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Generated: February 23, 2018

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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: Janssen Pharmaceutica, N.V. (BE)
Filing Date:Jul 07, 2008
Application Number:12/168,331
Claims:1. A Form .beta. crystal of 5({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1- h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, wherein said crystal is characterized by a powder X-ray diffraction patterns having powder X-ray diffraction peaks at about 11.0, 12.4, and 15.2 degrees 2-theta.

2. The .beta. crystal of claim 1, wherein said 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.

3. The .beta. crystal of claim 1, wherein said 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.

4. 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 said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 2.

5. 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 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.
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