PROGESTERONE RECEPTOR MODULATORS HAVING AN INCREASED ANTIGONADOTROPIC ACTIVITY FOR USE IN FEMALE FERTILITY TESTING AND HORMONE REPLACEMENT THERAPY

摘要

4-(17beta-Hydroxy-3-oxo-estra-4,9-dien-11beta-yl)-benzaldehyde-1-(E)-oximes (I) are new. 4-(17beta-Hydroxy-3-oxo-estra-4,9-dien-11beta-yl)-benzaldehyde-1-(E)-oxime derivatives of formula (I) are new. R1 = H, 1-10C alkanoyl, optionally substituted benzoyl of 6-10C or CONHR5; R5 = H, 1-10C alkyl, 1-10C acyl, 6-10C aralkyl or 6-10C alkaryl; R2 = H, halo or CF3; R3 = H or CH2X; X = H, OH, halo, Me, Et or -(CH2)nCH2Y, or CkFmHp; n = 0 or 1; Y = halo; k = 1-5; m = more than 1; m + p = k + 1; R4 = H, 1-10C alkyl, 1-10C alkanoyl, optionally substituted benzoyl having 6-10C or CONHR5; R15, R16 = H or together form a double bond; and provided that: (1) X can be a group of formula CkFmHp if R2 is halo; and (2) the compounds 4-(17alpha-chloromethyl-17beta-hydroxy-3-oxo-estra-4,9-dien-11beta-yl)-benzaldehyde-1-(E)-oxime and 4-(17alpha-chloromethyl-17beta-methoxy-3-oxo-estra-4,9-dien-11beta-yl)-benzaldehyde-1-(E)-oxime are excluded.