21-Substituted progesterone derivatives as novel anti-progesterone

摘要

A compound having the general formula: in which: RSUP1 /SUPis a member selected from the group consisting of -OCHSUB3/SUB, -SCHSUB3/SUB, -N(CHSUB3/SUB)SUB2/SUB, -NHCHSUB3/SUB, -CHO, -COCHSUB3 /SUBand -CHOHCHSUB3/SUB; RSUP2 /SUPis a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; RSUP3 /SUPis a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; RSUP4 /SUPis 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-ORSUP5/SUP, wherein RSUP5 /SUPis 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.