C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/4709 (2006.01) C07D 209/44 (2006.01) C07D 215/32 (2006.01) C07D 215/56 (2006.01)
Patent
CA 2307824
This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula [1] which is useful as an antibacterial agent, and an intermediate thereof: Image wherein R1 represents a hydrogen atom or a carboxyl- protecting group; R2 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R3 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R4 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R4 bonds; R5 represents a hydrogen atom, an amino- protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R6 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C-R7 in which R7 represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7- isoindoline-quinolonecarboxylic acid represented by the general formula [1], a hydrate thereof and a composition comprising them as an active ingredient.
Procédés servant à préparer des dérivés 7-isoindolinequinolonecarboxyliques utiles en tant qu'agents antibactériens et représentés par la formule générale suivante (1), ainsi que leurs intermédiaires; sels de dérivés 7-isoindolinequinolonecarboxyliques représentés par la formule (1) et leurs hydrates; compositions les contenant en tant qu'ingrédient actif: (1) dans laquelle R<1> représente hydrogène ou un groupe protecteur carboxyle; R<2> représente cycloalkyle etc.; R<3> représente au moins un élément sélectionné dans hydrogène, halogène etc.; R<4> représente au moins un élément sélectionné dans hydrogène, alkyle éventuellement substitué etc.; R<5> représente hydrogène, alkyle éventuellement substitué etc.; R<6> représente hydrogène etc.; A représente CH ou C-R<7>, dans laquelle R<7> représente alkoxy etc..
Hamamoto Shoichi
Hayashi Kazuya
Kiyoto Taro
Kotsubo Hironori
Matsukura Hiroko
Marks & Clerk
Toyama Chemical Co. Ltd.
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