Pharmaceutical compositions comprising a jak inhibitor

Abstract

Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.

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 ( 1 H 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.