C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 73/00 (2006.01) A61K 31/58 (2006.01)
Patent
CA 2044921
8370/SCM109 18139 TITLE OF THE INVENETION SPECIFIC 17.beta.-THIOBENZOYL-4-AZA-5a-ANDROST- 1-EN-3-ONES AS ANTIANDROGENIC AGENTS ABSTRACT OF THE INVENTION SPECIFIC 17.beta.-THIOBENZOYL-4-AZA-5a-ANDROST- 1-EN-3-ONES AS ANTIANDROGENIC AGENTS OF THE FORMULA: Image 8370/SCM109 18139 wherein R is selected from hydrogen, methyl and ethyl and R2 is phenyl substituted with one or more of: -SH, -SC1-C4 alkyl, -SO-C1-C4alkyl, -SO2-C1-C4 alkyl, -SO2N-(C1-C4 alkyl)2, C1-C4 alkyl, -(CH2)mSH, -S(CH2)nOCOCH3, where m is 1-4, n is 1-3, and providing C1-C4 alkyl is only present when one of the above sulfur- containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents 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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