Sulphur analogues of 21-hydroxy-6,19-oxidoprogesterone...

C - Chemistry – Metallurgy – 07 – J

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C07J 71/00 (2006.01) A61K 31/58 (2006.01) A61P 5/46 (2006.01)

Patent

CA 2419887

The present invention is related to novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues, their use as antiglucocorticoids for the treatment and/or prophylaxis of diseases associated to an excess of glucocorticoids. In particular, the invention relates to the use of novel 21-hydroxy-6,19- oxidoprogesterone (21OH-6OP) analogues having the formula FORMULAwherein X is S, SO and SO2, and R is either H or OH, for treating Cushing's syndrome, iatrogenic hypercortisolism or depression. Also the present invention is related to methods of preparing the novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues.

La présente invention concerne des nouveaux analogues de 21-hydroxy-6,19-oxydoprogestérone (21OH-6OP), leur utilisation comme anti-glucocorticoïdes pour le traitement et/ou la prévention de maladies associées à un excès de glucocorticoïdes. Plus particulièrement, l'invention concerne l'utilisation de nouveaux analogues 21-hydroxy-6,19-oxydoprogestérone (21OH-6OP) présentant la formule (I), dans laquelle X représente S, SO et SO¿2?, et R représente soit H soit OH, permettant de traiter le syndrome de Cushing, l'hypercolisolisme iatrogénique ou la dépression. En outre, l'invention concerne des procédés de préparation de nouveaux analogues de 21-hydroxy-6,19-oxydoprogésterone (21OH-6OP).

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