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    Compounds that modulate TRH actions
    6.
    发明授权
    Compounds that modulate TRH actions 有权
    调节TRH作用的化合物

    公开(公告)号：US07713935B2

    公开(公告)日：2010-05-11

    申请号：US11576228

    申请日：2005-10-03

    申请人： Julie Kelly

    发明人： Julie Kelly

    IPC分类号： A61K38/16 ,  A01N43/74

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/1024

    摘要： The invention relates to compounds that inhibit thyrotropin-releasing hormone (TRH) degrading ectoenzyme and/or enhance, and/or mimic the biological actions of TRH. The compounds find therapeutic application, particularly in conditions involving neuronal cell injury and disturbances in neurobiological function.

    摘要翻译： 本发明涉及抑制促甲状腺激素释放激素（TRH）降解胞外酶和/或增强和/或模拟TRH的生物学作用的化合物。 该化合物发现治疗应用，特别是涉及神经元细胞损伤和神经生物功能障碍的病症。

    TRH-like peptide derivatives as inhibitors of the TRH-degrading ectoenzyme
    10.
    发明申请
    TRH-like peptide derivatives as inhibitors of the TRH-degrading ectoenzyme 有权

    公开(公告)号：US20060293247A1

    公开(公告)日：2006-12-28

    申请号：US11345649

    申请日：2006-02-01

    申请人： Julie Kelly

    发明人： Julie Kelly

    IPC分类号： A61K38/06 ,  C07K7/06

    CPC分类号： C07K5/0821 ,  A61K38/00 ,  C07K5/0825

    摘要： Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula Ia: wherein: R1 is an optionally substituted 4-, 5- or 6-membered heterocyclic ring having one or more heteroatoms, in which at least one carbon atom of the ring is substituted with O or S; X1 is —CO— or —CS— or —CH2CO— or CH(R4) wherein R4 is H or optionally substituted alkyl or —COOH or —COOR11 wherein R11 is optionally substituted alkyl; X2 and X3 (which may be the same or different) are —CO— or —CS—; Z is —CH2— or —S—or —O— or —NH—; Q is O or S; R2 is H or optionally substituted alkyl or an optionally substituted carbocyclic ring; R3 is H or optionally substituted alkyl or an optionally substituted mono- or polycyclic ring, optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring; or R2 and R3 together form an optionally substituted mono- or polycyclic ring optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring; R5 and R6 (which may be the same or different) are H, or lower alkyl; R7 and R8 (which may be the same or different) are H, or optionally substituted lower alkyl; R9 and R10 (which may be the same or different) are H, or optionally substituted alkyl, or an optionally substituted carbocyclic ring; Y is —(CH2)n— where n is 0, 1, 2 or 3 provided that when R2 and R3 form part of the ring n is 0; and pharmaceutically acceptable salts thereof.