8-methoxy-quinolonecarboxylic acid derivatives

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 401/04 (2006.01) A61K 31/47 (2006.01) A61K 31/535 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2152828

8-Methoxy-quinolonecarboxylic acid derivatives of the formula Image (I) wherein Rl is a hydrogen atom, a lower alkyl, a phenylalkyl or an ester residue hydrolyzable in the living body, R2 is a hydrogen atom or methyl and n is an integer of 0 or 1, optical isomers thereof, pharmaceutically acceptable salts thereof and hydrates thereof. The 8-methoxy-quinolonecarboxylic acid derivatives of the present invention have enforced and a wide range of in vitro and in vivo antibacterial effects against Gram-positive bacteria, while retaining a strong antibacterial effect against Gram- negative bacteria, that the conventional quinolonecarboxylic acid antibacterial agents have. In addition, the compounds of the present invention scarcely show problematic side-effects and are low toxic. Therefore, they are expected to show more superior clinical effects as antibacterial agents.

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