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公开(公告)号：CA2545704A1
公开(公告)日：2005-05-26
申请号：CA2545704
申请日：2004-11-11
Applicant: SOLVAY PHARM GMBH
Inventor： SCHNEIDER GYULA , JOHANSSON NINA , KOSKIMIES PASI , HULSHOF JOHANNES BERNARDUS EVE , ADAMSKI JERZY , THOLE HEINRICH-HUBERT , VAN STEEN BARTHOLOMEUS JOHANNE , HUSEN BETTINA , MESSINGER JOSEF
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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32.发明专利
公开(公告)号：AU2007299010B2
公开(公告)日：2013-01-31
申请号：AU2007299010
申请日：2007-09-17
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , HUSEN BETTINA , KALLIO LILA , SCHOEN UWE , THOLE HEINRICH-HUBERT , KOSKIMIES PASI
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 dependent disease or disorder requiring the inhibition of a 17&bgr;-hydroxysteroid dehydrogenase (17&bgr;-HSD) such as 17&bgr;-HSD type 1, type 2 or type 3 enzyme.
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公开(公告)号：PL1976997T3
公开(公告)日：2009-09-30
申请号：PL07712041
申请日：2007-01-16
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , THOLE HEINRICH-HUBERT , RASCHE HEINZ-HELMER , SCHMIDT MICHAEL , HAKALA JUHA
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公开(公告)号：AT431351T
公开(公告)日：2009-05-15
申请号：AT04804787
申请日：2004-12-13
Applicant: SOLVAY PHARM GMBH
Inventor： HIRVELAE LEENA , HUSEN BETTINA , KIVINIEMI JOHANNA , KOSKIMIES PASI , LEHTOVUORI PEKKA , MESSINGER JOSEF , PENTIKAEINEN OLLI TANELI , KALLIO LILA , SAARENKETO PAULI , THOLE HEINRICH-HUBERT , UNKILA MIKKO , VAN STEEN BARTHOLOMEUS JOHANNES
IPC: C07D495/04 , A61K31/519
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35.发明专利
公开(公告)号：MX2009002579A
公开(公告)日：2009-03-20
申请号：MX2009002579
申请日：2007-09-17
Applicant: SOLVAY PHARM GMBH
Inventor： KOSKIMIES PASI , MESSINGER JOSEF , THOLE HEINRICH-HUBERT , HUSEN BETTINA , SCHOEN UWE , KALLIO LILA
Abstract: Esta invención se refiere a estratrien-triazoles nuevos de fórmula general (I) útiles en la terapia, especialmente para el uso en el tratamiento y/o la prevención de un trastorno dependiente de hormonas esteroideas, preferiblemente una enfermedad o trastorno dependiente de hormonas esteroideas que requiere la inhibición de una enzima 17ß-hidroxiesteroide deshidrogenasa (17ß-HSD) tal como 17ß-HSD de tipo 1, tipo 2 o tipo 3. (ver fórmula I).
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Patent Agency Ranking
公开(公告)号：ES2314478T3
公开(公告)日：2009-03-16
申请号：ES04804529
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
IPC: C07J1/00 , A61K31/565
Abstract: Un compuesto de fórmula general I, (Ver fórmula) en la cual (i) X representa: (a) un enlace, (b) -NR 3 -, o (c) -O-; A representa: (a) -CO-, o (b) con la condición de X represente -NR 3 , A representa -SO2-; Y representa: (a) -NR 4 -, (b) -O-, con la condición de que X represente un enlace o -NR 3 -, (c) un enlace, (d) -NH-SO2-, con la condición de que X represente -NR 3 y A represente -CO-, (e) -NH-SO2-NR 4 , con la condición de que X represente -O-, o (f) -NH-NR 4 -, con la condición de que X represente un enlace, o (ii) -X-A-Y- conjuntamente representa -O-; y en donde...
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公开(公告)号：PT1685150E
公开(公告)日：2008-11-12
申请号：PT04804529
申请日：2004-11-11
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , JOHANSSON NINA , KOSKIMIES PASI , THOLE HEINRICH-HUBERT , HUSEN BETTINA , STEEN BARTHOLOMEUS JOHANNES VAN , SCHNEIDER GYULA , HULSHOF JOHANNES BERNARDUS EVERARDUS , ADAMSKI JERZY
IPC: C07J1/00 , A61K31/565
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公开(公告)号：NO20076616L
公开(公告)日：2008-02-01
申请号：NO20076616
申请日：2007-12-21
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , WESKE MICHAEL , KOSKIMIES PASI , THOLE HEINRICH-HUBERT , HUSEN BETTINA , PIRKKALA LILA
IPC: C07J41/00
Abstract: The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17ß-hydroxysteroid dehydrogenase type I (17ß-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 17ß-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17ß-estradiol concentration.
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公开(公告)号：BRPI0416551A
公开(公告)日：2007-02-27
申请号：BRPI0416551
申请日：2004-11-11
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , THOLE HEINRICH-HUBERT , HUSEN BETTINA , STEEN BARTHOLOMEUS JOHANNES VA , SCHNEIDER GYULA , HULSHOF JOHANNES BERNARDUS EVA , KOSKIMIES PASI , JOHANSSON NINA , ADAMSKI JERZY
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：CA2609726A1
公开(公告)日：2006-11-30
申请号：CA2609726
申请日：2006-05-24
Applicant: SOLVAY PHARM GMBH
Inventor： HUSEN BETTINA , THOLE HEINRICH-HUBERT , KOSKIMIES PASI , PIRKKALA LILA , MESSINGER JOSEF , WESKE MICHAEL
Abstract: The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17ß-hydroxysteroid dehydrogenase type I (17ß-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 17ß-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17ß-estradiol concentration.
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