发明名称 17 Beta-Substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors.
摘要 <p>17 beta -N-monosubstituted carbamoyl or 17 beta -acyl-4-aza-5 alpha -androst-1-en-3-ones of the formula: &lt;CHEM&gt; in which R is hydrogen, methyl or ethyl; R&lt;2&gt; 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 R&lt;2&gt; 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.</p>
申请公布号 EP0155096(A2) 申请公布日期 1985.09.18
申请号 EP19850301122 申请日期 1985.02.20
申请人 MERCK & CO. INC. 发明人 RASMUSSON, GARY H.;REYNOLDS, GLENN F.
分类号 C07D213/00;A61K31/58;A61P5/00;C07C62/38;C07D221/18;C07J73/00;(IPC1-7):C07J73/00;A61K31/435 主分类号 C07D213/00
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