9-alpha-substituted estratrienes as selectively active...

Details 9-alpha-substituted estratrienes as selectively active... 9-alpha-substituted estratrienes as selectively active...

C - Chemistry, Metallurgy

07

J

C07J 43/00 (2006.01) A61K 31/56 (2006.01) A61K 31/58 (2006.01) A61P 9/00 (2006.01) A61P 15/00 (2006.01) A61P 19/00 (2006.01) C07J 1/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 63/00 (2006.01)

Patent

CA 2486495

This invention describes the new 9.alpha.-substituted estratrienes of general formula (I), in which R3, R7, R7', R13, R16 as well as R17 and R17' have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency--induced diseases and conditions.

La présente invention concerne des estratriènes 9.alpha.-substitués de la formule générale (I) dans laquelle R?3¿, R?7¿, R?7'¿, R?13¿, R?13'¿, R?17¿ et R?17'¿ ont la signification donnée dans le descriptif, et R?9¿ est un reste alcényle portant 2 à 6 atomes de carbone, linéaire ou ramifié, éventuellement partiellement ou entièrement halogéné, ou un reste éthinyl ou prop-1-inyl. Lesdits composés servent d'agents actifs pharmaceutiques présentant in vitro une plus grande affinité à des préparations de récepteurs d'oestrogènes de prostate de rat, qu'à des préparations de récepteurs d'oestrogènes d'utérus de rat, et in vivo de préférence un effet sur l'ovaire plutôt que sur l'utérus. L'invention concerne également la fabrication de ces composés, leur application thérapeutique et des formes d'administration pharmaceutiques contenant ces nouveaux composés. L'invention concerne par ailleurs l'utilisation desdits composés pour le traitement de maladies et troubles liés à une insuffisance en oestrogènes.

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