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Claims for Patent: 5,969,156

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Claims for Patent: 5,969,156

Title: Crystalline [R- (R*,R*)]-2-(4-Dfluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)- 3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt (atorvastatin)
Abstract:Crystalline forms of atorvastatin and hydrates thereof are useful hypolipidemic and hypocholesterolemic agents.
Inventor(s): Briggs; Christopher A. (Holland, MI), Jennings; Rex A. (Holland, MI), Wade; Robert (Holland, MI), Harasawa; Kikuko (Sagamihara, JP), Ichikawa; Shigeru (Machida, JP), Minohara; Kazuo (Sagamihara, JP), Nakagawa; Shinsuke (Sagamihara, JP)
Assignee: Warner-Lambert Company (Morris Plains, NJ)
Application Number:08/945,812
Patent Claims: 1. A crystalline Form I atorvastatin hydrate having an X-ray powder diffraction containing at least one of the following 2.theta. values measured using CuK.sub..alpha. radiation: 11.9 or 22.0.

2. A crystalline Form I atorvastatin hydrate having an X-ray powder diffraction containing the following 2.theta. values measured using Cuk.sub..alpha. radiation: 11.9, 21.6 and 22.0.

3. A crystalline Form I atorvastatin hydrate having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 17.1, 19.5 and 21.6.

4. A crystalline Form I atorvastatin hydrate having an X-ray powder diffraction containing the following 2.theta. values measured using Cuk.sub..alpha. radiation: 9.2, 9.5, 10.3, 10.6, 11.9, 12.2, 17.1, 19.5, 21.6, 22.0, 22.7, 23.3, 23.7, 24.4, 28.9 and 29.2.

5. A crystalline Form I atorvastatin hydrate having an X-ray powder diffraction containing the following 2.theta. values measured using Cuk.sub..alpha. radiation: 9.150, 9.470, 10.266, 10.560, 11.853, 12.195, 17.075, 19.485, 21.626, 21.960, 22.748, 23.335, 23.734, 24.438, 28.915 and 29.234.

6. A crystalline Form I atorvastatin hydrate characterized by solid state .sup.13 C nuclear magnetic resonance having a chemical shift difference between the lowest ppm resonance and another resonance of 5.1 or 51.8.

7. A crystalline Form I atorvastatin hydrate characterized by solid state .sup.13 C nuclear magnetic resonance and having the following chemical shift differences between the lowest ppm resonance and other resonances: 3.9, 5.1, 43.6, 46.8, 49.2 and 51.8.

8. A crystalline Form I atorvastatin hydrate characterized by solid-state .sup.13 C nuclear magnetic resonance having the following chemical shift differences between the lowest ppm resonance and other resonances: 3.9, 5.1, 18.9, 20.6, 26.1, 43.6, 46.8, 49.2, 51.8, 92.5, 96.9, 99.6, 102.2, 106.3, 108.2, 109.8, 113.6, 115.7, 138.0, 145.4, 157.1 and 161.5.

9. A crystalline Form I atorvastatin hydrate characterized by solid-state .sup.13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 21.3. 25.2, 26.4, 40.2, 41.9, 47.4, 64.9, 68.1, 70.5, 73.1, 113.8, 118.2, 120.9, 123.5, 127.6, 129.5, 131.1, 134.9, 137.0, 159.3, 166.7 (broad), 178.4 and 182.8.

10. The crystalline Form I atorvastatin hydrate of claim 1 containing about 1 to 8 moles of water.

11. The crystalline Form I atorvastatin hydrate of claim 1 containing 3 moles of water.

12. The crystalline Form I atorvastatin hydrate of claim 2 containing about 1 to 8 moles of water.

13. The crystalline Form I atorvastatin hydrate of claim 2 containing 3 moles of water.

14. The crystalline Form I atorvastatin hydrate of claim 3 containing about 1 to 8 moles of water.

15. The crystalline Form I atorvastatin hydrate of claim 3 containing 3 moles of water.

16. The crystalline Form I atorvastatin hydrate of claim 4 containing about 1 to 8 moles of water.

17. The crystalline Form I atorvastatin hydrate of claim 4 containing 3 moles of water.

18. The crystalline Form I atorvastatin hydrate of claim 5 containing about 1 to 8 moles of water.

19. The crystalline Form I atorvastatin hydrate of claim 5 containing 3 moles of water.

20. The crystalline Form I atorvastatin hydrate of claim 6 containing about 1 to 8 moles of water.

21. The crystalline Form I atorvastatin hydrate of claim 6 containing 3 moles of water.

22. The crystalline Form I atorvastatin hydrate of claim 7 containing about 1 to 8 moles of water.

23. The crystalline Form I atorvastatin hydrate of claim 7 containing 3 moles of water.

24. The crystalline Form I atorvastatin hydrate of claim 8 containing about 1 to 8 moles of water.

25. The crystalline Form I atorvastatin hydrate of claim 8 containing 3 moles of water.

26. The crystalline Form I atorvastatin hydrate of claim 9 containing about 1 to 8 moles of water.

27. The crystalline Form I atorvastatin hydrate of claim 9 containing 3 moles of water.

28. Crystalline Form II atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 9.0 and 20.5.

29. Crystalline Form II atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 8.5 and 9.0.

30. Crystalline Form II atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 5.6, 7.4, 8.5, 9.0, 12.4 (broad), 15.8 (broad), 17.1-17.4 (broad), 19.5, 20.5, 22.7-23.2 (broad), 25.7 (broad) and 29.5.

