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19 条记录 (耗时 0.028 秒)

    17.beta.-substituted 4-aza-5.alpha.-androstan-3-one derivatives
    6.
    发明授权
    17.beta.-substituted 4-aza-5.alpha.-androstan-3-one derivatives 失效
    17β-取代的4-氮杂-5α-雄甾烷-3-酮衍生物

    公开(公告)号：US5418238A

    公开(公告)日：1995-05-23

    申请号：US98935

    申请日：1993-07-29

    申请人： Achille Panzeri ,  Marcella Nesi ,  Enrico di Salle

    发明人： Achille Panzeri ,  Marcella Nesi ,  Enrico di Salle

    IPC分类号： A61K31/58 ,  C07J73/00 ,  C12N9/99

    CPC分类号： C07J73/005

    摘要： A compound of formula (I): ##STR1## wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl or a C.sub.6 -C.sub.10 cycloalkylalkyl group, aryl or a C.sub.7 -C.sub.10 arylalkyl group, or a C.sub.6 -C.sub.10 heterocyclylalkyl group;R.sub.3 is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aryl or a C.sub.7 -C.sub.10 arylalkyl group;Z is a C.sub.1 -C.sub.6 alkyl group, an --OR.sub.5 group wherein R.sub.5 is a C.sub.1 -C.sub.6 alkyl group, ##STR2## group wherein each of R.sub.6 and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl or R.sub.6 and R.sub.7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol represents a single or a double bond, is a testosterone 68 5.alpha.-reductase inhibitor and is therapeutically useful in benign prostatic hyperplasia, prostatic and breast cancers, seborrhoea, female hirsutism and male pattern baldness.

    摘要翻译： 式（I）的化合物：其中R是氢原子或C 1 -C 4烷基; A是单键或直链或支链C1-C6亚烷基链; R1是氢原子或C1-C6烷基; R2是C1-C6烷基，C5-C7环烷基或C6-C10环烷基烷基，芳基或C7-C10芳基烷基或C6-C10杂环基烷基; R3是氢，C1-C4烷基或芳基或C7-C10芳烷基; Z是C1-C6烷基，其中R5是C1-C6烷基的-OR5基团，其中R6和R7各自是氢，C1-C6烷基，C5-C7环烷基，苯基或R6和 R7与它们所连接的氮一起形成五原子或六原子饱和杂单环; 符号表示单键或双键，是睾酮685α-还原酶抑制剂，可用于良性前列腺增生，前列腺和乳腺癌，皮脂溢，女性多毛症和男性型秃发。

    1,2-beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation
    8.
    发明授权
    1,2-beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation 失效
    1,2-β-亚甲基-4-取代雄甾烯-3,17-二酮衍生物及其制备方法

    公开(公告)号：US4810423A

    公开(公告)日：1989-03-07

    申请号：US86607

    申请日：1987-08-18

    申请人： Franco Buzzetti ,  Enrico di Salle ,  Paolo Lombardi

    发明人： Franco Buzzetti ,  Enrico di Salle ,  Paolo Lombardi

    IPC分类号： C07J53/00 ,  C07J71/00 ,  A61K31/56 ,  C07C117/00

    CPC分类号： C07J53/005 ,  C07J71/001 ,  Y02P20/55

    摘要： The invention relates to new aromatase inhibitor agents having the general formula (I) ##STR1## wherein R.sub.1 is hydrogen or a group=CHR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl; the symbol indicates the presence of a single or double bond in such a way that, when R.sub.1 is hydrogen, (a) is single bond and (b) is either single or double bond, while, when R.sub.1 is a group.dbd.CHR.sub.3 as defined above, (a) is double bond and (b) is single bond; R.sub.2 is hydrogen or fluorine; and R is(1) a group --OR.sub.4 wherein R.sub.4 is(a) hydrogen;(b) C.sub.1 -C.sub.6 alkyl;(c) a phenyl or benzyl group, each unsubstituted or ring-substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, halogen, trifluoromethyl, nitro, amino, hydroxy and C.sub.1 -C.sub.4 alkoxy;(d) a group--COR.sub.5 wherein R.sub.5 is(i) a C.sub.1 -C.sub.22 saturated or C.sub.2 -C.sub.22 unsaturated aliphatic hydrocarbon radical;(ii) a C.sub.4 -C.sub.7 monocycloalkyl group; or(iii) a phenyl or benzyl group, each unsubstituted or ring substituted as reported above; or(e) a hydroxy protecting group;(2) a group--SR.sub.6 wherein R.sub.6 either has one of the meanings (a) to (d) indicated above for R.sub.4 or is a group --SR.sub.7 wherein R.sub.7 is(iv) C.sub.1 -C.sub.6 alkyl;(v) a phenyl or benzyl group, each unsubstituted or ring-substituted as reported above; or(vi) a steroidic residue of formula ##STR2## wherein R.sub.1, R.sub.2, (a), (b) and the symbol are as defined above; (3) the group --N.sub.3 ; or(4) a group ##STR3## wherein each of R.sub.8 and R.sub.9, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, which are useful in therapy, in particular, as anti-cancer agents.