New polycyclic phthalazine derivatives and the use thereof

Details New polycyclic phthalazine derivatives and the use thereof New polycyclic phthalazine derivatives and the use thereof

C - Chemistry, Metallurgy

07

D

C07D 237/26 (2006.01) A61K 31/50 (2006.01)

Patent

CA 2261756

New polycyclic phthalazins, in particular 2-substituted maduraphthalazins (10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-1,2,6,7,9,14- hexahydronaphtaceno-1,2-g-phthalazins), of formula (I) and their use are disclosed. The disclosed compounds are effective against gram-positive bacterial strains, in particular against multiresistant staphylococci (MRSA) and against glycopeptide-resistant, for example vancomycin-resistant enterococci, and are thus suitable for preparing anti-bacterially effective medicaments. In formula (I), R1 is carboxyalkyl or carboxyaryl, and R2, R3 stand for H, acyl (for example CO-alkyl, COO-alkyl), R1 being different from optionally substituted carboxyphenyl when R3 stands for C1-8alkanoyl. The invention also relates to the salts, amides and esters of these compounds of Formula (I).

L'invention concerne de nouvelles phtalazines polycycliques, notamment des maduraphtalazines (10, 12,15,16-tétrahydroxy-8-méthoxy-11-méthyl-1,9,14-trioxo-1,2,6,7,9,14-hexahydronaphtacéno-[1,2-gl]-phtalazine) substituées en position 2, de la formule (I) et leur utilisation. Les composés sont actifs à l'encontre de souches bactériennes Gram positif, notamment à l'encontre de staphylocoques multirésistants (MRSA), ainsi qu'à l'encontre d'entérocoques glycopeptidorésistants, par ex. résistants à la vancomycine, et s'utilisent pour préparer des médicaments à action antibactérienne. Dans la formule (I), R?1¿ désigne carboxyalkyle ou carboxyaryle, et R?2¿, R?3¿ désignent H, acyle (par ex. CO-alkyle, COO-alkyle), R?1¿ étant différent de carboxyphényle éventuellement substitué, lorsque R?3¿ désigne alcanoyle C¿1-8?. L'invention concerne également les sels, amides et esters des composés répondant à la formule (I).

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