Novel quinolone 5-(n-heterosubstituted amino) antimicrobials

Details Novel quinolone 5-(n-heterosubstituted amino) antimicrobials Novel quinolone 5-(n-heterosubstituted amino) antimicrobials

C - Chemistry, Metallurgy

07

D

C07D 498/00 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 215/56 (2006.01) C07D 401/04 (2006.01) C07D 471/00 (2006.01) C07D 498/06 (2006.01) C07D 498/14 (2006.01) C07D 513/00 (2006.01) C07D 513/04 (2006.01) C07D 513/16 (2006.01) C07D 515/06 (2006.01)

Patent

CA 2188918

The invention relates to antimicrobial 5-(N-heterosubstituted amino) quinolone compounds having a structure according to formula (I) or (II), wherein: (1) R1, R2, R3, R9 and R10 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and (2) (a) R4 and R5 are, independently, hydrogen; lower alkyl; cycloalkyl; heteroalkyl; or -C(=O)-X-R8, where X is a covalent bond, N, O, or S, and R8 is lower alkyl, lower alkenyl, arylalkyl, a carbocyclic ring, or a heterocyclic ring; or (b) R4 and R5 together comprise a heterocyclic ring that includes the nitrogen to which they are bonded; and the pharmaceutically-acceptable salts, biohydrolyzable esters, biohydrolyzable amides, and solvates thereof. The invention also relates to compositions comprising these compounds, as well as methods for treating infectious disorders using the compounds and/or compositions of the present invention.

L'invention se rapporte à des composés antimicrobiens de quinolone 5-(N-hétérosubstitué amino) ayant une structure selon la formule (I) ou (II) dans laquelle: (1) R?1¿, R?2¿, R?3¿, R?9¿ et R?10¿ représentent n'importe quelle variété de quinolone et de structures hétérocycliques apparentées, similaires à celles de la technique antérieure pour avoir une activité antimicrobienne; et (2) (a) R?4¿ et R?5¿ représentent, indépendamment, hydrogène; alkyle inférieur; cycloalkyle; hétéroalkyle; ou bien -C(=O)-X-R?8¿, où X est une liaison covalente, N, O ou S, et R?8¿ représente alkyle inférieur, alcényle inférieur, arylalkyle, un noyau carbocyclique ou un noyau hétérocyclique; ou bien (b) R?4¿ et R?5¿ réunis comprennent un noyau hétérocyclique qui contient l'azote auquel ils sont liés. L'invention se rapporte également aux sels pharmaceutiquement acceptables, aux esters biohydrolysables, aux amides biohydrolysables et aux solvates de ceux-ci, ainsi qu'à des compositions comprenant ces composés et à des procédés de traitement de maladies infectieuses mettant en oeuvre ces composés et/ou les compositions de la présente invention.

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