IP Library › Granted Patent US 11,833,152
Granted Patent B2
US 11,833,152 · App. 17/379,336 · Granted Dec 5, 2023

JAK1 pathway inhibitors for the treatment of cytokine-related disorders

Inventors: Michael O'Neill Montgomery (Yardley, PA); Ahmad Naim (Hatboro, PA); Susan Snodgrass (Greenville, DE)
Assignee: Incyte Corporation
A61K31/519A61K31/4155A61K31/437A61K31/573A61P37/00A61P37/02C07K16/2866
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Quick Facts
Patent No.
US 11,833,152
App. No.
17/379,336
Granted
Dec 5, 2023
Kind
B2
Abstract

This disclosure relates to JAK1 pathway inhibitors and the use thereof in treating cytokine-related diseases or disorders such as cytokine release syndrome (CRS), hemophagocytic lymphohistiocytosis (HLH), macrophage activation syndrome (MAS), and CAR-T-cell-related encephalopathy syndrome (CRES).

Claims (26)

1. A method for treating cytokine release syndrome in a subject, said method comprising administering to the subject one or more pharmaceutical compositions each comprising a JAK1 selective pathway inhibitor which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers.

2. The method of claim 1 , wherein the JAK1 selective pathway inhibitor is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

3. The method of claim 1 , further comprising administering tocilizumab to said subject.

4. The method of claim 1 , further comprising administering a corticosteroid to said subject.

5. The method of claim 1 , further comprising administering prednisone to said subject.

6. The method of claim 1 , further comprising administering tocilizumab and a corticosteroid to said subject.

7. The method of claim 3 , wherein the JAK1 selective pathway inhibitor is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

8. The method of claim 4 , wherein the JAK1 selective pathway inhibitor is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

9. The method of claim 5 , wherein the JAK1 selective pathway inhibitor is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

10. The method of claim 6 , wherein the JAK1 selective pathway inhibitor is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

11. The method of claim 1 , wherein the method comprises administering to the subject a daily dose of from about 100 mg to 600 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

12. The method of claim 1 , wherein the method comprises administering to the subject a daily dose of about 100 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

13. The method of claim 1 , wherein the method comprises administering to the subject a daily dose of about 200 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

14. The method of claim 1 , wherein the method comprises administering to the subject a once-daily dose of about 200 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

15. The method of claim 1 , wherein the method comprises administering to the subject a daily dose of about 400 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

16. A method for treating cytokine release syndrome in a subject, said method comprising administering to the subject one or more pharmaceutical compositions each comprising a JAK1 selective pathway inhibitor which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers;

wherein the one or more pharmaceutical compositions are administered as one or more sustained release dosage forms each comprising the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof, and the one or more pharmaceutically acceptable carriers.

17. The method of claim 16 , wherein the method comprises administering to the subject a daily dose of from about 100 mg to 600 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

18. The method of claim 16 , wherein the method comprises administering to the subject a daily dose of about 100 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

19. The method of claim 16 , wherein the method comprises administering to the subject a daily dose of about 200 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

20. The method of claim 16 , wherein the method comprises administering to the subject a once-daily dose of about 200 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

21. The method of claim 16 , wherein the method comprises administering to the subject a daily dose of about 400 mg on a free base basis of the JAK1 selective pathway inhibitor, or a pharmaceutically acceptable salt thereof.

22. The method of claim 16 , wherein the one or more pharmaceutical compositions each comprise a JAK1 selective pathway inhibitor which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers selected from microcrystalline cellulose, a first hypromellose, a second hypromellose, lactose monohydrate, and magnesium stearate, or any combination thereof.

23. The method of claim 16 , wherein the one or more pharmaceutical compositions each comprise a JAK1 selective pathway inhibitor which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt, and one or more pharmaceutically acceptable carriers selected from microcrystalline cellulose, a first hypromellose, a second hypromellose, lactose monohydrate, and magnesium stearate, or any combination thereof.

24. The method of claim 16 , wherein the one or more pharmaceutical compositions each comprise a JAK1 selective pathway inhibitor which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, microcrystalline cellulose, a first hypromellose, a second hypromellose, lactose monohydrate, and magnesium stearate.

25. The method of claim 16 , wherein the one or more pharmaceutical compositions each comprise a JAK1 selective pathway inhibitor which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt, microcrystalline cellulose, a first hypromellose, a second hypromellose, lactose monohydrate, and magnesium stearate.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2021
From: MONTGOMERY, MICHAEL O'NEILL; NAIM, AHMAD; SNODGRASS, SUSAN
To: INCYTE CORPORATION
Reel/Frame 057067/0517 →
Continuity (4)
Continuation 16276157 · Feb 14, 2019
Provisional Application 62631825 · Feb 18, 2018
Provisional Application 62710446 · Feb 16, 2018
Related Publication 20220040187A1 · Feb 10, 2022
Cited By (2)
US 12,247,020 US 12,336,998