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Last Updated: March 28, 2024

Claims for Patent: 8,691,860


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Summary for Patent: 8,691,860
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. (Morrisville, NC)
Application Number:13/987,009
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,691,860
Patent Claims: 1. 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 .alpha. crystal of claim 1, wherein said 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 .alpha. crystal of claim 1, wherein said 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 .alpha. crystal of claim 1, wherein said 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 .alpha. crystal of claim 1, wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 1.

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

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

9. A method of treating a mammal suffering from irritable bowel syndrome, pain or another opioid receptor disorder comprising administering to said mammal an effective amount of 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.

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