New 11-arylsteroid compounds

C - Chemistry – Metallurgy – 07 – J

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167/193, 260/39,

C07J 41/00 (2006.01) A61K 31/565 (2006.01) C07J 43/00 (2006.01)

Patent

CA 1301162

Abstract The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: Image in which R1 is an aryl group with a -?-X group as substituent, X and Y each being separately H or a (1-4 C) hydro- carbyl group or together a (2-6 C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom; R2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group; R3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R2 and R3 to- gether form a ring system, with the proviso that if R3is hydroxyl, R2 is not hydrogen or hydroxyl; and R4 is a methyl or ethyl group; and the .alpha.- and .beta.-bonds are indicated by dashed (---) and wedged (?) lines respectively.

585297

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