STRUCTURAL MODIFICATION OF 19-NORPROGESTERONE I: 17-.ALPHA.-SUBSTITUTED, 11-.BETA.-SUBSTITUTED-4-ARYL AND 21-SUBSTITUTED 19-NORPREGNADIENEDIONE AS NEW ANTIPROGESTATIONAL AGENTS

摘要

The present invention relates, inter alia, to compounds having the general formula (I) in which: R1 is a member selected from the group consisting of -OCH3 -SCH3, -N(CH3)2, -NHCH3, -NC4H8, -NC5H10, -NC4H3O, -CHO, -CH(OH)CH3, -C(O)CH3, -O(CH2)2N(CH3)2, and -O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, -SCN, S-acyl and -OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g.. -CH2OCH3) and alkoxy (-OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of =0 and =N-OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.The compounds of Formula I antagonize progesterone.