Enzalutamide polymorphic forms and its preparation

US9701641B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9701641-B2
Application numberUS-201615292696-A
CountryUS
Kind codeB2
Filing dateOct 13, 2016
Priority dateSep 11, 2012
Publication dateJul 11, 2017
Grant dateJul 11, 2017

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  1. Title

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  2. Abstract

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  5. First independent claim

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Abstract

Official abstract text for this publication.

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.

First claim

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.

Assignees

Inventors

Classifications

  • C07D233/86Primary

    Oxygen and sulfur atoms, e.g. thiohydantoin · CPC title

  • Crystalline forms, e.g. polymorphs · CPC title

  • specific for metastasis · CPC title

  • H04W12/06Primary

    Authentication · CPC title

  • IP multimedia subsystem [IMS] · CPC title

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What does patent US9701641B2 cover?
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.
Who is the assignee on this patent?
Dr Reddys Laboratories Ltd
What technology area does this patent fall under?
Primary CPC classification C07D233/86. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Jul 11 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).