17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-diene-11-methylene oxyalkylene aryl derivatives, process for preparation thereof, and use thereof for treatment of diseases

摘要

The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene-11-methyleneoxyalkylenearyl derivative of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.

主权项

1. Compound of the formula I in which the phenyl substituent bearing the R1 and R2 radicals is joined to the phenyl ring in the m or p position, n is 0 or 1, R1 is hydrogen, C1-C10-alkyl, CH2OR4, CO2R5, CN, aryl or heteroaryl, R2 is hydrogen or C1-C10-alkyl, R3 is hydrogen, C1-C10-alkyl, aryl or C7-C20-aralkyl, R4 is hydrogen, —CH2-CH2—OH or CH2CO2R5, R5 is hydrogen or C1-C10-alkyl, X is oxygen, an NOR3 or ═NNHSO2R3 group, and the stereoisomers, or the salts thereof, and the α-, (β- or γ-cyclodextrin clathrates thereof.