New 11beta-halo-7alpha-substituted-estratriene derivatives are useful for treatment e.g. various cancers, anovulatolial infertility, male hair loss, osteoporosis, and contraceptives

11 beta -Halo-7 alpha -substituted-estratriene derivatives (I) are new. 11 beta -(Fluoro or chloro)-7 alpha -substituted-estratriene derivatives (I) are new: R3 = H, OH, phenoxy or a hydrocarbyl group with up to 8C optionally bonded via O; R7 = -A-B-Z-R20; A = a direct bond, CH-bonded benzylidene or...

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Hauptverfasser:	LESSL, MONIKA-BIOL. DR., 13467 BERLIN, DE, NISHINO, YUKISHIGE., 14089 BERLIN, DE, BOHLMANN, ROLF.., 14055 BERLIN, DE, KROLL, JORG.., 12157 BERLIN, DE, SAUER, GERHARD.., 13465 BERLIN, DE, ZORN, LUDWIG.., 13509 BERLIN, DE, HEINRICH, NIKOLAUS.., 12159 BERLIN, DE, HOFMEISTER, HELMUT.., 13465 BERLIN, DE, FRITZEMEIER, KARL-HEINRICH.., 13503 BERLIN, DE, PARCZYK, KARSTEN.-BIO., 12207 BERLIN, DE, SCHNEIDER, MARTIN, DR., 13469 BERLIN, DE, KUENZER, HERMANN.., 13347 BERLIN, DE, LICHTNER, ROSEMARIE-BIOL. DR., 10823 BERLIN, DE
Format:	Patent
Sprache:	eng ; ger
Schlagworte:	CHEMISTRY METALLURGY ORGANIC CHEMISTRY STEROIDS
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Beschreibung
Zusammenfassung:	11 beta -Halo-7 alpha -substituted-estratriene derivatives (I) are new. 11 beta -(Fluoro or chloro)-7 alpha -substituted-estratriene derivatives (I) are new: R3 = H, OH, phenoxy or a hydrocarbyl group with up to 8C optionally bonded via O; R7 = -A-B-Z-R20; A = a direct bond, CH-bonded benzylidene or phenyl; B = alkylene, alkenylene or alkynylene with 3-14C; Z = (i) -NR21-; and R20 = H, alkyl, alkenyl or alkynyl with up to 10C; or -D-CnF2n+1 (a), -L-CH=CF-CpF2p+1 (b), -D-O-(CH2)q-Ar (c) or -D-O-(CH2)rCnF2n+1 (d); or NR20R21 = an optionally substituted, saturated or unsaturated, 5-6 membered heterocycle optionally containing 1 or 2 additional N, O and/or S atoms; or Z = (ii) -SOx- and R20 = alkyl, alkenyl or alkynyl with up to 10C; or a group (a)-(d); or Z = (iii) -NR31- and R20 = alkyl, alkenyl or alkynyl with up to 14C optionally interrupted with 1-2 O, S, NH and/or N(1-3C alkyl) and/or optionally partly fluorinated; optionally mono- or disubstituted aryl, heteroaryl, 3-10C cycloalkyl, 4-15C cycloalkylalkyl, 7-20C aralkyl or heteroaryl-1-6C alkyl; or optionally substituted aminoalkyl; or R21 = 1-3C alkyl; D = alkylene, alkenylene or alkynylene with up to 8C; n = 1-8; L = alkylene, alkenylene or alkynylene with 2-7C; p = 2-7; q = 0-3; Ar = phenyl, 1- or 2-naphthyl or heteroaryl; r = 1-5; x = 0-2; R31 = -C(O)R33 or -(CH2)-R33; R33 = alkyl, alkenyl or alkynyl with up to 14C optionally interrupted with 1-2 O, S, NH and/or N(1-3C alkyl) and/or optionally partly fluorinated; optionally mono- or disubstituted aryl, heteroaryl, 3-10C cycloalkyl, 4-15C cycloalkylalkyl, 7-20C aralkyl or heteroaryl-1-6C alkyl; optionally substituted aminoalkyl; or biphenylene; R11 = F or Cl; R17 = H, OH or alkoxy with up to 8C bonded via O; Compounds in which R7 has any meaning for SK given in PCT/EP97/04517 are excluded.