Title:
NOVEL 2-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-ONES USED IN THE FORM OF INHIBITORS OF 17ß-HYDROXYSTEROIDDEHYDROGENASE OF TYPE 1
Document Type and Number:
WIPO Patent Application WO2006003013
Kind Code:
B1
Abstract:
The invention relates to novel 2-substituted estra-1,3,5(10)-trien-17-ones of formula (I), wherein R2 is an C1-C8 alkyl saturated or unsaturated group, an C1-C5-alkyloxy group, an aralkyl- or alkylaryl rest, an -O-CnFmHo rest, wherein n=1,2,3,4,5 or 6, m=1 and m = 2n+1, or a CH2XY group in which X is an oxygen atom and Y is an alkyl rest containing 1 to 4 carbon atoms, a halogen atom and a nitrile group, R13 is a hydrogen atomor a methyl group, R16 is a hydrogen or fluorine atom, Z is an oxygen or sulfur atom, each R4 and R6 independently of each other represents a or ß hydrogen atom, an C1-C5 alkyl, C1-C5-alkyloxy, C1-C5-acyl or hydroxy group or an aralkyl- or alkylaryl rest, R3 and R4 represent together an oxygen atom, R5 and R6 represent together an oxygen atom, each R7 and R8 represents a hydrogen atom or together an oxygen atom, each R7 and R8 represents a hydrogen atom or together a CH2 group. Pharmaceutically acceptable salts of said compounds, the production and use thereof in the form of drags which are usable for preventing and treating estrogen-dependent diseases and are influenced by inhibiting 17ß-hydroxysteroiddehydrogenase of type 1 are also disclosed.
Inventors:
HILLISCH ALEXANDER (DE)
REGENHARDT WILKO (DE)
GEGE CHRISTIAN (DE)
PETERS OLAF (DE)
BOTHE ULRICH (DE)
ADAMSKI JERZY (DE)
MOELLER GABRIELE (DE)
ROSINUS ANDREA (DE)
ELGER WALTER (DE)
SCHNEIDER BIRGITT (DE)
REGENHARDT WILKO (DE)
GEGE CHRISTIAN (DE)
PETERS OLAF (DE)
BOTHE ULRICH (DE)
ADAMSKI JERZY (DE)
MOELLER GABRIELE (DE)
ROSINUS ANDREA (DE)
ELGER WALTER (DE)
SCHNEIDER BIRGITT (DE)
Application Number:
PCT/EP2005/007315
Publication Date:
August 31, 2006
Filing Date:
July 04, 2005
Export Citation:
Assignee:
SCHERING AG (DE)
HILLISCH ALEXANDER (DE)
REGENHARDT WILKO (DE)
GEGE CHRISTIAN (DE)
PETERS OLAF (DE)
BOTHE ULRICH (DE)
ADAMSKI JERZY (DE)
MOELLER GABRIELE (DE)
ROSINUS ANDREA (DE)
ELGER WALTER (DE)
SCHNEIDER BIRGITT (DE)
HILLISCH ALEXANDER (DE)
REGENHARDT WILKO (DE)
GEGE CHRISTIAN (DE)
PETERS OLAF (DE)
BOTHE ULRICH (DE)
ADAMSKI JERZY (DE)
MOELLER GABRIELE (DE)
ROSINUS ANDREA (DE)
ELGER WALTER (DE)
SCHNEIDER BIRGITT (DE)
International Classes:
C07J1/00; A61K31/566; A61P5/32; C07J31/00; C07J41/00; C07J53/00
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