Compounds and methods for modulation of estrogen receptors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 217/18 (2006.01) A61K 31/472 (2006.01) A61P 35/00 (2006.01) C07D 209/44 (2006.01) C07D 217/04 (2006.01) C07D 217/20 (2006.01) C07D 223/16 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 405/04 (2006.01)

Patent

CA 2367895

Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-.beta. over ER-.alpha.. Methods are disclosed for modulating ER-.beta. in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-.beta.. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

L'invention concerne des composés servant à moduler des récepteurs des oestrogènes (ER) ainsi que des compositions pharmaceutiques contenant lesdits composés. Dans un mode de réalisation spécifique, les composés sont des modulateurs sélectifs d'ER- beta sur ER- alpha . L'invention concerne des techniques de modulation d'ER- beta dans des cellules et/ou des tissus l'exprimant, y compris dans des cellules et/ou des tissus exprimant de préférence ER- beta . D'une manière plus générale, l'invention concerne également des traitements de pathologies liées aux oestrogènes, et notamment le cancer du sein, le cancer des testicules, l'ostéoporose, l'endométriose, les maladies cardio-vasculaires, l'hypercholestérolémie, l'hypertrophie prostatique, les carcinomes prostatiques, l'obésité, les bouffées de chaleur, les troubles cutanés, les sautes d'humeur, l'amnésie, l'incontinence urinaire, la chute de cheveux, la cataracte, les déséquilibres hormonaux naturels, et les problèmes de la reproduction associés à l'exposition aux produits chimiques présents dans l'environnement.

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