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

C - Chemistry – Metallurgy – 07 – J

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167/191, 260/3

C07J 73/00 (2006.01) A61K 31/58 (2006.01)

Patent

CA 2023158

TITLE OF THE INVENTION 17.beta.-ACYL-4-AZA-5.alpha.-ANDROST-1-ENE-3-ONES AS 5.alpha.-REDUCTASE INHIBITORS ABSTRACT OF THE INVENTION 17.beta.-Acyl-4-aza-5.alpha.-androst-1-ene-3-ones of the formula: Image I - i - wherein R is selected from hydrogen, methyl and ethyl and R2 is 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; 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 for treatment of acne, seborrhea, female hirsutism, androgenic alopecin, prostatic carcinoma and benign prostatic hypertrophy.

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