4-azasteroids for treatment of hyperandrogenic conditions

Details 4-azasteroids for treatment of hyperandrogenic conditions 4-azasteroids for treatment of hyperandrogenic conditions

C - Chemistry, Metallurgy

07

J

C07J 73/00 (2006.01) A61K 31/435 (2006.01) A61K 31/58 (2006.01)

Patent

CA 2231041

Compounds of structural Formula (I), and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula (I) are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent anti-androgens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

L'invention porte sur des composés représentés par la formule développée (I), et sur leurs sels et leurs esters pharmaceutiquement acceptables, possédant une activité inhibitrice de 5.alpha.-réductase. Ces composés inhibent la 5.alpha.-réductase des types 1 et 2. Les composés de formule développée (I) servent au traitement curatif et préventif systémique - y compris oral, et parentéral - y compris local, d'états hyperandrogéniques, y compris de carcinomes prostatiques, de l'hyperplasie prostatique, de l'acné vulgaire, de la séborrhée, de l'alopécie androgénique (également appelée alopécie androgénétique), qui comprend la calvitie masculine et féminime, l'hirsutisme féminin et la prostatite. Des composés de la présente invention sont également de puissants anti-androgènes. L'invention porte également sur des compositions contenant de tels composés, sur leurs procédés d'utilisation et leurs procédés de fabrication.

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