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    NOVEL 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS
    3.
    发明申请
    NOVEL 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 审中-公开
    新型17β羟基脱氢酶脱氢酶I型抑制剂

    公开(公告)号：WO2005047303A3

    公开(公告)日：2005-08-25

    申请号：PCT/EP2004052925

    申请日：2004-11-11

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  THOLE HEINRICH-HUBERT ,  HUSEN BETTINA ,  VAN STEEN BARTHOLOMEUS JOHANNE ,  SCHNEIDER GYULA ,  HULSHOF JOHANNES BERNARDUS EVE ,  KOSKIMIES PASI ,  JOHANSSON NINA ,  ADAMSKI JERZY

    IPC: A61K31/565 ,  C07J1/00

    CPC classification number: C07J1/0059 ,  C07J1/00

    Abstract: The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17beta-hydroxysteroid dehydrogenase type I (17beta-HSD1), to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel 3, 15 substituted estrone derivatives, particularly their use in the treatment or prevention of steroid hor­mone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17beta-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17beta-estradiol concentration. In addition, the present invention relates to the general use of selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment and prevention of benign gynaecological disorders, in particular endometriosis.

    Abstract translation: 本发明涉及将17β-羟基类固醇脱氢酶I型（17β-HSD1）的抑制性化合物与其盐形成含有这些化合物的药物制剂的新型3,15取代的雌酮衍生物以及这些化合物的制备方法。 此外，本发明涉及所述新型3,15取代的雌酮衍生物的治疗用途，特别是其用于治疗或预防类固醇激素依赖性疾病或病症（例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症） I型酶和/或需要降低内源性17β-雌二醇浓度。 此外，本发明涉及选择性17β-羟类固醇脱氢酶1型抑制剂的一般用途，其具有对雌激素受体没有或仅有纯的拮抗性结合亲和力，用于治疗和预防良性妇科疾病，特别是子宫内膜异位症。

    17beta-HSD1 and STS inhibitors
    4.
    发明专利
    17beta-HSD1 and STS inhibitors 未知

    公开(公告)号：AU2006251154B2

    公开(公告)日：2012-06-28

    申请号：AU2006251154

    申请日：2006-05-24

    Applicant: SOLVAY PHARM GMBH

    Inventor： PIRKKALA LILA ,  MESSINGER JOSEF ,  HUSEN BETTINA ,  THOLE HEINRICH-HUBERT ,  WESKE MICHAEL ,  KOSKIMIES PASI

    IPC: C07J41/00 ,  A61K31/565 ,  A61K31/58 ,  A61P5/32 ,  C07J43/00 ,  C07J71/00

    Abstract: The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17&bgr;-hydroxysteroid dehydrogenase type I (17&bgr;-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&bgr;-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17&bgr;-estradiol concentration.

    5.
    发明专利
    未知

    公开(公告)号：DE602007000858D1

    公开(公告)日：2009-05-20

    申请号：DE602007000858

    申请日：2007-01-16

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  THOLE HEINRICH-HUBERT ,  RASCHE HEINZ-HELMER ,  SCHMIDT MICHAEL ,  HAKALA JUHA

    IPC: C12P33/08 ,  C07J7/00

    Abstract: The invention relates to the use of bacterial strains of the species Amycolatopsis mediterranei for the microbial transformation of 9ß,10a-steroids of general Formula (I) to their corresponding 11ß-hydroxyl analogues, as well as to specific strains of that species. In addition, the present invention relates to the process of transforming 9ß,10a-steroids to their corresponding 11ß-hydroxyl derivatives using bacterials strains of the species Amycolatopsis mediterranei, and to the subsequent isolation of the 11ß-hydroxyl derivatives from the bacterial culture medium. The resultant 11ß-hydroxylated products are useful intermediates for the preparation of novel steroidal compounds with 9ß,10a-confirmation carrying different kind of substituents in the 11ß-position.

    NOVEL 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS
    6.
    发明专利
    NOVEL 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 未知

    公开(公告)号：HRP20080603T3

    公开(公告)日：2009-03-31

    申请号：HRP20080603

    申请日：2008-11-21

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  THOLE HEINRICH-HUBERT ,  HUSEN BETTINA ,  STEEN BARTHOLOMEUS JOHANNES VAN ,  SCHNEIDER GYULA ,  HULSHOF JOHANNES BERNARDUS EVERARDUS ,  KOSKIMIES PASI ,  JOHANSSON NINA ,  ADAMSKI JERZY

    IPC: C07J1/00 ,  A61K31/565

    Abstract: The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17beta-hydroxysteroid dehydrogenase type I (17beta-HSD1), to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel 3, 15 substituted estrone derivatives, particularly their use in the treatment or prevention of steroid hor­mone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17beta-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17beta-estradiol concentration. In addition, the present invention relates to the general use of selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment and prevention of benign gynaecological disorders, in particular endometriosis.

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