| 摘要 |
The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonizing effect and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and also their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular of uterus fibroids (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeding, meningiomas, hormone-dependent breast cancers and troubles associated with the menopause or for monitoring fertility and emergency contraception. |
| 主权项 |
1. A compound that is a 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivative of the general formula I in which R1 and R2 are identical or different and arehydrogen,an optionally dimethylamine-substituted C1-C10-alkyl radical,a 6-10-membered aryl radical optionally mono-, di- or polysubstituted with halogen, —OH, —O-alkyl, —C(O)OH, —C(O)Oalkyl, —C(O)NH2, —C(O)NHalkyl, —C(O)Ndialkyl, —C(O)NHaryl, —C(O)NHheteroaryl, —NH2, —NH(C1-C10-alkyl), —N(C1-C10-alkyl)2, —NHC(O)alkyl, —NO2, —N3, —CN, —C1-C10-alkyl, —C1-C10-perfluoro alkyl, —C1-C10-acyl, —C1-C10-acyloxy, —SO2NH2, —SO2NHalkylor —SO2Ndialkyl,a 5-10-membered heteroaryl radical optionally mono-, di- or polysubstituted with the aforementioned substituents of the 6-10-membered aryl radical,a C1-C6-arylalkyl radical optionally mono-, di- or polysubstituted on the aryl ring with the aforementioned substituents of the 6-10-membered aryl radical ora C1-C6-heteroarylalkyl radical optionally mono-, di- or polysubstituted on the heteroaryl ring with the aforementioned substituents of the 6-10-membered aryl radical, or else R1 and R2 are together a constituent of a 3-10-membered ring which is optionally substituted on the carbon by alkyl, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, arylalkyl, heteroarylalkyl, aminoalkyl and/or on the nitrogen by alkyl, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, phenylalkyl, pyridinyl, pyrimidinyl, pyrazinyl, sulphonyl, benzoyl, alkylsulphonyl, arylsulphonyl, aminocarbonyl, aminocarbonylalkyl, arylalkyl, heteroarylalkyl, heterocyclylalkyl and aminoalkyl, and which optionally contains nitrogen, oxygen or sulphur atoms which is optionally oxidized with the sulphoxide or sulphone, where an aromatic is optionally fused onto the 3-10-membered ring, X is an oxygen atom or NOR3 or NNHSO2R3, R3 is hydrogen, C1-C10-alkyl, or aryl, or a salt thereof. |
