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Heterocyclic spiro-derivative

Imported: 23 Feb '17 | Published: 22 Oct '02

Makoto Takemura, Youichi Kimura, Hitoshi Ohki

USPTO - Utility Patents

Abstract

The present invention provides an antibacterial compound useful as medicines, animal drugs, fisheries drugs or antibacterial preservatives and to an antibacterial agent or preparation which contains the same, more particularly a compound which possesses high safety and excellent activity against a broad range of bacterial species including quinolone-resistant strains. A quinolone derivative of the following formula (I) which has a group derived from the heterocyclic spiro-compound at the 7-positioned R

2 and the halogenocyclopropyl group at the N

1-position, prefereably a compound of pure isomer, and an antibacterial agent containing the derivative compound.

Claims

1. A stereochemically pure (N

1-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivative represented by formula (I):

2. The compound or a salt thereof according to claim 1, wherein said halogenocyclopropyl group in the formula (I) is (1R,2S)-2-fluorocyclopropyl group.

3. The compound or a salt thereof according to claim 2, wherein X

1 is a fluorine atom.

4. A stereochemically pure 7-[1-amino-5-azaspiro[2.4]hetan-5-yl]-6-fluoro-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-8-methyl-4-oxoquinolin-3-carboxylic acid or a salt thereof.

5. A stereochemically pure 5-Amino-7-[1-amino-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or a salt thereof.

6. The compound represented by the following formula, or a salt thereof

7. The compound represented by the following formula, or a salt thereof