| 摘要 |
PURPOSE: To obtain a new tricyclic anilide derivative having steroid 5α-reductase inhibitory action, thus useful as a medicine for prostatomegaly, prostate cancer, alopecia and acne. CONSTITUTION: This new tricyclic anilide derivative (or a pharmacologically permissible salt thereof) is expressed by formula I [R<1> , R<2> and R<4> are each H or an alkyl; R<3> is H, a halogen, nitro or an alkyl; A is CH or N; Y is CH2 CH2 , CH=CH, CH2 O, OCH2 , CH2 S, SCH2 , O, S or a single bond; Z<1> -Z<2> is C=O or CHOR<5> (R<5> is H, an alkyl or aralkyl). X is O or S(O)q ((q) is 0-2); (n) is 1-6], e.g. 4-[2-(6,11-dihydrodibenz[b,e]-oxepin-11-on-2-yl) carboxamidophenoxy]butyric ethyl ester. A compound of formula Ia, one of the compounds of formula I (where, R<1> is an alkyl), is obtained by reaction between a compound of formula II and a compound of formula III, and then a compound of formula Ib, another one of the compounds of formula I (where, R<1> is H) is obtained.
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