15,16-methylene-17-(1'-propenyl)-17,3'-oxidoestra-4-en-3-one...

Details 15,16-methylene-17-(1'-propenyl)-17,3'-oxidoestra-4-en-3-one... 15,16-methylene-17-(1'-propenyl)-17,3'-oxidoestra-4-en-3-one...

C - Chemistry, Metallurgy

07

J

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

Patent

CA 2710486

The invention relates to 15,16-methylene-17-(1'-propenyl)-17-3'-oxidoestra-4- en-3-one derivatives with the general chemical formula I, where the Z, R4, R6a, R6b, R7 and R18 have the meanings stated in claim 1, and solvates, hydrates and salts thereof, including all crystal modifications and all stereoisomers of these compounds. The invention also relates to the use of these derivatives for the production of a drug for oral contraception and for the treatment of pre-, peri- and postmenopausal problems and drugs which contain such derivatives, in particular use in the aforesaid indications. The derivatives according to the invention have a progestational and in preferable cases also an antimineralcorticoid and neutral to slight androgenic activity. (see formula I)

L'invention concerne des dérivés de 15,16-méthylène-17-(1 '-propényl)-17-3'-oxydoestra-4-ène-3-one de formule chimique générale (I), dans laquelle Z, R4, R6a, R6b, R7 et R18 ont les significations indiquées dans la revendication 1, ainsi que leurs solvates, leurs hydrates et leurs sels, y compris toutes les modifications cristallines et 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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