申请人:Sankyo Company, Limited
公开号:US05536714A1
公开(公告)日:1996-07-16
The invention includes compounds of formula (I): ##STR1## in which R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl; and pharmaceutically acceptable salts and esters of the compounds. The compounds have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydro-testosterone.
该发明包括式(I)的化合物:##STR1##其中R.sup.1是氢,烷基,芳基取代的烷基或芳香杂环基取代的烷基;R.sup.2是芳基取代的烷基,芳香杂环基取代的烷基或二芳基胺基;R.sup.3是羧基或具有式--CONHSO.sub.2 R.sup.4的基团,其中R.sup.4是烷基;以及该化合物的药用可接受盐和酯。这些化合物具有有价值的5α-还原酶抑制活性,因此可用于治疗和预防前列腺肥大等疾病,以及由于5α-二氢睾酮水平过高而引起的其他疾病。