Novel heteroatom containing tetracyclic derivatives as...

C - Chemistry – Metallurgy – 07 – D

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C07D 493/04 (2006.01) A61K 31/35 (2006.01) A61P 19/10 (2006.01) C22B 3/06 (2006.01) C22B 3/10 (2006.01) C22B 11/00 (2006.01)

Patent

CA 2505857

The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceuticalcompositions contianing them, their use in the treatment and/or prevention of disorders mediated by oneor more estrogen receptors and processes for their preparation. The compounds of the invention areuseful in the treatment and/or prevention of disorders associated with the depletion of estrogen such ashot 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 nouveaux dérivés tétracycliques contenant des hétéroatomes, des compositions pharmaceutiques qui les contiennent, leur utilisation pour traiter et/ou prévenir des troubles liés à un ou plusieurs récepteurs d'oestrogène, et des procédés pour les préparer. Les composés de l'invention sont utiles pour traiter et/ou prévenir des troubles liés à la diminution du taux d'oestrogène tels que les bouffées de chaleur, la sécheresse vaginale, l'ostéopénie et l'ostéoporose, les cancers sensibles aux hormones et l'hyperplasie du sein, de l'endomètre, de la glaire cervicale et de la prostate, l'endométriose, les fibroïdes utérins, l'ostéoarthrite, et en tant qu'agents contraceptifs, seuls ou en combinaison avec un progestogène ou un antagoniste de progestogène.

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