17-(1'-propenyl)-17-3'-oxidoestra-4-en-3-one derivative, use...

C - Chemistry – Metallurgy – 07 – J

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C07J 21/00 (2006.01) A61K 31/58 (2006.01) A61P 5/26 (2006.01) A61P 5/34 (2006.01) A61P 5/42 (2006.01) C07J 41/00 (2006.01) C07J 53/00 (2006.01)

Patent

CA 2710934

The invention relates to 17-(1'-propenyl)-17-3'-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action. Image

L'invention concerne des dérivés de 17-(1'-propényle)-17-3'-oxydoestra-4-ène-3-one de formule chimique générale (I), dans laquelle les groupes Z, R4, R6a, R6b, R7, R15, R16a, R16b et R18 ont les significations indiquées dans la revendication 1, ainsi que leurs solvates, leurs hydrates et leurs sels, y compris tous les stéréoisomères de ces composés. L'invention concerne également l'utilisation de ces dérivés dans la fabrication d'un médicament destiné à la contraception orale et au traitement de troubles pré-, péri- et post-ménopausiques ainsi que des médicaments contenant des dérivés de ce type et destinés, en particulier, à être utilisés dans les cas susmentionnés. Les dérivés selon l'invention possèdent un effet gestagène et, dans des cas préférés, un effet antiminéralocorticoïde et neutre jusqu'à légèrement androgène.

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