21-SUBSTITUTED PROGESTERONE DERIVATIVES AS NEW ANTIPROGESTATIONAL AGENTS

A compound having the general formula: in which: R1 is a member selected from the group consisting of -OCH3, -SCH3, -N(CH3)2, -NHCH3, -CHO, -COCH3 and -CHOHCH3 R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl 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 -O and -N-OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone to induce menses to treat endometriosis to treat dysmenorrhea to treat endocrine hormone-dependent tumors to treat uterine fibroids to inhibit uterine endometrial proliferation to induce labor and for contraception.