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Last Updated: December 4, 2020

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Claims for Patent: 7,635,704

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Summary for Patent: 7,635,704
Title:Stable crystal of 4-oxoquinoline compound
Abstract: Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-meth- oxy-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 2.theta.(.degree.) as measured by X-ray powder diffractmetry.
Inventor(s): Satoh; Motohide (Osaka, JP), Motomura; Takahisa (Osaka, JP), Matsuda; Takashi (Osaka, JP), Kondo; Kentaro (Osaka, JP), Ando; Koji (Osaka, JP), Matsuda; Koji (Osaka, JP), Miyake; Shuji (Osaka, JP), Uehara; Hideto (Osaka, JP)
Assignee: Japan Tobacco Inc. (Tokyo, JP)
Application Number:11/133,471
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,635,704
Patent Claims: 1. A crystal 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 having characteristic diffraction peaks at diffraction angles 2.theta. of 6.56.degree., 13.20.degree., 19.86.degree., 20.84.degree., 21.22.degree., 25.22.degree. as measured by X-ray powder diffractometer.

2. A crystal 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 having characteristic diffraction peaks at diffraction angles 2.theta. of 8.54.degree., 14.02.degree., 15.68.degree., 17.06.degree., 17.24.degree., 24.16.degree., 25.74.degree. as measured by X-ray powder diffractometer.

3. A crystal 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 extrapolated onset temperature of 162.1.+-.5.0.degree. C.

4. A pharmaceutical composition comprising the crystal of any one of claims 1-3, and a pharmaceutically acceptable carrier, wherein said carrier is not a liquid carrier.

5. The pharmaceutical composition of claim 4 wherein the composition is in the form of a tablet, pill, powder or granule.

6. The pharmaceutical composition of claim 5 wherein the composition is in the form of a tablet.

7. A method of inhibiting integrase comprising administering to a mammal an integrase-inhibiting amount of the crystal of any one of claims 1-3.

8. A method of treating a viral infection comprising administering to a mammal an anti-viral amount of the crystal of any one of claims 1-3.

9. A method for the treatment of an HIV infection comprising administering to an HIV-infected mammal an effective amount of the crystal of any one of claims 1-3.

10. An anti-HIV composition comprising the crystal of any one of claims 1-3 and one or more other anti-HIV active substances.

11. A method for the treatment of an HIV infection comprising administering to an HIV-infected mammal an effective amount of the crystal of any one of claims 1-3 and one or more other anti-HIV active substances.

12. The method of claim 7 wherein the mammal is a human.

13. The method of claim 8 wherein the mammal is a human.

14. The method of claim 9 wherein the mammal is a human.

15. The method of claim 11 wherein the mammal is a human.

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