Selective estrogen receptor modulators

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/135 (2006.01) C07C 211/00 (2006.01) C07C 225/22 (2006.01) C07C 255/47 (2006.01) C07C 255/58 (2006.01) C07D 295/092 (2006.01) C07D 307/46 (2006.01)

Patent

CA 2456150

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.

La présente invention concerne des composés et des dérivés de ceux-ci, la synthèse et l'utilisation de ces composés comme modulateurs des récepteurs d'oestrogène. Les composés de cette invention sont des ligands des récepteurs d'oestrogènes et en tant que tels ils conviennent pour le traitement ou la prévention de diverses pathologies associées à la fonction oestrogénique comprenant: la perte osseuse, des fractures osseuses, l'ostéoporose, une maladie osseuse métastatique, la maladie de Paget, la parodonthopathie, la dégénération cartilagineuse, l'endométriose, le fibrome utérin, les bouffées de chaleur, des niveaux élevés de cholestérol LDL, une maladie cardio-vasculaire, un dérèglement des fonctions cognitives, des affections dégénératives cérébrales, la resténose, la gynécomastie, la prolifération cellulaire des muscles lisses de la paroi vasculaire, l'obésité, l'incontinence et le cancer, en particulier le cancer du sein, de l'utérus et de la prostate.

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