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US 12,662,483 B2Granted
Cocrystalline forms of FGFR3 inhibitors
AssigneeEli Lilly and Company
InventorsDavid Andrew Coates, Lori Raquel Hilden, Gislaine Kuminek, Jeffrey A. Peterson
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Abstract
Provided herein are cocrystalline forms of FGFR3 inhibitors and gallic acid or nicotinamide coformers useful in the treatment and prevention of diseases which can be treated with a FGFR3 inhibitor, including FGFR3-associated diseases and disorders, characterizations and methods of making these cocrystalline forms.
Claims63
A cocrystalline form of
- and a gallic acid coformer.
A cocrystalline form,
- obtainable by adding 4-[4-[3-Chloro-4-[1-(5-fluoro-2-pyridyl)-2-hydroxy-ethoxy]pyrazolo[1,5-a]pyridin-6-yl]-5-methyl-triazol-1-yl]piperidine-1-carbonitrile, Isomer 2 and gallic acid to a solvent to give a slurry, and
- adding cyclopentyl methyl ether to the slurry to form a white precipitate, wherein the crystalline form has improved solubility relative to a freebase form of Isomer 2:
A cocrystalline form,
- obtainable by heating
- to form a dehydrated hydrate wherein the crystalline form has improved solubility relative to a freebase form of Isomer 2:
A cocrystalline form,
- obtainable by combining
- with acetonitrile, wherein the crystalline form has improved solubility relative to a freebase form of Isomer 2:
A cocrystalline form of Isomer A:
- and a gallic acid coformer or a nicotinamide coformer.
A cocrystalline form,
- obtainable by adding gallic acid to
- dissolved in ethyl acetate, wherein the crystalline form has improved solubility relative to a freebase form of Isomer A:
A cocrystalline form,
- or a pharmaceutically acceptable salt thereof, obtainable by dissolving
- in ethyl acetate saturated with nicotinamide, wherein the crystalline form has improved solubility relative to a freebase form of Isomer A:
Dependencies are inferred from the claim text.