Patent Number: 7,087,591

Title: 21-substituted progesterone derivatives as new antiprogestational agents

Abstract: A compound having the general formula: ##STR00001## in which: R.sup.1 is a member selected from the group consisting of --OCH.sub.3, --SCH.sub.3, --N(CH.sub.3).sub.2, --NHCH.sub.3, --CHO, --COCH.sub.3 and --CHOHCH.sub.3; R.sup.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.sup.3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R.sup.4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of .dbd.O and .dbd.N--OR.sup.5, wherein R.sup.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.

Inventors: Kim; Hyun K. (Bethesda, MD), Blye; Richard P. (Highland, MD), Rao; Pemmaraju N. (San Antonio, TX), Cessac; James W. (San Antonio, TX), Acosta; Carmie K. (San Antonio, TX)

Assignee: The United States of America as represented by the Department of Health and Human Services

International Classification: A61K 31/56 (20060101); C07J 5/00 (20060101)

Expiration Date: 8/08/02018