Substituted N-aryl pyridinones
Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
1. An inhalable pharmaceutical composition comprising a pharmaceutically acceptable carrier together with a compound having the structural formula:
wherein each of said positions represented as D has deuterium enrichment of at least 10%.
2. The composition as recited in claim 1 , wherein each of said positions represented as D has deuterium enrichment of at least 50%.
3. The composition as recited in claim 1 , wherein each of said positions represented as D has deuterium enrichment of at least 90%.
4. The composition as recited in claim 1 , wherein each of said positions represented as D has deuterium enrichment of at least 98%.
5. The composition as recited in claim 1 , wherein said composition is formulated as an solution or suspension.
6. The composition as recited in claim 5 , wherein said suspension comprises particles having an average size of 50 micrometers or less.
7. The composition as recited in claim 5 , wherein said suspension comprises particles having an average size of 10 micrometers or less.
8. The composition as recited in claim 5 , wherein said solution or suspension comprises ethanol, water, or mixtures thereof.
9. The composition as recited in claim 5 , wherein said solution or suspension comprises an agent for dispersing, solubilizing, or extending release of the active ingredient.
10. The composition as recited in claim 5 , wherein said solution or suspension comprises a surfactant selected from the group consisting of sorbitan trioleate, oleic acid, and an oligolactic acid.
11. The composition as recited in claim 5 , wherein said solution or suspension is administered to a subject using a device selected from the group consisting of a pressurized container, a pump, a sprayer, an atomizer, and a nebulizer.
12. The composition as recited in claim 11 , wherein said nebulizer is used in combination with a propellant.
13. The composition as recited in claim 12 , wherein said propellant is 1,1,1,2-tetrafluoroethane.
14. The composition of claim 12 , wherein said propellant is 1,1,1,2,3,3,3-heptafluoropropane.
15. The composition as recited in claim 1 , wherein said composition is formulated as an aerosol.
16. The composition as recited in claim 15 , wherein said composition comprises particles having an average size of 50 micrometers or less.
17. The composition as recited in claim 16 , wherein said composition comprises particles having an average size of 10 micrometers or less.
18. The composition as recited in claim 11 , wherein said solution or suspension comprises ethanol, water, or mixtures thereof.
19. The composition as recited in claim 11 , wherein said solution or suspension comprises an agent for dispersing, solubilizing, or extending release of the active ingredient.
20. The composition as recited in claim 11 , wherein said solution or suspension comprises a surfactant selected from the group consisting of sorbitan trioleate, oleic acid, and an oligolactic acid.
21. The composition as recited in claim 15 , wherein said solution is administered to a subject using a device selected from the group consisting of a pressurized container, a pump, a sprayer, an atomizer, and a nebulizer.
22. The composition as recited in claim 21 , wherein said nebulizer is used in combination with a propellant.
23. The composition as recited in claim 22 , wherein said propellant is 1,1,1,2-tetrafluoroethane.
24. The composition of claim 22 , wherein said propellant is 1,1,1,2,3,3,3-heptafluoropropane.
25. The composition as recited in claim 1 , wherein said pharmaceutically acceptable carrier comprises a powder base selected from the group consisting of lactose, lactose monohydrate, and starch.
26. The composition as recited in claim 1 , wherein said pharmaceutically acceptable carrier comprises a performance modifier selected from the group consisting of l-leucine, mannitol, and magnesium stearate.
27. The composition as recited in claim 1 , wherein said pharmaceutically acceptable carrier is selected from the group consisting of lactose, lactose monohydrate, starch, l-leucine, mannitol, magnesium stearate, dextran, glucose, maltose, sorbitol, xylitol, fructose, sucrose, and trehalose.
28. The composition as recited in claim 1 , wherein said pharmaceutically acceptable carrier comprises a flavoring agent selected from the group consisting of menthol and levomenthol.
29. The composition as recited in claim 1 , wherein said pharmaceutically acceptable carrier comprises a sweetener selected from the group consisting of saccharin and saccharin sodium.