发明申请
WO2006003013A3 NOVEL 2-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-ONES USED IN THE FORM OF INHIBITORS OF 17ß-HYDROXYSTEROIDDEHYDROGENASE OF TYPE 1
审中-公开
基本信息:
- 专利标题： NOVEL 2-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-ONES USED IN THE FORM OF INHIBITORS OF 17ß-HYDROXYSTEROIDDEHYDROGENASE OF TYPE 1
- 专利标题（中）：NEW 2-取代的雌-1,3,5（10） - 三烯-17-酮作为17-β-羟类固醇脱氢酶类型1抑制剂
- 申请号：PCT/EP2005007315 申请日：2005-07-04
- 公开(公告)号：WO2006003013A3 公开(公告)日：2006-06-22
- 发明人： HILLISCH ALEXANDER , REGENHARDT WILKO , GEGE CHRISTIAN , PETERS OLAF , BOTHE ULRICH , ADAMSKI JERZY , MOELLER GABRIELE , ROSINUS ANDREA , ELGER WALTER , SCHNEIDER BIRGITT
- 申请人： SCHERING AG , HILLISCH ALEXANDER , REGENHARDT WILKO , GEGE CHRISTIAN , PETERS OLAF , BOTHE ULRICH , ADAMSKI JERZY , MOELLER GABRIELE , ROSINUS ANDREA , ELGER WALTER , SCHNEIDER BIRGITT
- 专利权人： SCHERING AG,HILLISCH ALEXANDER,REGENHARDT WILKO,GEGE CHRISTIAN,PETERS OLAF,BOTHE ULRICH,ADAMSKI JERZY,MOELLER GABRIELE,ROSINUS ANDREA,ELGER WALTER,SCHNEIDER BIRGITT
- 当前专利权人： SCHERING AG,HILLISCH ALEXANDER,REGENHARDT WILKO,GEGE CHRISTIAN,PETERS OLAF,BOTHE ULRICH,ADAMSKI JERZY,MOELLER GABRIELE,ROSINUS ANDREA,ELGER WALTER,SCHNEIDER BIRGITT
- 优先权： DE102004032674 2004-07-02
- 主分类号： C07J1/00
- IPC分类号： C07J1/00 ; A61K31/566 ; A61P5/32 ; C07J31/00 ; C07J41/00 ; C07J53/00
摘要：
The invention relates to novel 2-substituted estra-1,3,5(10)-trien-17-ones of formula (I), wherein R 2 is an C 1 -C 8 alkyl saturated or unsaturated group, an C 1 -C 5 -alkyloxy group, an aralkyl- or alkylaryl rest, an -O-C n F m H o rest, wherein n=1,2,3,4,5 or 6, m=1 and m = 2n+1, or a CH 2 XY 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, R 13 is a hydrogen atom or a methyl group, R 16 is a hydrogen or fluorine atom, Z is an oxygen or sulfur atom, each R 4 and R 6 independently of each other represents a or ß hydrogen atom, an C 1 -C 5 alkyl, C 1 -C 5 -alkyloxy, C 1 -C 5 -acyl or hydroxy group or an aralkyl- or alkylaryl rest, R 3 and R 4 represent together an oxygen atom, R 5 and R 6 represent together an oxygen atom, each R 7 and R 8 represents a hydrogen atom or together an oxygen atom, each R 7 and R 8 represents a hydrogen atom or together a CH 2 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.
摘要（中）：
本发明涉及新的2-取代的雌-1,3,5（10） - 三烯-17-酮的通式（I），其中R 2 是饱和或不饱和的C 1 < / SUB> -C 8 烷基，一个C 1 -C 5 烷氧基，芳烷基或烷芳基，基团-O-C < SUB>名词˚F米ħ 0 ，其中n = 1,2,3,4,5或6中，m = 1且m = 2n + 1个 ，或基团CH 2 XY，其中X表示氧原子，Y是碳原子数为1〜4的烷基，卤素原子或腈基，R 13 氢原子或甲基，R 16 代表氢原子或氟原子，Z是氧或硫原子，R 3 和R 5 各自独立地为 表示α-或β-位置氢原子，R 4 和R 6 各自独立地为α-或β-位置氢原子，C 1 -C 5 烷基，一个C 1 -C 5 - 烷氧基，C 1 -C 5 酰基，或羟基或芳烷基或烷芳基，R 3 和R 4 一起为氧原子，R 5 和R 6 一起为氧原子，R 7 和R 8 各自为氢原子或一起CH 2 是一个基团，及其药学上可接受的盐，它们的制备和作为药物的雌激素依赖性疾病的预防和治疗为特征的抑制17-Hydroxysteroiddehydro-的使用 首先影响脱氢酶类型