8beta-vinyl-11beta-(alpha-substituted)alkyl-estra-1,3,5(10)-...

C - Chemistry – Metallurgy – 07 – J

Patent

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C07J 1/00 (2006.01) A61K 31/56 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01)

Patent

CA 2522354

The invention relates to 8.beta.-vinyl-11.beta.-(.omega.-substituted)alkyl- estra-1,3,5(10)-trienes of general formula (I), which have ER.beta.- antagonistic activity, methods for the production thereof, the intermediate products thereof, pharmaceutical preparations containing the inventive compounds, and the use thereof for producing medicaments. The novel compounds can be used for contraceptive purposes in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver and while also being suitable for the treatment of benign or malignant proliferous ovarian diseases, such as ovarian carcinoma and granulosa cell tumors.

L'invention concerne des 8bêta-vinyle-11bêta- alkyle (substitué oméga)-estra-1,3,5(10)-triènes de formule I (I), à activité antagoniste ERbêta. La présente invention porte également sur un procédé de préparation associé, sur des produits intermédiaires, sur des préparations pharmaceutiques contenant les composés de l'invention, et sur leur utilisation pour produire des médicaments. Ces nouveaux composés sont des contraceptifs pour l'homme et la femme, et ils n'influencent pas d'autres organes sensibles aux oestrogènes tels que l'utérus ou le foie. Ils sont également utiles dans le traitement de maladies proliférantes des ovaires, bénignes ou malignes, telles que les carcinomes ovariens et les tumeurs de la granulosa.

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