Compounds and methods for modulation of estrogen receptors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 311/16 (2006.01) A61K 31/37 (2006.01) A61P 35/00 (2006.01) C07D 311/18 (2006.01)

Patent

CA 2356986

Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having structure I, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.

L'invention concerne des composés modulant l'expression génique par l'intermédiaire du récepteur d'oestrogènes (ER) et correspondant à la formule (I), de même que des compositions pharmaceutiques contenant ces composés. Dans cette formule, R¿1?, R¿2?, R¿3?, n et p possèdent les notations données dans la description. L'invention concerne également des procédés de modulation du récepteur d'oestrogènes dans de cellules et/ou tissus exprimant celui-ci, tels que les os, le sein, la prostate, l'utérus, le système nerveux central ou le système cardio-vasculaire. L'invention concerne encore des méthodes de traitement de pathologies associées aux oestrogènes, notamment le cancer du sein, l'ostéoporose, l'endométriose, les maladies cardio-vasculaires, l'hypercholestérolémie, l'hypertrophie de la prostate, les cancers de la prostate, l'obésité, les bouffées de chaleur, les problèmes dermatologiques, les sautes d'humeurs, les pertes de mémoire et les effets préjudiciables à la reproduction associés à l'exposition aux produits chimiques présents dans l'environnement ou aux déséquilibres hormonaux naturels.

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