Forendo Pharma Ltd

Organon R&d Finland Oy

Organon R&d Finland Ltd

Marjo Hakola

Pasi Koskimies

Leena Hirvelä

Risto A Lammintausta

Maire Eloranta

Tero Linnanen

Camilla Stjernschantz

Kaisa Illikainen

Leena Hirvela

Olli PENTIKÄINEN

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

Growing community of inventors

Kempele, Finland

Marjo Hakola