Topical formulation for a JAK inhibitor

Patent metadata

Field	Value
Publication number	US-12564593-B2
Application number	US-202519274086-A
Country	US
Kind code	B2
Filing date	Jul 18, 2025
Priority date	May 21, 2010
Publication date	Mar 3, 2026
Grant date	Mar 3, 2026

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)-1 H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.

First claim

What is claimed is:

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, C 16-18 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 from 0.5%-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 C 16-18 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 C 16-18 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, C 16-18 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 C 16-18 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 C 16-18 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, C 16-18 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 C 16-18 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 C 16-18 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 . The formulation of claim 1 , wherein the (R)-3-cyclopentyl-3-[4-(7H-pyrrolo [2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl] propanenitrile phosphoric acid salt is present in an amount from 0.5% to 1% by weight of the formulation on a free base basis.

17 . 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 C 16-18 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 formulatio

Assignees

• Incyte Corp
• Incyte Holdings Corp

Inventors

• Parikh Bhavnish
• Shah Bhavesh
• Yeleswaram Krishnaswamy

Classifications

• A61K47/36

  Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin · CPC title

• A61K47/26

  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 · CPC title

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title