Stable crystal of 4-oxoquinoline compound
Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2θ(°) as measured by X-ray powder diffractometry.
1. A crystal form of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, having an X-ray powder diffraction pattern comprising a characteristic diffraction peak at 8.54±0.2° ⊖.
2. The crystal form of claim 1 , having an X-ray powder diffraction pattern comprising a characteristic diffraction peak at 8.54±0.1° 2⊖.
3. The crystal form of claim 1 , having an X-ray powder diffraction pattern comprising a characteristic diffraction peak at 8.54±0.06° 2⊖.
4. The crystal form of claim 1 , having an X-ray powder diffraction pattern further comprising a characteristic diffraction peak at 17.24°±0.2° 2⊖.
5. The crystal form of claim 2 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.1° and 17.24°±0.1° 2⊖.
6. The crystal form of claim 3 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.06° and 17.24°±0.06° 2⊖.
7. The crystal form of claim 4 , having an X-ray powder diffraction pattern further comprising a characteristic diffraction peak at 14.02±0.2°, 2⊖.
8. The crystal form of claim 5 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.1°, 14.02±0.1°, and 17.24±0.1° 2⊖.
9. The crystal form of claim 7 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.06°, 14.02±0.06°, and 17.24±0.06° 2⊖.
10. A crystal form of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.2°, 14.02±0.2°, 15.8±0.2°, 17.06±0.2°, 17.24±0.2°, 24.16±0.2°, and 25.74±0.2° 2⊖.
11. The crystal form of claim 10 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.1°, 14.02±0.1°, 15.68±0.1°, 17.24±0.1°, 24.16±0.1°, and 25.74±0.1° 2⊖.
12. The crystal form of claim 10 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 8.54±0.06°, 14.02±0.06°, 15.68±0.06°, 17.06±0.06°, 17.24±0.06°, 24.16±0.06°, and 25.74±0.06° 2⊖.
13. Crystal form III of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid having an X-ray powder diffraction pattern as shown in FIG. 1 .
14. The crystal form of any one of claims 1 and 2 to 13 having a purity of crystal of not less than 70%.
15. The crystal form of any one of claims 1 and 2 to 13 having a purity of crystal of not less than 80%.
16. The crystal form of any one of claims 1 and 2 to 13 having a purity of crystal of not less than 90%.
17. The crystal form of any one of claims 1 and 2 to 13 having a purity of crystal of not less than 95%.
18. The crystal form of any one of claims 1 and 2 to 13 having a purity of crystal of not less than 98%.
19. A pharmaceutical composition comprising the crystal form of any one of claims 1 and 2 to 13 and a pharmaceutically acceptable carrier.
20. The pharmaceutical comppsition of claim 19 wherein the composition is in the form of a tablet, pill, powder or granule.