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Claims for Patent: 9,205,076

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Claims for Patent: 9,205,076

Title:Compounds as opioid receptor modulators
Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). ##STR00001## The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
Inventor(s): Breslin; Henry J. (Lansdale, PA), Cai; Chaozhong (North Wales, PA), He; Wei (Audubon, PA), Kavash; Robert W. (Glenside, PA)
Assignee: Janssen Pharmaceutica, N.V. (Beerse, BE)
Application Number:14/282,828
Patent Claims: 1. A method for treating or ameliorating diarrhea or visceral pain comprising administering a pharmaceutical composition comprising 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 to a subject in need of such treatment.

2. The method of claim 1, wherein the method is for treating or ameliorating diarrhea.

3. The method of claim 1, wherein the method is for treating or ameliorating visceral pain.

4. The method of claim 1, wherein the subject has diarrhea predominant irritable bowel syndrome.

5. The method of claim 1, wherein the method is for treating or ameliorating diarrhea in a subject with diarrhea predominant irritable bowel syndrome.

6. The method of claim 1, wherein the method is for treating or ameliorating visceral pain in a subject with diarrhea predominant irritable bowel syndrome.

7. The method of claim 1, wherein the 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 is ##STR00044##

8. The method of claim 1, wherein the pharmaceutical composition is administered in a solid dosage form.

9. The method of claim 8, wherein the pharmaceutical composition is formulated as a tablet.

10. The method of claim 1, wherein the pharmaceutical composition comprises about 50 mg to about 200 mg of 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl) -propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methox- y-benzoic acid.

11. The method of claim 1, wherein the pharmaceutical composition comprises about 75 mg 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.

12. The method of claim 1, wherein the pharmaceutical composition comprises about 100 mg 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.

13. The method of claim 1, wherein the pharmaceutically acceptable carrier comprises a diluent, a binder, an adhesive, a disintegrant, a lubricant, an antiadherent, a gildant, or a combination thereof.

14. The method of claim 13, wherein the pharmaceutical composition further comprises a a sweetener, flavorant, a colorant, a coating, or a combination thereof.

15. The method of claim 13, wherein the diluent is selected from the group consisting of starch; lactose; sucrose; sucrose based diluents such as confectioner's sugar, sucrose plus 7 to 10 weight percent invert sugar, sucrose plus about 3 weight percent modified dextrins; sucrose plus invert sugar, about 4 weight percent invert sugar, 0.1 to 0.2 weight percent cornstarch and magnesium stearate; dextrose; inositol; mannitol; sorbitol; microcrystalline cellulose; dicalcium phosphate; calcium sulfate dihydrate; and calcium lactate trihydrate.

16. The method of claim 13, wherein the binder and adhesive are selected from the group consisting of acacia gum; guar gum; tragacanth gum; sucrose; gelatin; glucose; starch; cellulosics such as methylcellulose, sodium carboxymethylcellulose, ethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose; and water soluble or dispersible binders such as alginic acid and salts thereof, magnesium aluminum silicate, hydroxyethylcellulose, polyethylene glycol, polysaccharide acids, bentonites, polyvinylpyrrolidone, polymethacrylates, and pregelatinized starch.

17. The method of claim 13, wherein the disintegrant is selected from the group consisting of starches such as corn starch and potato starch; sodium starch glycolates; pregelatinized starches such as corn starch; clays such as magnesium aluminum silicate; celluloses such as crosslinked sodium carboxymethylcellulose and microcrystalline cellulose; alginates; gums such as agar, guar, locust bean, karaya, pectin, and tragacanth gum; and cross-linked polyvinylpyrrolidone.

18. The method of claim 13, wherein the lubricant and antiadherent is selected from the group consisting of stearates such as magnesium stearate, calcium stearate and sodium stearate; stearic acid; talc waxes; stearowet; boric acid; sodium chloride; DL-leucine; carbowax 4000; carbowax 6000; sodium oleate; sodium benzoate; sodium acetate; sodium lauryl sulfate; and magnesium lauryl sulfate.

19. The method of claim 13, wherein the glidant is selected from the group consisting of talc, cornstarch, and silica.

20. The method of claim 1, wherein the pharmaceutically acceptable carrier is selected from mannitol, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, silica, magnesium stearate, a film coating, and a combination thereof.

21. The method of claim 1, wherein the pharmaceutical composition comprises 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, mannitol, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, silica, magnesium stearate and a film coating.

22. The method of claim 1, wherein the pharmaceutical composition is administered at a frequency of one to four administrations per day.

23. The method of claim 1, wherein the pharmaceutical composition is administered once daily.

24. The method of claim 1, wherein the pharmaceutical composition is administered twice daily.
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