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20 条记录 (耗时 0.03 秒)

    Akt inhibitors, pharmaceutical compositions, and uses thereof
    1.
    发明授权
    Akt inhibitors, pharmaceutical compositions, and uses thereof 有权

    公开(公告)号：US07378403B2

    公开(公告)日：2008-05-27

    申请号：US10526851

    申请日：2003-09-03

    申请人： Alan P. Kozikowski ,  Phillip Dennis ,  Haiying Sun ,  John Brognard

    发明人： Alan P. Kozikowski ,  Phillip Dennis ,  Haiying Sun ,  John Brognard

    IPC分类号： A61K31/662 ,  A61K31/683 ,  C07F9/09 ,  C07F9/30

    CPC分类号： C07C43/196 ,  C07C2601/14 ,  C07F9/117

    摘要： Disclosed are inhibitors of the serine/threonine kinase Akt, pharmaceutical compositions comprising such inhibitors, and a method of preventing or treating a disease or condition in an animal by the use of such inhibitors. The Akt inhibitors have the formula (I) wherein X and Y are independently selected from the group consisting of O, CF2, CH2, and CHF; wherein A is independently selected from the group consisting of P(O)OH, CH2000H, and CH(COOH)2; R2 is selected from the group consisting of H, OH, isosteres of OH, C1-C25 alkyloxy, C6-C10 aryloxy, C3-C8 cycloalkyloxy, C3-C8 cycloalkyl C1-C6 alkoxy, C2-C22 alkenyloxy, C3-C8 cycloalkenyloxy, C7-C32 aralkyloxy, C7-C32 alkylaryloxy, C9-C32 aralkenyloxy, and C9-C32 alkenylaryloxy; R3-R6 are independently selected from the group consisting of H, OH, isosteres of OH; and R1 and R7 are independently selected from the group consisting of C1-C25 alkyl, C6-C10 aryl, C3-C8 cycloalkyl, C2-C22 alkenyl, C3-C8 cycloalkenyl, C7-C32 aralkyl, C7-C32 alkylaryl, C9-C32 aralkenyl, and C9-C32 alkenylaryl; with the provisos that (i) when X is O, Y is O or CH2, and R3 is H, at least one of R2 and R4-R6 is not OH; (ii) when A is CH2COOH or CH(COOH)2, X and Y cannot be simultaneously O; and (iii) all of R2-R6 are not simultaneously H. The inhibitors can be in the form of a salt also