Merck + Co., Inc.

Glenn F Reynolds

Gary H Rasmusson

17.beta.-N-monosubstituted-carbamoyl-4-5.alpha.-androst-1-en-3-ones of the formula ##STR1## wherein R.sup.1 is selected from hydrogen, methyl and ethyl and R.sup.2 is a branched chain alkyl of from 3-12 carbons, and R', R', R'' are hydrogen or methyl are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of androgenic alopecia.

Methods of treating androgenic alopecia with finasteride

17.beta.-Acyl-4-aza-5.alpha.-androst-1-en-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and

17.beta.-acyl-4-aza-5.alpha.-androst-1-ene-3-ones as 5.alpha. reductase

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.

17.beta.-methoxycarbonyl-4-aza-androsten-1-en-3-ones

17.beta.-Acyl-4-aza-5.alpha.-Androst-1-end-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and

17 .beta.-acyl-4-aza-5 .alpha.-androst-1-ene-3-ones as 5

17.beta.-Acyl-4-aza-5.alpha.-androst-1-ene-3-ones of the formula ##STR1## wherein R is selected from hydrogen, methyl and ethyl and

17.beta.-acyl-4-aza-5.alpha.-androst-1-ene-3-ones as 5.alpha.-reductase

17 .alpha.-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase

This invention is for the compound 17.beta.-(N-t-butylcarbamoyl)-4-aza-5.alpha.-androst-1-en-3-one, pharmaceutical compositions containing the compound, methods of inhibiting testosterone 5.alpha.-reductase with the compound and methods of treating hyperandrogenic conditions with the compound, particularly benign prostatic hypertrophy.

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Westfield, NJ, United States of America

Glenn F Reynolds