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Details for Patent: 5,120,742

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Details for Patent: 5,120,742

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-end-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and R.sup.3 is cycloalkyl of from 4-8 carbons; and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, androgenic alopecia, prostatic carcinoma and benign prostatic hypertrophy.
Inventor(s): Rasmusson; Gary H. (Watchung, NJ), Reynolds; Glenn F. (Westfield, NJ)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Apr 09, 1991
Application Number:07/683,520
Claims:1. A compound of the formula: ##STR8## wherein R is hydrogen, methyl or ethyl; and

R.sup.3 is cycloalkyl of from 4-8 carbons.

2. A compound of claim 1 which is

17.beta.-(cyclobutylcarbonyl)-4-aza-5.alpha.-androst-1-ene-3-one;

17.beta.-(cyclopentylcarbonyl)-4-aza-5.alpha.-androst-1-ene-3-one;

17.beta.-(cyclohexylcarbonyl)-4-aza-5.alpha.-androst-1-ene-3-one;

17.beta.-(cycloheptylcarbonyl)-4-aza-5.alpha.-androst-1-ene-3-one;

17.beta.-(cyclooctylcarbonyl)-4-aza-5.alpha.-androst-1-ene-3-one.

3. A compound of claim 2 wherein the 4-hydrogen substituent is replaced by a 4-methyl substituent.

4. A compound of claim 2 which is 17.beta.-(cyclohexylcarbonyl)-4-aza-5.alpha.-androst-1-ene-3-one.

5. A method of treating the hyperandrogenic condition of acne vulgaris, seborrhea, female hirsutism, and benign prostatic hypertrophy comprising administration to a patient in need of such treatment of a therapeutically effective amount of a compound of claim 1.

6. 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 claim 1.

7. A pharmaceutical composition for inhibiting testosterone 5-alpha reductase which comprises a pharmaceutically acceptable carrier and an effective amount of a compound of claim 1.
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