利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

156 条记录 (耗时 0.059 秒)

    Thio-oxindole derivatives
    29.
    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。