IP Library Granted Patent US 8,691,860
Granted Patent B2
US 8,691,860 · App. 13/987,009 · Granted Apr 8, 2014

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

Inventors: Luigi Anzalone (West Chester, PA); Frank J. Villani (Perkasie, PA); Christopher A. Teleha (Fort Washington, PA); Penina Feibush (Ambler, PA); Barry Fegely (Quakertown, PA)
Assignee: Furiex Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,691,860
App. No.
13/987,009
Granted
Apr 8, 2014
Kind
B2
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.

Claims (9)

1. Form α 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 α 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 α 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 α 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 α 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 α 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 α 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 α 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 α 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.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2016
From: FOREST TOSARA LIMITED (F/K/A FOREST TOSARA UNLIMITED COMPANY)
To: ALLERGAN HOLDINGS UNLIMITED COMPANY
Reel/Frame 039897/0440 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 8, 2016
From: FOREST TOSARA UNLIMITED COMPANY
To: ALLERGAN HOLDINGS UNLIMITED COMPANY
Reel/Frame 039370/0273 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2015
From: FURIEX PHARMACEUTICALS, LLC.
To: FURIEX HOLDINGS UNLIMITED COMPANY
Reel/Frame 036603/0168 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2015
From: FURIEX HOLDINGS UNLIMITED COMPANY
To: FOREST TOSARA LIMITED
Reel/Frame 036603/0236 →
CHANGE OF NAME Recorded Sep 18, 2015
From: FURIEX PHARMACEUTICALS, INC.
To: FURIEX PHARMACEUTICALS, LLC.
Reel/Frame 036640/0469 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 17, 2013
From: JANSSEN PHARMACEUTICA N.V.
To: FURIEX PHARMACEUTICALS, INC.
Reel/Frame 031423/0579 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 17, 2013
From: ANZALONE, LUIGI; VILLANI, FRANK J.; TELEHA, CHRISTOPHER A.; FEIBUSH, PENINA; FEGELY, BARRY
To: JANSSEN PHARMACEUTICA N.V.
Reel/Frame 031423/0567 →
Continuity (4)
Continuation 13175342 · Jul 1, 2011
Division 12168331 · Jul 7, 2008
Provisional Application 60948584 · Jul 9, 2007
Related Publication 20140011851A1 · Jan 9, 2014