER THEREFOR, AQUEOUS SOLUTION PREPARATIONS CONTAINING PYRIDONECARBOXYLIC ACID AND PROCESS FOR PRODUCING THE SAME
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1044688A1

  公开（公告）日：2000-10-18

  The present invention relates to a method for solubilizing pyridonecarboxylic acid or a pharmacologically acceptable salt thereof, which includes incorporating glycyrrhetinic acid or a salt thereof and pyridonecarboxylic acid or a pharmacologically acceptable salt thereof, a solubilizer therefor, an aqueous solution containing the solubilized pyridonecarboxylic acid or a pharmacologically acceptable salt thereof, and a method of producing the aqueous solution. According to the solubilizing method of the present invention, the solubility of pyridonecarboxylic acid compound and salts thereof near physiological pH can be increased. Therefore, these compounds can be prepared into an aqueous solution to be applied as an eye drop, a nasal drop and an ear drop.

  本发明涉及一种增溶吡啶羧酸或其药理上可接受的盐的方法，它包括加入甘草酸或其盐和吡啶羧酸或其药理上可接受的盐、其增溶剂、含有增溶的吡啶羧酸或其药理上可接受的盐的水溶液，以及生产该水溶液的方法。根据本发明的增溶方法，可提高吡啶羧酸化合物及其盐在生理 pH 值附近的溶解度。因此，可以将这些化合物制备成水溶液，作为滴眼剂、滴鼻剂和滴耳剂使用。