Novel pyridone carboxylic acid derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/04 (2006.01) A61K 31/435 (2006.01) C07D 209/52 (2006.01) C07D 221/04 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2152817

Novel pyridone carboxylic acid derivatives and pharmaceutically acceptable salts and physiologically hydrolyzable esters thereof are provided which are represented by formula (I), wherein R1 is a lower alkyl, a halogen-substituted lower alkyl, a lower alkenyl a cycloalkyl, or a substituted- or unsubstituted-phenyl group; R2 is a hydrogen atom, or a lower alkyl or an amino group; A is a nitrogen atom or the group C-X wherein X is a hydrogen or a halogen atom, or an alkoxy group; and Z is a group having formula (IV), wherein n is 1 or 2; R3 and R4 each represent a hydrogen atom or a lower alkyl group, with proviso that, if n is 2, one of R3 and R4, is a hydrogen atom; R5 and R6 each represent a hydrogen atom, or a hydroxy, a lower alkoxy or an amino group which is unsubstituted or substituted by a lower alkyl group, with proviso that one of R5 and R6 is a hydrogen atom; and R7 is a hydrogen atom or a lower alkyl group. The compounds of the present invention show potent and broad spectrum of antibacterial activities.

Divulgation concernant de nouveaux dérivés de l'acide pyridonecarboxylique et leurs sels pharmacocompatibles, ainsi que leurs esters physiologiquement hydrolysables, représentés par la formule (I), dans laquelle R1 est un alkyle inférieur, un alkyle inférieur avec substitution par un halogène, un alcényle inférieur, un cycloalkyle ou un phényle avec ou sans substitution; R2 est un atome d'hydrogène ou un alkyle inférieur ou un groupe amine; A est un atome d'azote ou le groupe C-X, X étant un atome d'hydrogène ou d'halogène, ou un groupe alcoxy; Z est un groupe de formule (IV), où n est 1 ou 2; R3 et R4 représentent chacun un atome d'hydrogène ou un alkyle inférieur, à la condition que, si n est 2, l'un de R3 ou de R4 soit un atome d'hydrogène; R5 et R6 représentent chacun un atome d'hydrogène ou un hydroxy, un alcoxy inférieur ou un groupe amine avec ou sans substitution par un alkyle inférieur, à la condition que l'un de R5 ou de R6 soit un atome d'hydrogène; R7 est un atome d'hydrogène ou un alkyle inférieur. Les composés de la présente invention offrent un spectre étendu et un grand potentiel d'activités antibactériennes.

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