Quinolonecarboxylic acid derivatives or salts thereof

Details Quinolonecarboxylic acid derivatives or salts thereof Quinolonecarboxylic acid derivatives or salts thereof

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/47 (2006.01)

Patent

CA 2327328

Novel quinolonecarboxylic acid derivatives of general formula (1) or salts thereof which have potent antibacterial effects on gram-positive bacteria in particular Propionibacterium acnes (see formula I) (wherein R1 represents a hydrogen atom or a carboxyl-protective group; R2 represents an optionally substituted cycloalkyl group; R3 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkoxy or alkylthio group, an optionally protected hydroxyl or amino group, or a nitro group; R4 represents an optionally substituted alkyl or alkoxy group; and Z represents a pyridin-4-yl or pyridin-3-yl group which is optionally substituted with at least one group selected from a halogen atom, an optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio or amino group and an optionally protected hydroxyl or amino group).

L'invention concerne des nouveaux dérivés d'acide quinolonecarboxylique représentés par la formule générale (1), et ayant des effets antibactériens puissants sur les bactéries gram-positif, notamment propionibacterium acnes. Dans ladite formule (1), R<1> représente hydrogène ou un groupe protecteur carboxyle ; R<2> représentent cycloalkyle éventuellement substitué ; R<3> représente hydrogène, halogéno, alcoxy, alkylthio ou alkyle éventuellement substitué, amino, nitro ou hydroxy éventuellement protégé; R<4> représente alcoxy ou alkyle éventuellement substitué ; Z représente halogéno, alcényle, cycloalkyle, alcoxy, alkylthio, amino, pyridin-4-yle ou pyridin-3-yle ou alkyle substitué, possédant un ou plusieurs substituants choisis parmi amino et hydroxy éventuellement substitué.

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