C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 41/00 (2006.01) C07J 7/00 (2006.01) C07J 21/00 (2006.01)
Patent
CA 2514169
The invention relates to a method of obtaining 17.alpha.-acetoxy-11.beta.-(4- N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione. The inventive method consists in: (a) forming crystals of the isopropanol hemisolvate of 17.alpha.-acetoxy-11.beta.-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene- 3,20-dione (VA-2914), by means of dissolution in isopropanol followed by crystallisation; (b) separating the VA-2914 isopropanol hemisolvate crystals; and (c) converting said VA-2914 isopropanol hemisolvate into VA-2914. Compound VA-2914 is a steroid with anti-progestational and anti-glucocorticoid activity, which can be used in therapeutic gynaecological and contraceptive indications and in the treatment of Cushing syndrome and glaucoma.
L'invention concerne un procédé d'obtention de 17.alpha.-acetoxy-11.beta.-(4-N,N-diméthylaminophénil)-19-norpregna-4,9-diène-3,20-dione (VA-2914) consistant à (a) former des cristaux de l'hémisolvate isopropanol 17.alpha.-acetoxy-11.beta.-(4-N,N-diméthylaminophénil)-19-norpregna-4,9-diène-3,20-dione (VA-2914) en vue de la dissolution dans l'isopropanol et de sa cristallisation ultérieure ; (b) séparer les cristaux de l'hémisolvate d'isopropanol de VA-2914 ; et (c) convertir en VA-2914 ledit hémisolvate d'isopropanol de VA-2914. Le composé VA-2914 est un stéroïde ayant une activité antiprogestative et antiglucocorticoïdale, utile dans des indications gynécologiques thérapeutiques et anticonceptives et dans le traitement du syndrome de Cushing et du glaucome.
Gutierrez Fuentes Luis Gerardo
Roson Nino Carlos
Silva Guisasola Luis Octavio
Crystal Pharma S.a.
Ridout & Maybee Llp
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