IP Library Granted Patent US 11,273,159
Granted Patent B2
US 11,273,159 · App. 16/349,042 · Granted Mar 15, 2022

Pharmaceutical formulations

Inventors: Cheryl A. Grice (Encinitas, CA); Nicole S. White (San Diego, CA); Joel P. Zingerman (Carlsbad, CA); Hibreniguss Terefe (Piscataway, NJ); Isaac Ghebre-Sellassie (Morris Plains, NJ)
Assignee: H. LUNDBECK A/S
A61K31/497A61K9/0056A61K47/02A61K47/26A61K47/58
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Quick Facts
Patent No.
US 11,273,159
App. No.
16/349,042
Granted
Mar 15, 2022
Kind
B2
Abstract

Provided herein are pharmaceutical formulations comprising a monoacylglycerol lipase (MAGL) inhibitor, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

Claims (31)

1. A pharmaceutical formulation in a solid dosage form comprising:

(a) 1 mg to 60 mg of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, or a pharmaceutically acceptable salt thereof;

(b) 50 mg to 175 mg of microcrystalline cellulose;

(c) 6 mg to 15 mg of croscarmellose sodium; and

(d) 0.5 mg to 2.5 mg of magnesium stearate.

2. The pharmaceutical formulation of claim 1 , wherein the 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate is a hydrochloride salt.

3. The pharmaceutical formulation in a solid dosage form according to claim 1 comprising:

(a) 2.1 mg of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate hydrochloride salt;

(b) 156 mg of microcrystalline cellulose;

(c) 10 mg of croscarmellose sodium; and

(d) 1.7 mg of magnesium stearate.

4. The pharmaceutical formulation in a solid dosage form according to claim 1 comprising:

(a) 10.7 mg of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate hydrochloride salt;

(b) 147 mg of microcrystalline cellulose;

(c) 10.2 mg of croscarmellose sodium; and

(d) 1.7 mg of magnesium stearate.

5. The pharmaceutical formulation in a solid dosage form according to claim 1 comprising:

(a) 53.6 mg of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate hydrochloride salt;

(b) 104 mg of microcrystalline cellulose;

(c) 10 mg of croscarmellose sodium; and

(d) 1.7 mg of magnesium stearate.

6. The pharmaceutical formulation of claim 1 , wherein the solid dosage form is a tablet.

7. The pharmaceutical formulation of claim 2 , wherein the solid dosage form is a tablet.

8. The pharmaceutical formulation of claim 3 , wherein the solid dosage form is a tablet.

9. The pharmaceutical formulation of claim 4 , wherein the solid dosage form is a tablet.

10. The pharmaceutical formulation of claim 5 , wherein the solid dosage form is a tablet.

11. The pharmaceutical formulation of claim 1 , wherein the solid dosage form is a capsule.

12. The pharmaceutical formulation of claim 2 , wherein the solid dosage form is a capsule.

13. The pharmaceutical formulation of claim 3 , wherein the solid dosage form is a capsule.

14. The pharmaceutical formulation of claim 4 , wherein the solid dosage form is a capsule.

15. The pharmaceutical formulation of claim 5 , wherein the solid dosage form is a capsule.

Assignments (6)
CORRECTIVE ASSIGNMENT TO CORRECT THE THE RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 055679 FRAME: 0885. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jun 11, 2021
From: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
To: H. LUNDBECK A/S
Reel/Frame 056544/0697 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2021
From: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
To: H. LUNDBECK A/S.
Reel/Frame 055679/0885 →
MERGER Recorded Mar 23, 2021
From: ABIDE THERAPEUTICS, INC.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 057434/0784 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 5, 2020
From: GRICE, CHERYL A.; WHITE, NICOLE S.; ZINGERMAN, JOEL P.; TEREFE, HIBRENIGUSS; GHEBRE-SELLASSIE, ISAAC
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 051732/0230 →
CHANGE OF NAME Recorded Jan 9, 2020
From: ABIDE THERAPEUTICS, INC.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 051471/0554 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 6, 2020
From: GRICE, CHERYL A.; WHITE, NICOLE S.; ZINGERMAN, JOEL P.; TEREFE, HIBRENIGUSS; GHEBRE-SELLASSIE, ISAAC
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 051429/0136 →
Continuity (3)
Provisional Application 62545857 · Aug 15, 2017
Provisional Application 62423124 · Nov 16, 2016
Related Publication 20200188393A1 · Jun 18, 2020