17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone...

C - Chemistry – Metallurgy – 07 – J

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C07J 9/00 (2006.01) A61K 31/575 (2006.01) C07J 3/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01) C07J 51/00 (2006.01)

Patent

CA 2067265

18147IA TITLE OF THE INVENTION 17.beta.-ACYL-3-CARBOXY-ANDROSTA-3,5-DIENES AS TESTOSTERONE 5.alpha.-REDUCTASE INHIBITORS ABSTRACT OF THE INVENTION 17.beta.-ACYL,3-CARBOXY-ANDROSTA-3,5-DIENES AS TESTOSTERONE 5.alpha.-REDUCTASE INHIBITORS OF THE FORMULA: Image 8373/SCMlll - ii - 18147IA wherein R is C1-C6 linear or branched alkyl; C3-C8 cycloalkyl, which can be substituted with C1-C4 alkoxy or C1-C4 linear/branched alkyl; C6-C12 aryl, which can be substi- tuted with one or more of: -OH, -OC1-C4 alkyl. C1-C4 alkyl, -(CH2)mOH, -(CH2)n COOH, including protected -OH, where m is 1-4, n is 1-3, and pharmaceutically acceptable salts or esters thereof. Also described is a pharmaceutical formulation. The above compounds are active as testosterone 5a-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

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