IP Library Granted Patent US 11,213,528
Granted Patent B2
US 11,213,528 · App. 16/806,244 · Granted Jan 4, 2022

Salts of the janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Inventors: Hui-Yin Li (Hockessin, DE); James D. Rodgers (Landenberg, PA)
Assignees: Incyte Holdings Corporation; Incyte Corporation
A61K31/519A61K9/0053A61K9/20A61P17/06A61P17/08A61P17/12C07D487/04C07B2200/07C07B2200/13
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Quick Facts
Patent No.
US 11,213,528
App. No.
16/806,244
Granted
Jan 4, 2022
Kind
B2
Abstract

The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Claims (16)

1. A pharmaceutical composition comprising a compound that is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt and one or more pharmaceutically acceptable excipients; wherein the composition is suitable for providing sustained release of the compound.

2. The composition of claim 1 , wherein the composition is a unit dosage form.

3. The composition of claim 2 , wherein the unit dosage form is a tablet.

4. The composition of claim 2 , wherein the unit dosage form is a capsule.

5. The composition of claim 1 , wherein the unit dosage form further comprises an enteric layer.

6. The composition of claim 2 , wherein the unit dosage form comprises from about 5 to about 1000 mg of the compound.

7. The composition of claim 1 , wherein said one or more excipients comprise lactose, dextrose, sucrose, sorbitol, mannitol, starches, gum acacia, calcium phosphate, alginates, tragacanth, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, or methyl cellulose.

8. The composition of claim 1 , wherein said one or more excipients comprise microcrystalline cellulose.

9. The composition of claim 8 , wherein said one or more excipients comprise lactose.

10. The composition of claim 9 , wherein the unit dosage form is a tablet.

11. The composition of claim 1 , wherein said one or more excipients comprise lactose.

12. The composition of claim 1 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt.

13. The composition of claim 12 , wherein said crystalline salt is a 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt.

14. The composition of claim 13 , wherein the unit dosage form is a tablet.

15. The composition of claim 1 , wherein the composition suitable for providing sustained release of the compound is administered orally.

16. The composition of claim 1 , wherein the composition suitable for providing sustained release of the compound is administered topically.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 17, 2022
From: RODGERS, JAMES D.; LI, HUI-YIN
To: INCYTE CORPORATION
Reel/Frame 059030/0242 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 17, 2022
From: INCYTE CORPORATION
To: INCYTE CORPORATION; INCYTE HOLDINGS CORPORATION
Reel/Frame 059030/0389 →
Continuity (7)
Continuation 16003210 · Jun 8, 2018
Continuation 15164518 · May 25, 2016
Continuation 14270915 · May 6, 2014
Continuation 14097588 · Dec 5, 2013
Continuation 12137892 · Jun 12, 2008
Provisional Application 60943705 · Jun 13, 2007
Related Publication 20200197401A1 · Jun 25, 2020
Cited By (2)
US 12,428,426 US 12,479,851