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公开(公告)号:CA2609726C
公开(公告)日:2013-10-01
申请号:CA2609726
申请日:2006-05-24
Applicant: SOLVAY PHARM GMBH
Inventor: MESSINGER JOSEF , THOLE HEINRICH-HUBERT , HUSEN BETTINA , KOSKIMIES PASI , KALLIO LILA , WESKE MICHAEL
Abstract: The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17.beta.-hydroxysteroid dehydrogenase type I (17.beta.-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.beta.-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17.beta.-estradiol concentration.
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公开(公告)号:AU2004289459B2
公开(公告)日:2010-08-19
申请号:AU2004289459
申请日:2004-11-11
Applicant: SOLVAY PHARM GMBH
Inventor: THOLE HEINRICH-HUBERT , KOSKIMIES PASI , SCHNEIDER GYULA , JOHANSSON NINA , HUSEN BETTINA , STEEN BARTHOLOMEUS JOHANNES VAN , ADAMSKI JERZY , HULSHOF JOHANNES BERNARDUS EVERARDUS , MESSINGER JOSEF
IPC: A61K31/565 , A61P5/30 , 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.
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公开(公告)号:AU2007327653A1
公开(公告)日:2008-06-05
申请号:AU2007327653
申请日:2007-11-27
Applicant: SOLVAY PHARM GMBH
Inventor: KOSKIMIES PASI , MESSINGER JOSEF , SCHOEN UWE , THOLE HEINRICH-HUBERT , HUSEN BETTINA , UNKILA MIKKO
IPC: C07J41/00 , A61K31/565 , A61K31/566 , A61K31/58 , A61P5/32 , C07J43/00 , C07J51/00
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公开(公告)号:CA2663242A1
公开(公告)日:2008-03-27
申请号:CA2663242
申请日:2007-09-17
Applicant: SOLVAY PHARM GMBH
Inventor: SCHOEN UWE , KOSKIMIES PASI , THOLE HEINRICH-HUBERT , MESSINGER JOSEF , HUSEN BETTINA , KALLIO LILA
Abstract: This invention relates to novel estratrien-triazoles of general formula ( I) useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone depend ent disease or disorder requiring the inhibition of a 17.beta.-hydroxysteroi d dehydrogenase (17.beta.-HSD) such as 17.beta.-HSD type 1, type 2 or type 3 enzyme.
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15.
公开(公告)号:AU2007299010A1
公开(公告)日:2008-03-27
申请号:AU2007299010
申请日:2007-09-17
Applicant: SOLVAY PHARM GMBH
Inventor: SCHOEN UWE , HUSEN BETTINA , MESSINGER JOSEF , KOSKIMIES PASI , KALLIO LILA , THOLE HEINRICH-HUBERT
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公开(公告)号:CA2624015A1
公开(公告)日:2007-04-12
申请号:CA2624015
申请日:2006-09-28
Applicant: SOLVAY PHARM GMBH
Inventor: HINAJE MARIA , KLINGER-DABRAL VIBHUTI , BOECKER CHRISTIANE , THOLE HEINRICH-HUBERT , MESSINGER JOSEF , HUSEN BETTINA , MARK CHRISTOPH , BUCHHOLZ MONIKA
Abstract: Described herein are new retrosteroidal compounds of general formula (I), representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. Said compounds are preferably used for the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for HRT.
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17.
公开(公告)号:AU2004325692A1
公开(公告)日:2006-06-22
申请号:AU2004325692
申请日:2004-12-13
Applicant: SOLVAY PHARM GMBH
Inventor: HIRVELA LEENA , KOSKIMIES PASI , MESSINGER JOSEF , LEHTOVUORI PEKKA , THOLE HEINRICH-HUBERT , SAARENKETO PAULI , HUSEN BETTINA , STEEN BARTHOLOMEUS JOHANNES VA , PIRKKALA LILA , KIVINIEMI JOHANNA , PENTIKAINEN OLLI TANELI , UNKILA MIKKO
IPC: C07D495/04 , A61K31/519
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公开(公告)号:AU2004289459A1
公开(公告)日:2005-05-26
申请号:AU2004289459
申请日:2004-11-11
Applicant: SOLVAY PHARM GMBH
Inventor: THOLE HEINRICH-HUBERT , KOSKIMIES PASI , SCHNEIDER GYULA , JOHANSSON NINA , HUSEN BETTINA , STEEN BARTHOLOMEUS JOHANNES VA , ADAMSKI JERZY , HULSHOF JOHANNES BERNARDUS EVE , MESSINGER JOSEF
IPC: A61K31/565 , 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.
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公开(公告)号:CA2545704C
公开(公告)日:2012-06-26
申请号:CA2545704
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 17.beta.-hydroxysteroid dehydrogenase type I (17.beta.-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 hor~mone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17.beta.-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17.beta.-estradiol concentration. In addition, the present invention relates to the general use of selective 17.beta.-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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20.
公开(公告)号:AU2004325692B2
公开(公告)日:2012-01-19
申请号:AU2004325692
申请日:2004-12-13
Applicant: SOLVAY PHARM GMBH
Inventor: HIRVELA LEENA , KOSKIMIES PASI , MESSINGER JOSEF , LEHTOVUORI PEKKA , THOLE HEINRICH-HUBERT , SAARENKETO PAULI , HUSEN BETTINA , VAN STEEN BARTHOLOMEUS JOHANNES , KALLIO LILA , KIVINIEMI JOHANNA , PENTIKAINEN OLLI TANELI , UNKILA MIKKO
IPC: C07D495/04 , A61K31/519
Abstract: This invention relates to novel substituted thiophenepyrimidinone derivatives and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorder, such as steroid hormone dependent diseases or disorders requiring inhibition of 17&bgr;-hydroxysteroid dehydrogenase enzymes.
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