31. Crystalline Form II atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using Cuk.sub..alpha. radiation: 5.582, 7.384, 8.533, 9.040, 12.440 (broad), 15.771 (broad), 17.120-17.360 (broad), 19.490, 20.502, 22.706-23.159 (broad), 25.697 (broad) and 29.504.

32. Crystalline Form II atorvastatin or a hydrate thereof characterized by solid state .sup.13 C nuclear magnetic resonance having a chemical shift difference between the lowest ppm resonance and another resonance of 4.7 or 47.8.

33. Crystalline Form II atorvastatin or a hydrate thereof characterized by solid state .sup.13 C nuclear magnetic resonance having the following chemical shift differences between the lowest ppm resonance and other resonances: 4.7, 44.5, 45.2, 46.2 and 47.8.

34. Crystalline Form II atorvastatin or a hydrate thereof characterized by solid-state .sup.13 C nuclear magnetic resonance having the following chemical shift differences between the lowest ppm resonance and other resonances: 4.7, 17.4, 18.9, 19.5, 20.6, 44.5, 45.2, 46.2, 47.8, 91.9, 92.9, 94.3, 96.2, 97.5, 98.6, 100.1, 106.2, 110.5, 112.0, 117.7, 138.2, 140.2 and 158.2.

35. Crystalline Form II atorvastatin or a hydrate thereof characterized by solid-state .sup.13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 22.8 (broad), 27.5, 40.2, 41.7, 42.3, 43.4, 67.3, 68.0, 69.0, 70.6, 114.7, 115.7, 117.1, 119.0, 120.3, 121.4, 122.9, 129.0, 133.3, 134.8, 140.5, 161 (broad), 163 (broad) and 181 (broad).

36. Crystalline Form IV atorvastatin or a hydrate thereof having an X-ray powder diffraction containing at least one of the following 2.theta. values measured using CuK.sub..alpha. radiation: 8.0 or 9.7.

37. Crystalline Form IV atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 4.9, 8.0 and 9.7.

38. Crystalline Form IV atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 8.0, 9.7 and 19.6.

39. Crystalline Form IV atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 4.9, 5.4, 5.9, 8.0, 9.7, 10.4, 12.4, 17.7, 18.4, 19.2, 19.6, 21.7, 23.0, 23.7 and 24.1.

40. Crystalline Form IV atorvastatin or a hydrate thereof having an X-ray powder diffraction containing the following 2.theta. values measured using CuK.sub..alpha. radiation: 4.889, 5.424, 5.940, 7.997, 9.680, 10.416, 12.355, 17.662, 18.367, 19.200, 19.569, 21.723, 23.021, 23.651 and 24.143.

41. Crystalline Form IV atorvastatin or a hydrate thereof characterized by solid state .sup.13 C nuclear magnetic resonance having a chemical shift difference between the lowest ppm resonance and another resonance of 8.0 or 53.6.

42. Crystalline Form IV atorvastatin or a hydrate thereof characterized by solid state .sup.13 C nuclear magnetic resonance having the following chemical shift differences between the lowest ppm resonance and other resonances: 1.5, 2.4, 8.0, 45.6, 48.4, 50.0 and 53.6.

43. Crystalline Form IV atorvastatin or a hydrate thereof characterized by solid-state .sup.13 C nuclear magnetic resonance having the following chemical shift differences between the lowest ppm resonance and other resonances: 1.5, 2.4, 8.0, 22.1, 24.2, 25.5, 28.2, 45.6, 48.4, 50.0, 53.6, 97.8, 101.9, 104.8, 109.2, 111.3, 116.8, 120.2, 141.1, 148.2, 161.4, 163.5, 167.0 and 168.5.

44. Crystalline Form IV atorvastatin or a hydrate thereof characterized by solid-state .sup.13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 17.9, 19.4, 20.3, 25.9, 40.0, 42.1, 43.4, 46.1, 63.5, 66.3, 67.9, 71.5, 115.7, 119.8, 122.7, 127.1,129.2, 134.7, 138.1 (broad), 159.0 (broad), 166.1 (broad), 179.3, 181.4, 184.9 and 186.4.
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