New 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl-derivatives are progesterone receptor antagonists useful to treat and prevent e.g. uterine fibroids, endometriosis, heavy menstrual bleeding and meningioma
Die Erfindung betrifft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate der Formel I mit Progesteron antagonisierender Wirkung und Verfahren zu ihrer Herstellung, ihre Verwendung zur Behandlung und/oder Prophylaxe von Krankheiten sowie ihre Verwendung zur Herstellung von Arzneimitteln zur Behandlung und/oder Prophylaxe von Krankheiten, insbesondere von Uterusfibroiden (Myomen, uterine Leiomyome), der Endometriose, von schweren Menstruationsblutungen, Meningiomen, hormonabhängigen Mammakarzinomen und von mit der Menopause assoziierten Beschwerden oder zur Fertilitätskontrolle und Notfallkontrazeption.17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl-derivatives (I) and their salts, solvates, solvate of the salts or subsequently all crystal modifications are new. 17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl-derivatives of formula (I) and their salts, solvates, solvate of the salts or subsequently all crystal modifications are new. Either R 1>；, R 2>；6-10 membered aryl, 5-10-membered heteroaryl, 1-6C-arylalkyl or 1-6C-heteroarylalkyl (all optionally mono-, di-or poly-substituted by halo (F, Cl, Br, I), -OH, -O-alkyl, -C(O)OH, -C(O)Oalkyl, -C(O)NH 2, -C(O)NHalkyl, -C(O)Ndialkyl, -C(O)NHaryl, -C(O)NHheteroaryl, -NH 2, -NH(1-10C-alkyl), -N(1-10C-alkyl) 2(preferably -N(CH 3) 2), -NHC(O)alkyl, -NO 2, -N 3, -CN, -1-10C-alkyl, 1-10C-perfluoro-alkyl, -1-10C-acyl, 1-10C-acyloxy, -SO 2NH 2or -SO 2NHalkyl of -SO 2Ndialkyl), H or optionally dimethylamine-substituted 1-10C-alkyl； or R 1>；R 2>；3-10 membered ring (optionally substituted on carbon by alkyl, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, arylalkyl, heteroarylalkyl or aminoalkyl, or optionally substituted on N by alkyl, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, phenylalkyl, pyridinyl, pyrimidinyl, pyrazinyl, sulfonyl, benzoyl, alkylsulfonyl, arylsulfonyl, aminocarbonyl, aminocarbonylalkyl, arylalkyl, heterocycloalkyl, heteroarylalkyl or aminoalkyl, where the r
