8-beta-substituted estratrienes as selectively active estrogens

Details 8-beta-substituted estratrienes as selectively active estrogens 8-beta-substituted estratrienes as selectively active estrogens

C - Chemistry, Metallurgy

07

J

C07J 1/00 (2006.01) A61K 31/565 (2006.01) A61P 5/30 (2006.01)

Patent

CA 2692727

The invention refers to 80-substituted estra-1,3,5(10)-triene derivatives of general formula (I), their use as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.

La présente invention concerne des dérivés estra-1,3,5(10)-triènes à substitution 8ß de formule générale (I) ; leur utilisation en tant que principes actifs pharmaceutiques, qui présentent, in vitro, vis-à-vis de préparations de récepteurs d'strogènes de la prostate de rats, une affinité supérieure à celle relative aux préparations de récepteurs d'strogènes de l'utérus de rats, et ayant de préférence, in vivo, une action plus marquée sur les ovaires que sur l'utérus ; leur production ; leur utilisation aux fins thérapeutiques et leur formes pharmaceutiques, destinées à être administrées, renfermant ces nouveaux composés.

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