Pyridine imidazoles and aza-indoles as progesterone receptor...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/437 (2006.01) A61P 15/00 (2006.01)

Patent

CA 2585544

The present invention is directed to novel pyrimidine imidazoles and aza- indoles according to formulae (I) and (II), pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

La présente invention concerne des pyridine imidazoles et aza-indoles représentés par les formules (I) et (II), des compositions pharmaceutiques contenant ces composés et leur utilisation dans le traitement de troubles à médiation par un ou plusieurs récepteurs d'oestrogène. Les composés selon l'invention servent au traitement de troubles associés à une déplétion d'oestrogène, tels que les bouffées de chaleur, la sécheresse vaginale, l'ostéopénie et l'ostéoporose ; les cancers hormono-dépendants et l'hyperplasie de la poitrine, de l'endomètre, du col de l'utérus et de la prostate ; l'endométriose, les fibroïdes utérins et l'ostéoarthrite. Lesdits composés peuvent également servir d'agents contraceptifs seuls ou en combinaison avec un progestogène ou un antagoniste de progestogène.

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