Claims
- 1. Polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl }phenyl)acetamide.
- 2. The polymorph Form III of claim 1 wherein the polymorph exhibits a predominant endotherm at about 191° C. as measured by as measured by a TA 2920 Modulated Differential Scanning Calorimeter (DSC) at a scan rate of 10° C. per minute.
- 3. The polymorph Form III of claim 1 wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ(+/−0.20°θ) at 18.9 and 28.1.
- 4. The polymorph Form III of claim 3 wherein the polymorph exhibits an additional characteristic peak expressed in degrees 2θ (+/−0.2°θ) at 10.2.
- 5. The polymorph Form III of claim 4 wherein the polymorph exhibits additional characteristic peaks expressed in degrees 2θ (+/−0.2°θ) at 13.3, 20.7, 22.2 and 30.8.
- 6. The polymorph Form III of claim 1 wherein the polymorph exhibits an X-ray powder diffraction pattern as shown in FIG. 2.
- 7. The polymorph Form III of claim 1 wherein the polymorph exhibits a single crystal x-ray crystallographic analysis at 150°K with crystal parameters as the following:
- 8. The polymorph Form III of claim 1 wherein the polymorph exhibits a Raman FT Infrared spectrum as shown in FIG. 3.
- 9. The polymorph Form III of claim 1 wherein the polymorph contains less than 2% by weight total impurities, less than 1% by weight water, and less than 0.5% by weight organic solvent.
- 10. The polymorph Form III of claim 1 wherein the polymorph contains less than 1% by weight total impurities, less than about 0.75% by weight water, and less than 0.4% by weight residual organic solvent.
- 11. A composition comprising polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide.
- 12. The composition of claim 11, further comprising N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide in a crystalline, solvate or amorphous form other than polymorph Form III.
- 13. The composition of claim 11 further comprising polymorph Form I.
- 14. The composition of claim 11 further comprising polymorph Form II.
- 15. A composition comprising polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide in combination with a pharmaceutically acceptable carrier.
- 16. The composition of claim 15 wherein the composition is formulated for oral administration.
- 17. The composition of claim 16 wherein the composition is in the form of a pill, capsule or tablet.
- 18. The composition of claim 15 wherein polymorph Form III is present in the pill, capsule or table in a unit dosage form in an amount from 0.1 to 250 mg.
- 19. A composition comprising (a) polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (“Compound 1”) and (b) a crystalline, solvate, amorphous or other form of Compound 1 other than polymorph Form III, wherein the total weight of Compound 1 in the composition is the sum of (a) plus (b).
- 20. The composition of claim 19 wherein the composition comprises less than 0.1% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 21. The composition of claim 19 wherein the composition comprises less than 0.5% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 22. The composition of claim 19 wherein the composition comprises less than 1% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 23. The composition of claim 19 wherein the composition comprises less than 2% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 24. The composition of claim 19 wherein the composition comprises less than 5% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 25. The composition of claim 19 wherein the composition comprises less than 10% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 26. The composition of claim 19 wherein the composition comprises less than 20% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 27. The composition of claim 19 wherein the composition comprises less than 30% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 28. The composition of claim 19 wherein the composition comprises less than 40% by weight of polymorph Form III based on the total weight of Compound 1 in the composition.
- 29. The composition of claim 19 wherein the composition comprises less than 50% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 30. The composition of claim 19 wherein the composition comprises at least 50% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 31. The composition of claim 19 wherein the composition comprises at least 60% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 32. The composition of claim 19 wherein the composition comprises at least 70% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 33. The composition of claim 19 wherein the composition comprises at least 80% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 34. The composition of claim 19 wherein the composition comprises at least 90% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 35. The composition of claim 19 wherein the composition comprises at least 95% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 36. The composition of claim 19 wherein the composition comprises at least 97% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 37. The composition of claim 19 wherein the composition comprises at least 98% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 38. The composition of claim 19 wherein the composition comprises at least 99% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 39. The composition of claim 19 wherein the composition comprises at least 99.5% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 40. The composition of claim 19 wherein the composition comprises at least 99.9% by weight of polymorph Form III based upon the total weight of Compound 1 in the composition.
- 41. The composition of claim 19 wherein the composition is in the form of a pill, capsule or tablet.
- 42. The composition of claim 19 wherein the composition is in the form of a slurry.
- 43. A method for treating insomnia in a patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 15.
- 44. A method for inducing sleep in a patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 15.
- 45. A method for inducing sedation or hypnosis in a patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 15.
- 46. A method for inducing skeletal muscle relaxation in a patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 15.
CROSS-REFERENCE TO RELATED APPLICATION
[0001] This application claims the benefit of U.S. Provisional Application No. 60/406,072 filed Aug. 26, 2002, which is hereby incorporated by reference in its entirety.
Provisional Applications (1)
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Number |
Date |
Country |
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60406072 |
Aug 2002 |
US |