17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active...

Details 17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active... 17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active...

C - Chemistry, Metallurgy

07

J

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

Patent

CA 2244823

The invention related to 4-aza-17.beta.-(cyclopropoxy)-androst-5.alpha.- androstan-3-one, 4-aza-17.beta.-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5.alpha.-reductase and C17.alpha.- hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen- dependent disorders also includes a combination therapy with known androgen- receptor antagonists, such as flutamide. The compounds of the invention have general formula (I).

Cette invention concerne des composés 4-aza-17.beta.-(cyclopropoxy)-androst-5.alpha.-androstan-3-one, des composés 4-aza-17.beta.-(cyclopropylamino)-androst-4-en-3-one, et leurs composés apparentés, ainsi que des compositions contenant ces composés. Cette invention concerne également l'inhibition de C¿17-20? lyase, de 5.alpha.-reductase et de C¿17.alpha.?-hydroxylase, ainsi que l'utilisation des composés susmentionnés dans le traitement de troubles déclenchés par des androgènes et des oestrogènes comme, par exemple, l'hyperplasie prostatique bénigne, le cancer de la prostate déclenché par des androgènes, le cancer du sein déclenché par des oestrogènes et les troubles déclenchés par DHT tels que l'acné. Les troubles liés à une synthèse excessive de cortisol, tel que le syndrome de Cushing, peuvent également être traités de cette manière. Le traitement de troubles liés à des androgènes comprend également une thérapie combinatoire faisant appel à des antagonistes de récepteurs d'androgènes connus, tel que du flutamide. Les composés décrits dans la présente invention correspondent à la formule générale (I).

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