FIELD: organic chemistry, steroids, pharmacy. SUBSTANCE: invention describes new 16-substituted 4-azaandrostanes of the general formula (I) where values R1-R4 are given in p. 1 of the invention claim. Compounds are selective inhibitors of isozyme 5α-reductase. Invention describes also methods of inhibition of 5α-reductase or its isoenzyme activity, methods of treatment of patients with acnes vulgaris, androgenic alopecia, hirsutism in females, prostate benign hyperplasia, prostatitis and/or prophylaxis of prostate cancer, method of ceasing and reversal of an anfocus alopecia and hair growth stimulation, method of inhibition of metabolism of testosterone to dihydrotestosterone in mammals. Invention relates to also a pharmaceutical composition containing therapeutically effective amount of the compound of the general formula (I). EFFECT: enhanced effectiveness of compounds, valuable inhibiting properties. 23 cl, 85 ex
Authors
Dates
1999-12-20—Published
1994-10-21—Filed