Solid forms, salts and polymorphs of anti-fibrotic compounds
AssigneeCerta Therapeutics Pty Ltd
InventorsDarren James Kelly, Gareth Rhys Lewis, Lorna Helen Mitchell
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Abstract
The present disclosure relates to solid forms and salts, crystalline and otherwise, of (E)-2-[[3-(3-methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid and pharmaceutical compositions comprising same. The use of such solid forms, salts, and pharmaceutical compositions, for treating, preventing, or ameliorating diseases or conditions associated with fibrosis, inflammation and/or proliferation are disclosed.
Claims30
A crystalline form of a pharmaceutically acceptable salt of the compound of Formula (I):
- wherein the crystalline form has a water sorption of from 0.49% to 8.82% at 25° C. and 80% relative humidity as determined by dynamic vapor sorption.
A solid form of a pharmaceutically acceptable salt of the compound of Formula (I):
- having a bioavailability of at least 1.4× compared to a bioavailability of a free acid form of the compound of Formula (I).
A crystalline form of a pharmaceutically acceptable salt of the compound of Formula (I):
- wherein the crystalline form exhibits an X-ray powder diffraction pattern having (i) at least two peaks selected from 8.4±0.2, 14.0±0.2, and 17.5±0.2 degrees 2θ, (ii) at least two peaks selected from 7.5±0.2, 12.9±0.2, 15.3±0.2, and 23.9±0.2 degrees 2θ, or (iii) at least two peaks selected from 5.8±0.2, 12.2±0.2, 15.9±0.2, and 17.2±0.2 degrees 2θ.
A crystalline form of a pharmaceutically acceptable salt of the compound of Formula (I):
- wherein the crystalline form has at least one of (i) an endothermic onset of from 29° C. to 187° C. as measured by differential scanning calorimetry and (ii) a melting point of from 57° C. to 199° C. as measured by differential scanning calorimetry.
A crystalline form of a pharmaceutically acceptable salt of the compound of Formula (I):
- wherein the crystalline form exhibits an X-ray powder diffraction pattern having (i) at least two peaks selected from 9.8±0.2, 10.6±0.2, 14.1±0.2, and 25.1±0.2 degrees 2θ (±0.2 degrees 2θ), (ii) at least two peaks selected from 8.1±0.2, 11.7±0.2, 17.6±0.2, and 26.6±0.2 degrees 2θ, or iii) at least two peaks selected from 11.8±0.2, 14.5±0.2, 18.6±0.2, and 27.2±0.2 degrees 2θ.
Dependencies are inferred from the claim text.