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Last Updated: December 16, 2025

Claims for Patent: 6,906,055


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Summary for Patent: 6,906,055
Title:Phosphonocephem compound
Abstract:A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.
Inventor(s):Tomoyasu Ishikawa, Shohei Hashiguchi, Yuji Iizawa
Assignee:Takeda Pharmaceutical Co Ltd
Application Number:US10/343,285
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,906,055
Patent Claims: 1. A compound of the formula: wherein X is CH3COOH or CH3CH2COOH, and n is 0 to 5.

2. The compound of claim 1, which is in the form of a crystal.

3. The compound of claim 1, wherein n is 1.

4. The compound of claim 1, wherein X is CH3COOH.

5. The compound of claim 4, having peaks near diffraction angles of 16.32, 19.06, 19.90, 20.98 and 23.24° in powder X-ray diffraction (CuKα).

6. The compound of claim 4, having peaks near diffration angles of 11.82, 17.16, 17.80, 19.32, 20.00, 21.20, 21.78, 22.94, 24.10 and 27.02° in powder X-ray diffraction (CuKα).

7. The compound of claim 1, wherein X is CH3CH2COOH.

8. The compound of claim 7, having peaks near diffraction angles of 16.30, 18.84, 19.70, 21.80 and 23.18° in powder X-ray diffraction (CuKα).

9. A pharmaceutical composition, comprising the compound of claim 1 and a pharmaceutically acceptable carrier, diluent or exipient.

10. A production method of a crystal of a compound represented by the formula: wherein X is CH3COOH or CH3CH2COOH, and n is 0 to 5, which comprises mixing [i] a compound represented by the formula: [ii] CH3COOH or CH3CH2COOH and [iii] water, dissolving them and allowing crystallization to take place.

11. The production method of claim 10, wherein the proportion (volume ratio) to be used of CH3COOH or CH3CH2COOH:water is 1:0.1-10.

12. A crystal obtained by mixing [i] a compound represented by the formula: [iii] CH3COOH or CH3CH2COOH and [iii] water, dissolving them and allowing crystallization to take place.

13. A disodium salt of a compound represented by the formula:

14. The disodium salt of claim 13, which is in the form of a crystal.

15. The disodium salt of claim 13, having peaks near diffraction angles of 17.02, 18.94, 22.86, 23.36 and 26.48° in powder X-ray diffraction (CuKα).

16. The compound of claim 2, wherein X is CH3COOH.

17. The compound of claim 2, wherein X is CH3CH2COOH.

18. A pharmaceutical composition, comprising the compound of claim 2 and a pharmaceutically acceptable carrier, diluent or excipient.

19. The disodium salt of claim 14, having peaks near diffraction angles of 17.02, 18.94, 22.86, 23.36 and 26.48° in powder X-ray diffraction (CuKα).

20. A method for making a crystal of a compound of formula (I): wherein X is CH3COOH or CH3CH2COOH, and n is 0 to 5, comprising crystallizing a compound of formula (Ia): from CH3COOH or CH3CH2COOH and water.

21. A crystal obtained by crystallizing a compound of formula (Ia): from CH3COOH or CH3CH2COOH and water.

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