US2022235009A1PendingUtilityA1

Stable crystal of 4-oxoquinoline compound

76
Assignee: JAPAN TOBACCO INCPriority: May 20, 2004Filed: Aug 24, 2021Published: Jul 28, 2022
Est. expiryMay 20, 2024(expired)· nominal 20-yr term from priority
Inventors:Motohide SatohTakahisa MotomuraTakashi MatsudaKentaro KondoKoji AndoKoji MatsudaShuji MiyakeHideto Uehara
A61K 31/47A61P 31/00C07D 215/56A61P 31/18
76
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Claims

Abstract

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.

Claims

exact text as granted — not AI-modified
1 - 14 . (canceled) 
     
     
         15 . A crystal form of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-meth-oxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, having an X-ray powder diffraction pattern comprising a characteristic diffraction peak at 6.56±0.2° 2θ. 
     
     
         16 . The crystal form of  claim 15 , having an X-ray powder diffraction pattern comprising a characteristic diffraction peak at 6.56±0.1° 2θ. 
     
     
         17 . The crystal form of  claim 15 , having an X-ray powder diffraction pattern comprising a characteristic diffraction peak at 6.56±0.06° 2θ. 
     
     
         18 . The crystal form of  claim 15 , having an X-ray powder diffraction pattern further comprising a characteristic diffraction peak at 21.22±0.2° 2θ. 
     
     
         19 . The crystal form of  claim 16 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.1° and 21.22±0.1° 2θ. 
     
     
         20 . The crystal form of  claim 17 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.06°. and 21.22±0.06° 2θ. 
     
     
         21 . The crystal form of  claim 18 , having an X-ray powder diffraction pattern further comprising a characteristic diffraction peak at 13.20±0.2° 2θ. 
     
     
         22 . The crystal form of  claim 19 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.1°, 13.20±0.1°, and 21.22±0.1° 2θ. 
     
     
         23 . The crystal form of  claim 21 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.06°, 13.20±0.06°, and 21.22±0.06° 2θ. 
     
     
         24 . A crystal form of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-meth-oxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.2°, 13.20±0.2°, 19.86±0.2°, 20.84±0.2°, 21.22±0.2°, and 25.22±0.2° 2θ. 
     
     
         25 . The crystal form of  claim 24 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.1°, 13.20±0.1°, 15.68±0.1°, 21.22±0.1°, and 25.22±0.1° 2θ. 
     
     
         26 . The crystal form of  claim 24 , having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 6.56±0.06°, 13.20±0.06°, 15.68±0.06°, 20.84±0.06°, 21.22±0.06°, and 25.22±0.06° 2θ. 
     
     
         27 . Crystal form I of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-meth-oxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid having an X-ray powder diffraction pattern as shown in  FIG. 1 . 
     
     
         28 . The crystal form of any one of  claims 15  to  27  having a purity of crystal of not less than 70%. 
     
     
         29 . The crystal form of any one of  claims 15  to  27  having a purity of crystal of not less than 80%. 
     
     
         30 . The crystal form of any one of  claims 15  to  27  having a purity of crystal of not less than 90%. 
     
     
         31 . The crystal form of any one of  claims 15  to  27  having a purity of crystal of not less than 95%. 
     
     
         32 . The crystal form of any one of  claims 15  to  27  having a purity of crystal of not less than 98%. 
     
     
         33 . A pharmaceutical composition comprising the crystal form of any one of  claims 15  to  27  and a pharmaceutically acceptable carrier. 
     
     
         34 . The pharmaceutical composition of  claim 33  wherein the composition is in the form of a tablet, pill, powder or granule.

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