| 摘要 |
The invention relates to 11-aryl steroid derivatives, having the structure (See Fig. I) wherein: R1 is a homocyclic or heterocylic aryl group having one of the following substituents: an optionally saturated or unsaturated, branched or unbranched hydrocarbon radical containing 1-10 carbon atoms, the hydrocarbon radical being optionally provided with a hydroxyimino, oxo and/or hydroxyl group, or a (See Fig. II) group, where X and Y are each separately H or a hydrocarbon (1-4 C) radical or are together a hydrocarbon (2-6 C) radical; R2 is an alkyl group containing 1-4 carbon atoms; R3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, optionally provided with one or more hydroxyl, azido, nitrile, oxo and/or halogen groups, or is a (1-18 C) acyloxy or (2-8 C) alkoxyalkyl or (1-18 C) acyl or (1-12 C) alkoxy group; R4 is H, OH, a saturated or unsaturated hydrocarbon group containing 1-8 carbon atoms, optionally provided with one or more hydroxyl, azido, nitrile, oxo and/or halogen groups, or is a (1-18 C) acyloxy or (2-8 C) alkoxyalkyl or (1-18 C) acyl or (1-12 C) alkoxy group; or R3 and R4 together form a ring system or an alkylidene group having 1-6 carbon atoms and the dotted line represents an optional bond between the carbon atoms 16 and 17 of the steroid skeleton, with the proviso that R3 or R4 is absent if said bond between said carbon atoms 16 and 17 is present and to processes for their preparation and to pharmaceuticals comprising these compounds. These compounds exhibit a strong anti-progestinic activity and a weak or non-existent anti-glucocorticoid activity.
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