17β-Acyl-3-carboxy-androsta-3,5-dienes as testosterone 5α-reductase inhibitors of the formula:
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 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.
17β-酰基-3-羧基-雄甾-3,5-二烯类化合物作为雄激素5α-还原酶
抑制剂的公式如下:其中R为C₁-C₆线性或支链烷基;C₃-C₈环烷基,可用C₁-C₄烷氧基或C₁-C₄线性/支链烷基取代;C₆-C₁₂芳基,可被一个或多个取代基取代:-OH,-OC₁-C4烷基,C₁-C₄烷基,-(CH₂)mOH,-(CH₂)nCOOH,包括保护的-OH,其中m为1-4,n为1-3,并且其药学上可接受的盐或酯。还描述了一种药物制剂。上述化合物作为雄激素5α-还原酶
抑制剂具有活性,因此在治疗痤疮、脂溢性皮炎、女性多毛症的局部治疗和良性前列腺增生的全身治疗中有用。