Fused cyclic modulators of nuclear hormone receptor function
    8.
    发明授权
    Fused cyclic modulators of nuclear hormone receptor function 有权
    核激素受体功能的融合循环调节剂

    公开(公告)号:US07001911B2

    公开(公告)日:2006-02-21

    申请号:US10322306

    申请日:2002-12-18

    摘要: The invention pertains to fused cyclic compounds having the formula, wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7′ or NR10, and M′ is a bond or NR10, with the proviso that at least one of M or M′ must be a bond; E is C═Z2, CR7CR7′, SO2, P═OR2, or P═OOR2; Z1 is O, S, NH, or NR6; Z2 is O, S, NH, or NR6; A1 is CR7 or N; A2 is CR7 or N; Y is J—J′—J″ where J is (CR7R7′)n and n=0-3, J′ is a bond or O, S, S═O, SO2, NH, NR6, C═O, OC═O, NR1C═O, CR7R7′, C═CR8R8′, R2P═O, OPOOR2, OPO2, OSO2, C═N, NHNH, NHNR6, NR6NH, N═N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J″ is (CR7R7′)n and n=0-3; W is CR7R7′—CR7R7′, CR8═CR8′, CR7R7′—C═O, NR9—CR7R7′, N═CR8, N═N, NR9—NR9′, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, or aryl or substituted aryl; and O, R2, R6, R7, R7′, R8, R8′, R9, R9′, and R10 are as defined in the specification, to methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and to pharmaceutical compositions containing such compounds.

    摘要翻译: 本发明涉及具有甲醛的稠合环状化合物

    Hexahydroimidazopyrazin-3-one compounds useful as modulators of androgen receptor function
    9.
    发明授权
    Hexahydroimidazopyrazin-3-one compounds useful as modulators of androgen receptor function 有权
    六氢咪唑并吡嗪-3-酮化合物可用作雄激素受体功能的调节剂

    公开(公告)号:US07776859B2

    公开(公告)日:2010-08-17

    申请号:US11546965

    申请日:2006-10-12

    IPC分类号: A61K31/4985

    CPC分类号: C07D487/04

    摘要: The present invention is directed to compounds having the formula (I), and/or pharmaceutically-acceptable salts thereof, useful in the treatment of androgen-receptor associated conditions, wherein Ar is aryl, substituted aryl, heteroaryl, or substituted heteroaryl; L is a linker as defined in the specification; R1 may be hydrogen, cyano, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclo, substituted heterocyclo, heteroaryl, or substituted heteroaryl, as defined in the specification; R2 is hydrogen, lower alkyl, or substituted lower alkyl; and R3, R4 and R5 are optionally non-interfering substituents as defined in the specification.

    摘要翻译: 本发明涉及可用于治疗雄激素受体相关病症的式(I)化合物和/或其药学上可接受的盐,其中Ar为芳基,取代的芳基,杂芳基或取代的杂芳基; L是说明书中定义的接头; R 1可以是如本说明书中定义的氢,氰基,烷基,取代的烷基,芳基,取代的芳基,环烷基,取代的环烷基,杂环,取代的杂环,杂芳基或取代的杂芳基; R2是氢,低级烷基或取代的低级烷基; 并且R 3,R 4和R 5是本说明书中定义的任选的非干扰取代基。