Claims for Patent: 12,226,419

Summary for Patent: 12,226,419

Title:	Topical formulation for a JAK inhibitor
Abstract:	This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
Inventor(s):	Bhavnish Parikh, Bhavesh Shah, Krishnaswamy Yeleswaram
Assignee:	Incyte Corp , Incyte Holdings Corp
Application Number:	US18/588,626
Patent Claims:	1. A pharmaceutical formulation for topical skin application, wherein the formulation is an oil-in-water emulsion, the formulation comprising: from 35% to 65% by weight of the formulation of water; from 10% to 40% by weight of the formulation of a mixture of petrolatum, C16-18 fatty alcohols, mineral oil, a triglyceride, and a silicone oil; from 2% to 6% by weight of the formulation of a mixture of a glyceryl fatty ester and a sorbitan fatty ester; from 0.05% to 5% by weight of the formulation of a polysaccharide; from 10% to 35% by weight of the formulation of a mixture of an alkylene glycol and a polyalkylene glycol; and 1.5% of (R)-3-cyclopentyl-3-[4-(7H-pyrrolo [2,3-d] pyrimidin-4-yl)-1H- pyrazol-1-yl]propanenitrile phosphoric acid salt by weight of the formulation on a free base basis. 2. The formulation according to claim 1, wherein: the petroleum is white petrolatum; the C16-18 fatty alcohols are a mixture of cetyl alcohol and stearyl alcohol; the mineral oil is light mineral oil; the glyceride is medium chain triglycerides; the silicone oil is dimethicone; the glyceryl fatty ester is glyceryl stearate; the sorbitan fatty ester is polysorbate 20; the polysaccharide is xanthan gum; the alkylene glycol is propylene glycol; and the polyalkylene glycol is polyethylene glycol. 3. The formulation according to claim 1, wherein: the petroleum is white petrolatum; the C16-18 fatty alcohols are a mixture of cetyl alcohol and stearyl alcohol; the mineral oil is light mineral oil; the glyceride is medium chain triglycerides; the silicone oil is dimethicone; the glyceryl fatty ester is glyceryl stearate SE; the sorbitan fatty ester is polysorbate 20; the polysaccharide is xanthan gum; the alkylene glycol is propylene glycol; and the polyalkylene glycol is polyethylene glycol 200. 4. The formulation according to claim 2, further comprising: a chelating agent component; and from 0.05% to 3% by weight of the formulation of an antimicrobial preservative component. 5. The formulation of claim 3, further comprising: 0.1% by weight of the formulation of methyl paraben; 0.05% by weight of the formulation of propyl paraben; 0.05% by weight of the formulation of edetate disodium; and 0.5% by weight of the formulation of phenoxyethanol. 6. The formulation according to claim 1, wherein: the water comprises from 40% to 60% by weight of the formulation; the mixture of petrolatum, C16-18 fatty alcohols, mineral oil, a glyceride, and a silicone oil comprises from 17% to 27% by weight of the formulation; the mixture of a glyceryl fatty ester and a sorbitan fatty ester comprises from 3% to 5% by weight of the formulation; the polysaccharide comprises from 0.1% to 2% by weight of the formulation; and the mixture of an alkylene glycol and a polyalkylene glycol comprises from 15% to 30% by weight of the formulation. 7. The formulation according to claim 6, wherein: the petroleum is white petrolatum; the C16-18 fatty alcohols are a mixture of cetyl alcohol and stearyl alcohol; the mineral oil is light mineral oil; the glyceride is medium chain triglycerides; the silicone oil is dimethicone; the glyceryl fatty ester is glyceryl stearate; the sorbitan fatty ester is polysorbate 20; the polysaccharide is xanthan gum; the alkylene glycol is propylene glycol; and the polyalkylene glycol is polyethylene glycol. 8. The formulation according to claim 6, wherein: the petroleum is white petrolatum; the C16-18 patty alcohols are a mixture of cetyl alcohol and stearyl alcohol; the mineral oil is light mineral oil; the glyceride is medium chain triglycerides; the silicone oil is dimethicone; the glyceryl fatty ester is glyceryl stearate SE; the sorbitan fatty ester is polysorbate 20; the polysaccharide is xanthan gum; the alkylene glycol is propylene glycol; and the polyalkylene glycol is polyethylene glycol 200. 9. The formulation according to claim 7, further comprising: a chelating agent component; and from 0.05% to 3% by weight of the formulation of an antimicrobial preservative component. 10. The formulation of claim 8, further comprising: 0.1% by weight of the formulation of methyl paraben; 0.05% by weight of the formulation of propyl paraben; 0.05% by weight of the formulation of edetate disodium; and 0.5% by weight of the formulation of phenoxyethanol. 