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 less than 1.7% 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 39 F %.
A crystalline form of an ethanolamine salt of the compound of Formula (I):
- wherein the crystalline form exhibits an X-ray powder diffraction pattern having at least one peak selected from 6.6±0.2, 11.7±0.2, 15.0±0.2, 15.9±0.2, 17.7±0.2, 18.7±0.2, 19.2±0.2, 23.7±0.2, and 26.6±0.2 degrees 2θ.
A pharmaceutical composition comprising the ethanolamine salt of (E)-2-[[3-(3-methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid and at least one pharmaceutically acceptable carrier, wherein at least about 80%, at least 85%, at least 88%, at least 90%, at least 91%, at least 92%, at least 93%, at least 94%, or at least 95% of the ethanolamine salt of (E)-2-[[3-(3-methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid is crystalline Form I of the ethanolamine salt of (E)-2-[[3-(3-methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid.
Dependencies are inferred from the claim text.