Crystals of salts of phenylalanine derivatives
Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).
1. A crystal of a pharmaceutically acceptable acid-addition salt of the compound represented by the following formula (I):
2. The crystal as set forth in claim 1 , wherein it is a hydrochloride salt of the compound represented by the formula (I).
3. The crystal as set forth in claim 2 , wherein it is form Cl 1 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 20.8, 23.6, 25.3 and 26.9 in the powder X-ray diffraction pattern.
4. The crystal as set forth in claim 2 , wherein it is form Cl 2 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 5.24, 10.39, 21.04 and 21.41 in the powder X-ray diffraction pattern.
5. The crystal as set forth in claim 2 , wherein it is form Cl 3 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 4.21, 10.13, 10.30 and 16.17 in the powder X-ray diffraction pattern.
6. The crystal as set forth in claim 2 , wherein it is form Cl 4 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 4.07, 17.84, 23.83 and 24.87 in the powder X-ray diffraction pattern.
7. The crystal as set forth in claim 2 , wherein it is form Cl 5 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 4.09, 22.12, 23.17 and 27.76 in the powder X-ray diffraction pattern.
8. The crystal as set forth in claim 2 , wherein it is form Cl 6 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 22.32, 22.90, 26.43 and 26.77 in the powder X-ray diffraction pattern.
9. The crystal as set forth in claim 2 , wherein it is form Cl 7 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 16.65, 20.99, 22.61 and 24.70 in the powder X-ray diffraction pattern.
10. The crystal as set forth in claim 1 , wherein it is hydrobromide of the compound represented by the formula (I).
11. The crystal as set forth in claim 10 , wherein it is form Br1 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 14.3, 17.4, 20.5 and 24.9 in the powder X-ray diffraction pattern.
12. The crystal as set forth in claim 10 , wherein it is form Br2 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 18.9, 20.6, 23.3, 25.0 and 26.7 in the powder X-ray diffraction pattern.
13. The crystal as set forth in claim 10 , wherein it is form Br3 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 21.53, 22.12, 23.69 and 25.39 in the powder X-ray diffraction pattern.
14. The crystal as set forth in claim 10 , wherein it is form Br4 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 4.07, 17.78, 23.62 and 24.65 in the powder X-ray diffraction pattern.
15. The crystal as set forth in claim 10 , wherein it is form Br5 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 21.20, 21.98, 23.21 and 23.93 in the powder X-ray diffraction pattern.
16. The crystal as set forth in claim 10 , wherein it is form Br6 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 17.25, 23.38, 24.55 and 26.73 in the powder X-ray diffraction pattern.
17. The crystal as set forth in claim 1 , wherein it is sulfate of the compound represented by the formula (I).
18. The crystal as set forth in claim 17 , wherein it is form S1 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 18.2, 22.7, 24.8 and 25.5 in the powder X-ray diffraction pattern.
19. The crystal as set forth in claim 17 , wherein it is form S2 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 15.6, 16.2, 18.0 and 19.2 in the powder X-ray diffraction pattern.
20. The crystal as set forth in claim 17 , wherein it is form S3 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 13.0, 18.7, 22.1 and 22.5 in the powder X-ray diffraction pattern.
21. The crystal as set forth in claim 17 , wherein it is form S4 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 12.58, 21.08, 23.02 and 23.93 in the powder X-ray diffraction pattern.
22. The crystal as set forth in claim 17 , wherein it is form S5 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 4.04, 21.06, 21.46 and 25.75 in the powder X-ray diffraction pattern.
23. The crystal as set forth in claim 1 , wherein it is nitrate of the compound represented by the formula (I).
24. The crystal as set forth in claim 23 , wherein it is form N1 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 12.8, 22.5, 23.3 and 24.6 in the powder X-ray diffraction pattern.
25. The crystal as set forth in claim 23 , wherein it is form N2 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 18.9, 20.7, 23.5 and 26.5 in the powder X-ray diffraction pattern.
26. The crystal as set forth in claim 1 , wherein it is p-toluene-sulfonate of the compound represented by the formula (I).
27. The crystal as set forth in claim 26 , wherein it is form Ts1 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 12.9, 21.5 and 23.1 in the powder X-ray diffraction pattern.
28. The crystal as set forth in claim 1 , wherein it is methane-sulfonate of the compound represented by the formula (I).
29. The crystal as set forth in claim 28 , wherein it is form Ms1 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 10.1, 11.5, 21.2 and 21.9 in the powder X-ray diffraction pattern.
30. The crystal as set forth in claim 28 , wherein it is form Ms2 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 12.9, 15.9, 18.8 and 23.0 in the powder X-ray diffraction pattern.
31. The crystal as set forth in claim 28 , wherein it is form Ms3 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 11.2, 12.6, 22.9 and 25.5 in the powder X-ray diffraction pattern.
32. The crystal as set forth in claim 28 , wherein it is form Ms4 crystal characterized by the peaks appearing at angles (2θ) of diffraction of 17.99, 19.22, 19.75 and 25.64 in the powder X-ray diffraction pattern.
33. A pharmaceutical composition comprising a crystal as set forth in claim 1 .