Phosphonocephem compound
View Patent ↗A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH 3 COOH, CH 3 CH 2 COOH or CH 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.
1. A compound of the formula:
wherein X is CH 3 COOH or CH 3 CH 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 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° 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 CH 3 CH 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° 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 CH 3 COOH or CH 3 CH 2 COOH, and n is 0 to 5, which comprises mixing [i] a compound represented by the formula:
[ii] CH 3 COOH or CH 3 CH 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 3 COOH or CH 3 CH 2 COOH:water is 1:0.1-10.
12. A crystal obtained by mixing [i] a compound represented by the formula:
[iii] CH 3 COOH or CH 3 CH 2 COOH 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 CH 3 COOH.
17. The compound of claim 2 , wherein X is CH 3 CH 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° in powder X-ray diffraction (CuKα).
20. A method for making a crystal of a compound of formula (I):
wherein X is CH 3 COOH or CH 3 CH 2 COOH, and n is 0 to 5, comprising crystallizing a compound of formula (Ia):
from CH 3 COOH or CH 3 CH 2 COOH and water.
21. A crystal obtained by crystallizing a compound of formula (Ia):
from CH 3 COOH or CH 3 CH 2 COOH and water.