IP Library Granted Patent US 12,410,133
Granted Patent B2
US 12,410,133 · App. 18/143,765 · Granted Sep 9, 2025

Crystalline (r)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, compositions and methods of use thereof

Inventors: Lianfeng Huang (Basking Ridge, NJ); Nancy Tsou (Edison, NJ); Nicole Suzanne White (San Diego, CA); Jun Xu (Suzhou, CN); Qun Zhang (Suzhou, CN)
Assignees: Celgene Corporation; Lundbeck La Jolla Research Center, Inc.
C07D211/94A61P35/00C07B2200/13
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Quick Facts
Patent No.
US 12,410,133
App. No.
18/143,765
Granted
Sep 9, 2025
Kind
B2
Abstract

Provided herein are crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate. Pharmaceutical compositions comprising crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate are also disclosed.

Claims (21)

1. A single unit dosage form comprising a crystalline form of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, wherein:

the crystalline form is Form A of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.1, 20.1, and 22.3 degrees 2θ±0.2 degrees 2θ;

the crystalline form is Form B of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 16.2, 18.2, and 19.2 degrees 2θ±0.2 degrees 2θ;

the crystalline form is Form C of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.0, 20.0, and 21.0 degrees 2θ±0.2 degrees 2θ;

the crystalline form is Form D of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 13.4, 21.0, and 23.8 degrees 2θ±0.2 degrees 2θ; or

the crystalline form is Form E of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 17.8, 21.3, and 22.8 degrees 2θ±0.2 degrees 2θ.

2. The single unit dosage form of claim 1 , wherein the crystalline form is Form A of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.1, 20.1, and 22.3 degrees 2θ±0.2 degrees 2θ.

3. The single unit dosage form of claim 2 , wherein the X-ray powder diffraction pattern further comprises peaks at 9.9, 19.9, and 24.7 degrees 2θ±0.2 degrees 2θ.

4. The single unit dosage form of claim 1 , wherein the crystalline form is Form B of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 16.2, 18.2, and 19.2 degrees 2θ±0.2 degrees 2θ.

5. The single unit dosage form of claim 4 , wherein the X-ray powder diffraction pattern further comprises peaks at 15.1, 18.7, and 20.1 degrees 2θ±0.2 degrees 2θ.

6. The single unit dosage form of claim 1 , wherein the crystalline form is Form C of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.0, 20.0, and 21.0 degrees 2θ±0.2 degrees 2θ.

7. The single unit dosage form of claim 6 , wherein the X-ray powder diffraction pattern further comprises peaks at 12.3, 16.8, and 25.5 degrees 2θ±0.2 degrees 2θ.

8. The single unit dosage form of claim 1 , wherein the crystalline form is Form D of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 13.4, 21.0, and 23.8 degrees 2θ±0.2 degrees 2θ.

9. The single unit dosage form of claim 8 , wherein the X-ray powder diffraction pattern further comprises peaks at 18.3, 26.7, and 29.5 degrees 2θ±0.2 degrees 2θ.

10. The single unit dosage form of claim 1 , wherein the crystalline form is Form E of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 17.8, 21.3, and 22.8 degrees 2θ±0.2 degrees 2θ.

11. The single unit dosage form of claim 10 , wherein the X-ray powder diffraction pattern further comprises peaks at 15.8, 18.4, and 21.9 degrees 2θ±0.2 degrees 2θ.

12. The single unit dosage form of claim 1 , wherein the single unit dosage form is suitable for oral, mucosal, rectal, nasal, vaginal, parenteral, subcutaneous, intramuscular, bolus injection, intraarterial, intravenous, sublingual, transdermal, buccal, or topical administration.

13. The single unit dosage form of claim 12 , wherein the single unit dosage form is a tablet, caplet, capsule, powder, or sterile solid that can be reconstituted to provide a liquid dosage form.

14. The single unit dosage form of claim 12 , wherein the single unit dosage form is a tablet, caplet, capsule, or liquid suitable for oral administration.

15. The single unit dosage form of claim 12 , wherein the single unit dosage form is a solution ready for injection, dry product ready to be dissolved or suspended in a pharmaceutically acceptable vehicle for injection, suspension ready for injection, or an emulsion ready for injection.

16. The single unit dosage form of claim 1 comprising about 0.1 mg to about 1,000 mg of the crystalline form.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2025
From: XU, JUN; ZHANG, QUN
To: CRYSTAL PHARMATECH CO., LTD
Reel/Frame 070815/0657 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2025
From: CRYSTAL PHARMATECH CO., LTD
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 070815/0673 →
MERGER Recorded Apr 11, 2025
From: ABIDE THERAPEUTICS, INC.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 070815/0756 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2025
From: WHITE, NICOLE SUZANNE
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 070824/0581 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2025
From: HUANG, LIANFENG; TSOU, NANCY
To: CELGENE CORPORATION
Reel/Frame 070824/0584 →
Continuity (4)
Continuation 17338182 · Jun 3, 2021
Division 16569578 · Sep 12, 2019
Provisional Application 62731014 · Sep 13, 2018
Related Publication 20230382861A1 · Nov 30, 2023
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