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Details for Patent: 5,151,429

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Details for Patent: 5,151,429

Title: 17.beta.-acyl-4-aza-5.alpha.-androst-1-ene-3-ones as 5.alpha. reductase inhibitors
Abstract: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 R.sup.2 is 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 formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
Inventor(s): Rasmusson; Gary H. (Watchung, NJ), Reynolds; Glenn F. (Westfield, NJ)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Sep 23, 1991
Application Number:07/764,047
Claims:1. A compound of formula: ##STR8## wherein R is selected from hydrogen, methyl and ethyl; and

R.sup.2 is a monovalent radical selected from benzyl and phenethyl or heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl, and

R', R", R'" are each selected from hydrogen or methyl.

2. A compound of claim 1 wherein the compound is 17.beta.(2-pyrrolylcarbonyl)-4-aza-5.alpha.-androst-1-en-3-one.

3. A compound of claim 1 wherein the compound is 4-methyl-17.beta.-(2-pyrrolylcarbonyl)-4-aza-5.alpha.-androst-1-en-3-one.

4. A method of treating the hyperandrogenic condition of acne vulgaris, seborrhea, female hirsutism, and benign prostatic hypertrophy comprising parenteral administration to a patient in need of such treatment of a therapeutically effective amount of a compound of formula: ##STR9## wherein R and R.sup.2 are defined as in claim 1.

5. A method of inhibiting testosterone 5.alpha.-reductase in a patient in need of such inhibiting treatment, comprising administration to such a patient of a therapeutically effective amount of a compound of the formula: ##STR10## wherein R and R.sup.2 are defined as in claim 1,

R' is hydrogen or methyl,

R" is hydrogen of .beta.-methyl,

R"' is hydrogen, .alpha.-methyl or .beta.-methyl.

6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of formula: ##STR11## wherein R and R.sup.2 are defined as in claim 1.
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