11. The formulation according to claim 1, wherein: the water comprises from 45% to 55% by weight of the formulation; the mixture of petrolatum, C16-18 fatty alcohols, mineral oil, a glyceride, and a silicone oil comprises from 20% to 27% by weight of the formulation; the mixture of a glyceryl fatty ester and a sorbitan fatty ester comprises from 3% to 5% by weight of the formulation; the polysaccharide comprises from 0.3 to 0.5% by weight of the formulation; and the mixture of an alkylene glycol and a polyalkylene glycol comprises from 20% to 25% by weight of the formulation. 12. The formulation according to claim 11, wherein: the petroleum is white petrolatum; the C16-18 fatty alcohols are a mixture of cetyl alcohol and stearyl alcohol; the mineral oil is light mineral oil; the glyceride is medium chain triglycerides; the silicone oil is dimethicone; the glyceryl fatty ester is glyceryl stearate; the sorbitan fatty ester is polysorbate 20; the polysaccharide is xanthan gum; the alkylene glycol is propylene glycol; and the polyalkylene glycol is polyethylene glycol. 13. The formulation according to claim 11, wherein: the petroleum is white petrolatum; the C16-18 fatty alcohols are a mixture of cetyl alcohol and stearyl alcohol; the mineral oil is light mineral oil; the glyceride is medium chain triglycerides; the silicone oil is dimethicone; the glyceryl fatty ester is glyceryl stearate SE; the sorbitan fatty ester is polysorbate 20; the polysaccharide is xanthan gum; the alkylene glycol is propylene glycol; and the polyalkylene glycol is polyethylene glycol 200. 14. The formulation according to claim 12, further comprising: a chelating agent component; and from 0.05% to 3% by weight of the formulation of an antimicrobial preservative component. 15. The formulation of claim 13, further comprising: 0.1% by weight of the formulation of methyl paraben; 0.05% by weight of the formulation of propyl paraben; 0.05% by weight of the formulation of edetate disodium; and 0.5% by weight of the formulation of phenoxyethanol. 16. A pharmaceutical formulation for topical skin application, wherein the formulation is an oil-in-water emulsion, the formulation comprising: 45% to 55% by weight of the formulation of water; 7% by weight of the formulation of a petrolatum; 4.75% by weight of the formulation of C16-18 fatty alcohols; 4% by weight of the formulation of a mineral oil; 5% by weight of the formulation of a glyceride; 1% by weight of the formulation of a silicone oil; 3% by weight of the formulation of a glyceryl fatty ester; 1.25% by weight of the formulation of a sorbitan fatty ester; 0.4% by weight of the formulation of a polysaccharide; 15% by weight of the formulation of an alkylene glycol; 7% by weight of the formulation of a polyalkylene glycol; and 1.5% of (R)-3-cyclopentyl-3-[4-(7H-pyrrolo [2,3-d] pyrimidin-4-yl)-1H- pyrazol-1-yl]propanenitrile phosphoric acid salt by weight of the formulation on a free base basis. 17. The formulation of claim 16, further comprising: 0.1% by weight of the formulation of methyl paraben; 0.05% by weight of the formulation of propyl paraben; 0.05% by weight of the formulation of edetate disodium; and 0.5% by weight of the formulation of phenoxyethanol. 18. A pharmaceutical formulation for topical skin application, wherein the formulation is an oil-in-water emulsion, the formulation comprising: 45% to 55% by weight of the formulation of water; 7% by weight of the formulation of white petrolatum; 3% by weight of the formulation of cetyl alcohol; 1.75% by weight of the formulation of stearyl alcohol; 4% by weight of the formulation of light mineral oil; 5% by weight of the formulation of medium chain triglycerides; 1% by weight of the formulation of dimethicone; 3% by weight of the formulation of glyceryl stearate; 1.25% by weight of the formulation of polysorbate 20; 0.4% by weight of the formulation of xanthan gum; 15% by weight of the formulation of propylene glycol; 7% by weight of the formulation of polyethylene glycol; and 1.5% of (R)-3-cyclopentyl-3-[4-(7H-pyrrolo [2,3-d] pyrimidin-4-yl)-1H- pyrazol-1-yl]propanenitrile phosphoric acid salt by weight of the formulation on a free base basis. 19. The formulation of claim 18, further comprising: 0.1% by weight of the formulation of methyl paraben; 0.05% by weight of the formulation of propyl paraben; 0.05% by weight of the formulation of edetate disodium; and 0.5% by weight of the formulation of phenoxyethanol. 20. The formulation of claim 2, wherein the oil-in-water emulsion has a pH of not greater than 3.6.