| 摘要 |
18147 TITLE OF THE INVENTION 17.beta.-ACYL-3-CARBOXY-ANDROSTA-3,5-DIENES AS TESTOSTERONE 5.alpha.-REDUCTASE INHIBITORS 17.beta.-ACYL-3-CARBOXY-ANDROSTA-3,5-DIENES AS TESTOSTERONE 5.alpha.-REDUCTASE INHIBITORS OF THE FORMULA: 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 substituted 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.
|
