Polymorphic forms of a steroid-like compound and methods for the preparation and use thereof

Patent metadata

Field	Value
Publication number	US-10065984-B2
Application number	US-201414568450-A
Country	US
Kind code	B2
Filing date	Dec 12, 2014
Priority date	Dec 13, 2013
Publication date	Sep 4, 2018
Grant date	Sep 4, 2018

Abstract

Provided herein are multiple solid forms of a defined steroid-like compound, and methods for the preparation and use thereof. In one aspect, there is provided a crystalline form of said steroid-like compound, and methods for the preparation and use thereof. In another aspect, there is provided a substantially amorphous form of said steroid-like compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like. In still another aspect of the present invention, there are provided kits containing compounds according to the present invention and/or compositions containing same.

First claim

That which is claimed is:

1. A method for preparing crystalline form 1, having an X-ray powder diffraction pattern with peaks at about 7.4, 10.2, 11.4, 12.4, 14.3, 14.7, 17.4, 20.2, 22.4 and 31.6 degrees 2θ, of the compound:

said method comprising:
dissolving the compound in a suitable diluent selected from the group consisting of anisole, dichloromethane, dioxane, tetrahydrofuran, chloroform, heptane, and a 9:1 (v:v) mixture of dioxane and water, and
subjecting the solution of the compound in the diluent to conditions suitable for evaporation of the diluent therefrom, wherein the conditions suitable for the evaporation of the diluent therefrom are selected from the group consisting of elevated temperatures at atmospheric pressure, ambient temperature at reduced pressures, and a combination of elevated temperature and reduced pressure.

2. The method of claim 1 , wherein the conditions suitable for evaporation of diluent comprise elevated temperatures at atmospheric pressure.

3. The method of claim 1 , wherein the conditions suitable for evaporation of diluent comprise ambient temperature at reduced pressures.

4. The method of claim 1 , wherein the conditions suitable for evaporation of diluent comprise a combination of elevated temperature and reduced pressure.

5. A method for converting amorphous form of the compound:

into crystalline form 1, having an X-ray powder diffraction pattern with peaks at about 7.4, 10.2, 11.4, 12.4, 14.3, 14.7, 17.4, 20.2, 22.4 and 31.6 degrees 2θ, said method comprising subjecting said compound to elevated humidity and/or temperature for at least 72 hours.

6. The method of claim 5 , wherein the elevated humidity is a relative humidity of greater than 50%.

7. The method of claim 5 , wherein the elevated temperature is a temperature of at least 35° C.

Assignees

• Allergan Inc

Inventors

• Feng Shaoxin
• Smith Scott W
• Lambert Olivier M G
• Buttar Suzanne M

Classifications

• A61P27/06

  Antiglaucoma agents or miotics · CPC title

• A61P27/04

  Artificial tears; Irrigation solutions · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• C07J5/0053 Primary

  not substituted in position 16 · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title