Solid state forms of lucerastat and process for preparation thereof
The present disclosure encompasses solid state forms of Lucerastat, in embodiments crystalline Lucerastat: L-Pyroglutamic acid, crystalline Lucerastat: Salicylic acid, crystalline Lucerastat: Fumaric acid, crystalline Lucerastat: Benzoic acid and crystalline Lucerastat: o-Acetylsalicylic acid, solid state form thereof, processes for preparation thereof, and pharmaceutical compositions thereof.
1 . A crystalline Form LC-1 of L-pyroglutamic acid salt of Lucerastat, which is characterized by data selected from one or more of the following:
a) an XRPD pattern having peaks at 10.1, 13.3, 16.3, 20.3 and 30.7 degrees 2-theta ±0.2 degrees 2-theta; and/or
b) an XRPD pattern as depicted in FIG. 1 .
2 . The crystalline Form LC-1 of L-pyroglutamic acid salt of Lucerastat according to claim 1 , characterized by an XRPD pattern having peaks at 10.1, 13.3, 16.3, 20.3 and 30.7 degrees 2-theta ±0.2 degrees 2-theta, and also having one, two, three, four or five additional peaks selected from 8.3, 14.5, 18.4, 21.8 and 22.9 degrees two theta ±0.2 degrees two theta.
3 . The crystalline Form LC-1 of L-pyroglutamic acid salt of Lucerastat according to claim 1 , characterized by an XRPD pattern having peaks at 8.3, 10.1, 13.3, 14.5, 16.3, 18.4, 20.3, 21.8, 22.9 and 30.7 degrees 2-theta ±0.2 degrees 2-theta.
4 . A crystalline Form LC-2 of Salicylic acid salt of Lucerastat, which is characterized by data selected from one or more of the following:
a) an XRPD pattern having peaks at 5.2, 16.6, 18.2, 22.3 and 23.7 degrees 2-theta ±0.2 degrees 2-theta; and/or
b) an XRPD pattern as depicted in FIG. 2 .
5 . The crystalline Form LC-2 of Crystalline Salicylic acid salt of Lucerastat according to claim 4 , characterized by an XRPD pattern having peaks at 5.2, 16.6, 18.2, 22.3 and 23.7 degrees 2-theta ±0.2 degrees 2-theta, and also having one, two, three, four or five additional peaks selected from 17.3, 19.5, 25.5, 22.9 and 34.2 degrees two theta ±0.2 degrees two theta.
6 . The crystalline Form LC-2 of Salicylic acid salt of Lucerastat according to claim 4 , characterized by an XRPD pattern having peaks at 5.2, 16.6, 17.3, 18.2, 19.5, 22.3, 22.9, 23.7, 25.5 and 34.2 degrees 2-theta ±0.2 degrees 2-theta.
7 . The crystalline Form LC-2 of Salicylic acid salt of Lucerastat according to claim 4 containing less than 10 wt % water.
8 . The crystalline Form LC-2 of Salicylic acid salt of Lucerastat according to claim 4 , which is non-deliquescent.
9 . A pharmaceutical formulation comprising the crystalline Form LC-2 of Salicylic acid salt of Lucerastat according to claim 4 in the form of a tablet, capsule, or solution for injection.
10 . A medicament comprising the crystalline Form LC-2 of Salicylic acid salt of Lucerastat according to claim 4 .
11 . A method of treating Fabry disease, comprising administering a therapeutically effective amount of the crystalline Form LC-2 of Salicylic acid salt of Lucerastat according to claim 4 to a subject in need of treatment.