8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones...

Details 8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones... 8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones...

C - Chemistry, Metallurgy

07

D

C07D 513/04 (2006.01) A61K 31/437 (2006.01) A61P 31/04 (2006.01) A61P 33/02 (2006.01)

Patent

CA 2587485

The invention provides compounds and salts of Formula I and Formula II which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and /or selective inhibitors of bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.

L'invention concerne des composés et des sels représentés par les formules (I) et (II), qui possèdent une activité antimicrobienne. L'invention concerne également de nouveaux intermédiaires synthétiques utilisés dans la préparation des composés des formules (I) et (II). Les variables n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 et R9 sont telles que définies dans la description de l'invention. Certains composés des formules (I) et (II) constituent des inhibiteurs puissants et/ou sélectifs de la synthèse d'ADN bactérien et de la réplication bactérienne. De plus, l'invention concerne des compositions antimicrobiennes, y compris des compositions pharmaceutiques, qui contiennent un ou plusieurs composés de formule (I) ou (II), ainsi qu'un ou plusieurs vecteurs, excipients, ou diluants. Des telles compositions peuvent contenir un composé de formule (I) ou (II) comme seul principe actif, ou peuvent contenir une combinaison de composés de formule (I) ou (II) et un ou plusieurs autres principes actifs. L'invention concerne par ailleurs des méthodes de traitement des infections antimicrobiennes chez les eucaryotes.

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