Hydrochloride salts of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and preparation process therefor
AssigneeOPKO Health, Inc.
InventorsMengwei Hu, Sunil Paliwal, Neng-Yang Shih, Frank Bruno Guenter, Ingrid Mergelsberg
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Abstract
Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
Claims21
1-39. (canceled)
A crystalline hydrochloride anhydrous Form I salt form of 8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one (Formula I),
- characterized by an X-ray powder diffraction pattern having peaks present at diffraction angles (in 2θ±0.2) of:
- 12.9;
- 15.4;
- 17.3;
- and 20.2.
A crystalline hydrochloride anhydrous Form II salt form of 8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one (Formula I),
- characterized by an x-ray powder diffraction pattern having peaks present at diffraction angles (in 2θ±0.2) of:
- 7.0;
- 9.0;
- 12.6;
- and 20.2.
A process for preparing a crystalline salt form of 8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
- comprising a step of treating Formula 1 with at least one equivalent of an acid selected from hydrochloric acid and 4-toluenesulfonic acid to provide the crystalline salt form of Formula 1.
Dependencies are inferred from the claim text.