Quinoline carboxylic acid derivatives having...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 401/04 (2006.01) A61K 31/435 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2151890

The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to a novel quinoline(naphthyri- dine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine sub- stituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quino- lone antibactrial agents having a weak activity against gram- positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property : Image (I) wherein R, R1, R2, R3, R4 and Q are defined as described in the specification. 129

La présente invention porte sur un nouveau quinolone possédant d'excellentes propriétés antibactériennes. Plus spécifiquement, l'invention porte sur un nouveau dérivé d'acide quinoline(naphtyridine)carboxylique, représenté par la formule (I), qui comporte un substituant 4-aminométhyl-3-oximepyrrolidine en position 7 du noyau de la quinolone et a un pouvoir antibactérien supérieur, comparativement aux agents antibactériens de type quinolone connus, n'agissant que faiblement contre les souches bactériennes gram-positives; le nouveau dérivé possède également un large spectre antibactérien et des propriétés pharmacocinétiques nettement améliorés. Dans la formule (I) Image : R, R1, R2, R3, R4 et Q correspondent aux définitions de la spécification

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