IP Library › Granted Patent US 12,365,689
Granted Patent B2
US 12,365,689 · App. 18/913,645 · Granted Jul 22, 2025

Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof

Inventors: Mohamed-Eslam F. Mohamed (Gurnee, IL); Ahmed A. Othman (Libertyville, IL); Aileen L. Pangan (La Grange, IL); Ben Klünder (Ludwigshafen, DE); Heidi S. Camp (Winnetka, IL); Robert J. Padley (Highland Park, IL); Jeffrey W. Voss (Hudson, MA); Cheng Thiam Tan (Grayslake, IL)
Assignee: AbbVie Inc.
C07D487/14A61K9/0053A61K31/4985A61K47/02A61K47/12A61K47/38C07D487/04C07B2200/13
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Quick Facts
Patent No.
US 12,365,689
App. No.
18/913,645
Granted
Jul 22, 2025
Kind
B2
Abstract

The present disclosure relates to solid-state forms and corresponding pharmaceutical compositions of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, and methods of treatment, including treatment of rheumatoid arthritis and juvenile idiopathic arthritis using the same. The treatment methods generally comprise administering to a patient (e.g., a pediatric patient) a therapeutically effective amount of upadacitinib as a stable liquid pharmaceutical composition or a solid dosage form, at a dose based on patient body weight.

Claims (33)

1. A method for treating juvenile idiopathic arthritis in a human patient in need thereof, comprising orally administering once daily to the patient a tablet comprising a therapeutically effective amount of (3S,4R)-3-ethyl-4-(3H-imidazo [1,2-a]pyrrolo [2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl) pyrrolidine-1-carboxamide (Compound 1), wherein the therapeutically effective amount is 15 mg.

2. The method of claim 1 , wherein the patient achieves an ACR50 score at week 12 of treatment.

3. The method of claim 1 , wherein the patient achieves an ACR70 score at week 12 of treatment.

4. A method for treating polyarticular course juvenile idiopathic arthritis (pcJIA) in a pediatric patient in need thereof, the method comprising administering a therapeutically effective amount of upadacitinib to the pediatric patient, wherein:

if the pediatric patient has a body weight in a range from about 10 kg to less than about 20 kg, administering upadacitinib twice daily as an oral pharmaceutical solution at a dose of 3 mg each (3 mg BID);

if the pediatric patient has a body weight in a range from about 20 kg to less than about 30 kg, administering upadacitinib twice daily as an oral pharmaceutical solution at a dose of 4 mg each (4 mg BID); and

if the pediatric patient has a body weight of about 30 kg or greater, administering upadacitinib twice daily as an oral pharmaceutical solution at a dose of 6 mg each (6 mg BID), or administering upadacitinib once daily as a tablet at a dose of 15 mg (15 mg QD).

5. The method of claim 4 , wherein the pediatric patient has a body weight in a range from about 10 kg to less than about 20 kg, and the method comprises administering upadacitinib twice daily as an oral pharmaceutical solution at a dose of 3 mg each (3 mg BID).

6. The method of claim 4 , wherein the pediatric patient has a body weight in a range from about 20 kg to less than about 30 kg, and the method comprises administering upadacitinib twice daily as an oral pharmaceutical solution at a dose of 4 mg each (4 mg BID).

7. The method of claim 4 , wherein the pediatric patient has a body weight of about 30 kg or greater, and the method comprises administering upadacitinib twice daily as an oral pharmaceutical solution at a dose of 6 mg each (6 mg BID).

8. The method of claim 4 , wherein the pediatric patient has a body weight of about 30 kg or greater, and the method comprises administering upadacitinib once daily as a tablet at a dose of 15 mg (15 mg QD).

9. The method of claim 4 , wherein the pcJIA is rheumatoid factor-positive JIA.

10. The method of claim 4 , wherein the pcJIA is rheumatoid factor-negative polyarticular JIA.

11. The method of claim 4 , wherein the pcJIA is extended oligoarticular JIA.

12. The method of claim 4 , wherein the pcJIA is systemic JIA with active arthritis and without active systemic features.

13. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 30 response at 12 weeks after the first daily administration.

14. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 50 response at 12 weeks after the first daily administration.

15. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 70 response at 12 weeks after the first daily administration.

16. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 90 response at 12 weeks after the first daily administration.

17. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 30 response at 48 weeks after the first daily administration.

18. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 50 response at 48 weeks after the first daily administration.

19. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 70 response at 48 weeks after the first daily administration.

20. The method of claim 4 , wherein the pediatric patient achieves a JIA ACR pediatric 90 response at 48 weeks after the first daily administration.

21. The method of claim 1 , wherein the subject has had an inadequate response or intolerance to one or more disease-modifying antirheumatic drugs (DMARDs).

22. The method of claim 21 , wherein the DMARD is methotrexate.

23. The method of claim 21 , wherein the DMARD is an anti-TNF biologic agent.

24. The method of claim 4 , wherein the subject has had an inadequate response or intolerance to one or more disease-modifying antirheumatic drugs (DMARDs).

25. The method of claim 24 , wherein the DMARD is methotrexate.

26. The method of claim 24 , wherein the DMARD is an anti-TNF biologic agent.

27. The method of claim 4 , wherein the pediatric patient has an age in a range from about 2 to less than about 18 years.

28. The method of claim 27 , wherein the subject has had an inadequate response or intolerance to one or more disease-modifying antirheumatic drugs (DMARDs).

29. The method of claim 28 , wherein the DMARD is methotrexate.

30. The method of claim 28 , wherein the DMARD is an anti-TNF biologic agent.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2025
From: MOHAMED, MOHAMED-ESLAM F.; OTHMAN, AHMED A.; PANGAN, AILEEN L.; CAMP, HEIDI S.; PADLEY, ROBERT J.; VOSS, JEFFREY W.; TAN, CHENG THIAM
To: ABBVIE INC.
Reel/Frame 071444/0702 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2025
From: KLÜNDER, BEN
To: ABBVIE DEUTSCHLAND GMBH & CO. KG
Reel/Frame 071444/0849 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2025
From: ABBVIE DEUTSCHLAND GMBH & CO. KG
To: ABBVIE INC.
Reel/Frame 071659/0831 →
Continuity (16)
Continuation In Part 18812217 · Aug 22, 2024
Continuation 18533564 · Dec 8, 2023
Continuation 18137804 · Apr 21, 2023
Continuation 17902690 · Sep 2, 2022
Continuation 17184194 · Feb 24, 2021
Continuation 16656237 · Oct 17, 2019
Continuation 15891012 · Feb 7, 2018
Continuation 15295561 · Oct 17, 2016
Continuation In Part 18612955 · Mar 21, 2024
Provisional Application 62352380 · Jun 20, 2016
Provisional Application 62301537 · Feb 29, 2016
Provisional Application 62267672 · Dec 15, 2015
Provisional Application 62242797 · Oct 16, 2015
Provisional Application 63623994 · Jan 23, 2024
Provisional Application 63491665 · Mar 22, 2023
Related Publication 20250034157A1 · Jan 30, 2025
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US 12,570,664