Novel 17.beta.-substituted 4-azaandrostane derivatives,...

C - Chemistry – Metallurgy – 07 – J

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

Patent

CA 2146164

The invention relates to novel 17.beta.-substituted 4-azaandrostane derivatives of general Formula (I), wherein R means hy- drogen or a C1-3alkyl group; R1 and R2 are the same or different and stand for hydrogen or a C1-4alkyl group with the provi- so that both can mean hydrogen only in the case when n is higher than 5; or R1 and R2 together mean an .alpha.,.omega.-alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom; n is 4, 5, 6 or 7; and --- bond line represents a single or double bond. Furthermore, the invention relates to pharmaceutical composi- tion containing these compounds as well as a process for the preparation of the compounds of general Formula (I). The com- pounds of general Formula (I) exert a 5.alpha.-reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseas- es, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.

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