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Claims for Patent: 6,723,734

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Claims for Patent: 6,723,734

Title: Salt of naphthyridine carboxylic acid derivative
Abstract:7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-ox o-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.
Inventor(s): Kim; Ae Ri (Daejeon, KR), Lee; Jin Hwa (Daejeon, KR), Park; Ki Sook (Daejeon, KR), Choi; Jong Ryoo (Daejeon, KR), Lee; Tae Hee (Daejeon, KR), Chang; Jay Hyok (Daejeon, KR), Nam; Do Hyun (Daejeon, KR), Choi; Hoon (Daejeon, KR)
Assignee: LG Life Sciences, Ltd. (Seoul, KR)
Application Number:10/223,850
Patent Claims: 1. A crystal form of 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate.nH.sub.2 O, wherein n is in the range of from 1 to 4.

2. The compound according to claim 1 having peaks at 2.theta.=8.0, 12.2 and 14.7.degree. in its X-ray diffraction pattern.

3. The compound according to claim 1 having an X-ray diffraction pattern substantially as shown in FIG. 7.

4. The compound according to claim 1 having peaks at 2.theta.=7.7 and 11.8.degree. in its X-ray diffraction pattern.

5. The compound according to claim 1 having an X-ray diffraction pattern substantially as shown in FIG. 6.

6. A pharmaceutical composition comprising a compound according to claim 1, together with a pharmaceutically acceptable carrier or excipient.

7. A method of treating bacterial infections in humans and animals comprising administering a therapeutically effective amount of a compound according to claim 1.

8. A process for preparing a compound according to claim 1, comprising reacting 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid with methanesulfonic acid, crystallizing a resulting compound from a solution, and adjusting the hydration of the resulting compound.

9. A process for preparing a compound according to claim 1, comprising exposing 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate anhydrate, or a solvate thereof, to a relative humidity of at least 75%.

10. The process according to claim 9, wherein the solvate comprises at least one organic solvent which is C.sub.1 -C.sub.4 haloalkane or C.sub.1 -C.sub.8 alcohol.

11. A solvate comprising a crystal form of 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and at least one organic solvent.

12. The pharmaceutical composition according to claim 6, wherein n is 1.5.

13. The pharmaceutical composition according to claim 6, wherein the compound has peaks at 2.theta.=8.0, 12.2 and 14.7.degree. in its X-ray diffraction pattern.

14. The pharmaceutical composition according to claim 6, wherein the compound has an X-ray diffraction pattern substantially as shown in FIG. 7.

15. The pharmaceutical composition according to claim 6, wherein n is 3.

16. The pharmaceutical composition according to claim 6, wherein the compound has peaks at 2.theta.=7.7 and 11.8.degree. in its X-ray diffraction pattern.

17. The pharmaceutical composition according to claim 6, wherein the compound has an X-ray diffraction pattern substantially as shown in FIG. 6.

18. The pharmaceutical composition according to claim 6, wherein the compound has a moisture content of from 4 to 6%.

19. The pharmaceutical composition according to claim 6, wherein the compound has a moisture content of from 9 to 11%.

20. The process according to claim 8, wherein the resulting compound is 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate.nH.sub.2 O, wherein n is 1.5.

21. The process according to claim 8, wherein the resulting compound has peaks at 2.theta.=8.0, 12.2 and 14.7.degree. in its X-ray diffraction pattern.

22. The process according to claim 8, wherein the resulting compound has an X-ray diffraction pattern substantially as shown in FIG. 7.

23. The process according to claim 8, wherein the solution comprises at least one of C.sub.1 -C.sub.4 haloalkane, C.sub.1 -C.sub.8 alcohol, and water.

24. The process according to claim 23, wherein the solution comprises at least one of dichloromethane, chloroform, 1,2-dichloroethane, methanol, ethanol, propanol, and water.

25. The process according to claim 9, wherein the compound prepared is 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate.nH.sub.2 O, wherein n is 1.5.

26. The process according to claim 9, wherein the compound prepared is 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate.nH.sub.2 O, wherein n is 3.

27. The process according to claim 9, wherein the compound prepared has peaks at 2.theta.=7.7 and 11.8.degree. in its X-ray diffraction pattern.

28. The process according to claim 9, wherein the compound prepared has an X-ray diffraction pattern substantially as shown in FIG. 6.

29. The process according to claim 10, wherein the at least one organic solvent is ethanol, dichloromethane, isopropanol, or 2-methyl-2-propanol.

30. The solvate according to claim 11, wherein the at least one organic solvent is C.sub.1 -C.sub.4 haloalkane or C.sub.1 -C.sub.8 alcohol.

31. The solvate according to claim 11, wherein the at least one organic solvent is ethanol, dichloromethane, isopropanol, or 2-methyl-2-propanol.

32. A process for preparing a solvate of 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate with at least one organic solvent, comprising: dissolving 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-o xo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate anhydrate in a mixture of ethanol and water to form a solution; heating the solution to 50.degree. C.; cooling the solution to -3.degree. C.; allowing the solution to stand at -3.degree. C., wherein a solid solvate forms; filtering the solid solvate; and washing the solid solvate with a mixture of ethanol and water.

33. A method for manufacturing a pharmaceutical composition comprising mixing a compound according to claim 1, and a pharmaceutically acceptable carrier or excipient.
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