Abbott Products Gmbh

Solvay Pharmaceuticals, Gmbh

Solvay Pharmaceuticals, B.v.

Universitaet Des Saarlandes

Heinrich-Hubert Thole

Josef Messinger

Pasi Koskimies

Bettina Husen

Lila Pirkkala

Uwe Schoen

Michael Weske

Mikko Unkila

Nina Johansson

Bartholomeus Johannes Van Steen

Rolf Wolfgang Hartmann

Tiina Annamaria Salminen

Mark Stuart Johnson

Tommi Nyroenen

Olli Taneli Pentikaeinen

Leena Hirvelae

Pekka Lehtovuori

Martin Frotscher

Pauli Saarenketo

Lila Kallio Nee Pirkkala

Johanna Kiviniemi

Jerzy Adamski

Johannes Bernardus Everardus Hulshof

Gyula Schneider

Erika Ziegler

Sandrine Oberwinkler

Johannes Bernardus Hulshof

Lila Kallio

The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases

Substituted steroid compounds which represent selective inhibitors of 17&#x3b2;-hydroxysteroid dehydrogenase type I (17&#x3b2;-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17&#x3b2;-estradiol concentration.

17-beta HSD1 and STS inhibitors

Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17&#x3b2;-hydroxysteroid dehydrogenase (17&#x3b2;-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds. 

Substituted estratriene derivatives as 17BETA HSD inhibitors

3,15-substituted estrone compounds which act as inhibitors of 17&#x3b2;-hydroxysteroid dehydrogenase type I (17&#x3b2;-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17&#x3b2;-estradiol concentration, as well as the general use of selective 17&#x3b2;-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.

17&#x3b2;-hydroxysteroid dehydrogenase type I inhibitors

Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17&#x3b2;-hydroxysteroid dehydrogenase (17&#x3b2;-HSD) such as 17&#x3b2;-HSD type 1, type 2 or type 3 enzyme. 

Therapeutically active triazoles and their use

The present invention relates to novel substituted steroid derivatives which represent selective inhibitors of the 17&#x3b2;-hydroxysteroid dehydrogenase type I (17&#x3b2;-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, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17&#x3b2;-estradiol concentration.

17&#x3b2;-HSD1 and STS inhibitors

Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase enzymes.

Compounds and their use in therapy

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Hannover, Germany

Heinrich-Hubert Thole