Estrogen receptor modulators

C - Chemistry – Metallurgy – 07 – J

Patent

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Details

C07J 1/00 (2006.01) A61K 31/56 (2006.01)

Patent

CA 2569152

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, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

La présente invention concerne des composés et leurs dérivés, leur synthèse ainsi que leur utilisation comme modulateurs des récepteurs oestrogéniques. Les composés de la présente invention sont des ligands pour les récepteurs oestrogéniques. Par conséquent, ils peuvent être utiles dans le traitement ou la prévention de diverses affections associées au fonctionnement des oestrogènes, telles que la perte osseuse, les fractures osseuses, l'ostéoporose, la maladie osseuse métastatique, la maladie de Paget, la parodontopathie, la dégénérescence cartilagineuse, l'endométriose, le fibrome utérin, les bouffées de chaleur, les taux accrus de LDL-cholestérol, la maladie cardiovasculaire, le trouble cognitif, les troubles de dégénérescence cérébrale, la resténose, la gynécomastie, la prolifération des cellules musculaires lisses vasculaires, l'obésité, l'incontinence, l'inflammation, la maladie intestinale inflammatoire, la dysfonction sexuelle, l'hypertension, la dégénérescence rétinienne et le cancer, notamment du sein, de l'utérus et de la prostate.

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