Estratriene derivatives comprising heterocyclic bioisosteres...

C - Chemistry – Metallurgy – 07 – J

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C07J 71/00 (2006.01) A61K 31/58 (2006.01) A61P 5/30 (2006.01)

Patent

CA 2731634

The present invention is directed to novel pyrazolo-estrien and triazolo- estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.

La présente invention concerne de nouveaux dérivés pyrazolo-estriènes et triazolo-estriènes, des compositions pharmaceutiques les contenant et leur utilisation dans le traitement ou la prévention de troubles et de maladies médiés par un récepteur dstrogène tels que les bouffées de chaleur, la sécheresse vaginale, lostéopénie, lostéoporose, lhyperlipidémie, la perte de la fonction cognitive, les maladies cérébrales dégénératives, les maladies cardiovasculaires, les maladies cérébrovasculaires, les cancers hormono-sensibles et lhyperplasie (dans les tissus comprenant le sein, lendomètre, et le col de lutérus chez les femmes, et la prostate chez les hommes), lendométriosse, les fibroïdes utérins, larthrose ; et comme agents contraceptifs soit seuls soit en association avec un progestogène ou un antagoniste de progestogène. Les composés de linvention sont des modulateurs sélectifs des récepteurs dstrogène.

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