IP Library › Granted Patent US 11,680,069
Granted Patent B2
US 11,680,069 · App. 17/951,332 · Granted Jun 20, 2023

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: Ayman Allian (Newbury Park, IL); Fredrik Lars Nordstrom (Ridgefield, CT); Ahmad Y. Sheikh (Lake Forest, IL); Thomas B. Borchardt (Kenosha, WI)
Assignee: AbbVie Inc.
C07D487/14A61K9/0053A61K31/4985A61K47/12A61K47/38C07B2200/13
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Quick Facts
Patent No.
US 11,680,069
App. No.
17/951,332
Granted
Jun 20, 2023
Kind
B2
Abstract

The present disclosure relates to processes for preparing (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, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Claims (30)

1. Crystalline freebase (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.

2. The crystalline freebase of claim 1 , wherein the crystalline freebase (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 is an anhydrate.

3. The crystalline freebase of claim 1 , wherein the crystalline freebase (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 is a hydrate.

4. The crystalline freebase of claim 3 , wherein the crystalline freebase (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 is a hemihydrate.

5. The crystalline freebase of claim 1 , wherein the crystalline freebase (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 is a solvate.

6. A pharmaceutical composition comprising crystalline freebase (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 a pharmaceutically acceptable carrier.

7. The pharmaceutical composition of claim 6 , wherein the pharmaceutical composition is a solid dosage form.

8. The pharmaceutical composition of claim 7 , wherein the solid dosage form is a tablet.

9. The pharmaceutical composition of claim 6 , wherein the crystalline freebase (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 is an anhydrate.

10. The pharmaceutical composition of claim 9 , wherein the pharmaceutical composition is a solid dosage form.

11. The pharmaceutical composition of claim 6 , wherein the crystalline freebase (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 is a hydrate.

12. The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is a solid dosage form.

13. The pharmaceutical composition of claim 6 , wherein the crystalline freebase (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 is a hemihydrate.

14. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is a solid dosage form.

15. The pharmaceutical composition of claim 6 , wherein the crystalline freebase (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 is a solvate.

16. The pharmaceutical composition of claim 15 , wherein the pharmaceutical composition is a solid dosage form.

17. A process for preparing a pharmaceutical composition comprising crystalline freebase (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 a pharmaceutically acceptable carrier, the process comprising combining crystalline freebase (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 a pharmaceutically acceptable carrier.

18. The process of claim 17 , wherein the pharmaceutical composition is a solid dosage form.

19. The process of claim 18 , wherein the solid dosage form is a tablet.

20. The process of claim 17 , wherein the crystalline freebase (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 is an anhydrate.

21. The process of claim 20 , wherein the pharmaceutical composition is a solid dosage form.

22. The process of claim 17 , wherein the crystalline freebase (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 is a hydrate.

23. The process of claim 22 , wherein the pharmaceutical composition is a solid dosage form.

24. The process of claim 17 , wherein the crystalline freebase (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 is a hemihydrate.

25. The process of claim 24 , wherein the pharmaceutical composition is a solid dosage form.

26. The process of claim 17 , wherein the crystalline freebase (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 is a solvate.

27. The process of claim 26 , wherein the pharmaceutical composition is a solid dosage form.

28. A pharmaceutical composition comprising crystalline freebase (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 a pharmaceutically acceptable carrier, prepared by the process of claim 17 .

29. The pharmaceutical composition of claim 28 , wherein the pharmaceutical composition is a solid dosage form.

30. The pharmaceutical composition of claim 28 , wherein the solid dosage form is a tablet.

Assignments (5)
CORRECTIVE ASSIGNMENT TO CORRECT THE FIRST INVENTOR'S EXECUTION DATE PREVIOUSLY RECORDED AT REEL: 062633 FRAME: 0138. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT . Recorded Mar 6, 2024
From: ALLIAN, AYMAN; JAYANTH, JAYANTHY; MOHAMED, MOHAMED-ESLAM F.; MULHERN, MATHEW M.; NORDSTROEM, LARS F.; OTHMAN, AHMED A.; ROZEMA, MICHAEL J.; BHAGAVATULA, LAKSHMI; MARROUM, PATRICK J.; MAYER, PETER T.
To: ABBVIE INC.
Reel/Frame 066674/0902 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2023
From: ALLIAN, AYMAN; JAYANTH, JAYANTHY; MOHAMED, MOHAMED-ESLAM F.; MULHERN, MATHEW M.; NORDSTROEM, LARS F.; OTHMAN, AHMED A.; ROZEMA, MICHAEL J.; BHAGAVATULA, LAKSHMI; MARROUM, PATRICK J.; MAYER, PETER T.
To: ABBVIE INC.
Reel/Frame 062633/0138 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2023
From: SHEIKH, AHMAD Y.; BORCHARDT, THOMAS B.
To: ABBVIE INC.
Reel/Frame 062633/0170 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2023
From: KLÜNDER, BEN
To: ABBVIE DEUTSCHLAND GMBH & CO. KG
Reel/Frame 062633/0231 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2023
From: ABBVIE DEUTSCHLAND GMBH & CO. KG
To: ABBVIE INC.
Reel/Frame 062633/0247 →
Continuity (10)
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
Provisional Application 62352380 · Jun 20, 2016
Provisional Application 62301537 · Feb 29, 2016
Provisional Application 62267672 · Dec 15, 2015
Provisional Application 62242797 · Oct 16, 2015
Related Publication 20230057084A1 · Feb 23, 2023
Cited By (1)
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