US 6,649,763 B1 · Optically active quinoline carboxylic acid derivatives with 7-pyrrolidine substituents causing optical activity and a process for the preparation thereof

Abstract

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)-alkoxyirninopyrrolidine 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.

Claims8

Dependent claims

An optically active quinoline carboxylic acid derivative represented by the following formula 1, containing optical activity-causing 4-aminomethyl-4-methyl-3-(Z)-alkoxyiminopyrrolidine substituents at the 7-position of the quinolone nuclei, or a pharmaceutically acceptable salt thereof:

wherein,
Q is selected from the group consisting of C—H, C—F and C—Cl;
Y is H or NH2;
R is a C1-C4 straight or branched alkyl group, an allyl group or a benzyl group;
and
* represents an optically pure chiral carbon atom.

3 more elements

Dependencies are inferred from the claim text.

Optically active quinoline carboxylic acid derivatives with 7-pyrrolidine substituents causing optical activity and a process for the preparation thereof

Life of this patent

Optically active quinoline carboxylic acid derivatives with 7-pyrrolidine substituents causing optical activity and a process for the preparation thereof

Life of this patent

Abstract

Claims8