D-homo-(16-en)-11.beta.-aryl-4-estrenes, process for...

C - Chemistry – Metallurgy – 07 – J

Patent

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C07J 63/00 (2006.01) A61K 31/56 (2006.01) C07J 1/00 (2006.01) C07J 21/00 (2006.01) H01S 3/032 (2006.01)

Patent

CA 2099017

ABSTRACT OF THE DISCLOSURE A new type of D-homo-(16-en)-11.beta.-aryl-4-estrenes having general formula (I), as well as their pharmacologically acceptable addition salts with acids are disclosed. In formula (I), X stands for an oxygen atom, the hydroxyimino grouping > N ~ OH or two hydrogen atoms; R1 stands for a hydrogen atom or a methyl group; R2 stands for a hydroxy group, a C1-C10-alkoxy or C1-C10-acyloxy group; R11 stands for a fluorine, chlorine or bromine atom, in which case R12 and R13 represent together an additional bond, or R11 stands for a straight or branched chain C1-C4alkyl residue or a hydrogen atom, in which case R12 and R13 each represent a hydrogen atom or together represent an additional bond; and R3 and R4 have the usual meaning for competitive progesterone antagonists given in the description. Also disclosed are a process for producing these new compounds, pharmaceutical compositions containing these compounds, their use for producing medicaments and new intermediate products required for carrying out the process. These new compounds have a strong affinity for the gestagen receptor and strong antigestagenous, antiglucocorticoidal, antimineralcorticoidal and antiandrogenous properties.

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