Solid state forms of Danicopan and process thereof
The present disclosure relates to Danicopan solid state forms, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
1 . A crystalline form of Danicopan, designated form DT2, which is characterized by an XRPD pattern having peaks at 8.5, 12.9, 14.7, 17.0 and 19.6 degrees 2-theta±0.2 degrees 2-theta.
2 . A crystalline form of Danicopan according to claim 1 , which is characterized by an XRPD pattern having peaks at 8.5, 12.9, 14.7, 17.0 and 19.6 degrees 2-theta±0.2 degrees 2-theta, and also having one, two, three or four additional peaks selected from 11.5, 22.0, 22.5 and 30.9 degrees two theta±0.2 degrees two theta; or combinations of these data.
3 . A crystalline form of Danicopan according to claim 1 , which is characterized by an XRPD pattern having peaks at 8.5, 12.9, 14.7, 17.0 and 19.6 degrees two theta±0.2 degrees two theta, and also having one, two, three, four, or optionally five additional peaks selected from 20.9, 22.0, 22.5, 27.0 and 30.9 degrees two theta±0.2 degrees two theta.
4 . A crystalline form of Danicopan according to claim 1 , which is characterized by an X-ray powder diffraction pattern having peaks at 8.5, 11.5, 12.9, 14.7, 17.0, 19.6, 22.0, 22.5 and 30.9 degrees two theta±0.2 degrees two theta.
5 . A crystalline form of Danicopan according to claim 1 , which is characterized by an X-ray powder diffraction pattern having peaks at 8.5, 12.9, 14.7, 17.0, 19.6, 20.9, 22.0, 22.5, 27.0 and 30.9 degrees two theta±0.2 degrees two theta.
6 . A crystalline form of Danicopan according to claim 1 , which is characterized by an X-ray powder diffraction pattern substantially as depicted in FIG. 2 or FIG. 3 .
7 . A crystalline form of Danicopan according to claim 1 , which contains no more than about 20% any other crystalline forms of Danicopan.
8 . A crystalline form of Danicopan according to claim 1 , which contains no more than about 20% of amorphous Danicopan.
9 . A crystalline form of Danicopan according to claim 1 , which is chemically pure.
10 . A pharmaceutical composition comprising a crystalline form of Danicopan according to claim 1 and at least one pharmaceutically acceptable excipient.
11 . A process for preparing a pharmaceutical composition comprising combining a crystalline form of Danicopan according to claim 1 with at least one pharmaceutically acceptable excipient.
12 . A medicament comprising the crystalline form of Danicopan according to claim 1 .
13 . A method of treating paroxysmal nocturnal hemoglobinuria (PNH), other complement mediated diseases, or geographic atrophy in age-related macular degeneration, comprising administering a crystalline form of Danicopan according claim 1 to a patient in need of treatment.
14 . The method of claim 13 , wherein the crystalline form of Danicopan is administered to the patient as an add-on therapy in combination with a component 5 inhibitor.
15 . The method of claim 14 , wherein the component 5 inhibitor is ravulizumab or eculizumab.