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)

Patent

CA 2471107

Novel Heteroatom Containing Tetracyclic Derivatives as Selective Estrogen Receptor ModulatorsAbstractThe present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and / or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and / or prevention 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.

Cette invention a trait à de nouveaux hétéroatomes contenant des dérivés tétracycliques, à des compositions pharmaceutiques les contenant, à leur utilisation pour le traitement et/ou la prévention de troubles provoqués par un ou plusieurs récepteurs des oestrogènes ainsi qu'à des procédés de préparation. Les composés selon l'invention se révèlent des plus utiles en matière de traitement et/ou de prévention de troubles associés à une déplétion oestrogénique, notamment, les bouffées de chaleur, la siccité vaginale, l'ostéopénie et l'ostéoporose. Ils sont également des plus utiles s'agissant de cancers sensibles aux hormones ainsi que de l'hyperplasie du sein, de l'endomètre, du col et de la prostate, de l'endométriose, des fibromes utérins et de l'arthrose. On peut également utiliser ces composés comme agents contraceptifs, seuls ou associés à un progestatif ou à un antagoniste des progestatifs.

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