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US 5,272,140 AGranted
11-aryl steroid derivatives
AssigneeAkzo N.V.
InventorHubert J. J. Loozen
Life of this patent
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Abstract
The invention relates to 11-aryl steroid derivatives, having the structure ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described in the specification 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.
Claims10
An 11-arylsteroid derivative having the structure:
- ##STR9## wherein:
- R.sub.1 is a homocyclic or heterocyclic aryl group having one of the following substituents:
- a saturated or unsaturated, branched or unbranched hydrocarbon radical containing 1-10 carbon atoms;
- R.sub.2 is an alkyl group containing 1-4 carbon atoms;
- R.sub.3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, an (1-18 C) acyloxy, (2-8 C) alkoxyalkyl, (1-18 C) acyl or (1-12 C) alkoxy group;
- R.sub.4 is H, OH, a saturated or unsaturated hydrocarbon group containing 1-8 carbon atoms, an (1-18 C) acyloxy, (2-8 C) alkoxyalkyl (1-18 C) acyl or (1-12 C) alkoxy group;
- or R.sup.3 and R.sub.4 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 R.sub.3 or R.sub.4 is absent if said bond between said carbon atoms 16 and 17 is present.
4 more elements
An 11-arylsteroid derivative having the structure:
- ##STR11## wherein:
- R.sub.1 is a homocyclic or heterocyclic aryl group having one of the following substituents:
- a saturated or unsaturated, branched or unbranched hydrocarbon radical containing 1-10 carbon atoms, said hydrocarbon radical having at least one substituent selected from the group consisting of hydroxyimino, oxo, hydroxyl and ##STR12## , wherein X and Y are each separately H or a (1-4 C) hydrocarbon radical, or together comprise a (2-6 C) hydrocarbon radical;
- R.sub.2 is an alkyl group containing 1-4 carbon atoms;
- R.sub.3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms having at least one substituent selected from the group consisting of hydroxyl, azido, nitrile, oxo, halogen, (1-18 C) acyloxy, (2-8 C) alkoxyalkyl, (1-18 C) acyl and (1-12 C) alkoxy groups;
- R.sub.4 is H, OH, a saturated or unsaturated hydrocarbon group containing 1-8 carbon atoms, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms having at least one substituent selected from the group consisting of hydroxyl, azido, nitrile, oxo, halogen (1-18 C) acyloxy, (2-8 C) alkoxyalkyl, (1-18 C) acyl and (1-12 C) alkoxy groups;
- or wherein R.sup.3 and R.sub.4 together form a ring system of 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 R.sub.3 or R.sub.4 is absent if said optional bond between said carbon atoms 16 and 17 is present.
4 more elements
Dependencies are inferred from the claim text.