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    21.
    发明专利
    未知

    公开(公告)号：AT427998T

    公开(公告)日：2009-04-15

    申请号：AT07712041

    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.

    23.
    发明专利
    未知

    公开(公告)号：DE602004016373D1

    公开(公告)日：2008-10-16

    申请号：DE602004016373

    申请日：2004-11-11

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  THOLE HEINRICH-HUBERT ,  HUSEN BETTINA ,  VAN STEEN BARTHOLOMEUS JOHANNES ,  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.

    24.
    发明专利
    未知

    公开(公告)号：AT407139T

    公开(公告)日：2008-09-15

    申请号：AT04804529

    申请日：2004-11-11

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  THOLE HEINRICH-HUBERT ,  HUSEN BETTINA ,  VAN STEEN BARTHOLOMEUS JOHANNES ,  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.

    17BETA-HSD1 E INHIBIDORES STS.
    25.
    发明专利
    17BETA-HSD1 E INHIBIDORES STS. 未知

    公开(公告)号：MX2007014736A

    公开(公告)日：2008-02-15

    申请号：MX2007014736

    申请日：2006-05-24

    Applicant: SOLVAY PHARM GMBH

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

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

    Abstract: La presente invencion se refiere a nuevos derivados de esteroides sustituidos que representan inhibidores selectivos de la enzima 17??-hidroxiesteroide deshidrogenasa tipo I (17??-HSD1) y, ademas, que pueden representar inhibidores del esteroide sulfatasa, asi como a sus sales, a preparaciones farmaceuticas que contienen a estos compuestos y a procedimientos para la preparacion de estos compuestos. Ademas de ello, la invencion concierne al uso terapeutico de dichos nuevos derivados de esteroides sustituidos, en particular a su uso en el tratamiento o la prevencion de enfermedades o trastornos dependientes de hormonas esteroides, tales como enfermedades o trastornos dependientes de la hormona esteroide que requieren la inhibicion de las enzimas 17??-hidroxiesteroide deshidrogenasa tipo I y/o sulfatasa esteroide y/o que requieren la reduccion de la concentracion de 17??-estradiol endogena.

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