IP Library › Granted Patent US 12,622,908
Granted Patent B2
US 12,622,908 · App. 17/541,439 · Granted May 12, 2026

Topical formulation for a JAK inhibitor

Inventors: Bhavnish Parikh (Avondale, PA); Bhavesh Shah (San Antonio, TX); Krishnaswamy Yeleswaram (Landenberg, PA)
Assignees: Incyte Corporation; Incyte Holdings Corporation
A61K31/519A61K9/0014A61K9/06A61K9/107A61K47/06A61K47/10A61K47/14A61K47/24A61K47/26A61K47/36A61P17/00A61P17/06
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Quick Facts
Patent No.
US 12,622,908
App. No.
17/541,439
Granted
May 12, 2026
Kind
B2
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 (27)

1 . A pharmaceutical composition for topical skin application to a human patient with a skin disorder comprising:

a therapeutically effective amount of a therapeutic agent present in an amount ranging from about 0.5% to about 1.0% by weight of the composition, wherein the therapeutic agent is (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

a means for effecting skin permeation of (R)-3-cyclopentyl-3-[4 (7H-pyrrolo [2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile or a pharmaceutically acceptable salt thereof to the patient.

2 . The pharmaceutical composition according to claim 1 , wherein the means for effecting skin permeation comprises water, an oil component, and an emulsifier component.

3 . The pharmaceutical composition according to claim 2 , wherein the oil component is present in an amount of about 20% to about 27%, by weight of the composition.

4 . The pharmaceutical composition according to claim 2 , wherein the oil component comprises one or more substances chosen from white petrolatum, cetyl alcohol, stearyl alcohol, light mineral oil, medium chain triglycerides, and dimethicone.

5 . The pharmaceutical composition according to claim 2 , wherein the oil component comprises an occlusive agent component.

6 . The pharmaceutical composition according to claim 5 , wherein the occlusive agent component is present in an amount of about 5% to about 10% by weight of the composition.

7 . The pharmaceutical composition according to claim 5 , wherein the occlusive agent component comprises white petroleum.

8 . The pharmaceutical composition according to claim 2 , wherein the oil component comprises a stiffening agent component.

9 . The pharmaceutical composition according to claim 8 , wherein the stiffening agent component is present in an amount of about 4% to about 7% by weight of the composition.

10 . The pharmaceutical composition according to claim 8 , wherein the stiffening agent component comprises one or more substances chosen from C 16-18 fatty alcohols.

11 . The pharmaceutical composition according to claim 2 , wherein the oil component comprises an emollient component.

12 . The pharmaceutical composition according to claim 11 , wherein the emollient component is present in an amount of about 7% to about 13% by weight of the composition.

13 . The pharmaceutical composition according to claim 11 , wherein the emollient component comprises one or more substances chosen from light mineral oil, medium chain triglycerides, and dimethicone.

14 . The pharmaceutical composition according to claim 2 , wherein the water is present in an amount of about 45% to about 55% by weight of the composition.

15 . The pharmaceutical composition according to claim 2 , wherein the emulsifier component is present in an amount of about 4% to about 7% by weight of the composition.

16 . The pharmaceutical composition according to claim 2 , wherein the emulsifier component comprises one or more substances chosen from glyceryl fatty esters and sorbitan fatty esters.

17 . The pharmaceutical composition according to claim 2 , further comprising a stabilizing agent component.

18 . The pharmaceutical composition according to claim 17 , wherein the stabilizing agent component is present in an amount of about 0.3% to about 0.5% by weight of the composition.

19 . The pharmaceutical composition according to claim 17 , wherein the stabilizing agent component comprises xanthan gum.

20 . The pharmaceutical composition according to claim 2 , further comprising a solvent component.

21 . The pharmaceutical composition according to claim 20 , wherein the solvent component is present in an amount of about 20% to about 25% by weight of the composition.

22 . The pharmaceutical composition according to claim 20 , wherein the solvent component comprises one or more substances chosen from alkylene glycols and polyalkylene glycols.

23 . The pharmaceutical composition according to claim 1 , wherein the therapeutic agent is present in an amount of about 0.5% by weight of the composition on a free base basis.

24 . The pharmaceutical composition according to claim 1 , wherein the therapeutic agent is present in an amount of about 1.0% by weight of the composition on a free base basis.

25 . The pharmaceutical composition according to claim 1 , wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo [2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 3, 2021
From: SHAH, BHAVESH; PARIKH, BHAVNISH; YELESWARAM, KRISHNASWAMY
To: INCYTE CORPORATION
Reel/Frame 058280/0420 →
ASSIGNOR'S INTEREST IN PART Recorded Dec 3, 2021
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 058300/0662 →
Continuity (7)
Continuation 16948408 · Sep 17, 2020
Continuation 16947735 · Aug 14, 2020
Division 16566625 · Sep 10, 2019
Continuation 14714820 · May 18, 2015
Continuation 13112370 · May 20, 2011
Provisional Application 61347132 · May 21, 2010
Related Publication 20220211707A1 · Jul 7, 2022
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