| 摘要 |
The present invention relates, inter alia, to compounds having the general formula: in which: R<SUP>1 </SUP>is a member selected from the group consisting of -OCH<SUB>3</SUB>, -SCH<SUB>3</SUB>, -N(CH<SUB>3</SUB>)<SUB>2</SUB>, -NHCH<SUB>3</SUB>, -NC<SUB>4</SUB>H<SUB>8</SUB>, -NC<SUB>5</SUB>H<SUB>10</SUB>, -NC<SUB>4</SUB>H<SUB>8</SUB>O, -CHO, -CH(OH)CH<SUB>3</SUB>, -C(O)CH<SUB>3</SUB>, -O(CH<SUB>2</SUB>)<SUB>2</SUB>N(CH<SUB>3</SUB>)<SUB>2</SUB>, and -O(CH<SUB>2</SUB>)<SUB>2</SUB>NC<SUB>5</SUB>H<SUB>10</SUB>; R<SUP>2 </SUP>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)R<SUP>6</SUP>, wherein R<SUP>6 </SUP>is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., -CH<SUB>2</SUB>OCH<SUB>3</SUB>) and alkoxy (-OCH<SUB>3</SUB>); R<SUP>3 </SUP>is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R<SUP>4 </SUP>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-OR<SUP>5</SUP>, wherein R<SUP>5 </SUP>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 meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.
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