Polymorphic forms and formulations of leriglitazone
AssigneeMinoryx Therapeutics S.L.
InventorsJosé Luis FÁBREGAS VIDAL, Montserrat MARTÍ PÉREZ
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Abstract
This disclosure provides crystalline forms of leriglitazone, pharmaceutical compositions or formulations comprising crystalline forms of leriglitazone, and methods of treating a disease, condition, or disorder in a patient comprising administering a composition comprising crystalline forms of leriglitazone to the patient.
Claims30
Crystalline leriglitazone hydrate Form C characterized as having:
- (i) a x-ray powder diffraction (XRPD) pattern with peaks at 12.7, 15.4, 19.1, 21.0, 23.8, and 25.9 degrees 2Θ using Cu Kα radiation, wherein the 2Θ values are ±0.2 degrees 2Θ;
- or
- (ii) a x-ray powder diffraction pattern with d-spacings at 6.99, 5.74, 4.65, 4.23, 3.73, and 3.44 Å using Cu Kα radiation;
- or
- (iii) a FT-Raman spectrum with peaks at 3056, 2960, 2992, 1735, 1608, 1205, 824, 656, and 170 cm−1, wherein the cm−1 values are ±4 cm−1;
- or
- (iv) a melting point with an onset temperature of about 149.45° C. and a peak temperature of about 153.50° C. based on differential scanning calorimetry;
- or
- a combination (i), (ii), (iii), and/or (iv).
2-14. (canceled)
(canceled)
Crystalline leriglitazone Form B characterized as having:
- (i) a x-ray powder diffraction (XRPD) pattern with peaks at 16.6, 18.8, 21.1, 21.8, 23.8, and 24.7 degrees 2Θ using Cu Kα radiation, wherein the 2Θ values are ±0.2 degrees 2ϑ;
- or
- (ii) a x-ray powder diffraction pattern with d-spacings at 5.33, 4.73, 4.21, 4.07, 3.73, and 3.60 Å using Cu Kα radiation;
- or
- (iii) a melting point with an onset temperature of about 149.34° C. and a peak temperature of about 153.56° C. based on differential scanning calorimetry;
- or
- a combination (i), (ii), and/or (iii).
19-32. (canceled)
35-38. (canceled)
41-51. (canceled)
(canceled)
(canceled)
60-83. (canceled)
(canceled)
A composition comprising 99.0 to 99.9 wt/wt % of leriglitazone (free base), leriglitazone hydrochloride, or leriglitazone hydrate, and:
- (i) 0.0001 to 0.2 wt/wt % of (Z)-5-(4-(2-(5-(1-hydroxyethyl)pyridin-2-yl)ethoxy)benzylidene)thiazolidine-2,4-dione, or the hydrochloride salt thereof;
- (ii) 0.0001 to 0.2 wt/wt % of 2,2′-disulfanediylbis(3-(4-(2-(5-(1-hydroxyethyl)pyridin-2-yl)ethoxy)phenyl) propanoic acid), or the hydrochloride salt thereof;
- (iii) 0.0001 to 0.2 wt/wt % of 2-((1-hydroxy-3-(4-(2-(5-(1-hydroxyethyl)pyridin-2-yl)ethoxy)phenyl) propan-2-yl)disulfaneyl)-3-(4-(2-(5-(1-hydroxyethyl)pyridin-2-yl)ethoxy)phenyl) propanoic acid, or the hydrochloride salt thereof;
- and/or
- (iv) 0.0001 to 0.15 wt/wt % of 5-(4-(2-(5-(1-hydroxyethyl)pyridin-2-yl)ethoxy)benzyl) thiazolidin-2-one, or the hydrochloride salt thereof.
90-92. (canceled)
Dependencies are inferred from the claim text.