3-Quinolinecarboxylic acid, 7-((4Z)-3-(aminomethyl)-4-(methoxyimino)-3-methyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-, monohydrochloride, (-)- | 309762-58-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 3-Quinolinecarboxylic acid, 7-((4Z)-3-(aminomethyl)-4-(methoxyimino)-3-methyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-, monohydrochloride, (-)-
• 英文别名: 7-[(4Z)-3-(aminomethyl)-4-methoxyimino-3-methylpyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid;hydrochloride
• CAS: 309762-58-1
• 化学式: C20H24ClFN4O4
• 分子量: 438.9
• InChiKey: CYZKABVRITVCDA-YFZNFVDXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.38
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• [EN] OPTICALLY ACTIVE QUINOLINE CARBOXYLIC ACID DERIVATIVES HAVING 7-PYRROLIDINE SUBSTITUTES CAUSING OPTICAL ACTIVITY AND A PROCESS FOR PREPARING THEREOF<br/>[FR] DERIVES D'ACIDE QUINOLEINE-CARBOXYLIQUE ACTIFS OPTIQUEMENT PRESENTANT DES SUBSTITUTS 7-PYRROLIDINES AMENANT UNE ACTIVITE OPTIQUE ET LEUR PROCEDE DE PREPARATION
  申请人：DONG WHA PHARM IND CO LTD

  公开号：WO2000071541A1

  公开（公告）日：2000-11-30

  The present invention relates to optically active quinoline carboxylic acid derivatives, pharmaceutically acceptable salts thereof, solvates thereof, and a process for preparation thereof. More particularly, the present invention relates to optically active quinoline carboxylic acid derivatives having 4-aminomethyl-4-methyl-3-(Z)-alkoxyiminopyrrolidine substitutes causing optical activity at 7-position of quinolone. As the compounds of the present invention have superior antibacterial activity to enantiomers thereof, racemic mixtures thereof and other antibacterial agents, have a good pharmacokinetic characteristic and show no phototoxicity, the compound of this invention is useful for an antibacterial agent.

  本发明涉及光学活性的喹啉羧酸衍生物、其药学上可接受的盐、溶剂化物及其制备方法。更具体地说，本发明涉及具有4-氨甲基-4-甲基-3-(Z)-烷氧基亚吡啶取代基在喹啉酮的7位引起光学活性的光学活性喹啉羧酸衍生物。由于本发明化合物具有优越的抗菌活性，比其对映体、混合物和其他抗菌剂更好，并具有良好的药代动力学特性和不显示光毒性，因此本发明化合物可用作抗菌剂。
• Optically active quinoline carboxylic acid derivatives with 7-pyrrolidine substituents causing optical activity and a process for the preparation thereof
  申请人：——

  公开号：US20040029915A1

  公开（公告）日：2004-02-12

  The present invention relates to optically active quinoline carboxylic acid derivatives, their pharmaceutically acceptable salts, their solvates, and a process for the preparation thereof. More specifically, the present invention relates to optically active)quinoline carboxylic acid derivatives containing 4-aminomethyl-4-methyl-3-(Z)-alkoxyiminopyrrolidine substituents causing optical activity at the 7-position of the quinolone nuclei. As the compounds of the present invention have superior antibacterial activity and pharmacokinetic profiles to their enantiomers, their racemates and conventional antibacterial agents, with nearly no phototoxicity, the compounds of this invention are useful for antibacterial agents.

  本发明涉及光学活性喹啉羧酸衍生物、它们的药学上可接受的盐、它们的溶解物以及它们的制备工艺。更具体地说，本发明涉及光学活性)喹啉羧酸衍生物，其含有 4-氨基甲基-4-甲基-3-(Z)-烷氧基亚氨基吡咯烷取代基，可在喹诺酮核的 7 位产生光学活性。由于本发明化合物的抗菌活性和药代动力学特征优于其对映体、外消旋体和传统抗菌剂，而且几乎没有光毒性，因此本发明化合物可用于抗菌剂。
• EP1187835A4
  申请人：——

  公开号：EP1187835A4

  公开（公告）日：2003-01-29
• OPTICALLY ACTIVE QUINOLINE CARBOXYLIC ACID DERIVATIVES HAVING 7-PYRROLIDINE SUBSTITUTES CAUSING OPTICAL ACTIVITY AND A PROCESS FOR PREPARING THEREOF
  申请人：DONG WHA PHARMACEUTICAL INDUSTRIAL CO. LTD.

  公开号：EP1187835A1

  公开（公告）日：2002-03-20
• US6649763B1
  申请人：——

  公开号：US6649763B1

  公开（公告）日：2003-11-18