DERIVADOS DE 17-HIDROXI-17-PENTAFLUOROETIL-ESTRA-4-9(10)-DIEN-11-ARILO COMO ANTAGONISTAS DE PROGESTERONA Y PROCEDIMIENTOS PARA SU PREPARACION

La presente invencion se refiere a derivados de 17-hidroxi-17-pentafluoroetil-estra-4,9(10)-dien-11-arilo de formula (I), sus estereoisomeros, sales, solvatos, solvatos de las sales, en donde: R1 es un radical Y o un anillo fenilo mono- o disustituido con Y; Y es SR2, S(O)R3, entre otros; R2 es H, a...

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Hauptverfasser:	SCHWEDE, Wolfgang, MOLLER, Carsten, BONE, Wilhelm, ROTGERI, Andrea, KLAR, Ulrich
Format:	Patent
Sprache:	spa
Schlagworte:	CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS STEROIDS
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Zusammenfassung:	La presente invencion se refiere a derivados de 17-hidroxi-17-pentafluoroetil-estra-4,9(10)-dien-11-arilo de formula (I), sus estereoisomeros, sales, solvatos, solvatos de las sales, en donde: R1 es un radical Y o un anillo fenilo mono- o disustituido con Y; Y es SR2, S(O)R3, entre otros; R2 es H, alquilo C1-C6, entre otros; R3 es alquilo C1-C6 o arilo; X es O, NRO7 o NNHSO2R7; R7 es H, alquilo C1-C10 o arilo. Son compuestos preferidos: (11?, 17?)-17-hidroxi-11-[4-(metilsulfanil)fenil]-17-(pentafluoroetil)estra-4,9-dien-3-ona; (11?, 17?)-11-[4-(etilsulfanil)fenil]-17-hidroxi-17-(pentafluoroetil)estra-4,9-dien-3-ona; entre otros. Estos compuestos tienen accion antagonista de progesterona siendo utiles en el tratamiento o prevencion de fibroides uterinos, endometriosis, entre otros 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.