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1. (US20180263997) PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR
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Claims

1. A pharmaceutical composition comprising a therapeutically effective amount of filgotinib maleate Form I and fumaric acid.
2. (canceled)
3. The pharmaceutical composition of claim 1, further comprising magnesium stearate.
4. The pharmaceutical composition of claim 1, further comprising magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, and colloidal silicon dioxide.
5. 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.
6. A pharmaceutical composition 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;
about 1.5 wt % magnesium stearate; and
about 5.0 wt % fumaric acid.
7. A pharmaceutical composition comprising:
about 29 wt % to about 35 wt % 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;
about 1.3 wt % to about 1.8 wt % magnesium stearate; and
about 4.5 wt % to about 5.5 wt % fumaric acid.
8. The pharmaceutical composition of claim 1 wherein the composition is in the form of a tablet.
9. The pharmaceutical composition of claim 1 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.
10. The pharmaceutical composition of claim 1 wherein the filgotinib maleate Form I is characterized by an XRPD pattern substantially the same as shown in FIG. 1.
11. 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.
12. 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.
13. The pharmaceutical composition of claim 1 wherein the filgotinib maleate Form I is characterized by a proton nuclear magnetic resonance spectrum ( 1H NMR) substantially the same as shown in FIG. 3.
14. A method of treating a disease or disorder mediated by JAK comprising administering a pharmaceutical composition according to claim 1.
15. The method of claim 14 wherein the disease or disorder is an inflammatory disease or disorder.
16. The method of claim 15 wherein the inflammatory disease or disorder is selected from the group consisting of rheumatoid arthritis, Crohn's disease, ulcerative colitis, alopecia areata, uveitis, acute graft-versus-host disease, cutaneous lupus nephritis, membranous lupus nephritis, atopic dermatitis, psoriasis, ankylosing spondylitis, and psoriatic arthritis.