利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

17 条记录 (耗时 0.033 秒)

    4,5-DIHYDROIMIDAZOLE DERIVATIVES AND THEIR USE AS HISTONE DEMETHYLASE (KDM2B) INHIBITORS
    1.
    发明申请
    4,5-DIHYDROIMIDAZOLE DERIVATIVES AND THEIR USE AS HISTONE DEMETHYLASE (KDM2B) INHIBITORS 审中-公开
    4,5-DIHYDROIMIDAZOLE衍生物及其用作HISTONE DEMETHYLASE（KDM2B）抑制剂

    公开(公告)号：WO2016112251A1

    公开(公告)日：2016-07-14

    申请号：PCT/US2016/012588

    申请日：2016-01-08

    申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

    发明人： ALBRECHT, Brian, K. ,  COTE, Alexandre ,  GEHLING, Victor ,  HSIAO-WEI TSUI, Vickie ,  KIEFER, James, Richard, Jr. ,  LIANG, Jun ,  MAGNUSON, Steven ,  NASVESCHUK, Christopher, G. ,  ROMERO, F. Anthony ,  TAYLOR, Alexander, M.

    IPC分类号： C07D403/12 ,  C07D233/44 ,  C07D401/04 ,  C07D235/02 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4995 ,  A61P35/00

    CPC分类号： C07D233/44 ,  C07D235/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

    摘要： The present invention relates to compounds of formula (I), (formula I) wherein: X is C(=0) or S(0) 2 ; R 1 is selected from the group consisting of N-linked piperazinyl, relinked piperidine, and N-linked diazabicyclo[3.2.1]octane, wherein R 1 is optionally substituted with one or more groups; R 2 and R 3 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl, wherein any C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl is optionally substituted with one or more groups; or R 2 and R 3 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups; R 4 and R 5 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl, wherein any C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl is optionally substituted with one or more groups; or R 4 and R 5 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups; and R 6 is a 5-10 membered heteroaryl, 5-10 membered heterocycle, or a 6-10 membered aryl, which 5-10 membered heteroaryl, 5-10 membered heterocycle, and 6-10 membered aryl is optionally substituted with one or more groups; useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

    摘要翻译： 本发明涉及式（I），（式I）的化合物，其中：X为C（= O）或S（O）2; R1选自N-连接的哌嗪基，再连接的哌啶和N-连接的二氮杂双环[3.2.1]辛烷，其中R 1任选被一个或多个基团取代; R 2和R 3各自独立地选自H，C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基，其中任何C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基任选被一个 或更多组; 或者R 2和R 3与它们所连接的碳一起形成任选被一个或多个基团取代的3-，4-，5-或6-元碳环; R 4和R 5各自独立地选自H，C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基，其中任何C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基任选被一个 或更多组; 或R 4和R 5与它们所连接的碳一起形成任选被一个或多个基团取代的3-，4-，5-或6-元碳环; 并且R 6是5-10元杂芳基，5-10元杂环或6-10元芳基，其中5-10元杂芳基，5-10元杂环和6-10元芳基任选被一个或多个 组; 可用作一种或多种组蛋白去甲基酶的抑制剂，例如KDM2b。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。