Solid state forms of AT-001 and process for preparation thereof
The present disclosure encompasses solid state forms of AT-001, in embodiments crystalline polymorphs of AT-001 or salts or co-crystals of AT-001, processes for preparation thereof, and pharmaceutical compositions thereof.
1 . A composition comprising a crystalline Form B of 2-(8-oxo-7-((5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)-7,8-dihydropyrazino[2,3-d]pyridazin-5-yl)acetic acid characterized by data selected from one or more of the following:
a) an XRPD pattern having peaks at 7.5, 16.6, 17.1, 27.9 and 31.1 degrees 2-theta±0.2 degrees 2-theta;
b) a solid state 13 C NMR spectrum having peaks at 36.6, 57.3, 118.7, 145, 148.8 and 168.3 ppm±0.2 ppm;
c) combinations of a) and b).
2 . The composition according to claim 1 , wherein the crystalline Form B of 2-(8-oxo-7-((5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)-7,8-dihydropyrazino[2,3-d]pyridazin-5-yl)acetic acid is a hydrate.
3 . The composition according to claim 1 , which contains no more than about 20% of any other crystalline forms of 2-(8-oxo-7-((5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)-7,8-dihydropyrazino[2,3-d]pyridazin-5-yl)acetic acid.
4 . The composition according to claim 1 , which contains no more than about 20% of amorphous 2-(8-oxo-7-((5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)-7,8-dihydropyrazino[2,3-d]pyridazin-5-yl)acetic acid.
5 . A pharmaceutical formulation comprising the composition according to claim 1 with at least one pharmaceutically acceptable excipient.
6 . A medicament comprising the composition according to claim 1 .