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Last Updated: September 21, 2021

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Claims for Patent: 9,700,542


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Summary for Patent: 9,700,542
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 NV (Beerse, BE)
Application Number:14/880,597
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,700,542
Patent Claims: 1. A pharmaceutical dosage formulation suitable for oral administration 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 and a pharmaceutically acceptable carrier.

2. The pharmaceutical dosage formulation of claim 1, wherein the formulation is present in a solid dosage form.

3. The pharmaceutical dosage formulation of claim 2, formulated as a tablet.

4. The pharmaceutical dosage formulation of claim 1, wherein 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 ##STR00047##

5. The pharmaceutical dosage formulation of claim 1, comprising 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-methoxy-benzoic acid.

6. The pharmaceutical dosage formulation of claim 1, comprising about 75 mg of 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-p- henyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

7. The pharmaceutical dosage formulation of claim 1, comprising about 100 mg of 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-p- henyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

8. The pharmaceutical dosage formulation 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.

9. The pharmaceutical dosage formulation of claim 8, further comprising a sweetener, a flavorant, a colorant, a coating, or a combination thereof.

10. The pharmaceutical dosage formulation of claim 8, 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.

11. The pharmaceutical dosage formulation of claim 8, 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.

12. The pharmaceutical dosage formulation of claim 8, 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.

13. The pharmaceutical dosage formulation of claim 8, 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.

14. The pharmaceutical dosage formulation of claim 8, wherein the glidant is selected from the group consisting of talc, cornstarch, and silica.

15. The pharmaceutical dosage formulation 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.

16. The pharmaceutical dosage formulation of claim 1, wherein the formulation 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.

17. A pharmaceutical dosage formulation for oral administration in solid form 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, mannitol, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, silica, magnesium stearate and a film coating.

18. The pharmaceutical dosage formulation of claim 17, 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 ##STR00048##

19. The pharmaceutical dosage formulation of claim 18, comprising 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.

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