Estrogen receptor modulators

Details Estrogen receptor modulators Estrogen receptor modulators

C - Chemistry, Metallurgy

07

D

C07D 307/02 (2006.01) A61K 31/341 (2006.01) A61K 31/381 (2006.01) C07C 45/28 (2006.01) C07C 45/46 (2006.01) C07C 45/63 (2006.01) C07C 45/67 (2006.01) C07C 45/68 (2006.01) C07C 45/73 (2006.01) C07C 49/747 (2006.01) C07C 49/755 (2006.01) C07C 255/47 (2006.01) C07C 255/56 (2006.01) C07D 333/10 (2006.01)

Patent

CA 2498339

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

L'invention concerne des composés et des dérivés correspondants, des procédés de synthèse de ceux-ci et l'utilisation de ces composés comme modulateurs des récepteurs des oestrogènes. Ces composés constituent des ligands des récepteurs des oestrogènes et peuvent, de ce fait, être utiles pour traiter ou prévenir diverses affections liées au fonctionnement des oestrogènes, notamment : perte osseuse, fractures osseuses, ostéoporose, maladie osseuse métastatique, maladie de Paget, parodontopathie, dégénérescence cartilagineuse, endométriose, fibrome utérin, bouffées de chaleur, taux élevé de cholestérol LDL, maladie cardio-vasculaire, troubles de la fonction cognitive, troubles cérébraux dégénératifs, resténose, gynécomastie, prolifération des cellules du muscle lisse vasculaire, obésité, incontinence et cancer, en particulier cancer du sein, de l'utérus et de la prostate.

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