公开(公告)号：DK1685150T3

公开(公告)日：2008-12-01

申请号：DK04804529

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.

公开(公告)号：CA2671075A1

公开(公告)日：2008-06-05

申请号：CA2671075

申请日：2007-11-27

Applicant: SOLVAY PHARM GMBH

Inventor： HUSEN BETTINA ,  MESSINGER JOSEF ,  UNKILA MIKKO ,  KOSKIMIES PASI ,  THOLE HEINRICH-HUBERT ,  SCHOEN UWE

IPC: C07J41/00 ,  A61K31/565 ,  A61K31/566 ,  A61K31/58 ,  A61P5/32 ,  C07J43/00 ,  C07J51/00

Abstract: This invention relates to novel substituted estratrien derivatives of gen eral formula (I) useful in therapy, especially for use in the treatment and/ or prevention of a steroid hormone dependent disorder requiring the inhibiti on of a 17.beta.-hydroxysteroid dehydrogenase (17- HSD) type 1, type 2 and/or type 3 enzyme, as well as to their salts, to pharmaceutical preparations c ontaining these compounds and to processes for the preparation of these comp ounds.

公开(公告)号：NO20076616A

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

CPC classification number: C07J71/0052 ,  C07J41/0072 ,  C07J43/003 ,  C07J71/0068

公开(公告)号：AU2006251154A1

公开(公告)日：2006-11-30

申请号：AU2006251154

申请日：2006-05-24

Applicant: SOLVAY PHARM GMBH

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

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

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.

公开(公告)号：AR046580A1

公开(公告)日：2005-12-14

申请号：ARP040104159

申请日：2004-11-11

Applicant: SOLVAY PHARM GMBH

Inventor： MESSINGER JOSEF ,  THOLE HEINRICH-HUBERT ,  HUSEN BETTINA ,  SCHNEIDER GYULA ,  HULSHOF JOHANNES BERNARDUS ,  KOSKIMIES PASI ,  JOHANSSON NINA ,  ADAMSKI JERZY ,  VAN STEEN BARTHOLOMEUS JOHANNES

IPC: A61K31/565 ,  C07J1/00 ,  C07J17/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  A61K31/566 ,  A61K31/58 ,  A61P5/32 ,  A61P19/02 ,  A61P35/00

Abstract: La presente se refiere a derivados de estrona 3,15-sustituidos que representan compuestos inhibidores de deshidrogenasa 17-hidroxiesteroide de tipo I (17-HSD1), a sus sales, a preparaciones farmacéuticas que contienen estos compuestos y a procedimientos para la preparación de estos compuestos. Además de ello, la invención se refiere al uso terapéutico de dichos derivados de estrona 3,15-sustituidos, particularmente su uso en el tratamiento o prevención de enfermedades o trastornos dependientes de hormonas esteroides, como enfermedades o trastornos dependientes de hormonas esteroides que requieren la inhibición de enzimas deshidrogenasa 17-hidroxiesteroide de tipo I y/o que requieren la disminución de la concentración de 17- estradiol endógeno. Además, la presente se refiere al uso general de inhibidores selectivos de deshidrogenasa 17-hidroxiesteroide de tipo I que poseen además ninguna o solamente las puras de las afinidades de unión antagonista al receptor de estrógenos para el tratamiento y prevención de trastornos ginecológicos benignos, en particular endometriosis.