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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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92.发明专利
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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公开(公告)号：AU2004276002B2
公开(公告)日：2010-07-22
申请号：AU2004276002
申请日：2004-09-23
Applicant: SOLVAY PHARM GMBH
Inventor： HOELTJE DAGMAR , ZIEGLER DIETER , MICHAELIS KATHRIN , PAHL AXEL , MESSINGER JOSEF , WESKE MICHAEL , TURSKI LECHOSLAW , HOEFER CONSTANZE , FISCHER YVAN , KARIMI-NEJAD YASMIN , IKONOMIDOU HRISSANTHI
Abstract: Described are novel compounds with neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity of the general formula (I), wherein the substituents R , R , R and R have the meanings given in the description and also medicaments containing these compounds, in particular medicaments suitable for treating or preventing cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
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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
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.
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公开(公告)号：UA85195C2
公开(公告)日：2009-01-12
申请号：UAA200604364
申请日：2004-09-23
Applicant: SOLVAY PHARM GMBH
Inventor： HOELTJE DAGMAR , FISCHER YVAN , CYGLER DITER , WESKE MICHAEL , MICHAELIS KATHRIN , KARIMI-NEJAD YASMIN , MESSINGER JOSEF , PAHL AXEL , HOEFER CONSTANZE , IKONOMIDOU HRISSANTHI , TURSKI LECHOSLAW
Abstract: Взаявкеописаныновыесоединения, которыепроявляютингибирующеевлияниенанейтральнуюэндопептидазу (НЭП) и/илирастворимуюэндопептидазучеловека (лРЭП), общейформулыІ EMBED ISISServer , Ів которойзаместители R1, R2, R3 и R4 имеютзначения, указанныев описании, атакжелекарственныесредства, которыесодержатэтисоединения, вчастностилекарственныесредства, пригодныедлялеченияилипредупреждениясердечно-сосудистыхзаболеваний, половойдисфункциии/илипатологическихсостояний, связанныхс апоптозом.
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Patent Agency Ranking
公开(公告)号：SI1685150T1
公开(公告)日：2008-12-31
申请号：SI200430862
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 , A61K31/00 , A61K31/565
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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.
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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.
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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
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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公开(公告)号：NO20073610L
公开(公告)日：2007-09-12
申请号：NO20073610
申请日：2007-07-12
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , HIRVELA LEENA , KOSKIMIES PASI , PENTIKAINEN OLLI TANELI , LEHTOVUORI PEKKA , THOLE HEINRICH-HUBERT , HUSEN BETTINA , KIVINIEMI JOHANNA , PIRKKALA LILA , SAARENKETO PAULI , UNKILA MIKKO , STEEN BARHOLOMEUS JOHANNES VAN
IPC: C07D495/04 , A61K31/519
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