Progesterone receptor antagonists

摘要

The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.

主权项

1. A compound of formula I in which R1 stands either for a residue Y or for a phenyl ring substituted with Y, Y stands for a group R2 and R3 are identical or different and stand for hydrogen,
an optionally —N(CH3)2, or —NHC(O)CH3 substituted C1-C6-alkyl residue,a residuea 6-10-membered aryl residue optionally substituted one, two or more times with halogen, —OH, —Oalkyl, —C(O)OH, —C(O)O-alkyl, —C(O)NH2, —C(O)NH-alkyl, —C(O)N-dialkyl, —C(O)NH-aryl, —C(O)NH-heteroaryl, —NH2, —NH(C1-C6-alkyl), —N(C1-C6-alkyl)2, —NHC(O)alkyl, —NO2, —N3, —CN, —C1-C6-alkyl, —C1-C6-perfluoro-alkyl, —C1-C6-acyl, —C1-C6-acyloxy, —SO2NH2, —SO2NH-alkyl or —SO2N-dialkyl,a 5-10-membered heteroaryl residue optionally substituted one, two or more times with the aforementioned substituents of the 6-10-membered aryl residue,a C1-C6-aralkyl residue optionally substituted on the aryl ring one, two or more times with the aforementioned substituents of the 6-10-membered aryl residue ora C1-C6-heteroarylalkyl residue optionally substituted on the heteroaryl ring one, two or more times with the aforementioned substituents of the 6-10-membered aryl residue or else, R2 and R3 are together a constituent of a 3-10-membered ring optionally substituted with alkyl-, carboxyl-, alkoxycarbonyl-, alkylcarbonyl-, aminocarbonyl-, aryl-, aralkyl-, heteroaryl-, heteroarylalkyl-, aminoalkyl- or dimethylaminoalkyl-substituted on the carbon or alkyl-, alkanoyl-, carboxyl-, alkoxycarbonyl-, aryl-, pyridinyl-, pyrimidinyl-, pyrazinyl-, sulphonyl-, benzoyl-, alkylsulphonyl-, arylsulphonyl-, aminocarbonyl-, dimethylaminocarbonyl-, aminocarbonylalkyl-, alkylaminocarbonylalkyl-, aralkyl-, heterocyclylalkyl-heteroarylalkyl-, aminoalkyl- or substituted on the nitrogen, which optionally contains nitrogen, oxygen or sulphur atoms, which is optionally oxidized to the sulphoxide or sulphone, wherein optionally an aromatic is condensed onto the 3-10-membered ring, X denotes an oxygen atom, NOR4 or NNHSO2R4 and R4 is selected from the group comprising hydrogen, C1-C6-alkyl and aryl or a salt thereof.