7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluorodethyl)-acid crystal
US-9090587-B2 · Jul 28, 2015 · US
US10918634B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10918634-B2 |
| Application number | US-201816189461-A |
| Country | US |
| Kind code | B2 |
| Filing date | Nov 13, 2018 |
| Priority date | Mar 13, 2015 |
| Publication date | Feb 16, 2021 |
| Grant date | Feb 16, 2021 |
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[Solution] A respiratory infection treating agent containing, as an active ingredient, 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
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The invention claimed is: 1. A method of treating a respiratory infection comprising, administering a compound, wherein the compound is 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, in an amount effective to treat the respiratory infection to a subject in need thereof, wherein the subject is human and wherein a dose of the compound per day is 75 mg or 150 mg. 2. The method of claim 1 , wherein the respiratory infection is one or more infections selected from the group consisting of pharyngitis, laryngitis, tonsillitis, acute bronchitis, pneumonia, and secondary infections of chronic respiratory diseases. 3. The method of claim 1 , wherein pathogenic bacteria causing the respiratory infection are one or more types of bacteria selected from the group consisting of bacteria belonging to Staphylococcus sp., bacteria belonging to Streptococcus sp., Moraxella catarrhalis , bacteria belonging to Klebsiella sp., Haemophilus influenzae , and Escherichia coli. 4. The method of claim 3 , wherein the pathogenic bacteria causing the respiratory infection are bacteria belonging to Streptococcus sp. or Staphylococcus sp. 5. The method of claim 3 , wherein pathogenic bacteria causing the respiratory infection have drug resistance. 6. A method of treating an infection which is one or more infections selected from the group consisting of pharyngitis, laryngitis, tonsillitis, acute bronchitis, pneumonia, secondary infections of chronic respiratory diseases, sinusitis, and tympanitis, and in which pathogenic bacteria are Streptococcus pneumoniae , the method comprising, administering a compound, wherein the compound is 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, in an amount effective to treat the respiratory infection to a subject in need thereof, wherein the subject is human and wherein a dose of the compound per day is 75 mg or 150 mg. 7. A method of treating an infection which is one or more infections selected from the group consisting of pharyngitis, laryngitis, tonsillitis, acute bronchitis, pneumonia, secondary infections of chronic respiratory diseases, sinusitis, and tympanitis, the method comprising administering a compound, wherein the compound is 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, to a subject in need thereof wherein a dose of the compound per day is 75 mg or 150 mg, wherein the subject is human. 8. The method of claim 1 , wherein a maximum plasma concentration of 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof after administration to the subject is 3 μg/mL or less. 9. The method of claim 1 , wherein a tissue distribution ratio of 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof into an alveolar epithelial lining fluid 1 hour after administration to the subject is 10 or more.
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