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    N-substituted benzoyl indoles as estrogenic agents
    3.
    发明授权
    N-substituted benzoyl indoles as estrogenic agents 失效
    N-取代苯甲酰基吲哚作为雌激素剂

    公开(公告)号：US06380185B1

    公开(公告)日：2002-04-30

    申请号：US09513807

    申请日：2000-02-25

    申请人： Marci C. Koko ,  John W. Ullrich ,  Arthur A. Santilli

    发明人： Marci C. Koko ,  John W. Ullrich ,  Arthur A. Santilli

    IPC分类号： A61K3155

    CPC分类号： C07D209/12

    摘要： The present invention provides compounds of the formula: wherein R1, R2, R3, R4, X, n Y and Z, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical formulations and methods of treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.

    摘要翻译： 本发明提供下式的化合物：其中R1，R2，R3，R4，X，nY和Z如说明书中所定义，或其药学上可接受的盐，以及药物制剂和治疗或预防的方法 使用这些化合物引起或与雌激素缺乏或过量雌激素引起或相关的疾病状态或综合征。

    Thio-oxindole derivatives
    7.
    发明授权
    Thio-oxindole derivatives 有权
    硫氧吲哚衍生物

    公开(公告)号：US06355648B1

    公开(公告)日：2002-03-12

    申请号：US09552033

    申请日：2000-04-19

    申请人： Andrew Fensome ,  Puwen Zhang ,  Marci C. Koko ,  Lin Zhi ,  Todd K. Jones ,  Jay E. Wrobel ,  Christopher M. Tegley ,  James P. Edwards ,  Edward G. Melenski

    发明人： Andrew Fensome ,  Puwen Zhang ,  Marci C. Koko ,  Lin Zhi ,  Todd K. Jones ,  Jay E. Wrobel ,  Christopher M. Tegley ,  James P. Edwards ,  Edward G. Melenski

    IPC分类号： A61K31505

    CPC分类号： C07D209/40 ,  C07D209/08 ,  C07D209/30

    摘要： This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl; 1-propynyl; or 3-propynyl; or R1 and R2 are joined to form an alkyl, alkenyl or heterocyclic ring; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, substituted alkynyl, or CORA; RA is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NH2, NO2, C1 to C6 alkyl, or substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; R5 is optionally substituted and selected from a benzene ring, a five or six membered heterocyclic ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR6; or an indol-4-yl, indol-7-yl or benzo-2-thiophene moiety; Q1 is S, NR7, CR8R9; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.

    摘要翻译： 本发明涉及作为孕酮受体激动剂的化合物，其具有以下通式结构：其中：R 1和R 2为H，烷基，取代的烷基; 哦; O（烷基）; O（取代的烷基）; OAc; 芳基; 取代芳基; 杂芳基; 取代的杂芳基; 烷基芳基 烷基杂芳基 1-丙炔基; 或3-丙炔基; 或R 1和R 2连接形成烷基，链烯基或杂环; 或R1和R2一起包含与CMe2的双键; C（环烷基），O或C（环醚）; R 3是H，OH，NH 2，C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3至C 6烯基，炔基，取代的炔基或CORA; RA为H，C1至C3烷基，取代C1至C3烷基，C1至C3烷氧基，取代C1至C3烷氧基，C1至C3氨基烷基或取代C1至C3氨基烷基; R 4是H，卤素，CN，NH 2，NO 2，C 1至C 6烷基或取代的C 1 -C 6烷基，C 1至C 6烷氧基，取代的C 1至C 6烷氧基，C 1至C 6氨基烷基或取代的C 1至C 6氨基烷基; R5任选被取代并选自苯环，具有1,2或3个选自O，S，SO，SO 2或NR 6的杂原子的五元或六元杂环; 或吲哚基-4-基，吲哚-7-基或苯并-2-噻吩部分; Q1是S，NR7，CR8R9; 或其药学上可接受的盐，以及使用这些化合物诱导避孕或治疗孕酮相关的癌和腺癌的方法。