17B(BETA)-ALQUIL-17a(ALFA)-OXI-ESTRATRIENOS

17b(beta)-alquil-17a(alfa)-oxi-estratrienos de fórmula (I), procesos para prepararlos, el uso de los 17b(beta)-alquil-17a(alfa)-oxi-estratrienos para preparar fármacos y preparaciones farmacéuticas que comprenden estos compuestos. 17-beta -Alkyl-17-alpha -oxy-estratriene compounds (I) and their enan...

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Hauptverfasser: JENS HOFFMANN, DR GEORG KETTSCHAU, SILKE MUELLER, MICHAEL SANDER, HERMANN KUENZER, ROLF BOHLMANN, TIM WINTERMANTEL, DIETER LANG, KARSTEN DENNER, JAN HUEBNER, NIKOLAUS HEINRICH, DR.PHILIP LIENAU, MICHAEL GERISCH
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Sprache:spa
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Zusammenfassung:17b(beta)-alquil-17a(alfa)-oxi-estratrienos de fórmula (I), procesos para prepararlos, el uso de los 17b(beta)-alquil-17a(alfa)-oxi-estratrienos para preparar fármacos y preparaciones farmacéuticas que comprenden estos compuestos. 17-beta -Alkyl-17-alpha -oxy-estratriene compounds (I) and their enantiomers, diastereomers, salts, solvate or salt of the solvates, are new. 17-beta -Alkyl-17-alpha -oxy-estratriene compounds of formula (I) and their enantiomers, diastereomers, salts, solvate or salt of the solvates, are new. Hal : F or C, where Hal is bonded to the 11-beta position of the estratriene component; R 1>, R 2>, R 4> : H, F, Cl or Br; R 3>, R17a : H, 1-4C-alkyl or 1-4C-alkanoyl; R17b : 1-4C-alkyl, 2-4C-alkenyl or 2-4C-alkynyl optionally fluorinated, where R17a is bonded to 17-alpha position of the estratriene component, and R17b is bonded to the 17-beta position of the estratriene component; U 1> : 1-13C-alkylene, 2-13C-alkenylene, 2-13C-alkynylene or A-B 1>; A : benzylidene or phenylene (which is bonded to estratriene component over CH 2) or 1-3C-alkylene-phenylene residue bonded to estratriene component over alkyl group; B 1> : 1-13C-alkylene, 2-13C-alkenylene or 2-13C-alkynylene, where A and B 1>are bonded over O atom; V 1> : methylene or -C(O)-; X : a bond or (1-3C)-alkylene; either R 5> : H, 1-4C-alkyl, 2-4C-alkenyl or 2-4C-alkynyl; and R 6> : H, CH 2R 6>or C(O)R 7>; or R 5>R 6> : non-fluorinated or partially fluorinated 1-6C-alkyl, 2-6C-alkenyl or 2-6C-alkynyl (optionally substituted by OH); or R 5>R 6>X, R 5>R 6>N : 4-6 membered heterocycle ring, which optionally further contains a heteroatom or a carbonyl group; R 7> : H; Y 1> : 5-8C-alkylene; and E 1> : 1-4C-perfluoroalkyl or phenyl (both 1-5 times substituted by halo or CF 3). An independent claim is included for a leaving group containing 17-beta -alkyl-17-alpha -oxy-estratriene compound of formula (IX). LG : a sulfonate group or halo. [Image] [Image] ACTIVITY : Cytostatic; Antiinfertility; Endocrine-Gen.; Gynecological; Contraceptive. MECHANISM OF ACTION : None given.