IP Library Granted Patent US 11,590,136
Granted Patent B2
US 11,590,136 · App. 17/704,180 · Granted Feb 28, 2023

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
A61K31/519A61P17/06
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Quick Facts
Patent No.
US 11,590,136
App. No.
17/704,180
Granted
Feb 28, 2023
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 (31)

1. A method of treating a skin disorder in a human patient in need thereof comprising:

applying to the patient's skin a pharmaceutically composition comprising: 1) a therapeutic agent present in an amount ranging from about 0.5% to about 1.5% 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 (2) 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 to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.

2. The method according to claim 1 , wherein the applying step comprises application up to 84 consecutive days to the patient's skin.

3. The method according to claim 1 , wherein the applying step is repeatable.

4. The method according to claim 1 , wherein the applying step comprises daily application to the patient's skin.

5. The method according to claim 1 , wherein the skin disorder is an autoimmune skin disorder.

6. The method according to claim 1 , wherein the skin disorder is associated with JAK1 and/or JAK2.

7. The method according to claim 1 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.

8. The method according to claim 1 , wherein the skin disorder is atopic dermatitis.

9. The method 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 salt.

10. A method of treating a skin disorder in a human patient in need thereof comprising:

applying to the patient's skin a pharmaceutical composition comprising: (1) a therapeutic agent present in an amount of about 0.5% 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 (2) 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 to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.

11. The method according to claim 10 , wherein the skin disorder is an autoimmune skin disorder.

12. The method according to claim 10 , wherein the skin disorder is associated with JAK1 and/or JAK2.

13. The method according to claim 10 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.

14. The method according to claim 10 , wherein the skin disorder is atopic dermatitis.

15. The method according to claim 10 , 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 salt.

16. A method of treating a skin disorder in a human patient in need thereof comprising:

applying to the patient's skin a pharmaceutical composition comprising: (1) a therapeutic agent present in an amount of 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 (2) 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 to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.

17. The method according to claim 16 , wherein the skin disorder is an autoimmune skin disorder.

18. The method according to claim 16 , wherein the skin disorder is associated with JAK1 and/or JAK2.

19. The method according to claim 16 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.

20. The method according to claim 16 , wherein the skin disorder is atopic dermatitis.

21. The method according to claim 16 , 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 salt.

22. A method of treating a skin disorder in a human patient in need thereof comprising:

applying to the patient's skin a pharmaceutical composition comprising: (1) a therapeutic agent present in an amount of about 1.5% 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 (2) 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 to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.

23. The method according to claim 22 , wherein the skin disorder is an autoimmune skin disorder.

24. The method according to claim 22 , wherein the skin disorder is associated with JAK1/JAK2.

25. The method according to claim 22 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.

26. The method according to claim 22 , wherein the skin disorder is atopic dermatitis.

27. The method according to claim 22 , 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 salt.

Assignments (2)
ASSIGNOR'S INTEREST IN PART Recorded Mar 25, 2022
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION
Reel/Frame 060199/0621 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 25, 2022
From: PARIKH, BHAVNISH; YELESWARAM, KRISHNASWAMY; SHAH, BHAVESH
To: INCYTE CORPORATION
Reel/Frame 059398/0902 →
Continuity (8)
Continuation 17541439 · Dec 3, 2021
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 20220378792A1 · Dec 1, 2022
Cited By (1)
US 12,201,636