发明名称 21-substituted progesterone derivatives as new antiprogestational agents
摘要 A compound 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>, -CHO, -COCH<SUB>3 </SUB>and -CHOHCH<SUB>3</SUB>; R<SUP>2 </SUP>is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; 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 uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.
申请公布号 US7087591(B2) 申请公布日期 2006.08.08
申请号 US20050065632 申请日期 2005.02.23
申请人 THE UNITED STATES OF AMERICA AS REPRESENTED BY THE DEPARTMENT OF HEALTH AND HUMAN SERVICES 发明人 KIM HYUN K.;BLYE RICHARD P.;RAO PEMMARAJU N.;CESSAC JAMES W.;ACOSTA CARMIE K.
分类号 A61K31/56;A61K31/57;A61K31/00;A61P5/24;C07J5/00;C07J7/00;C07J9/00;C07J21/00;C07J41/00;C07J51/00;C07J71/00 主分类号 A61K31/56
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