Pyridonecarboxylic acid derivatives substitued by a bicyclic...

Details Pyridonecarboxylic acid derivatives substitued by a bicyclic... Pyridonecarboxylic acid derivatives substitued by a bicyclic...

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/435 (2006.01) C07D 405/14 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2212007

This invention relates to a N1-(halogenocyclopropyl)- substituted pyridonecarboxylic acid derivative represented by the following formula (I): (see formula I) wherein X1 is a halogen atom or a hydrogen atom; X2 is a halogen atom; R1 is a hydrogen atom, a hydroxyl group, a thiol group, a halogenomethyl group, an amino group, an alkyl group or an alkoxy group which may have a substituent group; R2 is a group represented by the following formula (II): (see formula II) wherein R3 and R4 are independently a hydrogen atom or an alkyl group and n is an integer of 1 or 2; A is a nitrogen atom or a partial structure of the following formula (III): (see formula III) wherein X3 is a hydrogen atom, a halogen atom, a cyano group, an amino group, an alkyl group, a halogenomethyl group, an alkoxyl group or a halogenomethoxyl group which may have a substituent group; and R is a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidynyl group, a 5-alkyl-2-oxo- 1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxymethyl group or a phenylalkyl group, and provides a heterocyclic compound useful as antibacterial drugs.

Dérivés de l'acide pyridonecarboxylique à substitution N1-(halogénocyclopropyle) de formule (I) constituant des composés hétérocycliques à action antibactérienne. Dans la formule (I), X<1> représente halo ou hydrogène; X<2> représente halo; R<1> représente hydrogène, hydroxy, thiol, halométhyle, amino, alkyle ou alcoxy; R<2> représente un groupe de formule générale (II) (dans laquelle R<3> et R<4> représentent chacun hydrogène ou alkyle; et n représente 1 ou 2); A représente azote ou un groupe de formule générale (III) (dans laquelle X<3> représente halo, cyano, amino, alkyle, halométhyle, alcoxy ou halométoxy); et R représente hydrogène, phényle, acétoxyméthyle, pivaloyloxyméthyle, éthoxycarbonyle, choline, diméthylaminoéthyle, 5-indanyle, phtalidinyle, 5-alkyl-2-oxo-1, 3-dioxol-4-ylméthyle, 3-acétoxy-2-oxobutyle, alkyle, alcoxyméthyle ou phénylalkyle.

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