IP Library › Granted Patent US 12,502,394
Granted Patent B2
US 12,502,394 · App. 18/628,560 · Granted Dec 23, 2025

Pharmaceutical compositions comprising a JAK inhibitor

Inventors: David Alonzo (Foster City, CA); Bei Li (Foster City, CA); Dimitrios Stefanidis (Saratoga, CA)
Assignee: Alfasigma S.p.A.
A61K31/541A61K9/20A61K9/2009A61K9/2013A61K9/2018A61K9/2054A61K9/2059A61K47/12A61P29/00
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Quick Facts
Patent No.
US 12,502,394
App. No.
18/628,560
Granted
Dec 23, 2025
Kind
B2
Abstract

Pharmaceutical compositions comprising filgotinib maleate Form I, further comprising citric acid, and characterized by an XRPD pattern substantially the same as shown in FIG. 1 and uses thereof are described herein.

Claims (26)

1 . A pharmaceutical composition comprising a therapeutically effective amount of filgotinib maleate Form I, further comprising citric acid, wherein the filgotinib maleate Form I is characterized by an XRPD pattern substantially the same as shown in FIG. 1 .

2 . The pharmaceutical composition of claim 1 , further comprising magnesium stearate.

3 . The pharmaceutical composition of claim 1 , further comprising magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, and colloidal silicon dioxide.

4 . The pharmaceutical composition of claim 1 , further comprising magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, colloidal silicon dioxide, PEG 3350, polyvinyl alcohol, talc, titanium dioxide, and iron oxide red.

5 . A pharmaceutical composition according to claim 1 comprising:

about 32 wt % filgotinib maleate Form I;

about 36 wt % microcrystalline cellulose;

about 20 wt % lactose monohydrate;

about 5.0 wt % pregelatinized starch;

about 1.0 wt % colloidal silicon dioxide; and

about 1.5 wt % magnesium stearate.

6 . A pharmaceutical composition according to claim 1 comprising:

about 29 wt % to about 35wt % filgotinib maleate Form I;

about 32 wt % to about 40 wt % microcrystalline cellulose;

about 18 wt % to about 22 wt % lactose monohydrate;

about 4.5 wt % to about 5.5 wt % pregelatinized starch;

about 0.9 wt % to about 1.1 wt % colloidal silicon dioxide; and

about 1.3 wt % to about 1.8 wt % magnesium stearate.

7 . The pharmaceutical composition of claim 1 , wherein the composition is in the form of a tablet.

8 . The pharmaceutical composition of claim 1 , wherein the filgotinib maleate Form I is characterized by an XRPD pattern comprising peaks at 8.2, 11.9, 16.4, and 18.9° 2θ°±0.2° 2θ as determined on a diffractometer using Cu-Kα° radiation.

9 . The pharmaceutical composition of claim 1 , wherein the filgotinib maleate Form I is characterized by a differential scanning calorimetry (DSC) curve substantially the same as shown in FIG. 2 .

10 . The pharmaceutical composition of claim 1 wherein the filgotinib maleate Form I is characterized by thermogravimetric analysis (TGA) comprising a thermogram substantially the same as shown in FIG. 2 .

11 . The pharmaceutical composition of claim 1 wherein the filgotinib maleate Form I is characterized by a proton nuclear magnetic resonance spectrum ( 1 H NMR) substantially the same as shown in FIG. 3 .

12 . A method of treating an inflammatory disease or disorder mediated by JAK comprising administering a pharmaceutical composition to a patient in need thereof according to claim 1 , wherein the inflammatory disease or disorder is selected from rheumatoid arthritis, Chron's disease, ulcerative colitis, alopecia areata, uveitis, acute graft-versus host disease, cutaneous lupus nephritis, membrane lupus nephritis, atopic dermatitis, psoriasis, ankylosing spondylitis and psoriatic arthritis.

13 . The method of claim 12 wherein the inflammatory disease or disorder is ulcerative colitis.

14 . The pharmaceutical composition of claim 1 , wherein the filgotinib maleate Form I is characterized by an XRPD pattern comprising peaks at 28.9, 16.4, 8.2, 18.9, 20.0, 11.9, 14.9, 18.1, 20.5, and 22.6° 2θ°±0.2° 2θ as determined on a diffractometer using Cu-Kα° radiation.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2024
From: GALAPAGOS NV
To: ALFASIGMA S.P.A.
Reel/Frame 067126/0592 →
Continuity (6)
Continuation 17186446 · Feb 26, 2021
Continuation 16930803 · Jul 16, 2020
Continuation 15918765 · Mar 12, 2018
Provisional Application 62536614 · Jul 25, 2017
Provisional Application 62471171 · Mar 14, 2017
Related Publication 20240277725A1 · Aug 22, 2024
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