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Last Updated: September 21, 2021

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Claims for Patent: 9,789,125


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Summary for Patent: 9,789,125
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: Allergan Holdings Unlimited Company (IE)
Application Number:15/171,967
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,789,125
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, wherein the Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having any three or more powder X-ray diffraction peaks selected from the group consisting of powder X-ray diffraction peaks at about 10.2.+-.0.3, 11.3.+-.0.3, 11.8.+-.0.3, 14.0.+-.0.3, 14.3.+-.0.3, 14.7.+-.0.3, 16.1.+-.0.3, and 18.3.+-.0.3 degrees 2-theta.

2. The pharmaceutical composition of claim 1, wherein the Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having any three or more powder X-ray diffraction peaks selected from the group consisting of powder X-ray diffraction peaks at about 10.2.+-.0.25, 11.3.+-.0.25, 11.8.+-.0.25, 14.0.+-.0.25, 14.3.+-.0.25, 14.7.+-.0.25, 16.1.+-.0.25, and 18.3.+-.0.25 degrees 2-theta.

3. The pharmaceutical composition of claim 1, wherein the Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having any three or more powder X-ray diffraction peaks selected from the group consisting of powder X-ray diffraction peaks at about 10.2.+-.0.2, 11.3.+-.0.2, 11.8.+-.0.2, 14.0.+-.0.2, 14.3.+-.0.2, 14.7.+-.0.2, 16.1.+-.0.2, and 18.3.+-.0.2 degrees 2-theta.

4. The pharmaceutical composition of claim 1, wherein the Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 14.0.+-.0.2, 14.3.+-.0.2, 14.7.+-.0.2 degrees 2-theta.

5. The pharmaceutical composition of claim 1, wherein the Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2.+-.0.2, 11.3.+-.0.2, 14.0.+-.0.2, 14.3.+-.0.2, and 14.7.+-.0.2 degrees 2-theta.

6. The pharmaceutical composition of claim 1, wherein the Form .alpha. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2.+-.0.2, 11.3.+-.0.2, 11.8.+-.0.2, 14.0.+-.0.2, 14.3.+-.0.2, 14.7.+-.0.2, 16.1.+-.0.2, and 18.3.+-.0.2 degrees 2-theta.

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

8. The pharmaceutical composition of claim 1, wherein the 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.

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

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

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

12. The pharmaceutical composition of claim 11, wherein the dosage form is a solid.

13. The pharmaceutical composition of claim 11, 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.

14. The pharmaceutical composition of claim 11, wherein the dosage form as administered is a liquid.

15. The pharmaceutical composition of claim 11, wherein the dosage form as administered is selected from the group consisting of a suspension, a solution, a syrup, and an emulsion.

16. The pharmaceutical composition of claim 11, wherein the dosage form is a tablet.

17. A method of treating an opioid receptor disorder in a mammal comprising administering to the mammal an effective amount of the pharmaceutical composition of claim 1.

18. The method of claim 17, wherein the opioid receptor disorder is selected from the group consisting of irritable bowel syndrome, pain and a combination of both.

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

20. The method of claim 17, wherein the opioid receptor disorder is pain.

21. 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, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having any three or more powder X-ray diffraction peaks selected from the group consisting of powder X-ray diffraction peaks at about 11.0.+-.0.3, 12.4.+-.0.3, 14.9.+-.0.3, 15.2.+-.0.3, 22.1.+-.0.3, 25.6.+-.0.3, 27.4.+-.0.3, and 30.4.+-.0.3 degrees 2-theta.

22. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having any three or more powder X-ray diffraction peaks selected from the group consisting of powder X-ray diffraction peaks at about 11.0.+-.0.25, 12.4.+-.0.25, 14.9.+-.0.25, 15.2.+-.0.25, 22.1.+-.0.25, 25.6.+-.0.25, 27.4.+-.0.25, and 30.4.+-.0.25 degrees 2-theta.

23. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having any three or more powder X-ray diffraction peaks selected from the group consisting of powder X-ray diffraction peaks at about 11.0.+-.0.2, 12.4.+-.0.2, 14.9.+-.0.2, 15.2.+-.0.2, 22.1.+-.0.2, 25.6.+-.0.2, 27.4.+-.0.2, and 30.4.+-.0.2 degrees 2-theta.

24. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 11.0.+-.0.2, 12.4.+-.0.2, and 15.2.+-.0.2 degrees 2-theta.

25. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 11.0.+-.0.2, 12.4.+-.0.2, 14.9.+-.0.2, 15.2.+-.0.2, and 22.1.+-.0.2, degrees 2-theta.

26. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 11.0.+-.0.2, 12.4.+-.0.2, 14.9.+-.0.2, 15.2.+-.0.2, 22.1.+-.0.2, 25.6.+-.0.2, 27.4.+-.0.2, and 30.4.+-.0.2 degrees 2-theta.

27. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 2.

28. The pharmaceutical composition of claim 21, wherein the 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.

29. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a thermal gravimetric analysis (TGA) substantially similar to the TGA in FIG. 4.

30. The pharmaceutical composition of claim 21, wherein the Form .beta. crystal is characterized by a differential scanning calorimetry (DSC) measurement substantially similar to the DSC in FIG. 5.

31. The pharmaceutical composition of claim 21, in a dosage form suitable for oral administration.

32. The pharmaceutical composition of claim 31, wherein the dosage form is a solid.

33. The pharmaceutical composition of claim 31, 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.

34. The pharmaceutical composition of claim 31, wherein the dosage form as administered is a liquid.

35. The pharmaceutical composition of claim 31, wherein the dosage form as administered is selected from the group consisting of a suspension, a solution, a syrup, and an emulsion.

36. The pharmaceutical composition of claim 31, wherein the dosage form is a tablet.

37. A method of treating an opioid receptor disorder in a mammal comprising administering to the mammal an effective amount of the pharmaceutical composition of claim 21.

38. The method of claim 37, wherein the opioid receptor disorder is selected from the group consisting of irritable bowel syndrome, pain and a combination of both.

39. The method of claim 37, wherein the opioid receptor disorder is irritable bowel syndrome.

40. The method of claim 37, wherein the opioid receptor disorder is pain.

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