Treatment of hair loss disorders with deuterated JAK inhibitors

Patent metadata

Field	Value
Publication number	US-10561659-B2
Application number	US-201716098338-A
Country	US
Kind code	B2
Filing date	May 4, 2017
Priority date	May 4, 2016
Publication date	Feb 18, 2020
Grant date	Feb 18, 2020

Abstract

Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I), or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.

First claim

What is claimed is:

1. A method of treating a hair loss disorder in a mammalian subject, the method comprising administering to the subject 16 mg/day or 24 mg/day of a compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein each position in Compound (I) designated specifically as deuterium has at least 95% incorporation of deuterium.

2. The method of claim 1 , wherein the hair loss disorder is alopecia areata.

3. The method of any one of claim 1 , wherein the compound is administered orally.

4. The method of claim 1 , wherein the compound is administered in a pharmaceutical formulation which is a tablet.

5. The method of claim 1 , wherein the compound is administered once a day.

6. The method of claim 1 , wherein the compound is administered twice a day.

7. The method of claim 1 , wherein in Compound (I), any atom not designated as deuterium is present at its natural isotopic abundance.

8. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and 8 mg or 12 mg of a compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein each position in Compound (I) designated specifically as deuterium has at least 95% incorporation of deuterium.

9. A method of treating a hair loss disorder in a mammalian subject, the method comprising administering to the subject twice a day 8 mg of a compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein each position in Compound (I) designated specifically as deuterium has at least 95% incorporation of deuterium.

10. The method of claim 9 , wherein Compound (I) is administered as 10.5 mg of the phosphate salt twice per day.

11. A method of treating a hair loss disorder in a mammalian subject, the method comprising administering to the subject twice per day 12 mg of a compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein each position in Compound (I) designated specifically as deuterium has at least 95% incorporation of deuterium.

12. The method of claim 11 , wherein Compound (I) is administered as 15.8 mg of the phosphate salt twice per day.

13. The method of claim 1 , wherein each position in Compound (I) designated specifically as deuterium has at least 97% incorporation of deuterium.

14. The method of claim 1 , wherein the step of administering comprises administering to the subject 8 mg twice per day or 12 mg twice per day of Compound (I).

15. The method of claim 9 , wherein the hair loss disorder is alopecia areata.

16. The method of claim 9 , wherein the compound is administered orally.

17. The method of claim 9 , wherein each position in Compound (I) designated specifically as deuterium has at least 97% incorporation of deuterium.

18. The method of claim 11 , wherein the hair loss disorder is alopecia areata.

19. The method of claim 11 , wherein compound is administered orally.

20. The method of claim 11 , wherein each position in Compound (I) designated specifically as deuterium has at least 97% incorporation of deuterium.

21. The method of claim 14 , wherein the subject is a human.

Assignees

• Concert Pharmaceuticals Inc

Inventors

• Wagner Amanda T
• Cassella James V
• Graham Philip B
• Braman Virginia
• Uttamsingh Vinita
• Von Hehn Jana
• Hamilton Colleen E

Classifications

• A61P17/14

  for baldness or alopecia · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K31/519 Primary

  ortho- or peri-condensed with heterocyclic rings · CPC title

• A61K9/2027

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title