Forendo Pharma Ltd

Abbott Products Gmbh

Solvay Pharmaceuticals, B.v.

Solvay Pharmaceuticals, Gmbh

Organon R&d Finland Oy

Organon R&d Finland Ltd

Pasi Koskimies

Leena Hirvelä

Josef Messinger

Heinrich-Hubert Thole

Bettina Husen

Risto A Lammintausta

Mikko Unkila

Maire Eloranta

Nina Johansson

Marjo Hakola

Lauri V Kangas

Lila Pirkkala

Uwe Schoen

Michael Weske

Tero Linnanen

Tiina Annamaria Salminen

Mark Stuart Johnson

Olli Taneli Pentikaeinen

Tommi Nyroenen

Leena Hirvelae

Pekka Lehtovuori

Bartholomeus Johannes Van Steen

Camilla Stjernschantz

Pauli Saarenketo

Johanna Kiviniemi

Annamaria Lilienkampf

Kimmo Vihko

Kaisa Huhtinen

Sari Alho

Kristiina Waehaelae

Lila Kallio Nee Pirkkala

Jerzy Adamski

Johannes Bernardus Everardus Hulshof

Gyula Schneider

Leena Hirvela

Johannes Bernardus Hulshof

Lila Kallio

Leena HirvelÄ

The invention relates to compounds of formula (II), and pharmaceutically acceptable salts thereof,wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17&#x3b2;-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

Therapeutically active steroidal derivatives

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17&#x3b2;-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

The present invention accordingly provides novel compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the claims. The invention further relates to their in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. 

Prodrugs of 17&#x3b2;-HSD1-inhibitors

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17&#x3b2;-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof. 

Prodrugs of 17.BETA.-HSD1-inhibitors

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R6 are as defined in the claims. The invention further relates to their use as inhibitors of 17&#x3b2;-HSD and in treatment or prevention of steroid hormone de-pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof. 

Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2, R3, R4, R7 and R8 are as defined in the claims. The invention further relates to their use as inhibitors of 17&#x3b2;-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof. 

Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta-hydroxy-steroid dehydrogenase, type 1

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2 to R7 are as defined in the claims. The invention further relates to their use as inhibitors of 17&#x3b2;-HSD and in treatment or prevention of steroid hormone de-pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17&#x3b2;-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the afore-mentioned compounds or pharmaceutically acceptable salts thereof.

Therapeutically active 17-nitrogen substituted estratreinthiazole derivatives as inhibitors of 17&#x3b2;-hydroxysteroid dehydrogenase

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

Thiopheneprymidinone compounds 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&#x3b2;-hydroxysteroid dehydrogenase (17&#x3b2;-HSD) such as 17&#x3b2;-HSD type 1, type 2 or type 3 enzyme.

Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17&#x3b2; hydroxysteroid dehydrogenase compounds

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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Turku, Finland

Pasi Koskimies