A novel crystalline form of...

C - Chemistry – Metallurgy – 07 – D

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C07D 333/64 (2006.01) A61K 31/445 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2426007

The present invention is directed to a novel, non-solvated, anhydrous crystal form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]-phenoxy)-2-(4- methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, including inhibition of disease states associated with estrogen deprivation including cardiovascular disease, hyperlipidemia, and osteoporosis; and inhibition of other pathological conditions such as endometriosis, uterine fibrosis, estrogen-dependent cancer (including breast and uterine cancer), prostate cancer, benign prostatic hyperplasia, CNS disorders including Alzheimer's disease, prevention of breast cancer, and up-regulating ChAT.

L'invention concerne une nouvelle forme cristalline anhydre, non solvate, d'hydrochlorure de 6-hydroxy-3-(4-[2-(pipéridine-1-yl)éthoxy]-phénoxy)-2-(4-méthoxyphényl)benzo[b]thiophène, et ses utilisations, y compris pour l'inhibition de différents états pathologiques associés à une carence estrogénique, à savoir par exemple: maladie cardiovasculaire, hyperlipidémie, et ostéoporose; et l'inhibition d'autres états pathologiques, à savoir par exemple: endométriose, subinvolution de l'utérus, cancer de nature estrogénique (y compris le cancer du sein et le cancer de l'utérus), cancer de la prostate, hyperplasie prostatique bénigne, troubles du système nerveux central y compris la maladie d'Alzheimer. La substance considérée permet également de prévenir le cancer du sein et d'assurer la régulation positive ChAT.

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