Claims
- 1. A Type IV crystal of (Z)-N-[2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl]phenyl]-L-serinamide hydrochloride, which has a X ray powder diffraction pattern which has peaks at least at 13.4°, 18.7°, 19.4°, and 22.5° (2θ).
- 2. The crystal of claim 1, which has a X ray powder diffraction pattern which has peaks at least at 11.1°, 13.4°, 14.2°, 18.7°, 19.4°, 22.5° and 23.4° (2θ).
- 3. The crystal of claim 1, which has a water adsorption level less than 20 ml/g at a relative humidity of 80% on a prepared water adsorption isotherm.
- 4. The crystal of claim 1, which has been crystallized from a solvent, said solvent containing water in an amount of at most 2% by weight.
- 5. The crystal of claim 4, where said solvent is a mixture of methanol and isopropyl acetate and said solvent contains substantially no water.
- 6. A pharmaceutical composition, comprising a crystal according to claim 1 or being prepared by using said crystal.
- 7. The pharmaceutical composition of claim 6, further comprising a pharmaceutically acceptable carrier.
- 8. The pharmaceutical composition of claim 6, wherein said crystal has a water adsorption level less than 20 ml/g at a relative humidity of 80% on a prepared water adsorption isotherm.
- 9. The pharmaceutical composition of claim 6, wherein said crystal has been crystallized from a solvent, said solvent containing water in an amount of at most 2% by weight.
- 10. The pharmaceutical composition of claim 6, where said solvent is a mixture of methanol and isopropyl acetate and said solvent contains substantially no water.
- 11. A method for producing a crystal of claim 1, comprising crystallizing (Z)-N-[2-methoxy-5-[2-(3 ,4,5-trimethoxyphenyl)vinyl]phenyl]-L-serinamide hydrochloride from a solvent, wherein said solvent contains water in an amount of at most 2% by weight, based on the weight of said solvent.
- 12. The method of claim 11, where said solvent is a combination solvent of a good solvent for (Z)-N-[2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl]phenyl]-L-serinamide hydrochloride and a poor solvent for (Z)-N-[2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl]phenyl]-L-serinamide hydrochloride.
- 13. The method of claim 12, where said good solvent is at least one compound selected from the group consisting of alcohols, chloroform, acetone, and acetonitrile; and said poor solvent is at least one compound selected from the group consisting of acetate esters, ethers, saturated hydrocarbons, and cyclic saturated hydrocarbons.
- 14. The method of claim 11, where said crystallizing comprises re-precipitation.
- 15. A method for preparing a pharmaceutical composition, comprising mixing a crystal according to claim 1 with a pharmaceutically acceptable carrier.
- 16. The method of claim 15, wherein said crystal has a X ray powder diffraction pattern which has peaks at least at 11.1°, 13.4°, 14.2°, 18.7°, 19.4°, 22.5° and 23.4° (2θ).
- 17. The method of claim 15, wherein said crystal has a water adsorption level less than 20 ml/g at a relative humidity of 80% on a prepared water adsorption isotherm.
- 18. A method of treating cancer, comprising administering an effective amount of a pharmaceutical composition according to claim 6, to a subject in need thereof.
- 19. The method of claim 18, wherein said pharmaceutical composition further comprising a pharmaceutically acceptable carrier.
- 20. The method of claim 18, wherein in said pharmaceutical composition, said crystal has a water adsorption level less than 20 ml/g at a relative humidity of 80% on a prepared water adsorption isotherm.
Priority Claims (1)
Number |
Date |
Country |
Kind |
2000-076887 |
Mar 2000 |
JP |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation of International Application PCT/JP01/02028, filed on Mar. 14, 2001, and claims priority to Japanese Patent Application No. 2000-076887, filed on Mar. 17, 2000, both of which are incorporated herein by reference in their entireties.
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/JP01/02028 |
Mar 2001 |
US |
Child |
10243649 |
Sep 2002 |
US |