6,7-MODIFIED 11BETA-ARYL-4-OESTRENEDERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING

摘要

Compounds having antigestagenic activity of the formula R4R1R2 R3XGMQ in which X represents an oxygen atom or the hydroxyimino grouping LN-OH, R1 represents a hydrogen atom or a methyl group, R2 represents a hydroxy group, a C1-C10- alkoxy group or a C1-C10-acyloxy group, R3 represents a hydrogen atom; the grouping - (CH2)nCH2Z wherein n is 0, 1, 2, 3, 4 or 5 and Z represents a hydrogen atom, a cyano group or the radical -OR5 in which R5 = H, C1-C10-alkyl or C1-C10-acyl; the grouping - (CH2)mC:C-Y wherein m is 0, 1 or 2 and Y represents a hydrogen, C1-C4 - alkyl, fluorine, chlorine, bromine or iodine atom, or a C1-C10-hydroxyalkyl, C1-C10- alkoxyalkyl or C1-C10-acyloxyalkyl radical; or the grouping -(CH2)p-CH=CH- (CH2)kCH2R6 wherein p is 0 or 1 and k is 0, 1 or 2 and R6 represents a hydrogen atom, a hydroxy group, a C1-C4-alkoxy radical or a C1-C4-acyloxy radical, or alternatively R2 and R3 together represent a radical of the formula x(H2c) O17 x(H2c) O17 or OO17 (CH2)x wherein x = 1 or 2, R4 represents a hydrogen atom; a cyano group; a chlorine, fluorine, bromine or iodine atom; a trialkylsilyl group; a trialkylstannyl group; a straight-chain or branched, saturated or unsaturated, C1-C8-alkyl, -acyl or-alkoxy-alkyl radical; an amino group - N R7R8 in which R7 and R8, each independently of the other, represents a hydrogen atom or a C1-C4-alkyl group; a corresponding amine oxide - N+R7OR8; or the grouping -OR9 or -S(O)iR9 in which i = 0, 1 or 2 and R9 represents a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or 2-dimethyl- aminoethyl group; or R4 represents a heteroaryl radical of the formula ABDER10 (Ia) in which A represents a nitrogen, oxygen or sulphur atom, -B-D-E- represents the sequence of elements -C-C-C-, -N-C-C- or -C-N-C and R10 represents a hydrogen atom; a cyano group; a chlorine, fluorine, bromine or iodine atom; a trialkylsilyl group; a trialkylstannyl group; a straight- chain or branched, saturated or unsaturated C1-C8-alkyl, -acyl or alkoxyalkyl radical; an amino group - NR7R8 in which R7 and R8, each independently of the other, represents a hydrogen atom or a C1-C4-alkyl group; a corresponding amine oxide - N+O-R7R8 ; or the grouping -OR9 or -S(O)iR9 in which i = 0, 1 or 2 and R9 represents a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or 2-dimethyl- aminoethyl group; or R4 represents a heteroaryl radical of the formula R10EDAB in which A represents a nitrogen atom and -B-D-E- represents the sequence of elements -C-C-C-, -N-C-C-, -C-N-C- or -C-C-N- and R10 has the meaning already given, or R4 represents a phenyl radical of the formula R10 in which R10 has the meaning already given, and G represents a hydrogen atom, a halogen atom or a C1-C4-alkyl radical, when M and Q are hydrogen atoms or together are an additional bond, Q represents a C1-C4 alkyl radical when M and G are hydrogen atoms, or G and M together represent a methylene or ethylidene group when Q is a hydrogen atom, with the proviso that G, M and Q are not all hydrogen atoms; and pharmacologically acceptable salts thereof.