Optically active quinoline carboxylic acid derivatives...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/04 (2006.01) A61K 31/47 (2006.01) C07D 401/04 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2374767

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.

La présente invention concerne des dérivés d'acide quinoléine-carboxylique actifs optiquement, leur sels et solvates acceptables sur le plan pharmaceutique, ainsi qu'un procédé permettant leur préparation. Plus particulièrement, la présente invention concerne des dérivés d'acide quinoléine-carboxylique actifs optiquement ayant des substituts 4-aminométhyl-4-méthyl-3-(Z)-alcoxyiminopyrrolidine provoquant une activité optique dans la position 7 de la quinolone. Etant donné que les composés de la présente invention présentent une activité antibactérienne supérieure à celle de leurs énantiomères, des mélanges racémiques de ceux-ci et d'autres agents antibactériens présentent une bonne caractéristique pharmacocinétique sans comporter de phototoxicité, le composé de cette invention s'avérant utile pour un agent antibactérien.

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