Metabolites of selective androgen receptor modulators and...

A - Human Necessities – 61 – K

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Details

A61K 31/275 (2006.01) A61K 31/70 (2006.01) C07C 233/05 (2006.01) C07G 3/00 (2006.01)

Patent

CA 2563908

This invention provides metabolites of a class of androgen receptor targeting agents (ARTA). The SARM compounds and their metabolites, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition, and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

L'invention concerne des métabolites d'une classe d'agents de ciblage du récepteur androgénique (ARTA). Les composés SARM et leurs métabolites sont utilisés, soit seuls, soit sous forme d'une composition pour a) la contraception masculine ; b) le traitement de divers troubles hormonaux, par exemple, de troubles associés au déclin androgénique chez l'homme agé (ADAM), tels que fatigue, dépression, diminution de la libido, dysfonctionnement sexuel, troubles érectiles, hypogonadisme, ostéoporose, perte des cheveux, anémie, obésité, sarcopénie, ostéopénie, hyperplasie prostatique bénigne, troubles de l'humeur et de la cognition, et cancer de la prostate ; c) le traitement de troubles associés au déclin androgénique chez la femme (ADIF), tels que dysfonctionnement sexuel, diminution de la libido, hypogonadisme, sarcopénie, ostéopénie, troubles de la cognition et de l'humeur, dépression, anémie, dépression, anémie, perte des cheveux, obésité, endométriose, cancer du sein, cancer de l'utérus et cancer ovarien ; d) le traitement et/ou la prévention des troubles de fonte musculaire aiguë et/ou chronique ; e) la prévention et/ou le traitement du syndrome de l'oeil sec ; f) la thérapie de remplacement androgénique oral ; g) la diminution de l'incidence de l'arrêt ou de la provocation d'une régression du cancer de la prostate ; et/ou l'induction d'apoptose dans une cellule cancéreuse.

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