Topical formulation for a JAK inhibitor

Patent metadata

Field	Value
Publication number	US-10869870-B2
Application number	US-202016947735-A
Country	US
Kind code	B2
Filing date	Aug 14, 2020
Priority date	May 21, 2010
Publication date	Dec 22, 2020
Grant date	Dec 22, 2020

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.

First claim

What is claimed is:

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.

2. The method of claim 1 , wherein the applying step comprises application up to 84 consecutive days.

3. The method of claim 1 , wherein the autoimmune skin disorder is psoriasis or atopic dermatitis.

4. 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%.

5. The method of claim 4 , wherein the composition further comprises a stabilizing agent component.

6. 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.

7. The method of claim 1 , wherein the oil-in-water emulsion has a pH of 2.9 to 3.6.

8. 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.

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.

10. The method of claim 9 , wherein the applying step comprises application up to 84 consecutive days.

11. The method of claim 9 , wherein the skin disorder is an autoimmune skin disorder.

12. The method of claim 11 , wherein the skin disorder is atopic dermatitis.

13. 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.

14. The method of claim 13 , wherein the composition further comprises a stabilizing agent component.

15. 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.

16. The method of claim 9 , wherein the oil-in-water emulsion has a pH of 2.9 to 3.6.

17. 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.

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.

19. The method of claim 18 , wherein the applying step comprises application up to 84 consecutive days.

20. 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%.

21. The method of claim 20 , wherein the composition further comprises a stabilizing agent component.

22. The method of claim 18 , wherein the oil-in-water emulsion has a pH of 2.9 to 3.6.

23. The method of claim 18 , wherein treating is ameliorating atopic dermatitis.

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.

25. The method of claim 24 , wherein the applying step comprises application up to 84 consecutive days.

26. 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%.

27. The method of claim 26 , wherein the composition further comprises a stabilizing agent component.

28. The method of claim 24 , wherein the oil-in-water emulsion has a pH of 2.9 to 3.6.

29. The method of claim 24 , wherein treating is ameliorating atopic dermatitis.

Assignees

• Incyte Corp
• Incyte Holdings Corp

Inventors

• Parikh Bhavnish
• Shah Bhavesh
• Yeleswaram Krishnaswamy

Classifications

• A61P17/06

  Antipsoriatics · CPC title

• A61P17/00

  Drugs for dermatological disorders · CPC title

• A61K9/06

  Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} · CPC title

• A61K47/36

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

• A61K47/24

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