Patent References 2227876 3239417 3264301 3285918 Preparation of 4-aza-17-substituted-5-androstan-3-ones useful as 5-reductase inhibitors 4-Aza-17ଲ-substituted-5-androstan-3-one-reductase inhibitors 17ଲ-N-monosubstituted carbamoyl-4-aza-5-androst-1-en-3-ones which are active as testosterone 5-reductase inhibitors Patent #: 4760071 InventorsAssigneeApplicationNo. 07/129335 filed on 12/03/1987US Classes:514/284, Tetracyclo ring system having the six-membered hetero ring as one of the cyclos514/859, Acne546/77The six-membered hetero ring shares ring members with one other cyclo onlyExaminersPrimary: Sutto, Anton H.Assistant: Rivers, Diana G. Attorney, Agent or FirmInternational ClassesC07J 73/00 (20060101)C07C 62/00 (20060101) C07C 62/38 (20060101) Abstract17ଲ-Acyl-4-aza-5-androst-1-en-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR2 is a monovalent radical selected from straight 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-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.Other References
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