Novel estrogen receptor ligands and methods iii

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 39/17 (2006.01) A61K 31/05 (2006.01) A61K 31/085 (2006.01) A61P 19/10 (2006.01) A61P 35/00 (2006.01) C07C 39/23 (2006.01) C07C 39/42 (2006.01) C07C 43/21 (2006.01) C07C 43/23 (2006.01) C07C 43/253 (2006.01) C07C 45/67 (2006.01) C07C 45/68 (2006.01) C07C 49/747 (2006.01) C07C 49/753 (2006.01) C07C 251/44 (2006.01) C07D 295/08 (2006.01) C07D 295/092 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2430769

The present invention relates to compounds of formula (I) and derivatives thereof, in which the variables are as defined in the claims, 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, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell profileration, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prostate.

L'invention concerne des composés de formule (I), des dérivés de ces composés, dans lesquels les variables sont définies dans les revendications, leur synthèse, et leur utilisation en tant que modulateurs de récepteur d'oestrogène. Les composés de l'invention sont des ligands destinés à des récepteurs d'oestrogène et en tant que tels, ils peuvent être utiles pour le traitement ou la prévention d'une variété de troubles se rapportant au fonctionnement d'oestrogènes, y compris des troubles de perte osseuse, de fractures osseuses, d'ostéoporose, de dégénérescence de cartilage, d'endométriose, de myome de l'utérus, de bouffées de chaleur, d'augmentation de taux de cholestérol LDL, cardio-vasculaire, de déficience de fonction cognitive, de dégénérescence cérébrale, de rétinose, de gynécomastie, auto-immuns, de prolifération cellulaire de muscle lisse vasculaire, d'obésité, d'incontinence, et des cancers du poumon, du colon, du sein, de l'utérus et de la prostate.

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