Modulators of resistant androgen receptor
US-2017320849-A1 · Nov 9, 2017 · US
US9701641B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9701641-B2 |
| Application number | US-201615292696-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 13, 2016 |
| Priority date | Sep 11, 2012 |
| Publication date | Jul 11, 2017 |
| Grant date | Jul 11, 2017 |
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The present application relates to crystalline and amorphous forms of Enzalutamide. The present application further relates to amorphous solid dispersions of Enzalutamide with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of Form R1 of Enzalutamide.
Opening claim text (preview).
The invention claimed is: 1. A process for preparing crystalline form R1 of enzalutamide characterized by a powder X-ray diffraction (PXRD) pattern having peaks at 12.3±0.2, 13.1±0.2, 15.0±0.2, and 17.5±0.2 degrees 2-theta, which comprises: a) providing a solution of enzalutamide in a single solvent selected from the group consisting of methanol, ethanol, isopropyl alcohol, n-butanol, acetic acid, tetrahydrofuran, toluene, methyl isopropyl ketone, dimethyl sulphoxide, methyl ethyl ketone, acetonitrile, ethyl acetate, xylene, N, N-dimethyl formamide, and N-methyl-2-pyrrolidone; and b) isolating crystalline enzalutamide form R1. 2. The process of claim 1 , wherein the isolation of crystalline form R1 in step b) is carried out by cooling, crash cooling, concentrating, adding an anti-solvent, and evaporation. 3. The process of claim 1 , wherein the single solvent is methanol. 4. The process of claim 1 , wherein the single solvent is isopropyl alcohol. 5. The process of claim 2 , wherein the anti-solvent is selected from water or n-heptane.
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