Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

摘要

The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.

主权项

1. A process for making a crystalline solvate form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), selected from Form D or Form E comprising:
a) dissolving Form XX of Compound 1 in a 75:25 mixture of acetonitrile and water in the process for making Form D, or a mixture of MEK and water, wherein the mixture of MEK and water is 99% MEK and 1% water, 90% MEK and 10% water, or 80% MEK and 20% water in the process for making Form E; b) heating the mixture until the solid has dissolved; c) precipitating the solid form by cooling the mixtures; and d) isolating the solid form by filtration;wherein,
Form XX possesses the XRPD pattern as shown in FIG. 1.