IP Library › Patent Application 19664320
Patent Application
App. No. 19/664,320

PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZ0[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF

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Patent No.
US None
App. No.
19/664,320
Abstract

The present disclosure relates to stable liquid pharmaceutical composition 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.

Claims (47)

1 . A stable oral pharmaceutical solution comprising (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) and an aqueous pharmaceutical carrier,

wherein Compound 1 is present in the stable oral pharmaceutical solution at a concentration of about 1 mg/mL, and

the stable oral pharmaceutical solution has a pH in a range from about 2 to about 5.

2 - 29 . (canceled)

30 . The stable oral pharmaceutical solution of claim 1 , further comprising a pH adjusting agent, and wherein the aqueous pharmaceutical carrier is water.

31 . The stable oral pharmaceutical solution of claim 30 , wherein the pH adjusting agent is selected from the group consisting of citric acid, phosphoric acid, tartaric acid, succinic acid, formic acid, acetic acid, and combinations thereof.

32 . The stable oral pharmaceutical solution of claim 30 , wherein the pH adjusting agent is citric acid.

33 . The stable oral pharmaceutical solution of claim 30 , further comprising a buffer.

34 . The stable oral pharmaceutical solution of claim 33 , wherein the buffer is selected from the group consisting of citrate, phosphate, tartrate, succinate, formate, acetate, and combinations thereof.

35 . The stable oral pharmaceutical solution of claim 33 , wherein the buffer is sodium citrate.

36 . The stable oral pharmaceutical solution of claim 33 , wherein the pH adjusting agent is citric acid and the buffer is sodium citrate.

37 . The stable oral pharmaceutical solution of claim 33 , further comprising a preservative.

38 . The stable oral pharmaceutical solution of claim 37 , wherein the preservative is selected from the group consisting of sodium benzoate, benzoic acid, propyl paraben, sodium metabisulfite, potassium sorbate, para-hydroxybenzoic acid, para-hydroxybenzoate, and combinations thereof.

39 . The stable oral pharmaceutical solution of claim 37 , wherein the preservative is sodium benzoate.

40 . The stable oral pharmaceutical solution of claim 37 , further comprising a sweetener.

41 . The stable oral pharmaceutical solution of claim 40 , wherein the sweetener is selected from the group consisting of sucralose, acesulfame potassium, sodium saccharin, neotame, sucrose, maltitol, xylitol, and combinations thereof.

42 . The stable oral pharmaceutical solution of claim 40 , wherein the sweetener is sucralose.

43 . The stable oral pharmaceutical solution of claim 40 , comprising:

Compound 1;

sodium benzoate;

sucralose;

citric acid;

sodium citrate; and

water.

44 . The stable oral pharmaceutical solution of claim 43 , comprising:

1.0 mg/mL of Compound 1;

0.3 mg/mL of sodium benzoate;

9.0 mg/mL of sucralose;

2.13 mg/mL of citric acid;

0.45 mg/mL of sodium citrate; and

water.

45 . A process for preparing the stable oral pharmaceutical solution of claim 1 , the process comprising combining a crystalline form of Compound 1 and the aqueous pharmaceutical carrier.

46 . A process for preparing the stable oral pharmaceutical solution of claim 1 , the process comprising combining amorphous freebase Compound 1 and the aqueous pharmaceutical carrier.

47 . A process for preparing the stable oral pharmaceutical solution of claim 33 , the process comprising combining a crystalline form of Compound 1 and the aqueous pharmaceutical carrier.

48 . A process for preparing the stable oral pharmaceutical solution of claim 33 , the process comprising combining amorphous freebase Compound 1, the pH adjusting agent, the buffer, and the water.

49 . A stable oral pharmaceutical solution comprising (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) and an aqueous pharmaceutical carrier;

wherein Compound 1 is present in the stable oral pharmaceutical solution at a concentration of about 1 mg/ml;

wherein the stable oral pharmaceutical solution has a pH in a range from about 2 to about 5; and

wherein the stable oral pharmaceutical solution is produced by a process comprising combining Compound 1 and the aqueous pharmaceutical carrier.

50 . The stable oral pharmaceutical solution of claim 49 , produced by a process comprising combining a crystalline form of Compound 1 and the aqueous pharmaceutical carrier.

51 . The stable oral pharmaceutical solution of claim 49 , produced by a process comprising combining amorphous freebase Compound 1 and the aqueous pharmaceutical carrier.

52 . The stable oral pharmaceutical solution of claim 49 , further comprising a pH adjusting agent, produced by a process comprising combining a crystalline form of Compound 1, the pH adjusting agent, and the aqueous pharmaceutical carrier.

53 . The stable oral pharmaceutical solution of claim 49 , further comprising a pH adjusting agent, produced by a process comprising combining amorphous freebase Compound 1, the pH adjusting agent, and the aqueous pharmaceutical carrier.

54 . The stable oral pharmaceutical solution of claim 49 , further comprising a pH adjusting agent and a buffer, produced by a process comprising combining a crystalline form of Compound 1, the pH adjusting agent, the buffer, and the aqueous pharmaceutical carrier.

55 . The stable oral pharmaceutical solution of claim 49 , further comprising a pH adjusting agent and a buffer, produced by a process comprising combining amorphous freebase Compound 1, the pH adjusting agent, the buffer, and the aqueous pharmaceutical carrier.

56 . The stable oral pharmaceutical solution of claim 49 , further comprising a pH adjusting agent, a buffer, and a preservative, produced by a process comprising combining a crystalline form of Compound 1, the pH adjusting agent, the buffer, the preservative, and the aqueous pharmaceutical carrier.

57 . The stable oral pharmaceutical solution of claim 49 , further comprising a pH adjusting agent, a buffer, and a preservative, produced by a process comprising combining amorphous freebase Compound 1, the pH adjusting agent, the buffer, the preservative, and the aqueous pharmaceutical carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2026
From: KLÜNDER, BEN
To: ABBVIE DEUTSCHLAND GMBH & CO. KG
Reel/Frame 075932/0116 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2026
From: MOHAMED, MOHAMED-ESLAM F.; OTHMAN, AHMED A.; TAN, CHENG THIAM
To: ABBVIE INC.
Reel/Frame 075932/0274 →