17.beta.-n-monosubstituted carbamoyl -4-aza-5.-...

C - Chemistry – Metallurgy – 07 – J

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167/194, 260/3

C07J 73/00 (2006.01) A61K 31/58 (2006.01) C07C 62/38 (2006.01)

Patent

CA 1314541

ABSTRACT OF THE DISCLOSURE 17.beta.-N-monosubstituted carbamoyl or 17.beta.-acyl-4-aza- 5.alpha.-androst-1-en-3-ones as 5.alpha.reductase inhibitors of the for- mulae (A) and (B), respectively Image (A) Image (B) wherein R is selected from hydrogen, methyl and ethyl and R2 is a branched chain alkyl of from 3-12 carbons, R4 is a branched chain alkyl of from 3-12 carbon atoms or aralkyl selected from benzyl and phenethyl or a 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; pharmaceutical formulations of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and are useful for treatment of acne, seborrhea, female hirsutism and in the treatment of benign prostatic hypertrophy.

475184

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