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公开(公告)号：SK5862002A3
公开(公告)日：2003-01-09
申请号：SK5862002
申请日：2002-04-26
Applicant: SOLVAY PHARM GMBH
Inventor： SCHON UWE , MESSINGER JOSEF , BRUCKNER REINHARD , ZIEGLER DIETER
IPC: A61K31/435 , A61K31/439 , A61P9/00 , A61P9/06 , C07D221/00 , C07D471/08 , C07D471/10 , A61K31/00
Abstract: 7-Alkyl-3-(substituted phenyl)-9,9-(dialkyl or alkylene)-3,7-diazabicyclo (3.3.1) nonane derivatives (I) are new. Diazabicyclononane derivatives of formula (I) and their acid addition salts are new. R1 = 1-6C alkyl or 4-7C cycloalkylalkyl; R2, R3 = 1-4C alkyl; or R2 + R3 = 3-6C alkylene; and R4 = phenyl (monosubstituted in the ortho- or para-position by NO2, CN or 2-5C alkanoyl) or 2,4-dinitrophenyl. An Independent claim is also included for the preparation of (I).
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公开(公告)号：NO20023112A
公开(公告)日：2002-12-30
申请号：NO20023112
申请日：2002-06-27
Applicant: SOLVAY PHARM GMBH
Inventor： SCHOEN UWE , MESSINGER JOSEF , BRUECKNER REINHARD , ZIEGLER DIETER
IPC: A61K31/435 , A61K31/439 , A61P9/00 , A61P9/06 , C07D221/00 , C07D471/08 , C07D471/10 , C07D487/08
CPC classification number: C07D471/08 , C07D471/10
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公开(公告)号：PL184336B1
公开(公告)日：2002-10-31
申请号：PL31343396
申请日：1996-03-22
Applicant: SOLVAY PHARM GMBH
Inventor： WALDECK HARALD , HOELTJE DAGMAR , MESSINGER JOSEF , ANTEL JOCHEN , WURL MICHAEL , THORMAEHLEN DIRK
IPC: C07D223/16 , A61K31/33 , A61K31/423 , A61K31/428 , A61K31/55 , A61K31/554 , A61K38/00 , A61K38/05 , A61P7/10 , A61P9/00 , A61P43/00 , C07D267/14 , C07D281/10 , C07K5/078 , C07D405/12
Abstract: Benzazepin-, benzoxazepin- and benzothiazepin-N-acetic acid derivs. of formula (I) and their salts are new. R = lower alkoxy(lower)alkyl (in which the alkoxy is opt. substd. by lower alkoxy) or phenyl(lower)alkyl, or phenoxy(lower)alkyl (opt. ring substd. by lower alkyl or alkoxy or halo) or naphthyl(lower)alkyl; A = CH2, O or S; R , R = H or halogen; R , R = H or a biolabile ester containing gp.
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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
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.
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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
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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Patent Agency Ranking
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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公开(公告)号：PL1685150T3
公开(公告)日：2009-02-27
申请号：PL04804529
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
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公开(公告)号：BRPI0419229A
公开(公告)日：2007-12-18
申请号：BRPI0419229
申请日：2004-12-13
Applicant: SOLVAY PHARM GMBH
Inventor： HIRVEL LENNA , HUSEN BETINA , KIVINIEMI JOHANNA , KOSKIMIES PASI , LEHTOVUORI PEKKA , MESSINGER JOSEF , PENTIKOINEN OLLI TANELI , PIRKKALA LILA , SAARENKETO PAULI , THOLE HEINRICH-HUBERT , UNKILA MIKKO , STEEN BARTHOLOMEUS JOHANNES VA
IPC: C07D495/04 , A61K31/519
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公开(公告)号：NO20073610A
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
CPC classification number: C07D495/04
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公开(公告)号：HK1099309A1
公开(公告)日：2007-08-10
申请号：HK07106357
申请日：2007-06-13
Applicant: SOLVAY PHARM GMBH
Inventor： MESSINGER JOSEF , HEINRICH-HUBERT THOLE H , HUSEN BETTINA , STEEN BARTHOLOMEUS JOHANNES VAN , SCHNEIDER GYULA , JOHANNES BERNARDUS EVERARDUS HULSHOF J , KOSKIMIES PASI , JOHANSSON NINA , ADAMSKI JERZY
IPC: A61K20060101 , A61K31/565 , C07J20060101 , 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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