17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives (I) are new. 17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) and their stereoisomers, salts, solvate or solvate of the salts, including all crystal modifications, are new. R 1> : Y 1>or a phenyl ring substituted by 1 or 2 Y 1> Y 1> : SR 2>, S(O)R 3>, S(O) 2R 3>, S(O)(NH)R 3>, S(O)(NR 4>)R 3>or S(O) 2NR 9>R 10> R 2> : H, 1-6C-alkyl, 7-10C-aralkyl or aryl R 3> : 1-6C-alkyl or aryl R 4> : S(O) 2R 6> R 6> : phenyl or 4-methylphenyl X : O, NOR 7>or NNHSO 2R 7> either R 9>, R 10> : H, 1-10C-alkyl or aryl or R 9>R 10>N : an optionally saturated 3-8-membered heterocyclic ring and R 7> : H, 1-10C-alkyl or aryl. An independent claim is included for a medicament comprising (I) in combination with a further active agent and an auxiliary material. [Image] ACTIVITY : Gynecological Cytostatic Contraceptive. MECHANISM OF ACTION : Progesterone receptor antagonist. The progesterone receptor A antagonistic activity of (I) was tested using stable transfectant human neuroblastoma cells. The results showed that 4-[(11beta , 17beta )-17-hydroxy-3-oxo-17-(pentafluoroethyl)estra-4,9-dien-11-yl]-N,N-dimethylbiphenyl-4-sulfonamide exhibited an IC 5 0value of 0.01 nmole/l.本発明は、プロゲステロン拮抗作用を持つ一般式(I)の17-ヒドロキシ-17-ペンタフルオロエチル-エストラ-4,9(10)-ジエン-11-アリール誘導体と、その製造方法と、その誘導体を利用した諸疾患の治療および/または予防と、その誘導体を利用した諸疾患(特に子宮類線維腫(筋腫、子宮平滑筋腫)、子宮内膜症、重い月経出血、髄膜腫、ホルモン依存性乳がん、更年期に伴う愁訴)の治療用および/または予防用の医薬製品、または出生抑制用と緊急避妊用の医薬製品の製造とに関する。
