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Claims for Patent: 9,115,091

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Claims for Patent: 9,115,091

Title:Crystals and process of making 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- -1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid
Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- 1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- 1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
Inventor(s): Anzalone; Luigi (West Chester, PA), Villani; Frank J. (Perkasie, PA), Teleha; Christopher A. (Fort Washington, PA), Feibush; Penina (Ambler, PA), Fegely; Barry (Quakertown, PA)
Assignee: FURIEX PHARMACEUTICALS, INC. (Parsippany, NJ)
Application Number:14/459,514
Patent Claims: 1. A pharmaceutical composition comprising a Form .alpha. crystal of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- 1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

2. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 14.0, 14.3, and 14.7 degrees 2-theta.

3. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2, 11.3, 14.0, 14.3, and 14.7 degrees 2-theta.

4. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2, 11.3, 11.8, 14.0, 14.3, 14.7, 16.1, and 18.3 degrees 2-theta.

5. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 1.

6. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially similar to the powder X ray diffraction peaks of FIG. 1.

7. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a thermal gravimetric analysis (TGA) substantially similar to the TGA in FIG. 2.

8. The pharmaceutical composition of claim 1, wherein said Form .alpha. crystal is characterized by a differential scanning calorimetry (DSC) measurement substantially similar to the DSC in FIG. 3.

9. The pharmaceutical composition of claim 1, in a dosage form suitable for oral administration.

10. The pharmaceutical composition of claim 9, wherein the dosage form is a solid.

11. The pharmaceutical composition of claim 9, wherein the dosage form is selected from the group consisting of a tablet, a caplet, a hard gelatin capsule, a starch capsule, a hydroxypropyl methylcellulose (HPMC) capsule, and a soft elastic gelatin capsule.

12. The pharmaceutical composition of claim 9, wherein the dosage form as administered is a liquid.

13. The pharmaceutical composition of claim 9, wherein the dosage form as administered is selected from the group consisting of a suspension, a solution, a syrup, and an emulsion.

14. The pharmaceutical composition of claim 9, wherein the dosage form is a tablet.

15. A method of treating a disease in a mammal, wherein the disease is an opioid receptor disorder, comprising administering to said mammal an effective amount of a pharmaceutical composition comprising a Form .alpha. crystal of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- 1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

16. The method of claim 15, wherein the opioid receptor disorder is selected from the group consisting of irritable bowel syndrome, pain and a combination of both.

17. The method of claim 15, wherein the opioid receptor disorder is irritable bowel syndrome.

18. The method of claim 15, wherein the opioid receptor disorder is pain.

19. The method of claim 15, wherein the pharmaceutical composition is administered in a dosage form suitable for oral administration.

20. The method of claim 19, wherein the pharmaceutical composition is administered in a solid dosage form.

21. The method of claim 19, wherein the dosage form is selected from the group consisting of a tablet, a caplet, a hard gelatin capsule, a starch capsule, a hydroxypropyl methylcellulose (HPMC) capsule, and a soft elastic gelatin capsule.

22. The method of claim 19, wherein the dosage form is a tablet.

23. The method of claim 15, wherein the mammal is a human.

24. A pharmaceutical composition comprising a Form .beta. crystal of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- 1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

25. A method of treating a disease in a mammal, wherein the disease is an opioid receptor disorder, comprising administering to said mammal an effective amount of a pharmaceutical composition comprising a Form .beta. crystal of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-- 1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

26. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 11.0, 12.4, and 15.2 degrees 2-theta.

27. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 11.0, 12.4, 14.9, 15.2, and 22.1 degrees 2-theta.

28. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 11.0, 12.4, 14.9, 15.2, 22.1, 25.6, 27.4, and 30.4 degrees 2-theta.

29. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 2.

30. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially similar to the powder X ray diffraction peaks of FIG. 1.

31. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a thermal gravimetric analysis (TGA) substantially similar to the TGA in FIG. 4.

32. The pharmaceutical composition of claim 24, wherein said Form .beta. crystal is characterized by a differential scanning calorimetry (DSC) measurement substantially similar to the DSC in FIG. 5.

33. The pharmaceutical composition of claim 24, in a dosage form suitable for oral administration.

34. The pharmaceutical composition of claim 33, wherein the dosage form is a solid.

35. The pharmaceutical composition of claim 33, wherein the dosage form is selected from the group consisting of a tablet, a caplet, a hard gelatin capsule, a starch capsule, a hydroxypropyl methylcellulose (HPMC) capsule, and a soft elastic gelatin capsule.

36. The pharmaceutical composition of claim 33, wherein the dosage form as administered is a liquid.

37. The pharmaceutical composition of claim 33, wherein the dosage form as administered is selected from the group consisting of a suspension, a solution, a syrup, and an emulsion.

38. The pharmaceutical composition of claim 33, wherein the dosage form is a tablet.

39. The method of claim 25, wherein the opioid receptor disorder is selected from the group consisting of irritable bowel syndrome, pain and a combination of both.

40. The method of claim 25, wherein the opioid receptor disorder is irritable bowel syndrome.

41. The method of claim 25, wherein the opioid receptor disorder is pain.

42. The method of claim 25, wherein the pharmaceutical composition is administered in a dosage form suitable for oral administration.

43. The method of claim 42, wherein the pharmaceutical composition is administered in a solid dosage form.

44. The method of claim 42, wherein the dosage form is selected from the group consisting of a tablet, a caplet, a hard gelatin capsule, a starch capsule, a hydroxypropyl methylcellulose (HPMC) capsule, and a soft elastic gelatin capsule.

45. The method of claim 42, wherein the dosage form is a tablet.

46. The method of claim 25, wherein the mammal is a human.
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