# US 10,869,870 B2 · Topical formulation for a JAK inhibitor > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,869,870 B2 - Document ID: US10869870B2 - Status: Granted - Kind: B2 - Application number: 16/947,735 - Filed: 2020-08-14 - Published: 2020-11-26 - Granted: 2020-12-22 - Earliest claimed: 2010-05-21 - Assignees: Incyte Corporation - Applicants: Incyte Corporation; Incyte Holdings Corporation - Inventors: Bhavnish Parikh; Bhavesh Shah; Krishnaswamy Yeleswaram - Web page: https://patentgrep.com/patent/US10869870B2 ## CPC - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)} - A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} - A61K 47/06: Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin - A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin - A61P 17/00: Drugs for dermatological disorders - A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like - A61P 17/04: Antipruritics - A61P 17/06: Antipsoriatics - A61P 37/02: Immunomodulators - A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## 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. ## Claims ### Claim 1 A method of treating a skin disorder in a human patient in need thereof, comprising: applying to the patient's skin a pharmaceutically acceptable composition 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 and further wherein the oil-in-water emulsion has a pH of not greater than 3.6; wherein treating is one or more of inhibiting the skin disorder and ameliorating the skin disorder; and wherein the skin disorder is an autoimmune skin disorder. ### Claim 2 (depends on 1) The method of claim 1, wherein the applying step comprises application up to 84 consecutive days. ### Claim 3 (depends on 1) The method of claim 1, wherein the autoimmune skin disorder is psoriasis or atopic dermatitis. ### Claim 4 (depends on 1) The method 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%. ### Claim 5 (depends on 4) The method of claim 4, wherein the composition further comprises a stabilizing agent component. ### Claim 6 (depends on 1) The method of claim 1, wherein 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 is present. ### Claim 7 (depends on 1) The method of claim 1, wherein the oil-in-water emulsion has a pH of 2.9 to 3.6. ### Claim 8 (depends on 7) The method of claim 7, wherein 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 is present. ### Claim 9 A method of inhibiting JAK1 and/or JAK2 in a human patient suffering from a skin disorder, comprising: applying to the patient's skin a pharmaceutically acceptable composition 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 and further wherein the oil-in-water emulsion has a pH of not greater than 3.6. ### Claim 10 (depends on 9) The method of claim 9, wherein the applying step comprises application up to 84 consecutive days. ### Claim 11 (depends on 9) The method of claim 9, wherein the skin disorder is an autoimmune skin disorder. ### Claim 12 (depends on 11) The method of claim 11, wherein the skin disorder is atopic dermatitis. ### Claim 13 (depends on 9) The method of claim 9, 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. ### Claim 14 (depends on 13) The method of claim 13, wherein the composition further comprises a stabilizing agent component. ### Claim 15 (depends on 9) The method of claim 9, wherein 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 is present. ### Claim 16 (depends on 9) The method of claim 9, wherein the oil-in-water emulsion has a pH of 2.9 to 3.6. ### Claim 17 (depends on 16) The method of claim 16, wherein 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 is present. ### Claim 18 A method of treating atopic dermatitis in a human patient, comprising: applying to the patient's skin a pharmaceutically acceptable composition 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 and further wherein the oil-in-water emulsion has a pH of not greater than 3.6; and wherein treating is one or more of inhibiting atopic dermatitis and ameliorating atopic dermatitis. ### Claim 19 (depends on 18) The method of claim 18, wherein the applying step comprises application up to 84 consecutive days. ### Claim 20 (depends on 18) The method of claim 18, 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%. ### Claim 21 (depends on 20) The method of claim 20, wherein the composition further comprises a stabilizing agent component. ### Claim 22 (depends on 18) The method of claim 18, wherein the oil-in-water emulsion has a pH of 2.9 to 3.6. ### Claim 23 (depends on 18) The method of claim 18, wherein treating is ameliorating atopic dermatitis. ### Claim 24 A method of treating atopic dermatitis in a human patient, comprising: applying to the patient's skin a pharmaceutically acceptable composition 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 and further wherein the oil-in-water emulsion has a pH of not greater than 3.6; and wherein treating is one or more of inhibiting atopic dermatitis and ameliorating atopic dermatitis. ### Claim 25 (depends on 24) The method of claim 24, wherein the applying step comprises application up to 84 consecutive days. ### Claim 26 (depends on 24) The method of claim 24, 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%. ### Claim 27 (depends on 26) The method of claim 26, wherein the composition further comprises a stabilizing agent component. ### Claim 28 (depends on 24) The method of claim 24, wherein the oil-in-water emulsion has a pH of 2.9 to 3.6. ### Claim 29 (depends on 24) The method of claim 24, wherein treating is ameliorating atopic dermatitis.