Antiandrogens with marginal agonist activity and methods of use

Details Antiandrogens with marginal agonist activity and methods of use Antiandrogens with marginal agonist activity and methods of use

C - Chemistry, Metallurgy

07

J

C07J 21/00 (2006.01) A61K 31/58 (2006.01) A61P 5/28 (2006.01) C07J 1/00 (2006.01)

Patent

CA 2522784

The instant invention provides potent antiandrogen compounds, such as 3.beta. - acetoxyandrost-1,5-diene-17-ethylene ketal and 3.beta.-hydroxyandrost-1, 5- diene-17ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

L'invention concerne des composés antiandrogènes puissants, tels que 3?-acétoxyandrost-1,5-diène-17-éthylène cétal et 3?-hydroxyandrost-1,5-diène-17-éthylène cétal, et des méthodes d'utilisation des composés antiandrogènes pour la prévention ou le traitement d'affections biologiques induites par des récepteurs des androgènes. Ainsi, les composés de l'invention sont par exemple utiles pour la prévention et le traitement du cancer de la prostate. De plus, l'on a découvert que les composés de l'invention sont utiles pour la prévention et le traitement de cancers indépendants des androgènes, tels que le cancer de la prostate indépendant des androgènes. Enfin, les composés de l'invention peuvent être utilisés pour traiter un syndrome de sevrage induites par les androgènes.

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