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Last Updated: April 29, 2024

Claims for Patent: 4,980,470


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Summary for Patent: 4,980,470
Title: 8-alkoxyquinolonecarboxylic acid and salts thereof
Abstract:Quinolonecarboxylic acid derivatives of the following formula: ##STR1## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR2## (here, n is 0 or 1, R.sup.3 indicates a hydrogen atom or lower alkyl group, R.sup.4 indicates a hydrogen atom, lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.
Inventor(s): Masuzawa; Kuniyoshi (Koga, JP), Suzue; Seigo (Kuki, JP), Hirai; Keiji (Kuki, JP), Ishizaki; Takayoshi (Saitama, JP)
Assignee: Kyorin Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:07/003,822
Patent Claims: 1. 8-Alkoxyquinolonecarboxylic acid derivatives represented by a general formula (I); ##STR27## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR28## where, n is 0 or 1, R.sup.3 indicates a lower alkylgroup, R.sup.4 indicates a hydrogen atom, lower alkyl group, hydroxy-substituted lower alkyl group or halogenated lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group, the hydrates or the pharmaceutically acceptable acid addition or alklai salts thereof.

2. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-7-(1-piperazinyl)-3-qui nolinecarboxylic acid.

3. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(4-methyl-1-piperazinyl)-4- oxo-3-quinolinecarboxylic acid.

4. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4- oxo-3-quinolinecarboxylic acid.

5. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 7-(cis-3-amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro -8-methoxy-4-oxo-3-quinolinecarboxylic acid.

6. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 7-(trans-3-amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihyd ro-8-methoxy-4-oxo-3-quinolinecarboxylic acid.

7. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 7-(3-amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-m ethoxy-4-oxo-3-quinolinecarboxylic acid.

8. 8-Alkoxyquinolonecarboxylic acid derivative as claimed in claim 1, wherein said derivative is 1-cyclopropyl-6-fluoro-1,4-dihydro-8-ethoxy-4-oxo-7-(1-piperazinyl)-3-quin olinecarboxylic acid.

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