Indole derivatives
    1.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号:US5312829A

    公开(公告)日:1994-05-17

    申请号:US956579

    申请日:1992-10-06

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is carboxy or pharmaceutically acceptable salts and esters thereof;R.sup.2 is hydrogen, lower alkyl or halogen;R.sup.3 is phenyl, naphthyl, phenyl or naphthyl each substituted by from one to three C.sub.1-6 alkyl groups, mono-, di- or triphenyl (C.sub.1-6)alkyl; or substituted mono-, di- or triphenyl (C.sub.1-6) alkyl;A is lower alkylene which may be substituted by oxo or lower alkenylene,Q is carbonyl or lower alkylene,X is ##STR2## in which R.sup.4 is hydrogen or C.sub.1-6 alkyl, andR.sup.5 is hydrogen, C.sub.1-6 alkyl or Y--Z--R.sup.3,Y is a bond or lower alkylene,Z is lower alkylene ##STR3## in which R.sup.6 is hydrogen, (C.sub.1 -C.sub.6) alkyl, mono-, di- or triphenyl(C.sub.1-10) alkyl, C.sub.1-6 alkyl or lower alkoxycarbonyl substituted mono-, di- or triphenyl(C.sub.1-6)alkyl or pharmaceutically acceptable carboxylic acid acyl, and pharmaceutically acceptable salts thereof. The compound is useful as a testosterone 5.alpha.-reductase inhibitor.

    摘要翻译: 下式的化合物:其中R 1是羧基或其药学上可接受的盐和酯; R2是氢,低级烷基或卤素; R 3为苯基,萘基,苯基或萘基,各自被一至三个C 1-6烷基,单 - ,二 - 或三苯基(C 1-6)烷基取代; 或取代的单 - ,二 - 或三苯基(C 1-6)烷基; A是可被氧代或低级亚烯基取代的低级亚烷基,Q是羰基或低级亚烷基,X是其中R 4是氢或C 1-6烷基,R 5是氢,C 1-6烷基或YZ-R 3 ,Y为键或低级亚烷基,Z为低级亚烷基,其中R6为氢,(C1-C6)烷基,单 - ,二 - 或三苯基(C1-10)烷基,C1-6烷基或低级烷氧基羰基 取代的单 - ,二 - 或三苯基(C 1-6)烷基或药学上可接受的羧酸酰基及其药学上可接受的盐。 该化合物可用作睾酮5α-还原酶抑制剂。

    Indole derivatives useful as testosterone 5.alpha.-reductase inhibitors
    5.
    发明授权
    Indole derivatives useful as testosterone 5.alpha.-reductase inhibitors 失效
    吲哚衍生物可用作睾丸激素5α-还原酶抑制剂

    公开(公告)号:US5530019A

    公开(公告)日:1996-06-25

    申请号:US338533

    申请日:1995-03-08

    摘要: A compound of the formula (I): ##STR1## wherein R.sup.1 is an optionally protected carboxy(lower)alkyl, R.sup.2 is a hydrogen, an optionally substituted aryl or a carboxy,X is a bond, --0--, --NH-- or a cycloalkylene, andY is an alkylene which may be interrupted by an oxygen atom, an alkenylene or an alkadienylene,or a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a testosterone 5.alpha.-reductase inhibitor and effective against testosterone 5.alpha.-reductase-mediated diseases such as prostatism, prostatic hypertrophy, prostatic cancer, alopecia, hirsutism (e.g. female hirsutism), androgenic alopecia (or male-pattern baldness), acne (e.g. acne vulgaris, pimple), and other hyperandrogenisms.

    摘要翻译: PCT No.PCT / JP94 / 00406 Sec。 371日期:1995年3月8日 102(e)日期1995年3月8日PCT 1994年3月14日PCT公布。 第WO94 / 22821号公报 (I)化合物:其中R 1为任选保护的羧基(低级)烷基,R 2为氢,任选取代的芳基或羧基,X为 键,-O - , - NH-或亚环烷基,Y是可被氧原子,亚烯基或链二烯基或其可药用盐间隔的亚烷基。 本发明的化合物可用作睾丸激素5α-还原酶抑制剂,并且有效地抵抗睾酮5α-还原酶介导的疾病,例如前列腺炎,前列腺肥大,前列腺癌,脱发,多毛症(例如雌性多毛症),雄激素性脱发(或 男性型秃发),痤疮(例如寻常痤疮,疙瘩)和其他雄激素过多。