Crystalline polymorph of bazedoxifene acetate
AssigneeWyeth
InventorsChristopher Demerson, Silvio Iera, Kadum A. Ali
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Abstract
The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.
Claims91
A crystalline polymorph (Form A) of bazedoxifene acetate having a powder X ray diffraction pattern comprising characteristic peaks, in terms of 2θ, at about 12.7° and about 18.5°.
A method of preparing bazedoxifene acetate polymorphic Form A comprising:
- a) reacting hexamethyleneimino benzyloxyindole with a hydrogenating reagent in a solvent and optionally in the presence of a hydrogenation catalyst for a time and under conditions suitable for forming a reaction mixture comprising bazedoxifene free base;
- b) treating said reaction mixture with acetic acid for a time and under conditions suitable for forming bazedoxifene acetate polymorph Form A.
A method of preparing bazedoxifene acetate polymorphic Form A comprising crystallizing bazedoxifene acetate from a solution comprising an alcohol wherein said solution is maintained at a temperature below about 20° C.
Dependencies are inferred from the claim text.