Claims for Patent: 10,758,543

Summary for Patent: 10,758,543

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):	Parikh; Bhavnish (Avondale, PA), Shah; Bhavesh (San Antonio, TX), Yeleswaram; Krishnaswamy (Landenberg, PA)
Assignee:	INCYTE CORPORATION (Wilmington, DE)
Application Number:	16/566,625
Patent Claims:	1. A pharmaceutical composition suitable for topical skin application, comprising: an oil-in-water emulsion, comprising: water, an oil component, an emulsifier component, a solvent component, and from about 0.5% to about 1.5% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt, wherein the oil-in-water emulsion in the composition is a solubilized cream for topical skin application and further wherein the oil-in-water emulsion has a pH of not greater than 3.6. 2. The composition of claim 1, wherein said solubilized cream is suitable for application to the skin for up to 84 consecutive days. 3. The composition of claim 1, further comprising a stabilizing agent component. 4. The composition of claim 1, wherein the water is present in an amount ranging from about 40% to about 60% by weight of the composition, and the oil component is present in an amount ranging from about 17% to about 27% by weight of the composition. 5. The composition of claim 4, further comprising a stabilizing agent component present in an amount of about 0.3% to about 0.5% by weight of the composition. 6. The composition of claim 1, wherein about 0.5% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt is present. 7. The composition of claim 1, wherein about 1.0% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt is present. 8. A pharmaceutical composition suitable for topical skin application, comprising: an oil-in-water emulsion, comprising: water, an oil component, an emulsifier component, a solvent component, and about 1.5% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt, wherein the oil-in-water emulsion in the composition is a solubilized cream for topical skin application and further wherein the oil-in-water emulsion has a pH of not greater than 3.6. 9. The composition of claim 1, wherein about 0.5% to about 1.0% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt is present. 10. The composition of claim 1, wherein said oil-in-water emulsion has a pH of not greater than 3.6 at 0 months at 25.degree. C. 11. The composition of claim 1, wherein said oil-in-water emulsion has a pH of not greater than 3.6 at 6 months at 25.degree. C. 12. The composition of claim 1, wherein said oil-in-water emulsion has a pH of not greater than 3.6 at 12 months at 25.degree. C. 13. The composition of claim 1, wherein said oil-in-water emulsion has a pH of not greater than 3.6 at 24 months at 25.degree. C. 14. A pharmaceutical composition suitable for topical skin application comprising: an oil-in-water emulsion, comprising: water, an oil component, an emulsifier component, a solvent component, and from about 0.5% to about 1.5% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]- propanenitrile phosphoric acid salt, wherein the oil-in-water emulsion in the composition is a solubilized cream for topical skin application and further wherein the oil-in-water emulsion has a pH of 2.9 to 3.6. 15. The composition of claim 14, wherein said solubilized cream is suitable for application to the skin for up to 84 consecutive days. 16. The composition of claim 14, wherein the water is present in an amount ranging from about 40% to about 60% by weight of the composition, and the oil component is present in an amount ranging from about 17% to about 27% by weight of the composition. 17. The composition of claim 14, wherein about 0.5% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt is present. 18. The composition of claim 14, wherein about 1.0% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt is present. 19. A pharmaceutical composition suitable for topical skin application comprising: an oil-in-water emulsion, comprising: water, an oil component, an emulsifier component, a solvent component, and about 1.5% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt, wherein the oil-in-water emulsion in the composition is a solubilized cream for topical skin application and further wherein the oil-in-water emulsion has a pH of 2.9 to 3.6. 20. The composition of claim 14, wherein about 0.5% to about 1.0% by weight of the emulsion on a free base basis of 1:1 (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl-- ]propanenitrile phosphoric acid salt is present.