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Claims for Patent: 6,906,055

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Claims for Patent: 6,906,055

Title: Phosphonocephem compound
Abstract:A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH.sub.3 COOH, CH.sub.3 CH.sub.2 COOH or CH.sub.3 CN, 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. ##STR1##
Inventor(s): Ishikawa; Tomoyasu (Otsu, JP), Hashiguchi; Shohei (Toyonaka, JP), Iizawa; Yuji (Muko, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:10/343,285
Patent Claims: 1. A compound of the formula: ##STR11##

wherein X is CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH, 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 CH.sub.3 COOH.

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

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.degree. in powder X-ray diffraction (CuK.alpha.).

7. The compound of claim 1, wherein X is CH.sub.3 CH.sub.2 COOH.

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

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: ##STR12##

wherein X is CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH, and n is 0 to 5, which comprises mixing [i] a compound represented by the formula: ##STR13##

[ii] CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH 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 CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH:water is 1:0.1-10.

12. A crystal obtained by mixing [i] a compound represented by the formula: ##STR14##

[iii] CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH and [iii] water, dissolving them and allowing crystallization to take place.

13. A disodium salt of a compound represented by the formula: ##STR15##

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.degree. in powder X-ray diffraction (CuK.alpha.).

16. The compound of claim 2, wherein X is CH.sub.3 COOH.

17. The compound of claim 2, wherein X is CH.sub.3 CH.sub.2 COOH.

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.degree. in powder X-ray diffraction (CuK.alpha.).

20. A method for making a crystal of a compound of formula (I): ##STR16##

wherein X is CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH, and n is 0 to 5, comprising crystallizing a compound of formula (Ia): ##STR17##

from CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH and water.

21. A crystal obtained by crystallizing a compound of formula (Ia): ##STR18##

from CH.sub.3 COOH or CH.sub.3 CH.sub.2 COOH and water.
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