C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 73/00 (2006.01) A61K 31/58 (2006.01)
Patent
CA 2044922
8367/SCM107 18142 TITLE OF THE INVENTION NOVEL 17.beta.-HYDROXYBENZOYL-4-AZA-5a-ANDROST- 1-EN-3-ONES AS TESTOSTERONE REDUCTASE INHIBITORS ABSTRACT OF THE INVENTION Novel 17.beta.-hydroxybenzoyl-4-aza-5a-androst- 1-en-3-ones as testosterone reductase inhibitors of the f ormula: Image 8367/SCM107 18142 wherein R is selected from hydrogen, methyl and ethyl and R2 is phenyl substituted with one or more of: -OH, -OC1-C4 alkyl, C1-C4 alkyl, -(CH2)mH, -(CH2)n COOH, including protected -OH, where m is 1-4, n is 1-3, and providing C1-C4 alkyl is only present when one of the above oxygen containing radicals is present, wherein the dotted line represents a double bond which can be present, pharmaceutically acceptable salts and esters thereof, and a pharmaceutical formulation thereof. The above compounds are active as testosterone reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
Rasmusson Gary H.
Salzmann Thomas N.
Steinberg Nathan G.
Merck & Co. Inc.
Rasmusson Gary H.
Salzmann Thomas N.
Steinberg Nathan G.
Swabey Ogilvy Renault
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