摘要 |
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; R1 and R2 are H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R1 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, NH2, alkyl, alkenyl, or CORC; 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 o f the invention include stimulation of food intake.
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申请人 |
AMERICAN HOME PRODUCTS CORPORATION;LIGAND PHARMACEUTICALS, INC. |
发明人 |
GRUBB, GARY S.;ZHI, LIN;VIET, ANDREW Q.;JONES, TODD K.;TEREFENKO, EUGENE A.;TEGLEY, CHRISTOPHER M.;WROBEL, JAY E.;EDWARDS, JAMES P.;SANTILLI, ARTHUR A.;PUWEN, ZHANG;FENSOME, ANDREW |