[EN] CYCLIC REGIMENS USING CYCLIC UREA AND CYCLIC AMIDE DERIVATIVES<br/>[FR] SCHEMAS POSOLOGIQUES CYCLIQUES COMPRENANT DE L'UREE CYCLIQUE ET DES DERIVES CYCLIQUES D'AMIDE
申请人:AMERICAN HOME PROD
公开号:WO2000066103A2
公开(公告)日:2000-11-09
This invention concerns cyclic combination therapies using indoline derivatives which are progesterone receptor antagonists of general structure (I) wherein: A, B and D are N or CH, though not all can be CH; R?1 and R2¿ are H, COR?A, NRBCORA¿, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R?1 and R2¿ form a spirocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, alkyl alkyl; R3 is H, OH, NH¿2?, alkyl, alkenyl, or COR?C; RC¿ is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is benzene or a 5 or 6 memebered heteroaromatic ring; RF is H, alkyl, aryl, alkoxy, or aminoalkyl; RG is H or alkyl; R5 is H or alkyl; W is O or a chemical bond; or a pharmaceutically acceptable salt thereof. These methods may be used for contraception or treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.