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

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

C - Chemistry, Metallurgy

07

J

C07J 9/00 (2006.01) A61K 31/56 (2006.01) A61K 31/695 (2006.01) C07J 7/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 51/00 (2006.01)

Patent

CA 2045866

18147 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/SCM111 18147 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 18 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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