Novel 21-substituted progesterone derivatives as antiprogestational agents medicoments containing the same, use thereof

• Main Authors: RAO PEMMARAJU N, KIM HYUN K, ACOSTA CARMIE K, CESSAC JAMES W, BLYE RICHARD P
• Format: Patent
• Language: English; Hungarian
• Published: 29.08.2016
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; STEROIDS

A compound having the general formula: in which: R1 is a member selected from the group consisting of -OCH3, -SCH3, -N(CH3)2, -NHCH3, -CHO, -COCH3 and -CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 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 R5 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.