17 beta -N-monosubstituted carbamoyl or 17 beta -acyl-4-aza-5 alpha -androst-1-en-3-ones of the formula: CHEM in which R is hydrogen, methyl or ethyl; R2 is a C1-12 straight or branched alkyl radical or a monocyclic aryl optionally containing one or more methyl or ethyl substituents and/or one or more Cl, F or Br substituents; and in Formula IA R2 may also be benzyl, phenethyl, 2-pyridyl, 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl; R min is hydrogen or methyl; R sec is hydrogen or beta -methyl and in Formula IA may also be alpha -methyl; and R''' is hydrogen, alpha -methyl or beta -methyl and pharmaceutical formulations containing the above compounds are active as testosterone 5 alpha -reductase inhibitors and thus are useful topically for treatment of acne, seborrhoea and female hirsutism, and systemically in the treatment of benign prostatic hypertrophy.
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机译:下式的17个β-N-单取代的氨基甲酰基或17个β-酰基-4-氮杂-5个α-雄酮-1-en-3-个其中R为氢,甲基或乙基的R; R 2为C 1-12直链或支链烷基或单环芳基,其任选地含有一个或多个甲基或乙基取代基和/或一个或多个Cl,F或Br取代基;在式IA中,R 2也可以是苄基,苯乙基,2-吡啶基,4-吡啶基,2-吡咯基,2-呋喃基或噻吩基; R min为氢或甲基; R sec是氢或β-甲基,并且在式IA中还可以是α-甲基; R”'是氢,α-甲基或β-甲基,并且含有上述化合物的药物制剂具有睾丸激素5α-还原酶抑制剂的活性,因此可局部用于治疗痤疮,脂溢性皮炎和女性多毛症,并在全身治疗前列腺肥大。
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