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|Abstract:||17.beta.-Acyl-4-aza-5.alpha.-androst-1-in-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl R.sup.2 is methoxy, a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl; and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulations of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, and benign prostatic hypertrophy.|
|Inventor(s):||Rasmusson; Gary H. (Watchung, NJ), Reynolds; Glenn F. (Westfield, NJ)|
|Assignee:||Merck & Co., Inc. (Rahway, NJ)|
|Filing Date:||May 09, 1991|
|Claims:||1. A compound of the formula: ##STR9## wherein R is selected from hydrogen, methyl and ethyl; R' is methyl; and R" and R'" are each selected from hydrogen and methyl. |
2. A compound of claim 1, wherein R is hydrogen or methyl and R" and R'" are hydrogen.
3. A compound of claim 2 which is 17.beta.-methoxycarbonyl-4-aza-5.alpha.-androst -1-en-one.
4. A compound of claim 2 which is 17.beta.-methoxycarbonyl-4-methyl-4-aza-5.alpha.-androst-1-en-3-one.