21-SUBSTITUTED PROGESTERONE DERIVATIVES AS NEW ANTIPROGESTATIONAL AGENTS

摘要

A compound having general formula (I) in which R<1> is a member selected from the group consisting of -OCH3, -SCH3, -N(CH3)2, -NHCH3, -CHO, -COCH3 and -CHOHCH3; R<2> is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R<3> is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R<4> 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 R<5> 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.